Uncategorised - Nurses Revision

Drugs Used in the Treatment of Cardiovascular Disorders

These drugs are used in the treatment of conditions such as:

Hypertension
Angina pectoris
Heart failure
Hyperlipidemia
Arrhythmias

Drugs Used in the Treatment of Hypertension

Hypertension

Hypertension is the persistent elevation of blood pressure higher than normal (140/90 mmHg).

Common Terms Used in Hypertension

Blood Pressure: This is the pressure of blood against the walls of the main arteries.
Diastolic Blood Pressure: This is the pressure exerted in the vessels when the ventricles are relaxing and refilling.
Systolic Pressure: This is the pressure exerted in the vessels when the ventricles are contracting.
Orthostatic Hypotension (Postural Hypotension): This is the decrease in blood pressure that occurs when a person stands erect.
Peripheral Vascular Resistance: This is the pressure that blood must overcome as it flows in the vessels.
Isolated Systolic Hypertension: This is defined as systolic blood pressure greater than or equal to 140 mmHg with diastolic blood pressure less than 90 mmHg. It is common in elderly patients.
Malignant Hypertension: This is a rapidly progressing, potentially fatal form of hypertension with diastolic pressure exceeding 120 mmHg.
Hypertensive Emergency: This is characterized by severe elevation in blood pressure > 180/120 mmHg complicated by target organ dysfunction. These situations require immediate reduction of blood pressure to limit target organ damage.
Hypertensive Urgency: This is a situation with severe elevation of blood pressure without target organ dysfunction.

Table 1: Stages of Hypertension

Category	Systolic	Diastolic
Normal	< 130	< 80
High Normal (Pre-hypertension)	130-139	81-89
Mild Hypertension (Stage I)	140-159	90-99
Moderate Hypertension (Stage 2)	160-179	100-109
Severe Hypertension (Stage 3)	180-209	110-119
Very Severe Hypertension (Stage 4)	> 209	> 119

Classification of Hypertension

Hypertension may be classified as:

Essential (Primary) Hypertension
Secondary Hypertension

Essential Hypertension

Essential hypertension is the most common type of hypertension, contributing to over 90% of the cases of hypertension encountered in medical practice. The cause of essential hypertension is not known.

Secondary Hypertension

Secondary hypertension is an elevation of blood pressure due to an identifiable cause such as:

Renal disease
Drugs like oral contraceptives
Pre-eclampsia
Renovascular disease

Treatment is directed at elimination of the cause.

Management of Hypertension

Non-Pharmacological Measures

Encourage regular exercise (e.g., walking, jogging)
Advise the patient to lose weight (if overweight)
Advise the patient to limit alcohol intake
Advise the patient to restrict salt intake
Advise the patient to stop smoking
Encourage a diet high in fruits and vegetables
Advise the patient to relax and manage stress
Diet should be low in saturated fats and cholesterol

Note: Non-pharmacological measures may be employed alone in pre-hypertension or in combination with drugs in mild to severe hypertension.

Drugs used in the treatment of hypertension may be classified as follows:

Beta blockers
ACE inhibitors
Alpha-II blockers
Diuretics
Centrally acting antihypertensives
Calcium channel blockers
Angiotensin II antagonists
Direct vasodilators

Table 2: Choice of Antihypertensives in Different Conditions

Comorbid Disease	Drugs Recommended
Diabetes mellitus	Calcium channel blockers, ACE inhibitors
Congestive heart failure	Diuretics, ACE inhibitors
Angina pectoris	Beta blockers, calcium channel blockers, ACE inhibitors, and diuretics as alternative
Asthma, chronic pulmonary disease	Calcium channel blockers, diuretics, and ACE inhibitors
Hyperlipidemia	ACE inhibitors, calcium channel blockers
Previous myocardial infarction	Beta blockers, calcium channel blockers, ACE inhibitors, and diuretics
Chronic renal disease	Diuretics, calcium channel blockers, beta blockers, and ACE inhibitors

Beta Blockers

These drugs are recommended in the treatment of hypertension, angina pectoris, and post-myocardial infarction.

Beta blockers are classified as follows:

Non-selective beta blockers

Propranolol
Sotalol

Selective beta-1 blockers

Atenolol
Bisoprolol
Metoprolol

Alpha and beta blockers

Carvedilol
Labetalol

Mode of Action

Beta blockers competitively block the response to beta receptors, resulting in a decrease in heart rate and heart contractility, thereby lowering blood pressure.

Atenolol

Available Preparations:

Tablets: 25 mg, 50 mg, 100 mg

Available Brands: Tenormin®, Totamol®, Velorin®, Atelor®, Betagard®, Cardinol®, Tensimin®

Combinations:

Tenoret® (Atenolol/Chlorthalidone) 50/12.5 mg
Tenoretic® (Atenolol/Chlorthalidone) 100/25 mg

Pharmacokinetics

About half of the dose is absorbed following oral administration, crosses the placenta, and is distributed into breast milk. Atenolol undergoes little or no hepatic metabolism and is excreted unchanged in the urine.

Indications

Hypertension
Angina pectoris
Cardiac arrhythmias
Prophylaxis in migraine
Acute myocardial infarction

Contraindications

Hypersensitivity to atenolol
Sinus bradycardia
Second and third-degree heart block
Symptomatic heart failure

Dosage

Hypertension: 25-100 mg once daily (100 mg is only slightly better than 50 mg)
Angina: 100 mg once daily or 50 mg twice daily
Arrhythmias: 50-100 mg daily
Migraine Prophylaxis: 50-100 mg daily

Side Effects

Fatigue
Hypotension
Impotence
Muscle ache
Dizziness
Wheezing
Insomnia

Drug Interactions

Cimetidine may increase atenolol blood concentration
Diuretics and other antihypertensives may increase the hypotensive effect of atenolol
Atenolol may mask the symptoms of hypoglycemia and prolong the hypoglycemic effect of insulin and oral hypoglycemics
NSAIDs may decrease the antihypertensive effects of atenolol
Alcohol enhances the hypotensive effect of atenolol
Concurrent use with digoxin increases the risk of AV block and bradycardia
Oral contraceptives antagonize the hypotensive effect of atenolol
Concurrent use with verapamil results in severe hypotension and heart failure

Key Issues to Note

Atenolol should be used with caution in patients with diabetes since it may mask symptoms of hypoglycemia
Atenolol may be administered with or without food
Abrupt withdrawal of the drug should be avoided; it should be discontinued over 1-2 weeks through gradual reduction of the dose

Calcium Channel Blockers

These drugs are used in the treatment of hypertension and angina pectoris and are safe for patients with asthma, hyperlipidemia, diabetes, and renal dysfunction. They are subdivided into two groups:

Dihydropyridines
Non-dihydropyridines

Dihydropyridines: Drugs in this group produce significant blockage of calcium channels in blood vessels and minimal in the heart.

Examples:

Nifedipine
Amlodipine
Felodipine

Non-Dihydropyridines: These drugs act on vascular smooth muscle and the heart. Since they suppress AV conduction, they are useful in cardiac arrhythmias.

Examples:

Verapamil
Diltiazem

Mode of Action

Calcium channel blockers decrease the influx of calcium into smooth muscles, thereby reducing vascular tone, which results in a reduction of peripheral resistance and blood pressure.

Nifedipine

Available Preparations:

Tablets: 10 mg, 20 mg retard, 30 mg long-acting

Available Brands: Adalat®, Nifelat®, Nifedipine-denk®

Pharmacokinetics

Nifedipine is rapidly and almost completely absorbed from the gastrointestinal tract, but bioavailability is reduced by first-pass metabolism. It is extensively metabolized in the liver and excreted in the urine as inactive metabolites.

Indications

Hypertension
Prophylaxis of angina pectoris

Contraindications

Hypersensitivity to nifedipine
Unstable or acute attacks of angina
Porphyria
Cardiogenic shock

Dosage

The dose and frequency of administration vary depending on the preparations used.

Short-acting nifedipine is given 3 times a day
Nifedipine retard is given twice daily
Long-acting nifedipine is given once daily

Hypertension:

Adults: 10-20 mg twice daily, increased to 20-40 mg twice daily (Nifedipine retard)
Nifedipine long-acting: 30-90 mg once daily

Angina Pectoris:

Nifedipine retard: 10-40 mg twice daily or nifedipine long-acting: 30-90 mg once daily

Side Effects

Oedema of ankle
Headache
Flushing
Dizziness
Tachycardia
Palpitations
Impotence
Tremors
Muscle cramps
Dry mouth
Constipation
Nausea

Drug Interactions

Beta blockers may have additive hypotensive effects when given together with nifedipine
Nifedipine may increase digoxin blood concentration
Nifedipine increases the plasma concentration of digoxin
Rifampicin increases the metabolism of nifedipine, leading to reduced plasma concentrations

Key Issues to Note

Administer nifedipine with food and swallow sustained-release tablets without chewing
Advise the patient to avoid alcohol
Advise the patient to rise slowly from a prolonged sitting or lying position
Advise the patient not to stop using the drug suddenly
Inform the patient that excessive hypotension may occur, especially at the beginning of treatment

Amlodipine

Available Preparations:

Tablets: 5 mg, 10 mg
Capsules: 5 mg, 2.5 mg

Available Brands: Norvasc®, Amtas®, Asomex®, Amlong®, Lovasc®, Lofral®, Amlodac®, Amedin®

Pharmacokinetics

Amlodipine is well absorbed following oral administration. It is extensively metabolized in the liver and excreted in the urine.

Indications

Hypertension
Prophylaxis of angina pectoris

Contraindications

Unstable angina
Known hypersensitivity to amlodipine
Breastfeeding

Dosage

Hypertension or Angina: Initially 5 mg once daily, increased after 10-14 days to a max of 10 mg once daily if necessary

Side Effects

Headache
Dizziness
Oedema
Fatigue
Flushes
Hypotension
Malaise
Bradycardia
Palpitations
Taste disturbances
Abdominal pain

Drug Interactions

Cimetidine increases serum levels of amlodipine
Rifampicin may decrease serum concentrations of amlodipine
Erythromycin may reduce clearance of amlodipine
Barbiturates reduce plasma concentrations of amlodipine

Key Issues to Note

Amlodipine may be administered without regard to food but take with caution with grapefruit juice
Inform the patient not to discontinue the drug abruptly
Inform the patient to report to the clinician in case of irregular heartbeat, shortness of breath, swelling of the feet and hands, pronounced dizziness, and hypotension

Angiotensin-Converting Enzyme Inhibitors (ACEIs)

These drugs are useful in the treatment of hypertension and heart failure.

Examples:

Captopril
Enalapril
Ramipril
Lisinopril
Quinapril

Mode of Action

ACE inhibitors act by inhibiting the conversion of angiotensin I to angiotensin II (a powerful vasoconstrictor). This results in relaxation of blood vessels, which lowers blood pressure.

Captopril

Available Preparation:

Tablets: 25 mg

Available Brands: Epistron®, Angiopril®

Pharmacokinetics

Captopril is absorbed throughout the GIT, and the presence of food may reduce absorption. It is distributed to body tissues except the CNS, metabolized in the liver, and excreted in the urine and small amounts in feces.

Indications

Mild to moderate hypertension
Congestive heart failure
Diabetic nephropathy
Prophylaxis after infarction

Contraindications

Hypersensitivity to captopril and other ACE inhibitors
Pregnancy
Hereditary or idiopathic angioedema
Bilateral or single renal artery stenosis

Dosage

Hypertension: Initially 12.5 mg twice daily. Maintenance dose: 25 mg twice daily, max 50 mg twice daily in severe hypertension
Heart Failure (Adjunct): Initially 6.25-12.5 mg under close supervision. Maintenance dose: 25 mg 2-3 times daily, max 150 mg daily
Diabetic Nephropathy: 75-100 mg daily in divided doses

Side Effects

Hypotension
Chest pain
Palpitations
Fatigue
Non-productive cough
Tachycardia
Dyspepsia
Hyperkalemia
Taste disturbances
Malaise

Drug Interactions

Alcohol, diuretics may increase the effect of captopril
NSAIDs may decrease the effect of captopril
Potassium-sparing diuretics, potassium supplements may cause hyperkalemia

Key Issues to Note

Advise the patient to rise slowly to sitting or standing position to minimize orthostatic hypotension
Inform the patient that dizziness, fainting, lightheadedness may occur during the first few days of treatment
Advise the patient to take the drug on an empty stomach about one hour before food
Captopril should not be administered together with antacids because they hinder its absorption
The dose administered and frequency of administration should be reduced in renal impairment

Angiotensin II Receptor Antagonists

These drugs include:

Losartan
Valsartan
Telmisartan

They are normally used as an alternative in patients who cannot tolerate side effects such as dry cough associated with ACE inhibitors.

Mode of Action

They produce a fall in blood pressure by direct antagonism of the vasoconstrictor angiotensin II at the AT1 receptor site.

Losartan

Available Preparations:

Tablets: 50 mg, 100 mg

Available Brands: Losacar®, Tozaar®, Losartec®, Losartas®

Combinations:

Presartan-H50® (Losartan/Hydrochlorothiazide)
Tozaar-H®

Pharmacokinetics

Losartan is readily absorbed from the gastrointestinal tract following oral administration, undergoes first-pass metabolism forming active and inactive metabolites. Losartan is excreted in the urine and feces.

Indications

Hypertension
Diabetic nephropathy

Contraindications

Known hypersensitivity to losartan
Pregnancy (2nd and 3rd trimester)
Lactation

Dosage

Usually 50 mg once daily, increased after several weeks to 100 mg once daily if necessary

Side Effects

Dizziness
Taste disturbance
Myalgia
Fatigue
Diarrhea
Urticaria
Vertigo
Migraine

Drug Interactions

Fluconazole may decrease conversion of losartan to active metabolites resulting in loss of anti-hypertensive effects
NSAIDs may reduce the hypotensive effect of losartan
Potassium-sparing diuretics may increase the risk of hyperkalemia when given together with losartan
Cimetidine may increase the effect of losartan
Alcohol may potentiate the hypotensive effect of losartan

Key Issues to Note

Avoid tasks that require alertness until response to drug is established (possible dizziness effect)
Advise the patient not to take any OTC preparations or nasal decongestants without recommendation of a clinician
Advise the patient not to stop taking the medication unless told by the clinician
The drug may be taken with or without meals

Direct-Acting Vasodilators

These drugs are rarely used as first-line drugs and are reserved for resistant cases of hypertension and for treatment of hypertensive emergencies. These drugs also cause sodium and water retention; therefore, they are useful when combined with diuretics to counteract the sodium retention. They are also combined with beta blockers to prevent the reflex tachycardia.

Examples:

Hydralazine
Minoxidil

Mode of Action

Hydralazine reduces blood pressure by acting directly on the arterial smooth muscle to cause vasodilation and reduction in total peripheral vascular resistance.

Hydralazine

Available Preparations:

Injection: 20 mg/ml
Tablets: 25 mg

Available Brands: Apresoline®

Pharmacokinetics

Orally administered hydralazine is rapidly and completely absorbed from the gastrointestinal tract but undergoes considerable first-pass metabolism in the gastrointestinal mucosa and liver. It is widely distributed, metabolized in the liver by acetylation, and excreted in the urine as metabolites.

Indications

Hypertensive crisis
Moderate to severe hypertension
Moderate to severe chronic congestive heart failure (in combination with long-acting nitrates)
Hypertension secondary to pre-eclampsia/eclampsia

Contraindications

Known hypersensitivity to hydralazine
Severe tachycardia
Heart failure with high cardiac output
Myocardial insufficiency due to mechanical obstruction
Idiopathic systemic lupus erythematosus
Porphyria

Dosage

Hypertension: By mouth 25 mg twice daily, increased to usual max 50 mg twice daily
Heart Failure: 25 mg 3-4 times daily, increased every 2 days if necessary. Maintenance dose: 50-75 mg 4 times daily
By Intravenous Infusion, Hypertension with Renal Complications and Hypertensive Crisis: Initially 200-300 micrograms/minute, maintenance 50-150 micrograms/minute

Side Effects

Headache
Severe tachycardia
Hypotension
Angina
Oedema
Heart failure
Dizziness
Flushing
Palpitations
Joint swelling
Anorexia
Gastrointestinal disturbances

Drug Interactions

Diuretics, other antihypertensives may increase hypotensive effects of hydralazine
Indomethacin may decrease hypotensive effects of hydralazine

Key Issues to Note

Prolonged treatment of more than 6 months may induce lupus-like syndrome
Beta blockers and thiazides are often used with hydralazine to prevent tachycardia and fluid retention
Advise the patient to avoid driving until the effect of the drug is established

Centrally Acting Antihypertensive Drugs

These drugs are effective antihypertensives but are no longer considered drugs of choice as they are less tolerated than other antihypertensives. Methyldopa is a drug of choice in the treatment of hypertension in pregnancy.

Examples:

Methyldopa
Clonidine

Mode of Action

These drugs reduce blood pressure by acting in the CNS to reduce the activity of the sympathetic nervous system.

Methyldopa

Available Preparations:

Tablets: 250 mg

Available Brands: Aldomet®, Medopress®

Pharmacokinetics

Methyldopa is variably absorbed from the gastrointestinal tract when taken orally, crosses the blood-brain barrier, is extensively metabolized in the liver, and excreted in urine.

Indications

Hypertension, especially in pregnancy

Contraindications

Hypersensitivity to methyldopa
Active liver disease
Depression
Phaeochromocytoma
Porphyria

Dosage

Adult: Initially 250 mg 2-3 times daily, increased gradually at an interval of at least 2 days until the desired response is obtained, max 3 g daily
Elderly: Initially 125 mg twice daily, increased gradually, max 2 g daily

Side Effects

Sedation
Dry mouth
Stomatitis
Myalgia
Impaired mental acuity
Impotence
Hemolytic anemia
Dizziness
Constipation
Oedema
Postural hypotension
Decreased libido
Bradycardia

Drug Interactions

Enhanced hypotensive effect when methyldopa is given with ACE inhibitors, alcohol, atenolol, or propranolol
Methyldopa may impair tolbutamide metabolism, enhancing its hypoglycemic effects
Hypotensive effect of methyldopa is antagonized by NSAIDs
Hypotensive effect of methyldopa is antagonized by estrogen
Oral iron therapy reduces the bioavailability of methyldopa

Key Issues to Note

Methyldopa may be administered with or without regard to food
Advise the patient to avoid alcohol during treatment
Warn the patient that methyldopa may cause drowsiness and impair activities requiring mental alertness
Advise the patient to rise slowly from a prolonged sitting or lying position
Inform the patient that transient sedation or depression may occur
Advise the patient not to stop the drug abruptly

Alpha Adrenoceptor Blocking Drugs

These drugs may be used in combination with other drugs in the treatment of resistant hypertension. In addition to lowering blood pressure, they also improve urinary flow rates in benign prostatic hypertrophy.

Examples:

Prazosin
Doxazosin
Terazosin

Mode of Action

These drugs competitively inhibit postsynaptic alpha receptors, which results in vasodilation of veins and arterioles. This leads to a decrease in total peripheral resistance and blood pressure. They also block alpha receptors in non-vascular smooth muscle (e.g., the bladder neck), where alpha-blockade reduces resistance to urinary flow.

Prazosin

Available Preparations:

Tablets: 1 mg, 2 mg, 5 mg

Available Brands: Hypovase®, Minipress®

Pharmacokinetics

Prazosin is well absorbed after oral administration, extensively metabolized in the liver, and excreted in urine.

Indications

Hypertension
Congestive heart failure
Benign prostatic hyperplasia
Raynaud’s syndrome

Contraindications

Hypersensitivity to quinazolines
Congestive heart failure due to mechanical obstruction

Dosage

Hypertension: 0.5 mg twice daily, increased to 1 mg 2-3 times daily after 3-7 days, maintenance dose 20 mg daily in 2-3 divided doses
Heart Failure: 0.5 mg 2-4 times daily, increased to 4 mg daily in divided doses, maintenance dose 4-20 mg daily in divided doses
Benign Prostate Hyperplasia: Initially 0.5 mg twice daily for 3-7 days, maintenance dose 2 mg twice daily
Raynaud’s Syndrome: Initially 0.5 mg twice daily, increased if necessary after 3-7 days to the usual maintenance dose 1-2 mg twice daily

Side Effects

Headache
Dry mouth
Drowsiness
Oedema
Postural hypotension
Urinary incontinence
Priapism
Urinary frequency
Weakness
Palpitations
Nausea
Somnolence

Drug Interactions

Estrogen, NSAIDs may decrease the effect of prazosin
Concomitant use with propranolol or other beta blockers may cause severe hypotension

Key Issues to Note

Advise the patient to avoid alcohol
Inform the patient that prazosin may cause dizziness or drowsiness and impair the ability to perform activities requiring alertness
Advise the patient to rise slowly from sitting or lying position
Advise the patient to take the first dose of prazosin at bedtime to avoid dizziness

Drugs for Heart Failure

Heart failure is a clinical syndrome caused by the inability of the heart to pump sufficient blood to meet the metabolic demands of the body. Inadequate perfusion of the tissues leads to a variety of symptoms such as breathlessness, fatigue, and oedema. Drugs used in the treatment of heart failure include:

Diuretics
Cardiac glycosides
ACE inhibitors
Beta blockers

Diuretics

Diuretics are the first-line drugs in the treatment of heart failure. They are recommended in all patients with clinical evidence of fluid retention.

Classification of Diuretics

Diuretics are classified as follows:

Loop diuretics
Thiazide diuretics
Potassium-sparing diuretics
Carbonic anhydrase inhibitors

Loop Diuretics

Loop diuretics are potent diuretics used in the treatment of moderate to severe heart failure. They may be used alone or in combination with thiazides, especially metolazone, to achieve a profound diuresis.

Examples:

Frusemide
Bumetanide

Mode of Action

Loop diuretics inhibit reabsorption of sodium chloride from the ascending limb of the loop of Henle.

Frusemide

Available Preparations:

Tablets: 40 mg
Injection: 20 mg/ml

Available Brands: Lasix®, Agomide®, Frusina®

Pharmacokinetics

Frusemide is well absorbed from the GIT and excreted in the urine and partially metabolized in the liver and feces.

Indications

Oedema
Hypertension

Contraindications

Renal failure with anuria
Dehydration
Known hypersensitivity to frusemide
Hyponatraemia
Severe hypokalaemia
Severe hypernatraemia
Hypercalcaemia
Associates with liver cirrhosis

Dosage

Adult:

Oedema: Oral, initially 40 mg in the morning, maintenance 20-40 mg, 80 mg or more in resistant oedema
Children: 1-3 mg/kg daily, max 40 mg daily

Hypertension: 20-40 mg twice daily

Slow IV/IM: Initially 20-50 mg, increased if necessary in steps of 20 mg, not less than every 2 hours, doses greater than 50 mg by IV infusion only, max 20 mg daily

Side Effects

Gout
Rash
Nausea
Hypotension
Hypokalaemia
Hyponatraemia
Hypomagnesaemia
Hyperglycaemia
Tinnitus
Deafness
Dehydration
Abdominal cramps
Diarrhoea or constipation

Drug Interactions

Amphotericin B may increase the risk of nephrotoxicity caused by frusemide
Frusemide may decrease the effect of anticoagulants
Frusemide may increase the risk of lithium toxicity
Gentamycin may increase the risk of ototoxicity when given concurrently with frusemide
Cephalosporins enhance the nephrotoxicity caused by frusemide
Frusemide may increase the risk of digoxin toxicity

Key Issues to Note

Frusemide may be administered with food or milk to minimize GI distress
Frusemide may cause photosensitivity reactions (e.g., exposure to sunlight may cause severe sunburn)

Thiazide and Related Diuretics

Thiazide diuretics are used in the treatment of mild heart failure and are the diuretics of choice in the treatment of hypertension. They are relatively weak to be used alone in heart failure.

Examples:

Bendrofluazide
Hydrochlorothiazide
Chlorthalidone
Metolazone

Mode of Action

They act by inhibiting sodium and chloride reabsorption at proximal sites of the distal convoluted tubule. Excretion of potassium and magnesium is also enhanced, while calcium excretion is diminished.

Bendrofluazide

Available Preparations:

Tablets: 5 mg

Available Brands: Aprinox®, Benduric®

Pharmacokinetics

Bendrofluazide is completely absorbed from the gastrointestinal tract, a small percentage is metabolized in the liver, and is excreted unchanged in the urine.

Indications

Oedema
Hypertension

Contraindications

Hypersensitivity to bendrofluazide
Refractory hypokalaemia
Hyponatraemia
Symptomatic hyperuricaemia
Hypercalcaemia
Addison’s disease

Dosage

Oedema: Initially 5-10 mg daily in the morning or on alternate days, maintenance 5-10 mg 1-3 times weekly
Hypertension: 2.5 mg daily in the morning, higher doses rarely necessary

Side Effects

Gout
Fatigue
Impotence
Hypokalaemia
Hyperglycaemia
Hyponatraemia
Nausea
Dizziness
Postural hypotension
Hypomagnesaemia

Drug Interactions

The effects of digoxin may be increased by bendrofluazide
NSAIDs may reduce the diuretic effect of bendrofluazide
Bendrofluazide may increase lithium levels in the blood

Potassium-Sparing Diuretics

These drugs are relatively weak diuretics as single drugs for heart failure and are not effective for use alone in heart failure. They are used in combination with other diuretics to prevent loss of potassium caused by thiazide or loop diuretics.

Example:

Spironolactone

Mode of Action

They inhibit sodium reabsorption in the distal tubule by antagonizing aldosterone. As a result, distal tubule sodium-potassium exchange is reduced.

Spironolactone

Available Preparations:

Tablets: 25 mg, 50 mg

Available Brands: Aldactone®

Pharmacokinetics

Spironolactone is well absorbed from the gastrointestinal tract, metabolized in the liver, and excreted in urine and feces.

Indications

Liver cirrhosis associated with refractory oedema and ascites
Ascites associated with malignancy
Oedema in congestive heart failure
Nephrotic syndrome
Hypertension
Primary hyperaldosteronism

Contraindications

Pregnancy
Hyperkalaemia
Addison’s disease
Breastfeeding
Hyponatraemia
Severe renal impairment

Dosage

Congestive Heart Failure: 100 mg daily, increased to 400 mg daily in severe cases, maintenance dose 25-200 mg/day
Oedema: Initially 100 mg daily, maintenance 25-200 mg daily
Hypertension: 25-100 mg once daily
Nephrotic Syndrome: 100-200 mg/day

Side Effects

Ataxia
Nausea and vomiting
Confusion
Diarrhoea
Dehydration
Deepening of the voice
Menstrual irregularities
Hyperkalaemia
Hyponatraemia
Fever
Weakness
Headache
Impotence
Skin rash
Drowsiness
Renal impairment
Gynaecomastia

Drug Interactions

Serum concentration of digoxin may be increased when given together with spironolactone
NSAIDs may decrease the antihypertensive effects of spironolactone
Potassium supplements, ACE inhibitors, angiotensin II antagonists may increase the risk of hyperkalaemia caused by spironolactone
Spironolactone may decrease the anticoagulant effect of heparin

Key Issues to Note

Spironolactone may be administered with food
It may cause drowsiness and impair the ability to perform activities requiring mental alertness

Osmotic Diuretics

These drugs include:

Mannitol

Mode of Action

Osmotic diuretics induce diuresis by elevating the osmolarity of the glomerular filtrate, thereby hindering the tubular reabsorption of water. Excretion of sodium and chloride is increased.

Mannitol

Available Preparation:

Intravenous infusion: 20%

Pharmacokinetics

Following intravenous infusion, mannitol is excreted rapidly by the kidneys before any significant metabolism can take place in the liver.

Indications

Cerebral oedema
Acute anuria
Acute renal failure due to massive haemorrhage, trauma, shock, and major surgery
To promote urinary excretion of toxic substances (e.g., lithium and salicylates)

Contraindications

Pulmonary oedema
Intracranial bleeding
Congestive heart failure
Hypersensitivity to mannitol
Severe dehydration
Renal failure (anuria)

Dosage

Cerebral Oedema: By IV infusion 1 g/kg as a 20% solution
Diuresis: By IV infusion 50-200 g over 24 hours, preceded by a test dose of 200 mg/kg by slow intravenous injection

Side Effects

Oedema
Thrombophlebitis
Chills
Hypotension
Headache
Fever
Thirst
Electrolyte imbalance
Circulatory overload
Nausea and vomiting
Increased urinary frequency and urine volume

Drug Interactions

Mannitol may increase the risk of digoxin toxicity associated with mannitol-induced hypokalaemia

Hyperlipidaemia

Hyperlipidaemia refers to the presence in the blood of an abnormally high concentration of cholesterol and/or triglycerides in the form of lipoproteins. It may be divided into two:

Primary hyperlipidaemia
Secondary hyperlipidaemia

Primary hyperlipidaemia is where the raised plasma lipid concentration is the result of a genetic defect.

Secondary hyperlipidaemia may be due to metabolic problems such as diabetes mellitus, chronic renal failure, excessive alcohol intake, hypothyroidism, etc.

The main risk is atherosclerosis, in which fatty deposits called atheroma build up in the arteries, restricting and disrupting the flow of blood. The restriction of blood flow may lead to the formation of blood clots resulting in a stroke or heart attack.

Drugs used in the treatment of hyperlipidaemia include:

Statins
Bile acid binding resins
Fibrates
Nicotinic acid and its derivatives
Others (omega-3)

Statins

Statins include drugs such as:

Simvastatin
Atorvastatin
Fluvastatin
Pravastatin

Mode of Action

Statins competitively inhibit 3-hydroxy methylglutaryl co-enzyme (HMG-CoA) reductase enzyme, the rate-limiting enzyme in cholesterol synthesis, especially in the liver.

Atorvastatin

Available Preparations:

Tablets: 10 mg, 20 mg

Available Brands: Lipitor®, Atorva®, Atostin®, Lipiget®

Pharmacokinetics

Atorvastatin is rapidly absorbed from the gastrointestinal tract, undergoes first-pass metabolism, is metabolized in the liver, and excreted as metabolites in bile.

Indications

Combined or mixed hyperlipidaemia
Prevention of cardiovascular events in patients with type 2 diabetes
Primary hypercholesterolemia

Contraindications

Hypersensitivity to atorvastatin
Active liver disease
Pregnancy
Lactation

Dosage

Adults: Initially 10 mg daily, adjusted according to response at intervals of 4 weeks to 40 mg/day max
Children (10-17 years): 10 mg once daily
Prevention of Cardiovascular Events: 10 mg once daily

Side Effects

Insomnia
Weight gain
Back pain
Nausea
Skin rash
Impotence
Anorexia
Dizziness
Chest pain
Malaise
Headache
Muscle pain or weakness
Tinnitus
Peripheral neuropathy
Angina

Drug Interactions

Atorvastatin may increase the anticoagulant effect of warfarin, digoxin, itraconazole, oral contraceptives
May increase atorvastatin blood concentration resulting in severe muscle inflammation, pain, and weakness
Antacids and propranolol decrease atorvastatin activity
Clarithromycin and erythromycin elevate plasma concentrations of atorvastatin

Key Issues to Note

Take atorvastatin with or without regard to meals but preferably in the evening
Advise the patient to report symptoms of myalgia, muscle tenderness, weakness, or gastric upset
Female patients of childbearing age should be advised to use effective contraception

Blood and Blood Forming Organs

Anticoagulants

These are drugs that prevent the clotting of blood. Anticoagulants help to maintain normal blood flow in people who are at risk of clot formation. They can either prevent the formation of blood clots or stabilize an existing clot so that it does not break.

Anticoagulants are divided into two categories:

Parenteral anticoagulants
Oral anticoagulants

Parenteral Anticoagulants

These drugs are normally used when immediate action is required.

Examples:

Heparin
Enoxaparin (low molecular weight heparin)

Heparin

Available Preparations:

Injection: 5000 IU/ml

Available Brands: Cal-heparin®, Heparen®

Pharmacokinetics: After intravenous or subcutaneous injection, the onset of action is immediate, within 1-2 hours. Heparin is extensively bound to plasma proteins and is excreted in the urine mainly as metabolites.

Indications:

Deep vein thrombosis
Pulmonary embolism
Prophylaxis in general and gynecological surgery
Prophylaxis in orthopedic surgery
Myocardial infarction
Unstable angina

Contraindications:

Hemophilia
Severe hypertension
Recent eye surgery
Peptic ulcers
Known hypersensitivity to heparin
Acute bacterial endocarditis
Thrombocytopenia
Severe liver disease

Dosage:

Deep Venous Thrombosis, Pulmonary Embolism, and Unstable Angina:

Adults: By IV injection, loading dose of 5000 units (10,000 units in severe pulmonary embolism), followed by continuous infusion of 18 units/kg/hour or by SC injection of 15,000 units every 12 hours.
Children and small adults: Loading dose 50 units/kg, then 15-25 units/kg/hour by intravenous infusion or subcutaneous injection of 250 units/kg every 12 hours.

Side Effects:

Hemorrhage
Hyperkalemia
Chills
Epistaxis
Thrombocytopenia
Anaphylaxis
Headache
Nausea and vomiting
Urticaria

Drug Interactions:

Heparin increases the risk of hemorrhage when given together with oral anticoagulants like warfarin.

Key Issues to Note:

Advise the patient to report any signs of bleeding from the gums, under the skin, urine, or stool.
Advise the patient to limit alcohol intake during treatment.
Do not administer IM due to pain, irritation, and hematoma formation.
When given together with oral anticoagulants, heparin should be withdrawn once effective oral anticoagulation is established.

Oral Anticoagulants

Oral anticoagulants are effective in the primary and secondary prevention of venous thromboembolism.

Examples:

Warfarin

Warfarin

Available Preparations:

Tablets: 3 mg, 5 mg

Available Brands: Marevan®

Pharmacokinetics: Warfarin is readily absorbed from the gastrointestinal tract, crosses the placenta but does not occur in significant quantities in breast milk. It is extensively metabolized in the liver and excreted in urine and bile.

Indications:

Prophylaxis of embolism in rheumatic heart disease and atrial fibrillation
Prophylaxis after insertion of prosthetic heart valve
Prophylaxis and treatment of venous thrombosis and pulmonary embolism
Myocardial infarction

Contraindications:

Hypersensitivity to the drug
Peptic ulcer
Severe hypertension
Bacterial endocarditis
Pregnancy
Alcoholism
Bleeding disorders

Dosage:

Initially 5 mg daily for 2-5 days, then adjust according to response to the usual maintenance dose of 3-9 mg daily.

Side Effects:

Hemorrhage
Rash
Jaundice
Hepatic dysfunction
Vomiting
Skin rash
Nausea and vomiting
Hypersensitivity
Diarrhea
Headache
Pancreatitis
Urticaria
Abdominal cramps

Drug Interactions:

Drugs that decrease warfarin anticoagulant effect include alcohol, carbamazepine, phenytoin, cholestyramine, rifampicin, oral contraceptives, and vitamin K.
Concomitant use with amiodarone, metronidazole, cimetidine, and streptokinase may increase the anticoagulant effect of warfarin.

Key Issues to Note:

Warn the patient that bleeding may occur, especially at the beginning of treatment and with high doses.
Warfarin may be administered on an empty or full stomach.
Adequate anticoagulation is not observed until about 3-4 days after initial administration of warfarin; heparin should be used concurrently if immediate effect is required.

Antiplatelet Drugs

Antiplatelet drugs inhibit thrombus formation by decreasing platelet aggregation. They are used to prevent further thromboembolic events in patients who have suffered myocardial infarction, ischemic stroke or transient ischemic attacks, or unstable angina.

Examples:

Aspirin (low dose)
Clopidogrel
Dipyridamole

Aspirin

Available Preparations:

Tablets: 75 mg, 100 mg

Available Brands: Ecorin®, Aspirem®, Ascard®, Bayer Aspirin Cardio®

Indications:

Acute myocardial infarction
Unstable angina
Primary and secondary prevention of stroke

Contraindications:

Children and adolescents under 16 years
Hypersensitivity to aspirin or NSAIDs
Aspirin-sensitive asthma
Active peptic ulcer
Breastfeeding
Hemophilia

Dosage:

75 mg daily. 150-300 mg daily may be required in acute conditions (MI, acute ischemic stroke, unstable angina).

Side Effects:

Bronchospasms
Nausea and vomiting
Increased bleeding time
Urticaria
Ringing in the ears
Dizziness
Heartburn
Gastrointestinal bleeding

Drug Interactions:

Aspirin increases the risk of bleeding when given together with oral anticoagulants and heparin.
Aspirin decreases the diuretic effect of spironolactone and frusemide.
Aspirin decreases the antihypertensive effect of captopril and beta-blockers.

Key Issues to Note:

The drug should be administered with food.
Avoid alcohol while taking aspirin.
Avoid use of OTC preparations for pain without recommendation of a clinician.

Thrombolytics

Thrombolytics are drugs used to break up or dissolve blood clots that have already formed. Thrombolytic enzymes are used to lyse the thrombi that obstruct coronary or pulmonary arteries.

Examples:

Streptokinase
Urokinase

Mode of Action: They act by converting plasminogen to plasmin, which catalyzes the breakdown of fibrin and therefore is able to dissolve blood clots.

Streptokinase

Available Preparations:

Injection: 1,500,000 IU

Available Brands: Stpase®

Indications:

Acute myocardial infarction
Deep vein thrombosis
Pulmonary embolism
Acute arterial thromboembolism

Contraindications:

Active internal bleeding
Recent trauma to the head
Severe uncontrollable hypertension
Uncontrollable clotting disorders
Intracranial surgery
Recent cerebral vascular accident
Severe allergic reactions
Recent abortion or delivery

Dosage:

Myocardial Infarction: IV infusion 1,500,000 units over 30-60 minutes.
Deep Vein Thrombosis, Pulmonary Embolism, Acute Arterial Thromboembolism, Arterial Thrombosis: By IV infusion 250,000 units infused over 30 minutes, then 100,000 units/hour for up to 12-72 hours according to the patient\’s condition.

Side Effects:

Fever
Headache
Skin rash and itching
Vomiting
Convulsions
Nausea
Nephritis
Hypotension
Malaise
Superficial bleeding at puncture site

Drug Interactions:

Heparin, oral anticoagulants, aspirin, dipyridamole may increase the risk of bleeding when given together with streptokinase.

Antifibrinolytic Drugs

These drugs inhibit the dissolution of blood clots.

Examples:

Tranexamic acid

Tranexamic Acid

Available Preparations:

Tablets/Capsules: 500 mg

Available Brands: Tranlok®, Hemsamic®

Combinations: Tranfib-MF® (tranexamic acid/mefenamic acid) 500/250

Mode of Action: Tranexamic acid acts primarily by blocking the binding of plasminogen and plasmin to fibrin.

Pharmacokinetics: Tranexamic acid is rapidly and completely absorbed from the GIT, crosses the placenta, distributes into breast milk. It is metabolized in the liver and excreted in urine.

Indications:

Menorrhagia
Prevention of bleeding in prostatectomy and dental extraction in patients with hemophilia
Epistaxis
Thrombolytic overdose
Prophylaxis of hereditary angioedema

Contraindications:

Hypersensitivity to tranexamic acid
Severe renal impairment
Thromboembolic disease

Dosage:

Oral:

Menorrhagia (inhibited when menstruation has started): 1 g 3 times daily for 3-4 days
Hereditary Angioedema: 1-1.5 g 2-3 times daily
Epistaxis: 1 g 3 times daily for 7 days

Side Effects:

Nausea
Diarrhea
Thrombosis
Vomiting
Hypotension
Disturbances in color vision

Drug Interactions:

Heparin, oral anticoagulants, aspirin, dipyridamole may increase the risk of bleeding when given together with tranexamic acid.

Drugs Used in the Treatment of Anaemia

Anaemia is defined as a decrease in hemoglobin concentration below that necessary for tissue oxygenation. It may be caused by increased RBC loss, decreased production of RBCs, or increased destruction of RBCs.

Ferrous Sulphate

Available Preparations:

Tablets: 200 mg

Available Brands: Cyano Iron®, Ferol®

Indications:

Iron deficiency anaemia

Contraindications:

Haemolytic anaemias
Peptic ulcer disease
Patients receiving blood transfusion
Hemosiderosis
Haemochromatosis

Dosage:

Iron Deficiency Anaemia: 200 mg 2-3 times daily
Prophylaxis of Anaemia: 200 mg daily

Side Effects:

Constipation
Diarrhea
Anorexia
Epigastric pain
Dark stool
Gastrointestinal irritation
Nausea

Drug Interactions:

Antacids and cimetidine decrease the absorption of ferrous sulphate
Chloramphenicol may increase the serum levels of ferrous sulphate
Ferrous sulphate decreases the anti-infective effect of quinolones when given concurrently
The drug may be given with meals

Folic Acid

Available Preparations:

Tablets: 5 mg

Available Brands: Folacid®, Asflic®, Folon®

Pharmacokinetics: Folic acid is rapidly absorbed from the gastrointestinal tract, distributed to all body tissues, metabolized in the liver to the active form, and excreted in urine.

Indications:

Folate-deficient megaloblastic anaemia
Prophylaxis in chronic hemolytic states or renal dialysis
Prevention of neural tube defects in pregnancy
Nutritional supplement

Contraindications:

Folate-dependent malignant disease
Aplastic anaemia
Hypersensitivity to folic acid

Dosage:

Megaloblastic Anaemia: 5 mg once daily for 4 months, up to 15 mg daily may be given in malabsorption states
Prevention of Neural Tube Defect: 400 micrograms daily before conception and during the first 12 weeks of pregnancy
Prevention of Recurrence of Neural Tube Defect: 5 mg daily from at least 4 weeks before conception until 12 weeks of pregnancy
Children (Folic Acid Deficiency): 1-2 mg daily

Side Effects:

Nausea
Headache
Insomnia
Irritability
Skin rash
Fever
Diarrhea
Bronchospasm

Drug Interactions:

Folic acid may decrease serum phenytoin concentrations
Antifolate drugs such as trimethoprim may interfere with folic acid metabolism and may cause deficiency in patients with low folic acid stores
Chloramphenicol may antagonize the hematologic response to folic acid

Combination Preparations: Ferrous Salts with Folic Acid

Available Preparations:

Capsules
Suscaps
Tablets

Available Brands: Aktiferrin-F®, Fefol®, Fef®, Fefan®

Indications:

Prevention of iron and folic acid deficiencies in pregnancy, after delivery, and lactation

Contraindications:

Known hypersensitivity to any of the ingredients

Dosage:

One capsule/suscap/tablet once daily

Side Effects:

Sensation of fullness
Nausea and vomiting
Diarrhea
Constipation

Drugs Used in the Treatment of Cardiovascular Disorders Read More »

Drugs Acting on the Respiratory System

Drugs used in the treatment of respiratory tract disorders include:

Drugs for Asthma
Drugs for Allergic Rhinitis
Drugs for Cough
Drugs for Common Cold and Flu

Drugs Used in the Treatment of Asthma

Asthma is a chronic disease of the airways characterized by inflammation and reversible bronchospasm. It is associated with symptoms such as wheezing, breathlessness, chest tightness, and cough. Drugs used in the treatment of asthma are broadly divided into two categories:

Bronchodilators
Anti-inflammatory drugs

Table 1: Classification of Anti-Asthmatic Drugs

Class	Examples
Bronchodilators	Beta2 agonists, Xanthine derivatives, Anticholinergics
Anti-inflammatory drugs	Corticosteroids, Mast cell stabilizers, Leukotriene receptor antagonists

Beta2 Agonists

Beta2 agonists promote bronchodilation by stimulating beta2 receptors in bronchial smooth muscles. They are further divided into short-acting and long-acting beta2 agonists.

Short-acting beta2 agonists such as salbutamol and terbutaline have a rapid onset and short duration of action. They are recommended for the treatment of acute asthma attacks.
Long-acting beta2 agonists such as salmeterol and formoterol have a delayed onset and long duration of action. These drugs are usually combined with inhaled corticosteroids such as budesonide for the long-term control of chronic asthma.

Salbutamol

Available Preparations:

Inhaler: 100 mcg
Nebulized solution: 5 mg/ml
Syrup: 2 mg/5 ml
Tablets: 4 mg

Available Brands: Ventolin®, Vental®, Kamvent®

Pharmacokinetics: Salbutamol is readily absorbed from the gastrointestinal tract, metabolized in the liver, rapidly excreted in the urine as metabolites and as unchanged drug, and a small amount is excreted in the feces.

Indications:

Prophylaxis and treatment of asthma
Chronic obstructive pulmonary disease
Arrest premature labor

Contraindications:

Hypersensitivity to salbutamol
Eclampsia and severe preeclampsia

Dosage:

Oral:

Adults: 4 mg 3-4 times daily, max single dose 8 mg

Children:

7-12 years: 2 mg 3-4 times daily
2-6 years: 1-2 mg 3-4 times daily
1 month-2 years: 100 mcg/kg 3-4 times daily

Aerosol Inhalation:

Adults: 100-200 mcg (1-2 puffs, for persistent symptoms up to 4 times daily)
Children: 100 mcg (1 puff), increased to 200 mcg (2 puffs) if necessary, for persistent symptoms up to 4 times daily

Nebulized Solution:

Children: > 2 years: 2.5-5 mg, repeat 3-4 times daily as necessary
Children: < 2 years: 0.1 mg/kg up to 2.5 mg, repeat 3-4 times daily

Prophylaxis in Exercise-Induced Bronchospasm:

Adults: 200-400 mcg (2 puffs)
Children: 100-200 mcg up to 4 times daily

Side Effects:

Tachycardia
Arrhythmias
Nervousness
Angioedema
Fine tremor, especially of hands
Hypersensitivity reactions
Palpitations
Insomnia
Muscle cramps
Headache

Drug Interactions:

Diuretics or digoxin: risk of cardiac arrhythmias is increased
Corticosteroids: risk of hypokalemia and hyperglycemia is increased

Key Issues to Note:

Salbutamol may delay labor in pregnant mothers near term
Patients should swallow tablets whole with a glass of water
Do not administer salbutamol within 1 hour of ingesting antacids, milk, or dairy products
Salbutamide is habit-forming; therefore, long-term use may result in laxative dependency and loss of normal bowel function
Onset of action is 6-12 hours for tablets, 15-60 minutes for suppository
Warn the patient that prolonged use of salbutamol suppositories may cause proctitis

Xanthines

Xanthines include:

Aminophylline
Theophylline

They act by relaxing bronchial smooth muscle by inhibiting phosphodiesterase, the enzyme which breaks down cyclic AMP. Aminophylline is usually preferred to theophylline when greater solubility in water is required, particularly in intravenous formulations.

Aminophylline

Available Preparations:

Tablets: 100 mg
Injection: 250 mg/10 ml

Indications:

Acute severe asthma
Reversible airway obstruction
Relieve apnea in neonates
Nocturnal asthma

Contraindications:

Porphyria
Known hypersensitivity to aminophylline

Dosage:

Chronic Asthma:

Oral: 100-200 mg 3-4 times daily, after food

Acute Severe Asthma (not treated with theophylline before):

Adults: IV loading dose 5-6 mg/kg slowly over 20-30 min diluted in normal saline or dextrose 5%

Maintenance: IV infusion 0.5 mg/kg/hour

Children: IV loading dose 4-6 mg/kg slowly over 20-30 min suitably diluted and 1.5-2.5 mg per kg in those using oral theophylline

Maintenance: By IV infusion

6 months-9 years: 1 mg/kg/hour
10-16 years: 0.8 mg/kg/hour

Side Effects:

Restlessness
Anxiety
Palpitations
Insomnia
Convulsions
Urticaria
Gastrointestinal irritation
Hypotension, especially if given by rapid injection
Tremor
Headache
Dizziness
Arrhythmias
Epigastric pain

Drug Interactions:

Beta blockers: may decrease the effects of aminophylline
Cimetidine, ciprofloxacin, erythromycin, norfloxacin: may increase aminophylline blood concentration and risk of aminophylline toxicity
Phenytoin, rifampicin, carbamazepine: may increase aminophylline metabolism
Smoking: may decrease aminophylline blood concentration
Caffeine: may intensify the adverse effects of aminophylline on the CNS and heart

Key Issues to Note:

Rapid IV injection should be avoided as it may result in hypotension, seizures, and arrhythmias (less than 20-25 mg/min) is required
Patients taking oral aminophylline should not receive intravenous aminophylline unless plasma concentration is available to guide dosage
Patients should avoid caffeine-containing beverages and other sources of caffeine

Corticosteroids

Corticosteroids may be given parenterally, orally, or as inhalers. Inhaled corticosteroids include:

Beclomethasone
Budesonide
Fluticasone

These drugs are the most effective in the treatment of chronic asthma. Corticosteroids reduce bronchial mucosal inflammation and bronchial hyper-reactivity. They are recommended for the prophylaxis of asthma in patients who have not responded to beta2 agonists or if symptoms disturb sleep more than once a week. Corticosteroid inhalers must be used regularly for effective control of symptoms. Alleviation of symptoms usually occurs after 7 days of initiating treatment.

Beclomethasone

Available Preparations:

Metered Inhaler: 50 mcg

Available Brands: Becotide®, Beclate®

Indications:

Prophylaxis of asthma

Contraindications:

Status asthmaticus
Hypersensitivity to beclomethasone
Acute infections uncontrolled by antimicrobial chemotherapy

Dosage:

Adults: 200 mcg twice daily or 100 mcg 3-4 times daily
Children: 50-100 mcg 2-4 times daily or 100 mcg twice daily

Side Effects:

Oropharyngeal candidiasis
Hoarseness
Paradoxical bronchospasm
Adrenal suppression
Impaired bone metabolism
Glaucoma and cataracts

Systemic Corticosteroids

These drugs are given either orally or by injection. Examples include:

Prednisolone/Prednisone
Betamethasone
Triamcinolone
Hydrocortisone
Dexamethasone
Methylprednisolone

Table 2: Characteristics of Corticosteroids

Class	Examples
Short-acting	Hydrocortisone
Intermediate-acting	Prednisolone, Prednisone, Methylprednisolone, Triamcinolone
Long-acting	Dexamethasone, Betamethasone

Prednisolone

Available Preparations:

Tablets: 5 mg

Available Brands: Kampred®

Indications:

Bronchial asthma
Cerebral edema
Allergic reactions
Acute leukemia
Rheumatic disease
Inflammatory bowel disease
Suppression of inflammatory reactions
Acute or chronic adrenal insufficiency

Contraindications:

Systemic infection (unless life-threatening)
Avoid live virus vaccines
Hypersensitivity to prednisolone

Dosage:

Initially: 10-20 mg daily (up to 60 mg in severe diseases) preferably taken in the morning after breakfast, and often be reduced within a few days but may need to be continued for several weeks or months
Maintenance: 2.5-15 mg daily but higher doses may be needed
Children:

1-6 years: 5 mg daily up to 15 mg in severe cases
7-12 years: 5-10 mg daily up to 30 mg in severe cases

Side Effects:

Dyspepsia
Osteoporosis
Glaucoma
Skin atrophy
Weight gain
Menstrual irregularities
Peptic ulcer
Increased appetite
Acne
Adrenal suppression
Striae

Drug Interactions:

Prednisolone may decrease the effect of diuretics, insulin, oral antidiabetics, and potassium supplements
Prednisolone may increase the risk of digoxin toxicity caused by hypokalemia
Prednisolone may decrease the patient\’s antibody response to vaccines

Key Issues to Note:

Take the drug after meals, with food or milk to decrease GI upset
Advise the patient to avoid alcohol, limit caffeine
Advise the patient not to decrease the dose or discontinue without doctor\’s approval

Dexamethasone

Available Preparations:

Tablets: 0.5 mg
Injection: 4 mg/ml

Available Brands: Dexona®

Pharmacokinetics: Dexamethasone is readily absorbed from the gastrointestinal tract, crosses the placenta with minimal inactivation, and is excreted in urine within 24 hours.

Indications:

Cerebral edema
Rheumatic diseases
Anaphylaxis
Septic shock
Nausea and vomiting due to anti-cancer drugs
Bacterial meningitis (in combination with antibiotics)
Acute exacerbation of chronic allergic disorders

Contraindications:

Hypersensitivity to dexamethasone
Systemic infections
Avoid live virus vaccines

Dosage:

Oral:

Adults: 0.5-2 mg daily but higher doses may be required depending on the severity of the condition
Children: 100-1000 mcg/kg daily in 1-2 divided doses

Injection:

Adults: 1M or slow IV or infusion: 0.5-24 mg daily
Children: 200-400 mcg/kg daily in 1-2 divided doses

Cerebral Edema Associated with Malignancy:

IV injection (as dexamethasone phosphate): initially 10 mg then 4 mg by IM every 6 hours for 2-4 days gradually reduced and stopped over 5-7 days
Children: IV 0.25 mg/kg/day in divided doses for up to 2 days then gradually taper down over the next 5 days

Side Effects:

Hypertension
Hyperglycemia
Edema
Glaucoma
Weight gain
Growth suppression in children
Increased appetite
Muscle atrophy
Cataracts
Peptic ulcer
Hypokalemia

Drug Interactions:

Increased risk of hypokalemia when used concurrently with amphotericin B or loop diuretics
Concurrent use with aspirin may lead to increased gastrointestinal tract side effects

Key Issues to Note:

Administer the drug with food or milk to minimize GI side effects
Advise the patient to avoid alcohol and limit caffeine intake
Advise the patient to avoid exposure to measles or chickenpox
Inform the patient not to decrease the dose or stop treatment without doctor\’s recommendation

Hydrocortisone

Available Preparations:

Injection: 100 mg

Available Brands: Cardilan®, Primacort®, Stricort®

Indications:

Hypersensitivity reactions including anaphylaxis
Inflammatory bowel disease
Asthmatic attack
Hemorrhoids
Rheumatic diseases
Adrenocortical insufficiency
Angioedema

Contraindications:

Systemic infections
Avoid live virus vaccines in those receiving immunosuppressive doses
Hypersensitivity to hydrocortisone

Dosage:

Anaphylaxis; Acute Severe Asthma and Shock:

IV slow IV injection or infusion:

Adults: 100-500 mg 3-4 times daily

Children:

6-12 years: 100 mg 3-4 times daily
1-5 years: 50 mg 3-4 times daily
Up to 1 year: 25 mg 3-4 times daily

Side Effects:

Dyspepsia
Adrenal suppression
Weight gain
Glaucoma
Nausea
Peptic ulceration
Menstrual irregularities
Increased appetite
Acne
Malaise

Drug Interactions:

Anti-convulsants, rifampicin: reduce the effectiveness of hydrocortisone
Hydrocortisone: reduces the action of antidiabetic drugs
Hydrocortisone: reduces the effect of antihypertensive drugs
Hydrocortisone: may decrease the patient\’s antibody response to vaccines, increase vaccine side effects, and potentiate virus replication when given with live virus vaccine

Leukotriene Receptor Antagonists

This class includes:

Zafirlukast
Montelukast

These drugs act by suppressing the effects of leukotrienes, compounds that promote bronchoconstriction as well as eosinophil infiltration, mucus production, and airway edema.

Zafirlukast

Available Preparations:

Tablets: 20 mg

Available Brands: Accolate®

Pharmacokinetics: Zafirlukast is rapidly absorbed after oral administration, extensively metabolized in the liver, and excreted in feces.

Indications:

Prophylaxis of asthma
Exercise-induced asthma

Contraindications:

Hypersensitivity to zafirlukast
Breastfeeding
Hepatic impairment

Dosage:

Adults: 20 mg twice daily at least 1 hour before or 2 hours after meals
Children under 12 years: Not recommended

Side Effects:

Headache
Diarrhea
Insomnia
Dyspepsia
Dizziness
Nausea
Fever
Malaise
Vomiting
Abdominal pain

Drug Interactions:

Blood levels are increased by aspirin
Blood levels are decreased by erythromycin and theophylline
Zafirlukast increases the effects and risk of bleeding with warfarin

Key Issues to Note:

Give the drug at least 1 hour before or 2 hours after a meal
Advise the patient to take the drug as prescribed even during symptom-free periods
Do not use the drug to treat acute episodes of asthma
Advise the patient not to decrease the dose or stop unless instructed by the doctor
Nursing women should not take zafirlukast
Inform the patient to report symptoms such as abdominal pain, nausea, fatigue, itching, or anorexia

Drugs for Allergic Rhinitis

Rhinitis is an inflammation of the nasal mucous membrane and is characterized by periods of nasal discharge, sneezing, and nasal congestion.

Rhinitis may be allergic or non-allergic in origin.

Allergic Rhinitis

Allergic rhinitis is defined as a nasal mucous membrane inflammation caused by a hypersensitivity response to foreign allergens mediated by IgE antibodies.

Drugs used in the treatment of allergic rhinitis include:

Antihistamines
Decongestants
Corticosteroids
Mast cell stabilizers

Antihistamines

Antihistamines are the mainstay in the treatment of seasonal and perennial allergic rhinitis. They relieve symptoms such as rhinorrhea, edema, nasal itching, sneezing, and ocular symptoms such as conjunctivitis. They are more effective when taken before the start of symptoms.

Classification of Antihistamines

Antihistamines are classified as follows:

Sedating antihistamines
Non-sedating antihistamines

Sedating Antihistamines

They are also called first-generation antihistamines. Sedating antihistamines cross the blood-brain barrier and are associated with marked sedation and depression.

Examples:

Chlorpheniramine
Hydroxyzine
Promethazine
Cyproheptadine

Chlorpheniramine

Available Preparations:

Tablets: 4 mg
Syrup: 2 mg/5 ml

Available Brands: Piriton®, Piton®

Pharmacokinetics: Chlorpheniramine is well absorbed following oral administration, distributed to body tissues, including the placenta. It is metabolized in the liver and excreted in urine.

Indications:

Conjunctivitis
Allergic rhinitis
Pruritus of allergic origin
Acute urticaria
Insect stings
Severe angioedema

Contraindications:

Hypersensitivity to chlorpheniramine
Acute attack of asthma
Third trimester of pregnancy
Breastfeeding
Narrow-angle glaucoma

Dosage:

Adults and Children over 12 years: 4 mg every 4-6 hours

Children:

6-12 years: 2 mg every 4-6 hours
1-5 years: 1 mg 3 times daily
6 months-12 months: 1 mg twice daily

Side Effects:

Drowsiness
Dizziness
Epigastric pain
Headache
Palpitations
CNS depression
Urinary retention
Dry mouth
Blurred vision
Sweating
Tremor

Drug Interactions:

Chlorpheniramine potentiates sedative effects of barbiturates, hypnotics, opioid analgesics
Increased sedative effects with alcohol

Key Issues to Note:

Advise the patient to take the drug after food to minimize GI distress
Inform the patient that chlorpheniramine may cause drowsiness and impair the ability to perform activities requiring mental alertness
Advise the patient to avoid direct exposure to sunlight since it may cause severe sunburn
Avoid alcohol while taking chlorpheniramine

Non-Sedating Antihistamines

Non-sedating antihistamines are less sedating than the first generation.

Examples:

Cetirizine
Loratadine
Desloratadine
Levocetirizine
Ebastine

Cetirizine

Available Preparations:

Tablets: 10 mg
Syrup: 5 mg/5 ml

Available Brands: Zyrtec®, Finallergy®, Zyncet®, Allercet®, Alerid®

Pharmacokinetics: Cetirizine is rapidly and almost completely absorbed from the GIT, undergoes slow first-pass metabolism, and is excreted in urine primarily as unchanged drug.

Indications:

Symptomatic relief of allergy such as:

Allergic rhinitis
Allergic conjunctivitis
Atopic dermatitis
Chronic urticaria

Contraindications:

Hypersensitivity to cetirizine
Breastfeeding
Pregnancy
Acute attacks of asthma

Dosage:

Adults and Children over 6 years: 10 mg daily or 5 mg twice daily

Children:

2-5 years: 2.5 mg once daily or 2.5 mg twice daily
6 months-1 year: 2.5 mg once daily

Side Effects:

Somnolence
Insomnia
Headache
Dizziness
Dry mouth
Abdominal pain
Nausea and vomiting
Diarrhea
Bronchospasm
Pharyngitis
Malaise

Drug Interactions:

Alcohol and other CNS depressants may increase CNS depression

Key Issues to Note:

The drug can be given without regard to food
Cetirizine may cause drowsiness and impair the ability to perform activities requiring mental alertness
Cetirizine may cause dry mouth; therefore, advise the patient to drink a lot or to use sugarless gum
Avoid alcohol while taking cetirizine

Drugs Used in the Treatment of Cough

Cough is a useful natural response to irritation of the lungs and airways aimed at removing foreign substances or excessive secretions.

Cough may occur as a symptom of an underlying disorder such as asthma, pneumonia, sinusitis, or gastroesophageal reflux disease.

It may be classified as follows:

Non-productive cough
Productive cough

Productive Cough

Productive cough is characterized by the presence of sputum and may be associated with conditions such as chronic bronchitis, asthma, and pneumonia. It is commonly treated with cough expectorants or mucolytics.

Non-Productive Cough

This type of cough is associated with no mucus production and is regarded as a useless cough. It is commonly associated with the common cold and is treated with cough suppressants or antitussives.

Cough Expectorants

Cough expectorants facilitate the expulsion of mucus and other materials from the lungs. Cough expectorants contain one or more of the following:

Guaifenesin
Ammonium chloride
Ipecacuanha
Squill
Volatile oils
Guaiacol
Iodides
Sodium citrate
Creosote

Preparations which contain cough expectorants include:

Cadistin syrup®
Cadiphen syrup®
Histalin syrup®
Hydrylin syrup®
Delased chesty®
Actified expectorant®
Menthodex syrup®
Zecuf herbal syrup®

Mucolytic Expectorants

Mucolytics reduce the viscosity of bronchial secretions by breaking down the structure of tenacious sputum, thereby facilitating its removal by coughing. Mucolytics are often used in chronic bronchitis and chronic asthma where sputum production is high.

Examples:

Bromhexine
Carbocisteine
Ambroxol

Common compound preparations containing mucolytics include:

Rhinathiol syrup®
Brozedex®
Ascoril®
Bisolvin®
Ambrodil®

Demulcents

Demulcent cough preparations coat the mucosa of the pharynx and provide short-lived relief of the irritation that provokes the cough reflex. They contain soothing substances such as:

Glycerol
Honey
Liquorice
Sucrose syrup

Compound preparations containing demulcents include:

Simple linctus
Menthodex lozenges
Zecuf lozenges

Cough Suppressants

Cough suppressants act centrally to reduce the sensitivity of the cough center. They should be avoided in chronic obstructive airway diseases as they may also depress respiration. Most cough suppressants are opiate derivatives and may cause constipation and abuse. They should be avoided in children below one year.

Examples include codeine, pholcodine, and dextromethorphan; the latter two generally have fewer adverse effects than codeine.

Compound preparations containing cough suppressants include: Benylin with codeine®, Benylin DM®, Rhinathiol dry cough®, Piritex with codeine®, Hydryllin DM®, Piritex Junior®, Actifed syrup®, Delased dry cough®, and Zedex®.

Drugs Acting on the Respiratory System Read More »

Medicines Acting on Specific Body Systems

Medicines play a big role in modern healthcare, providing solutions to a wide range of diseases and disorders. The human body is a network of interconnected systems, each with its functions and challenges. To address these challenges, pharmacologists have developed drugs that act on specific body systems, ensuring targeted and effective treatment for various conditions.

These medicines are designed to interact with specific organs, tissues, or biochemical pathways, either by enhancing normal physiological functions or by correcting pathological imbalances. For example, cardiovascular drugs regulate heart function and blood pressure, while respiratory drugs help manage conditions like asthma and chronic obstructive pulmonary disease (COPD). Similarly, gastrointestinal drugs address issues such as acid reflux, ulcers, and irritable bowel syndrome, and endocrine drugs help manage hormonal imbalances like diabetes or thyroid disorders.

$\"Drugs$

Drugs Acting on the Gastrointestinal System

Drugs for Peptic Ulcer Disease

Peptic Ulcer Disease (PUD)

Peptic ulcer disease develops when there is an imbalance between mucosal protective substances such as mucus and bicarbonate, and destructive substances like acid, H. pylori bacteria, and pepsin. Drugs used in the treatment of peptic ulcer disease include:

Antacids
H2 receptor antagonists
Proton pump inhibitors
Mucosal protectives
Antibiotics

Antacids

These are alkaline compounds that neutralize stomach acid, raising the gastric pH and thereby relieving pain. They are often given concurrently with acid-suppressing drugs such as H2 receptor antagonists and proton pump inhibitors in the treatment of peptic ulcers and reflux esophagitis. Most antacids contain aluminum hydroxide, magnesium hydroxide, sodium bicarbonate, or calcium carbonate. Other ingredients added to antacids include simethicone and alginic acid.

Simethicone: Added to antacids to relieve flatulence and dyspepsia. It may be beneficial in relieving colic pain in infants. Common brands containing simethicone include Maalox Plus®, Alcid®, and Gestid®.
Alginates: Added to antacids as protectants and are useful in the treatment of reflux esophagitis. Common brands containing alginate include Gaviscon®.
Local anesthetics: Such as oxethazaine are added to antacids to reduce the pain associated with dyspepsia. Common brands containing oxethazaine include Mucogel® suspension and Mucaine® suspension.

Antacids containing sodium bicarbonate have a fast onset of action, but their absorption may worsen hypertension and heart failure.

Indications

Symptomatic relief of:

Dyspepsia
Gastroesophageal reflux disease
Peptic ulcer disease
Gastritis
Heartburn

Contraindications

Patients with severe abdominal pain of unknown cause
Lactation
Patients with cardiovascular problems (antacids with sodium)

Side Effects

Magnesium-containing antacids tend to cause diarrhea, whereas aluminum-containing antacids may cause constipation and delay gastric emptying. A combination of the two may reduce the side effects of each.

Key Issues to Note

Antacids should be taken between meals or at bedtime when symptoms are expected to occur.
Optimum antacid effect is obtained if taken 1-3 hours after meals.
Liquid antacids are generally more effective than tablets and have a rapid onset of action.
Antacids are effective for a short period and should be given on a 6-hourly basis.
Antacids may interact with numerous other drugs, affecting the rate and extent of their absorption. For example, tetracycline, ciprofloxacin, iron, indomethacin, and digoxin. A minimum interval of at least 2 hours should be left between the administration of antacids and other drugs.

Common Antacid Preparations

ACICONE-S®

Available Preparations: Tablets, Suspension

Composition:

Tablets: Magaldrate 720 mg, Simethicone 25 mg
Suspension: Magaldrate 540 mg, Simethicone 40 mg

Indications:

Heartburn in reflux esophagitis
Prophylaxis against ulcer complications
Adjunct to the treatment of peptic ulcers

Dosage:

Tablets: 1 tablet to be chewed 4 times daily after meals or at bedtime
Suspension: 5-10 ml 4 times daily after meals or at bedtime

AGOCID®

Available Preparations: Suspension

Composition: Dried aluminum gel 250 mg, Magnesium hydroxide 250 mg, Simethicone 50 mg

Indications:

Acid dyspepsia
Heartburn
Pregnancy heartburn
Adjunct to peptic ulcer treatment
Reflux esophagitis

Dosage: 5-10 ml 4 times daily between meals

ALCID®

Available Preparations: Suspension

Composition: Aluminum hydroxide gel 400 mg, Magnesium hydroxide 400 mg, Simethicone 50 mg

Indications:

Gastritis
Flatulence
Hiatus hernia
Adjunct to the treatment of peptic ulcers
Heartburn associated with reflux esophagitis
Heartburn in pregnancy

Dosage: 5-10 ml 4 times a day between meals and at bedtime

CENTACID®

Available Preparations: Suspension

Composition: Aluminum hydroxide gel 250 mg, Magnesium hydroxide 200 mg, Simethicone 40 mg

Indications:

Acid dyspepsia
Reflux esophagitis
Gastritis
Pregnancy heartburn
Hiatus hernia

Dosage: 5-10 ml 4 times a day between meals and at bedtime

RELCERGEL®

Available Preparations: Suspension

Composition: Aluminum hydroxide gel 6 g, Magnesium hydroxide 80 mg, Simethicone 100 mg, Deglycyrrhizinated liquorice 400 mg

Indications:

Gastritis
Flatulence
Heartburn associated with reflux esophagitis
Heartburn in pregnancy
Adjunct to the treatment of peptic ulcers

Dosage: 5-10 ml 3-4 times daily after meals

Mucosal Protective Drugs

Bismuth Subsalicylate

Has cytoprotective properties and is bactericidal against H. pylori. It promotes healing of peptic ulcers by forming a complex (bismuth/glycoprotein) that coats the base of the peptic ulcer.
It needs an acidic environment to work; hence, it should not be used in combination with antacids.

Available Preparations: Tablets (262 mg), Suspension

Available Brands: Pepto-Bismol®, Bismol®

Pharmacokinetics: Following oral administration, the drug is only slightly absorbed. Increased gastric pH may increase bismuth absorption. Unabsorbed drug is excreted in feces. The absorbed portion of the drug is distributed throughout body tissues and is slowly excreted in urine and bile.

Indications:

Peptic ulcer
Nausea
Diarrhea
Abdominal cramps
Indigestion
Prevention of traveler\’s diarrhea

Contraindications:

Hypersensitivity to bismuth salts
Moderate to severe renal impairment
Children under 3 years

Dosage:

Adults: 30 ml or 2 tablets 4 times daily, 30 minutes before food

Children:

9-12 years: 15 ml or 1 tablet 4 times daily
6-9 years: 10 ml 4 times daily
3-6 years: 5 ml 4 times daily

Side Effects:

Black stool
Discolors mucous membranes, tongue, and teeth
Constipation
Metallic taste
Skin reactions
Stomatitis

Drug Interactions:

Bismuth subsalicylate decreases the absorption of tetracyclines.
It increases the toxicity of aspirin due to the absorption of salicylate.

Key Issues to Note:

Chew or dissolve tablets in the mouth before swallowing.
Shake suspension before using.
Stop use if symptoms do not improve within 2 days.

Prostaglandin Analogues

Misoprostol

Available Preparations: Tablets (200 mcg)

Available Brands: Cytotec®

Mode of Action: Misoprostol helps to protect the stomach by suppressing secretion of gastric acid, promoting secretion of bicarbonate and cytoprotective mucus, and maintaining blood flow.

Indications:

Peptic ulcer disease
Prophylaxis of NSAID-induced ulcers
Induction of labor
Management of postpartum hemorrhage

Contraindications:

Pregnancy or those planning to become pregnant
Women in childbearing age
Breastfeeding
Patients allergic to prostaglandin derivatives
Inflammatory bowel disease

Dosage:

By mouth: 800 mcg daily in 2-4 divided doses with food for 4-8 weeks
Prophylaxis of NSAID-induced ulcers: 200 mcg 2-4 times daily taken with NSAID

Side Effects:

Diarrhea
Flatulence
Abdominal cramps
Dyspepsia
Dizziness
Nausea
Vomiting
Abnormal vaginal bleeding
Rashes

Drug Interactions:

Misoprostol diminishes the bioavailability of aspirin.
Magnesium antacids enhance diarrhea associated with misoprostol.

H2 Receptor Antagonists

H2 receptor antagonists reduce gastric acid secretion by blocking the action of histamine at the H2 receptor in the parietal cells of the stomach.

Examples:

Cimetidine
Famotidine
Nizatidine
Ranitidine

Ranitidine

Available Preparations: Tablets (150 mg, 300 mg), Injection (25 mg/ml, 2 ml)

Available Brands: Zantac®, Ranidenk®, Ranitin®, Rantac®, Aciloc®, R-Loc®

Pharmacokinetics: Ranitidine is readily absorbed from the gastrointestinal tract, widely distributed, metabolized in the liver, and excreted in urine.

Indications:

Peptic ulcer
Prophylaxis of NSAID-induced duodenal or gastric ulcer
Stress ulcer prophylaxis
Gastroesophageal reflux disease
Zollinger-Ellison syndrome
Dyspepsia

Contraindications:

Patients allergic to ranitidine
Children less than 8 years

Dosage:

Peptic ulcer:

Adults and children over 12 years: 150 mg twice daily or 300 mg at night for 4 to 8 weeks

Prophylaxis of NSAID-induced duodenal or gastric ulcer: 150 mg twice daily

Gastroesophageal reflux disease: 150 mg twice daily or 300 mg at night up to 8 weeks; moderate to severe cases: 150 mg every 6 hours daily for up to 12 weeks

Zollinger-Ellison syndrome: 150 mg 3 times daily

Stress ulcer prophylaxis: 150 mg twice daily until the risk factor is removed

Dyspepsia: 150 mg twice daily for 4-8 weeks

IV: 50 mg diluted to 20 ml with normal saline or dextrose 5% every 6-8 hours by slow injection over not less than 5 minutes
IV Infusion: 25 mg/hour for 2 hours may be repeated every 6-8 hours

Side Effects:

Skin rash
Visual disturbance
Gynecomastia
Headache
Diarrhea
Malaise
Tachycardia
Constipation
Hypersensitivity reaction
Myalgia

Drug Interactions:

Antacids may decrease the absorption of ranitidine.
Ranitidine may decrease the absorption of ketoconazole, cefpodoxime, cefuroxime.
Ranitidine may increase the hypoglycemic effects of glipizide.
Ranitidine may interfere with warfarin clearance.

Proton Pump Inhibitors

Proton pump inhibitors (PPIs) act by irreversibly binding to and inhibiting the enzyme H+/K+-ATPase (proton pump) of the gastric parietal cells, resulting in long-lasting but reversible acid suppression. PPIs inhibit gastric acid secretion more than H2 receptor antagonists.

Examples:

Omeprazole
Lansoprazole
Pantoprazole
Esomeprazole
Rabeprazole

Omeprazole

Available Preparations: Enteric-coated capsules/tablets (20 mg)

Available Brands: Gasec®, Omepren®, Omizac®, Ocid®, Belifax®

Pharmacokinetics: Omeprazole is rapidly but variably absorbed after oral administration. Absorption is not affected by food. It is almost completely metabolized in the liver, and 80% of the metabolites are excreted mainly in urine and the rest in feces.

Indications:

Peptic ulcers
Zollinger-Ellison syndrome
NSAID-associated duodenal or gastric ulcer
Gastric acid reduction during anesthesia
Gastroesophageal reflux disease
Acid-related dyspepsia

Contraindications:

Allergy to omeprazole or any other component in the capsule
Pregnancy
Lactation

Dosage:

Gastric ulcer or reflux esophagitis: 20-40 mg once daily for 4-8 weeks
Duodenal ulcer: 20 mg once daily for 4 weeks; continued for a further 4 weeks if not fully healed
NSAID-associated duodenal or gastric ulcer: 20 mg once daily for 4 weeks; continued for a further 4 weeks if not fully healed
Zollinger-Ellison syndrome: Initially 60 mg once daily, usual range 20-120 mg; doses over 80 mg given in 2 divided doses
Acid-related dyspepsia: 20 mg once daily for 2-4 weeks
Prophylaxis of acid aspiration: 40 mg on the evening before, then 40 mg 2-6 hours before surgery

Side Effects:

Headache
Nausea
Flatulence
Vomiting
Constipation
Skin rashes
Diarrhea
Abdominal pain
Dry mouth
Gynecomastia
Impotence

Drug Interactions:

Omeprazole increases the plasma concentration of diazepam, carbamazepine, digoxin, phenytoin
Omeprazole decreases the plasma concentration of itraconazole, ketoconazole, cefpodoxime, cefuroxime, iron salts, and cyanocobalamin
Omeprazole may increase the absorption and potential for hypoglycemia of glipizide, tolbutamide

Key Issues to Note:

Administer before food and the capsule should be swallowed whole without chewing
Capsules should be used within one month of opening the package
Possible malignancy must be excluded prior to starting treatment to avoid delay in diagnosis
Dosage reduction may be required in hepatic disease

Esomeprazole

Available Preparations: Tablets (20 mg, 40 mg)

Available Brands: Nexium®, S-prazo®, Nexpro®, Esoz®

Pharmacokinetics: Esomeprazole is rapidly absorbed following oral administration. It is extensively metabolized by the liver and excreted in urine and a small percentage in feces.

Indications:

Gastroesophageal reflux disease
Zollinger-Ellison syndrome
Peptic ulcer disease
Prevention of relapse of H. pylori-associated peptic ulcer
Prevention of gastric and duodenal ulcers associated with NSAID therapy

Contraindications:

Known hypersensitivity to benzimidazoles
Pregnancy

Dosage:

Peptic ulcer disease: Triple therapy regimen: 40 mg of esomeprazole once daily with amoxicillin 1 g twice daily and clarithromycin 500 mg twice daily for 7 days
Gastroesophageal reflux disease: 40 mg once daily for 4-8 weeks depending on the response; maintenance: 20 mg daily
Gastric ulcer associated with NSAID therapy: 20 mg once daily for 4-8 weeks

Side Effects:

Taste disturbances
Dizziness
Diarrhea
Nausea
Headache
Abdominal pain
Skin rash
Vomiting
Flatulence
Dry mouth

Drug Interactions:

Reduction in gastric acidity due to esomeprazole use may decrease the absorption of ketoconazole, itraconazole, digoxin, and iron

Key Issues to Note:

Food delays and decreases the absorption of esomeprazole; therefore, take it at least 1 hour before meals
The tablet should be swallowed whole; do not chew or crush

Lansoprazole

Available Preparations: Capsule (30 mg)

Available Brands: Lancid®, Lan-30®, Zolanas-30®

Pharmacokinetics: Lansoprazole is rapidly absorbed after oral administration, extensively metabolized in the liver, and metabolites are excreted primarily in feces via the bile.

Indications:

Peptic ulcers
Zollinger-Ellison syndrome
Gastroesophageal reflux disease
Acid-related dyspepsia
Prophylaxis of NSAID-associated duodenal and benign gastric ulcer

Contraindications:

Hypersensitivity to lansoprazole
Breastfeeding
Pregnancy

Dosage:

Benign gastric ulcer: 30 mg daily in the morning for 8 weeks
Duodenal ulcer: 30 mg daily in the morning for 4 weeks; maintenance: 15 mg daily
Zollinger-Ellison syndrome: Initially 60 mg once daily, adjusted according to response to a daily dose of 120 mg or more in two divided doses
Gastroesophageal reflux disease: 30 mg daily in the morning for 4-8 weeks; maintenance: 15-30 mg daily
Acid-related dyspepsia: 30 mg daily in the morning for 2-4 weeks

Side Effects:

Abdominal pain
Diarrhea or constipation
Fatigue
Nausea
Dizziness
Flatulence
Headache
Skin rash
Altered appetite
Impotence
Malaise
Vomiting

Drug Interactions:

Lansoprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability such as ketoconazole, itraconazole, ampicillin, iron salts, digoxin
Antacids may reduce the absorption of lansoprazole when given at the same time
Lansoprazole may reduce the effect of oral contraceptives, phenytoin, carbamazepine, warfarin, and theophylline

Key Issues to Note:

Swallow capsule whole without crushing or chewing
For patients unable to swallow, open the capsule and pour the contents onto a teaspoon and swallow
Take the drug after meals

Drugs for Nausea and Vomiting

Common Terms Used

Nausea: A sensation often leading to the urge to vomit.
Vomiting (Emesis): The forceful expulsion of gastric contents through the mouth, occurring due to stimulation of the vomiting center situated in the medulla oblongata of the brain.
Vomiting Center: The area in the brain involved in stimulating the events that lead to nausea and vomiting.
Chemoreceptor Trigger Zone: The area in the brain involved with the sensation of nausea and vomiting.
Prokinetic Drug: Drugs that increase the activity of gastrointestinal smooth muscles.
Antiemetic Drug: A drug given to relieve nausea and vomiting.

Vomiting is not a disease but a symptom of an underlying disease or disorder of the gastrointestinal tract (GIT). Common causes of vomiting include:

Drugs such as opioid analgesics and digoxin
Gastrointestinal disease
Motion sickness
Vestibular disorders like migraine headache
Early pregnancy (morning sickness)
Psychological factors
Infectious diseases

Drugs used in the treatment of vomiting include:

Promethazine
Dimenhydrinate
Metoclopramide
Prochlorperazine
Cinnarizine
Meclozine
Chlorpromazine
Domperidone
Cyclizine
Granisetron
Haloperidol

Key Issues to Note

Identify and treat the cause if possible
Ensure adequate hydration
Antiemetics should be prescribed only when the cause of vomiting is known
Antiemetics are more effective when given prophylactically than when given to stop vomiting that has already started
They are unnecessary and sometimes harmful, especially when the cause can be treated

Promethazine

Available Preparations:

Tablets: 25 mg
Injection: 25 mg/ml, 2 ml
Syrup: 5 mg/5 ml

Available Brands: Intamine®, Prozin®, Phenergan®

Pharmacokinetics: Promethazine is well absorbed after oral or intramuscular administration, widely distributed, metabolized in the liver, and excreted in urine and bile.

Indications:

Nausea and vomiting
Urticaria and angioedema
Vertigo
Postoperative emesis
Motion sickness
Allergic rhinitis
Pruritus in eczema

Contraindications:

Known hypersensitivity to promethazine
Porphyria
Children under 2 years
Severe CNS depression or coma
Vomiting of unknown cause
Lactation
Concomitant therapy with MAOIs

Dosage:

Nausea and Vomiting:

Adult (Oral): 25 mg repeated every 4-6 hours, max 100 mg daily
Adult (IM): 12.5-25 mg every 6 hours as needed
Children (5-12 years): 6.25-12.5 mg
Children (12-16 years): 12.5-25 mg

Morning Sickness:

Adult: 25 mg at bedtime or 2 hours before traveling, repeated if needed up to 4 times daily
Children (5-10 years): 10 mg at bedtime and the following morning if necessary
Children (2-5 years): 5 mg at night and the following morning if necessary

Side Effects:

Drowsiness
Anorexia
Dry mouth
Constipation
Sedation
Disorientation
Urinary retention
Hypotension
Skin rashes
Dizziness
Headache
Fatigue
Epigastric pain

Drug Interactions:

Alcohol and other CNS depressants may increase CNS depressant effects of promethazine
Promethazine may block the anti-Parkinsonian action of levodopa
Additive anticholinergic effects with anticholinergic drugs

Key Issues to Note:

Inform the patient that promethazine may cause drowsiness and impair the ability to perform activities requiring mental alertness
Advise the patient to avoid prolonged exposure to sunlight since promethazine may cause photosensitivity reactions
Maintain fluid intake
Avoid alcohol intake

Chlorpromazine

Available Preparations:

Tablets: 25 mg, 100 mg
Injection: 100 mg/2 ml

Available Brands: Largactil®

Pharmacokinetics: Chlorpromazine is readily absorbed from the gastrointestinal tract, undergoes first-pass metabolism, and is distributed to the body tissues. It is extensively metabolized in the liver and excreted in the urine.

Indications:

Nausea and vomiting due to radiation therapy and chemotherapy
Acute and chronic schizophrenia
Acute mania, as in bipolar disorder
Anxiety disorders
Intractable hiccup
Severe behavioral disturbances in children
Nausea and vomiting of terminal illness

Contraindications:

Hypersensitivity to chlorpromazine
Comatose states
Severe CNS depression
Bone marrow depression
Parkinson\’s disease
Liver damage
Cerebral or coronary arteriosclerosis

Dosage:

Schizophrenia, Mania, Severe Anxiety: Initially 25 mg 3 times daily or 75 mg at night, adjusted according to response. Maintenance dose: 75-300 mg daily

Intractable Hiccup: 25-50 mg 3-4 times daily

Severe Nausea and Vomiting: 10-25 mg 4 times daily

Children: 0.5-1 mg/kg 6 hourly

Deep Intramuscular Injection:

Adult: 25-50 mg every 4-6 hours until vomiting stops
Children (1-12 years): 0.5-1 mg/kg every 6-8 hours

Side Effects:

Drowsiness
Dry mouth
Slurred speech
Poor coordination
Hypotension
Blurred vision
Constipation
Urinary retention
Somnolence
Dizziness

Drug Interactions:

Chlorpromazine may reduce the effect of drugs for Parkinsonism
Alcohol and other CNS depressants may increase respiratory depression and hypotensive effects of chlorpromazine
Lithium may decrease the absorption of chlorpromazine and produce adverse neurologic effects
Concurrent use with antihypertensives may result in additive hypotensive effects

Key Issues to Note:

Administer chlorpromazine with water, food, or milk to decrease GI upset
Inform the patient that chlorpromazine may cause drowsiness and impair the ability to perform activities requiring mental alertness

Metoclopramide

Available Preparations:

Tablets: 10 mg
Injection: 5 mg/ml, 2 ml ampoule

Available Brands: Plasil®, Reglan®, Camet®

Pharmacokinetics: Metoclopramide is rapidly and almost completely absorbed from the gastrointestinal tract following oral administration, undergoes hepatic first-pass metabolism, and is widely distributed in the body. It is excreted in feces via the bile.

Indications:

Disorders of decreased gastrointestinal motility such as:

Dyspepsia
Gastroesophageal reflux disease
Diabetic gastroparesis
Stimulation of lactation

Nausea and vomiting due to:

Migraine
Following gastric surgery
Cancer therapy or radiotherapy

Contraindications:

Gastrointestinal obstruction
Intestinal perforation
3-4 days after gastrointestinal surgery
History of seizure disorders
Pheochromocytoma

Dosage:

Nausea and Vomiting:

Adult and Children (over 60 kg): 10 mg 3 times daily
Children (9-18 years): 5 mg 3 times daily
Children (5-9 years): 2.5 mg 3 times daily
Children (3-5 years): 2 mg 2-3 times daily
Children (1-3 years): 1 mg 2-3 times daily
Neonate: 100 mcg/kg every 6-8 hours

Stimulation of Lactation: 10 mg 3 times daily, reduce dose gradually over 7-10 days before stopping

Cancer Chemotherapy: Initial dose of up to 2 mg/kg by intravenous infusion over at least 15 minutes may be given in combination with dexamethasone before cancer therapy and repeated every 2 or 3 hours

Side Effects:

Hyperprolactinemia
Drowsiness
Tardive dyskinesia
Diarrhea
Edema
Skin rash
Hypotension
Depression
Dizziness
Pruritus
Headache
Restlessness
Parkinsonism

Drug Interactions:

Metoclopramide reduces the absorption of oral digoxin
Metoclopramide increases the absorption of aspirin, paracetamol, and diazepam

Key Issues to Note:

May cause drowsiness; therefore, warn the patient not to drive or operate machinery that requires mental alertness
Advise the patient to take the drug 30 minutes before meals and at bedtime

Drugs for Hemorrhoids and Piles

Hemorrhoids (Piles)

Hemorrhoids are clusters of venous swellings of the tissues around the anus caused by straining during bowel movements. They are associated with constipation, diarrhea, and prolonged straining. Hemorrhoids may be divided into two:

Internal hemorrhoids
External hemorrhoids

Most preparations for hemorrhoids contain any of the following:

Astringents (e.g., bismuth subgallate, zinc oxide, resorcinol)
Local anesthetics (e.g., lignocaine, cinchocaine)
Corticosteroids (e.g., hydrocortisone)
Lubricants
Vasoconstrictors
Antiseptics

Key Issues to Note:

Creams or ointments are used for external hemorrhoids
Suppositories are preferred for internal hemorrhoids
Hemorrhoids developing during pregnancy should be managed conservatively as most will resolve after delivery
Local anesthetics are used to relieve pain associated with hemorrhoids
Corticosteroids are used to reduce inflammation where infection is not present
In case of infection, metronidazole 400 mg 8 hourly for 5 days is used
Surgery may be required in resistant cases

Commonly Used Compound Preparations:

Anusol ointment/suppository
Preparation-H ointment
Scheriproct ointment/suppository
Sediproct ointment/suppository
Pylocaine ointment

Anusol

Available Preparations:

Ointment
Suppository

Composition:

Bismuth subgallate 59 mg
Bismuth oxide 24 mg
Zinc oxide 296 mg

Indications:

Soothe the pain and irritation of hemorrhoids

Contraindications:

Serious rectal pathology

Dosage:

Suppository: Insert 1 suppository at night and morning
Ointment: Apply twice daily, at night and morning

Side Effects:

Hypersensitivity reactions such as:

Redness
Irritation
Swelling

Sediproct

Available Preparations:

Cream
Suppository

Composition:

Hydrocortisone 500 mg
Cinchocaine 500 mg

Indications:

Hemorrhoids associated with inflammation
Anal fissures
Anal pruritus
Proctitis

Contraindications:

Hypersensitivity to any of the active ingredients

Dosage:

Cream: Apply the cream into the rectum twice daily, at night and morning after bowel movement
Suppository: Insert 1 suppository twice daily, at night and morning

Side Effects:

Local irritation
Skin rash

Scheriproct

Available Preparations:

Suppository
Ointment

Composition:

Cinchocaine 0.5%
Prednisolone 0.19%

Indications:

Hemorrhoids

Contraindications:

Known hypersensitivity to the active ingredients

Dosage:

Ointment: Apply twice daily for 5-7 days, then once daily for a few days after symptoms have cleared
Suppository: Insert 1 suppository daily after a bowel movement for 5-7 days (in severe cases, initially apply 2-3 times daily)

Side Effects:

Local irritation
Skin rash

Drugs for Inflammatory Bowel Disease

Inflammatory bowel disease is a chronic non-specific inflammatory condition of the gastrointestinal tract.

It is divided into two:

Crohn\’s disease (affects the gut from mouth to anus)
Ulcerative colitis (affects only the large bowel)

Both ulcerative colitis and Crohn\’s disease frequently run a course characterized by exacerbations and remissions, tend to be chronic in nature, have similar extra-intestinal manifestations, and may be associated with a positive family history of inflammatory bowel disease.

Drugs used in the treatment of inflammatory bowel disease either control symptoms or modify the disease by inducing and maintaining long-term bowel healing.

Examples:

Aminosalicylates
Corticosteroids

Aminosalicylates

This group of drugs includes:

Sulfasalazine
Mesalazine

Aminosalicylates treat mild to moderate inflammatory bowel disease and are equally effective. The choice is based on the location of the disease and the side effect profile of the individual drugs.

Sulfasalazine

Available Preparation: Tablets: 500 mg

Available Brands: Salazopyrin®

Indications:

Active ulcerative colitis
Severe rheumatoid arthritis
Active Crohn\’s disease

Contraindications:

Children less than 2 years
Pregnancy at term and lactation
Severe hepatic impairment
Severe renal dysfunction
Salicylate and sulfonamide hypersensitivity

Dosage:

Acute Attack:

Adult: 1-2 g 4 times daily until remission occurs (3 weeks), reduced to a maintenance dose of 500 mg 4 times daily
Children over 2 years:
Acute attack: 10-15 mg/kg 4-6 times daily until remission occurs
Maintenance: 30 mg/kg/day in 4 divided doses

Rheumatoid Arthritis:

Adult: 500-1000 mg/day for 1 week, increased by 0.5 g/week up to 3 g/day

Side Effects:

Anorexia
Vomiting
Fever
Skin rash
Abdominal discomfort
Nausea
Headache
Folate deficiency
Reversible male infertility

Drug Interactions:

Sulfasalazine may increase the effect of anticonvulsants, methotrexate, oral anticoagulants, and oral antidiabetics
Sulfasalazine may decrease the absorption of digoxin

Key Issues to Note:

Administer the drug with food to reduce stomach upset
Do not administer the drug with antacids
Sulfasalazine impairs the absorption of folic acid; therefore, folic acid supplements may be necessary during treatment

Corticosteroids

Corticosteroids are used for the treatment of both ulcerative colitis and Crohn\’s disease. They are often able to induce the remission of ulcerative colitis but have proved less valuable in maintaining remission.

Drugs for Constipation (Laxatives)

Constipation is a reduced frequency of defecation characterized by hardening of the stool, straining on defecation, or a feeling of incomplete evacuation.

It may be caused by any of the following:

Lack of fluid or fiber intake
Lack of exercise
Pregnancy
Drugs like aluminum-containing antacids, codeine, or iron
Irritable bowel syndrome
Anorectal conditions like hemorrhoids
Psychiatric and neurological disorders

Laxatives are drugs that stimulate defecation by forming bulk, stimulating peristalsis, or providing lubrication.

They increase the frequency of bowel evacuation or the passage of softer or bulkier stool. Laxatives are used in the treatment of constipation and for bowel evacuation before investigational procedures, such as endoscopy, radiological examination, or before surgery.

Classification of Laxatives

Laxatives are classified according to their mode of action as follows:

Bulk-forming laxatives
Saline laxatives
Lubricant laxatives
Stimulant laxatives
Osmotic laxatives

Bulk-Forming Laxatives

Mode of Action: Bulk-forming laxatives relieve constipation by absorbing water, thereby increasing fecal bulk, which stimulates peristalsis. They are useful for mild constipation, small hard stools, patients with hemorrhoids, fissures, and irritable bowel disease, and as adjuncts in ulcerative colitis. Adequate fluid intake is important to lubricate the colon and minimize the risk of intestinal obstruction.

Examples:

Methylcellulose
Wheat bran
Ispaghula husk

Ispaghula Husk

Available Preparations:

Granules: 3.5 g sachet

Available Brands: Fybogel®

Indications:

Constipation, especially in diverticular disease and irritable bowel syndrome
Constipation following anorectal surgery, hemorrhoids, pregnancy
Management of diarrhea
Adjusting fecal consistency in patients with colostomies

Contraindications:

Difficulty in swallowing
Intestinal obstruction
Colonic atony
Fecal impaction
Hypersensitivity to any of the ingredients

Dosage:

Adult: 1 sachet or 2 level 5 ml spoonfuls in water given morning and evening after meals
Children (6-12 years): 1/2 – 1 level 5 ml spoonful in water twice daily
Children (below 6 years): Give on doctor\’s advice only

Side Effects:

Flatulence and abdominal distension during the first few days of treatment
Gastrointestinal obstruction or impaction
Hypersensitivity reaction

Osmotic Laxatives

Mode of Action: Osmotic laxatives are poorly absorbed; therefore, the unabsorbed solute in the intestine draws water from the body into the bowel by osmosis, causing bowel distention, which in turn increases peristalsis. These drugs are used for acute and rapid evacuation of the bowel, except for lactulose.

Examples:

Lactulose
Magnesium salts

Lactulose

Available Preparations: Syrup: 3.350 g/5 ml

Available Brands: Laxolac®, Duphalac®, Sedalac®

Indications:

Constipation
Hepatic encephalopathy

Contraindications:

Intestinal obstruction
Known hypersensitivity to lactulose
Galactosemia

Dosage:

Constipation:

Adults: 15 ml twice daily
Children (6-12 years): 10 ml twice daily, adjusted according to response
Children (1-5 years): 5 ml twice daily, adjusted according to response
Children (less than 1 year): 2.5 ml twice daily, adjusted according to response

Hepatic Encephalopathy: 30-45 ml 3 times daily, adjust dose to produce 2-3 soft stools per day

Side Effects:

Flatulence
Cramps
Diarrhea
Nausea
Abdominal discomfort
Vomiting if excess doses are given

Key Issues to Note:

Administer the drug with juice, milk, or water to increase palatability
Do not take other laxatives while on lactulose therapy

Lubricants and Fecal Softeners

Mode of Action: They promote stool passage by coating the fecal surface with an oil layer that retains fecal fluid and prevents absorption of fecal water by the colon.

Examples:

Glycerol
Docusate sodium
Liquid paraffin
Mineral oil

Glycerol

Available Preparations:

Suppositories: 4 g

Indications:

Constipation

Contraindications:

Patients with known hypersensitivity to glycerin
Glycerin suppositories are contraindicated in patients who are recovering from rectal surgery

Dosage:

By rectum:

Adults: 4 g suppository moistened with water before use, once daily when required
Children (1-12 years): 2 g suppositories as required
Children (1 month – 1 year): 1 g suppository once daily when required

Side Effects:

Rectal discomfort
Diarrhea
Rectal mucosal erosion
Dizziness
Mild headache
Nausea
Mild hyperglycemia
Vomiting

Drug Interactions:

Concomitant use with diuretics may result in an additive effect

Key Issues to Note:

Onset of action is 5-30 minutes
Do not use longer than 1 week
Prolonged or frequent use may result in dependency

Stimulant Laxatives

Mode of Action: Stimulant laxatives increase peristalsis by directly stimulating nerve endings in the colonic mucosa, thereby increasing intestinal motility. They are useful for more severe forms of constipation, but tolerance is common with regular use, and they can produce abdominal cramps.

Examples:

Bisacodyl
Senna
Castor oil

Bisacodyl

Available Preparations:

Tablets: 5 mg
Suppository: 10 mg

Available Brands: Dulcolax®

Pharmacokinetics: Absorption of bisacodyl after oral administration is minimal; the absorbed drug is metabolized in the liver and excreted in urine, feces, and breast milk.

Indications:

Constipation
Bowel evacuation before investigational procedures or surgery

Contraindications:

Intestinal obstruction
Appendicitis
Severe dehydration
Acute inflammatory bowel disease
Hypersensitivity to the drug

Dosage:

Constipation:

Adults: 5-10 mg daily administered at night or 10 mg as a suppository or enema administered in the morning
Children (10-18 years): 5-10 mg at night, increased if necessary to max. 20 mg
Children (5-10 years): 5 mg at night
Children (2-5 years): 5 mg in the morning (rectally)

Complete Bowel Evacuation:

Adult: 10-20 mg followed by 10 mg as a suppository the next morning
Children (4-10 years): 5 mg at bedtime for 2 days before the procedure, increased if necessary by suppository 10 mg 1 hour before the procedure

Side Effects:

Nausea
Vomiting
Diarrhea
Faintness
Mild cramps
Abdominal discomfort
Suppositories may cause irritation and proctitis

Drug Interactions:

Antacids, cimetidine, famotidine, ranitidine, milk, and other drugs that increase gastric pH level may cause premature dissolution of the enteric coating of bisacodyl, resulting in abdominal cramping

Key Issues to Note:

Patients should swallow tablets whole with a glass of water
Do not administer bisacodyl within 1 hour of ingesting antacids, milk, or dairy products
Bisacodyl is habit-forming; therefore, long-term use may result in laxative dependency and loss of normal bowel function
Onset of action is 6-12 hours for tablets, 15-60 minutes for suppository
Warn the patient that prolonged use of bisacodyl suppositories may cause proctitis

Antidiarrheal Drugs

Diarrhea is the frequent passage of watery stools at least 3 times or more in a day. It affects all age groups and is more severe and life-threatening in children and immunocompromised patients. Diarrhea may be caused by any of the following:

Infections
Inflammation
Drugs such as antacids
Malabsorption

Drugs used in the treatment of diarrhea include:

Adsorbents
Antimotility drugs
Antisecretory compounds
Antimicrobials
Intestinal microflora

Adsorbent Drugs

Examples:

Kaolin
Pectin
Activated charcoal

Adsorbent drugs act by absorbing the toxins produced by pathogens, thereby reducing GIT motility. These drugs are used for symptomatic relief of diarrhea. They are not recommended for infectious acute diarrhea and when the patient is taking other drugs (prevent absorption of other drugs).

Antisecretory Drugs

Examples:

Bismuth subsalicylate

Bismuth subsalicylate appears to produce its antidiarrheal effect by inhibiting intestinal secretions. It is recommended in the treatment of infectious diarrhea such as traveler\’s diarrhea. It is available in the form of tablets and suspension.

Intestinal Microflora

Example: Lactobacillus

These drugs are intended to replace colonic microflora, which restores intestinal function and suppresses the growth of pathogenic microorganisms.

Antimotility Drugs

Examples:

Loperamide
Codeine
Diphenoxylate

Antimotility drugs act by reducing GIT motility, thereby allowing enough time for fluid absorption from gut contents. They are recommended in the treatment of acute and chronic diarrhea in combination with fluid replacement. They are not recommended in children less than 2 years and infectious diarrhea.

Loperamide

Available Preparations:

Capsules: 2 mg
Tablets: 2 mg

Available Brands: Imodium®, Loperium®, Loperax®, Kamodium®, Gallop®

Pharmacokinetics: About 40% of loperamide is absorbed from the gastrointestinal tract, undergoes first-pass metabolism in the liver, and is excreted in the feces as unchanged drug and a small amount in urine.

Indications:

Acute diarrhea
Chronic diarrhea
Traveler\’s diarrhea

Contraindications:

Known hypersensitivity to loperamide
Infants below 2 years of age
Abdominal distension
Acute inflammatory bowel disease
Antibiotic-associated colitis
Patients who must avoid constipation

Dosage:

Acute Diarrhea:

Adult: 4 mg start followed by 2 mg after each loose stool until diarrhea is relieved. Max dose 16 mg daily
Children (9-12 years): 2 mg 4 times daily up to 5 days
Children (4-8 years): 1 mg 3-4 times daily for up to 3 days only

Chronic Diarrhea:

Adult: 4-8 mg daily in 2 divided doses

Side Effects:

Flatulence
Blurred vision
Drowsiness
Headache
Fatigue
Constipation
Dry mouth
Hypersensitivity reaction
Abdominal cramps
Dizziness
Nausea and vomiting
Abdominal bloating
Urticaria
Toxic megacolon
Paralytic ileus

Drug Interactions:

Concomitant use of loperamide with opioid analgesics may cause severe constipation

Key Issues to Note:

Advise the patient to drink plenty of fluids to prevent dehydration
Do not exceed the maximum daily dosage
Loperamide may impair the ability to perform activities requiring mental alertness
Advise the patient to avoid the use of alcohol during treatment
Loperamide should not be used alone in patients with dysentery

Codeine

Available Preparations:

Tablets: 30 mg

Pharmacokinetics: Codeine is absorbed from the gastrointestinal tract, metabolized in the liver to morphine and other metabolites, and excreted in urine.

Indications:

Diarrhea
Pain
Cough suppression (lower dosage)

Contraindications:

Hypersensitivity to codeine
Premature infants
Conditions where inhibition of peristalsis should be avoided such as abdominal distension, ulcerative colitis, acute respiratory depression

Dosage:

Adults: 30-60 mg 3-4 times daily
Children: Not recommended

Side Effects:

Headache
Constipation
Anorexia
Abdominal pain
Dizziness
Hypotension
Sedation
Dry mouth
Nausea and vomiting
Respiratory depression
Somnolence
Decreased urination

Drug Interactions:

Alcohol, narcotic analgesics, hypnotics, and tricyclic antidepressants may increase CNS or respiratory depression

Key Issues to Note:

Administer codeine with water or food to decrease nausea and GI upset
Avoid long-term use because of addictive potential
Codeine may cause drowsiness; therefore, do not drive or operate machinery

Prokinetic Drugs

Prokinetic drugs enhance the tone and motility of the gastrointestinal tract. Examples include metoclopramide, domperidone, and cisapride. These drugs are used to treat gastroesophageal reflux disease (GERD), chemotherapy-induced nausea and vomiting, and diabetic gastroparesis. Metoclopramide, specifically, is used to suppress nausea and vomiting caused by anticancer drugs (e.g., cisplatin, dacarbazine), postoperative vomiting, radiation therapy-induced emesis, toxins, and opioids. It also treats diabetic gastroparesis and GERD.

Drugs for Obesity

Obesity is linked to numerous health problems, including diabetes mellitus, hypertension, and hyperlipidemia. Increased abdominal fat and waist circumference further elevate health risks.

Orlistat

Available preparations: 120mg capsules (brand name: Xenical®)

Mode of action: Inhibits lipases in the stomach and small intestine, preventing dietary fat absorption.

Indications: Obesity in adults with a body mass index (BMI) > 30, or > 27 with additional risk factors like hypertension or diabetes.

Contraindications: Chronic malabsorption syndrome, breastfeeding, cholestasis.

Dosage: Adults and children over 12 years: 120mg three times daily with each meal.

Side effects: Flatulence, fecal incontinence, headache, anxiety.

Drug interactions: Orlistat may reduce the absorption of fat-soluble vitamins. Supplementation with fat-soluble vitamins (including vitamin D and beta-carotene) may be necessary.

Key note: If a meal is fat-free, the dose can be omitted.

Medicines Acting on Specific Body Systems Read More »

Specific Anti-microbial Agents

ANTIBIOTICS

Antibiotics are chemical substances derived from microorganisms that either inhibit the growth of or destroy other microorganisms.

They are pivotal in combating bacterial infections and are divided into two primary categories:

Bacteriostatic Antibiotics: Inhibit bacterial growth.
Bactericidal Antibiotics: Directly kill bacteria.

Classification of Antibiotics

Antibiotics can be classified based on their:

Mechanism of Action
Spectrum of Activity
Chemical Structure

Mechanism of Action

Type	Description	Examples
Bacteriostatic	Inhibit bacterial growth, relying on the immune system to eliminate the pathogen.	Tetracyclines, Chloramphenicol, Erythromycin
Bactericidal	Kill bacteria directly, do not depend on the immune system.	Penicillins, Cephalosporins, Aminoglycosides, Fluoroquinolones

Spectrum of Activity

Type	Description	Examples
Narrow Spectrum	Effective against a limited group of bacteria (e.g., Gram-positive or Gram-negative).	Penicillin G, Aminoglycosides, Clindamycin
Broad Spectrum	Effective against a wide variety of Gram-positive and Gram-negative bacteria.	Tetracyclines, Ciprofloxacin, Chloramphenicol

Chemical Structure

Class	Examples	Mechanism of Action
Beta-Lactams	Penicillins, Cephalosporins, Carbapenems	Inhibit bacterial cell wall synthesis
Macrolides	Erythromycin, Azithromycin, Clarithromycin	Inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit
Tetracyclines	Tetracycline, Doxycycline, Minocycline	Inhibit protein synthesis by binding to the 30S ribosomal subunit
Aminoglycosides	Gentamicin, Amikacin	Inhibit protein synthesis by binding to the 30S ribosomal subunit, bactericidal
Quinolones	Ciprofloxacin, Levofloxacin	Inhibit bacterial DNA gyrase and topoisomerase IV
Sulphonamides	Cotrimoxazole, Sulphadoxine	Inhibit folic acid synthesis, essential for bacterial DNA replication
Nitroimidazoles	Metronidazole, tinidazole, nimorazole,	Disrupt the DNA of the susceptible bacteria and inhibit the protein synthesis of the cell wall leading to cell death; they act as bactericidal and antimicrobial agents.

During Pregnancy

Penicillins and Cephalosporins are drugs of choice in pregnancy and breastfeeding .

In pregnancy, avoid quinolones, tetracyclines, aminoglycosides, unless severe or life threatening infection,

high dose metronidazole, trimethoprim (in first trimester – folate antagonist) and nitrofurantoin (at term – risk of neonatal haemolysis).

British National Formulary (BNF) guidance with respect to antibiotic use in pregnancy states:

$\"checked\"$ penicillins and cephaloridines are safe to use throughout pregnancy
$\"unchecked\"$ sulfonamides interfere with the bile conjugating mechanism of the neonate, thus sulphonamides should be avoided if delivery is imminent
$\"unchecked\"$ tetracyclines should not be used in pregnancy. This group of drugs stains developing bone and teeth in the foetus. Also the use of tetracyclines, when administered intramuscularly, has occasionally produced maternal liver failure
$\"unchecked\"$ erythromycin – not known to be harmful
$\"unchecked\"$ metronidazole – manufacturer advises avoidance of high-dose regimens
$\"unchecked\"$ streptomycin may cause foetal auditory nerve damage
$\"unchecked\"$ trimethoprim – this is safe after the first trimester. However, the sulfonamide warning applies for trimethoprim – sulfonamide preparations

Breastfeeding

Penicillins and Cephalosporins are drugs of choice in breastfeeding.

Penicillins in breastfeeding :

all penicillin antibitotics can be used during breastfeeding with precautionary infant monitoring
flucloxacillin, phenoxymethylpenicillin (penicillin V) and the broad-spectrum penicillins, such as amoxicillin and ampicillin, are the preferred choices as there is more evidence and experience to support their use
pharmacokinetic properties and characteristics of all the penicillins are very similar although protein binding and bioavailability vary between the different penicillins, they are all acidic in nature and therefore only negligible quantities pass into milk
treatment choice should be primarily based on clinical indications and in line with national and local antimicrobial policy, with suitability in breastfeeding as a secondary consideration ideally treatment should be at the lowest therapeutic dose for shortest duration of time

A review has stated :

Safe for administration:

aminoglycosides
amoxicillin
amoxicillin-clavulanate
antitubercular drugs
cephalosporins
macrolides
trimethoprim-sulfamethoxazole
trimethoprim – the BNF states that \’..short-term use not known to be harmful\’

Effects not known/to be used with caution:

chloramphenicol
clindamycin
dapsone
mandelic acid
nalidixic acid
nitrofurantoin – the BNF states \’..avoid; only small amounts in milk but could be enough to produce haemolysis in G6PD-deficient infants..\’
tetracyclines

Not recommended:

quinolones

BETA-LACTAM ANTIBIOTICS

Definition: Beta-lactam antibiotics are a class of antibiotics characterized by a beta-lactam ring in their chemical structure. They primarily include:

Penicillins
Cephalosporins
Carbapenems

Mechanism of Action: Beta-lactam antibiotics inhibit bacterial cell wall synthesis by targeting peptidoglycan, a crucial component that provides rigidity to bacterial cell walls. They inhibit transpeptidases, also known as penicillin-binding proteins (PBPs), which are essential for peptidoglycan synthesis.

PENICILLINS

Origin: Penicillins are derived from the fungus Penicillium chrysogenum.

Classification:

Natural Penicillins
Semisynthetic Penicillins

Examples:

Natural Penicillins:

Sodium Penicillin G
Procaine Penicillin G
Benzathine Penicillin G
Phenoxymethyl Penicillin (Penicillin V)

Semisynthetic Penicillins:

Cloxacillin
Ampicillin
Amoxicillin
Amoxicillin + Clavulanic Acid

Pharmacokinetics of Penicillin G

Absorption: Destroyed by gastric acid; food interferes with absorption.
Distribution: Therapeutic concentrations can reach the CSF in the presence of inflammation.
Excretion: Primarily through the kidneys.

Dosage:

Benzylpenicillin: 0.5-4 million units (MU)
Procaine Penicillin: 0.5-2 MU
Benzathine Penicillin: 1.2 -2.4 MU

Indications for Penicillins

Pneumococcal Infections: Pneumonia, meningitis, osteomyelitis.
Streptococcal Infections: Pharyngitis, sinusitis, pneumonia, endocarditis.
Meningococcal Infections
Other Infections: Syphilis, diphtheria, tetanus, gas gangrene, anthrax, necrotizing fasciitis, prevention of rheumatic fever, bites, and mouth infections.

Side Effects

Allergic Reactions: Skin rashes, urticaria, fever, bronchospasm, serum sickness, anaphylaxis.
Neurological: Confusion, muscle twitching, convulsions, coma (from large doses).
Injection Site Reactions: Pain at the site of injection, thrombophlebitis with intravenous administration.

Drug Interactions

Probenecid: Inhibits renal excretion of penicillins.
Oral Contraceptives: Reduced effectiveness.
Methotrexate: May increase toxicity due to reduced excretion.

Nursing Considerations

Intramuscular administration of benzyl penicillin can be painful.
Intravenous penicillin must be given separately to avoid incompatibility.
Avoid large doses of intravenous benzyl penicillin to prevent convulsions.
Administer benzathine penicillin as two injections at separate sites.

AMPICILLIN

Description: Ampicillin is a semisynthetic penicillin with broad-spectrum activity against both gram-positive and gram-negative bacteria.

Pharmacokinetics:

Absorption: Poorly absorbed; food reduces its absorption.
Distribution: Widely distributed throughout the body.
Excretion: Primarily through the kidneys.

Dosage: 500 mg – 2 g.

Indications:

Infections: Bronchitis, septicaemia, urinary tract infections, endocarditis, gonorrhea, acute cholecystitis, pneumonia, typhoid, meningitis, sinusitis, otitis media.

Contraindications:

Hypersensitivity to penicillins.
Infectious mononucleosis.

Side Effects:

Nausea and vomiting, fever, diarrhea, rash, urticaria, antibiotic-related colitis, serum sickness-like reaction, pain at injection site.

Drug Interactions:

Allopurinol may increase the incidence of skin rashes.
May reduce the effectiveness of oral contraceptives.
Increased toxicity risk when combined with methotrexate or anticoagulants.

Nursing Considerations:

Take oral ampicillin 30 minutes before food.
Monitor for allergic reactions after administration.
Avoid mixing aminoglycosides with ampicillin during IV administration.

AMOXICILLIN

Dosage: 250-500 mg every 8 hours.

Pharmacokinetics:

Well absorbed orally; not affected by food.
Distributed in lungs, prostate, ears, tonsils, and sputum.
Partially metabolized in the liver and excreted in urine.

Indications:

Pneumonia, urinary tract infections, dental abscess, Lyme disease, otitis media, Helicobacter pylori eradication, biliary tract infections, sinusitis, chronic bronchitis.

Contraindications:

Known hypersensitivity to penicillin, infectious mononucleosis, penicillin-associated jaundice.

Side Effects:

Nausea, vomiting, diarrhea, skin rash, hepatitis, serum sickness-like syndrome, hemolytic anemia, urticaria.

Drug Interactions:

May decrease effectiveness of oral contraceptives.
Allopurinol may increase the incidence of skin rashes.
Probenecid may increase blood concentration and risk of toxicity.

Nursing Considerations:

Ensure the client completes the prescribed course of treatment.

CLOXACILLIN

Description: Cloxacillin is resistant to destruction by penicillinase, making it effective against beta-lactamase-producing Staphylococcus aureus.

Pharmacokinetics:

Poorly absorbed (50%); absorption reduced by food.
Partially metabolized in the liver and excreted unchanged in urine.

Indications:

Septicaemia, impetigo, staphylococcal endocarditis, pyomyositis, cellulitis, pneumonia, septic arthritis, osteomyelitis, prophylaxis in bone and joint surgery.

Contraindications:

Known hypersensitivity.

Side Effects:

Serum sickness-like reactions, antibiotic-associated colitis, joint pains, hemolytic anemia, candidiasis, diarrhea, skin rashes, nausea, vomiting, urticaria, hepatitis, pain, and inflammation at the injection site.

Drug Interactions:

Synergistic effect with aminoglycosides; probenecid decreases renal excretion and oral contraceptive effectiveness.

Nursing Considerations:

Administer on an empty stomach or one hour before meals.
Complete the prescribed treatment to avoid relapse.

AMOXICILLIN + CLAVULANIC ACID

Mechanism: Clavulanic acid binds to beta-lactamase, protecting amoxicillin from degradation.

Indications:

Pneumonia, sinusitis, urinary tract infections, wound infections, cellulitis, dental infections, animal bites, otitis media, tonsillitis, urethritis, boils, osteomyelitis, intra-abdominal sepsis, septic abortion, acute exacerbation of chronic bronchitis.

Contraindications:

Known hypersensitivity to penicillin.
History of jaundice or hepatic dysfunction associated with penicillin or amoxicillin.

Side Effects:

Diarrhea, nausea, vomiting, skin rashes, urticaria, gastritis, abdominal discomfort, vaginitis, anorexia, antibiotic-associated colitis.

Drug Interactions:

Reduces effectiveness of oral contraceptives.
Allopurinol may increase skin rash incidence.
Probenecid decreases renal excretion.

Nursing Considerations:

Take with meals to minimize gastrointestinal disturbance.
Maintain adequate hydration to prevent crystalluria.
Store parenteral clavulanic acid immediately after mixing; tablets in airtight containers due to degradation risk.

CEPHALOSPORINS

Description: Cephalosporins are semisynthetic beta-lactam antibiotics that are broad-spectrum and less susceptible to beta-lactamases. They are used when penicillins prove ineffective.

Mechanism of Action: Cephalosporins are bactericidal, inhibiting bacterial cell wall synthesis.

Classification:

First Generation: Cephalexin, Cefadroxil, Cefazolin (effective against gram-positive bacteria, limited gram-negative activity).
Second Generation: Cefuroxime, Cefaclor (increased gram-negative activity).
Third Generation: Ceftriaxone, Ceftazidime (more effective against resistant gram-negative bacteria).
Fourth Generation: Cefepime (increased activity against gram-negative organisms).

PHARMACOKINETICS OF CEPHALOSPORINS

CEFTRIAXONE

Definition: Ceftriaxone is a broad-spectrum cephalosporin antibiotic, primarily used to treat various bacterial infections. It is effective against a wide range of Gram-positive and Gram-negative bacteria.

Mechanism of Action:

Ceftriaxone works by inhibiting bacterial cell wall synthesis, leading to cell lysis and death. It binds to penicillin-binding proteins (PBPs), which are essential for cell wall integrity.

Available Preparations:

Injection: Available as a powder for reconstitution in vials (1 g, 2 g).

Dosage:

Adults:

Typical dose: 1-2 g IV/IM once daily.
In severe infections, doses may be increased to 4 g daily.

Children:

For children over 12 years or those weighing more than 50 kg, doses similar to adults may be used.
For younger children: 50-75 mg/kg/day, given once daily or divided every 12 hours.

Pharmacokinetics:

Absorption: Administered parenterally (IV or IM); not absorbed well from the gastrointestinal tract.
Distribution: Widely distributed in body tissues and fluids, including the central nervous system (CNS). It crosses the placenta and is excreted in breast milk.
Metabolism: Minimal hepatic metabolism.
Excretion: Primarily excreted unchanged in urine; about 50-60% of a dose is eliminated by the kidneys.

Indications:

Ceftriaxone is used to treat a variety of infections, including:

Respiratory Tract Infections: Pneumonia, bronchitis, and infections caused by Streptococcus pneumoniae and Haemophilus influenzae.
Skin and Soft Tissue Infections: Including cellulitis and abscesses.
Bone and Joint Infections: Such as osteomyelitis and septic arthritis.
Intra-abdominal Infections: Complicated intra-abdominal infections (often combined with metronidazole).
Meningitis: Effective against common pathogens causing bacterial meningitis.
Gonorrhea: Treatment of uncomplicated gonococcal infections.
Sepsis: Empirical treatment for severe infections and septic shock.

Contraindications:

Known hypersensitivity to ceftriaxone or other cephalosporins.
Severe allergic reactions to penicillin (cross-reactivity possible).
Newborns (particularly those requiring calcium treatment, due to risk of precipitation).

Side Effects:

Common Side Effects:

Nausea and vomiting
Diarrhea
Abdominal pain
Rash
Local irritation at injection site

Serious Side Effects:

Allergic reactions (anaphylaxis)
Superinfection (overgrowth of non-susceptible organisms)
Clostridium difficile-associated diarrhea (CDAD)
Hemolytic anemia
Liver enzyme elevations

Drug Interactions:

Probenecid: Can increase ceftriaxone levels by inhibiting renal excretion.
Calcium: Caution when administered simultaneously, especially in neonates, as it may lead to precipitation in the lungs and kidneys.
Anticoagulants: May enhance the anticoagulant effect of warfarin; monitoring is advised.

Nursing Considerations:

Administration: Ceftriaxone should be given IV or IM; ensure proper reconstitution if using the powder form.

Monitoring:

Monitor for signs of allergic reactions, especially after the first dose.
Assess liver and kidney function, as well as blood counts.
Watch for gastrointestinal symptoms and signs of superinfection.

Patient Education:

Advise patients to report any signs of rash, itching, or swelling.
Instruct on the importance of completing the full course of antibiotics.
Inform about potential side effects, including diarrhea, and when to seek medical attention.

CARBAPENEMS

Description: Carbapenems are broad-spectrum beta-lactam antibiotics resistant to most beta-lactamases.

Examples:

Imipenem + Cilastatin
Meropenem
Ertapenem

Pharmacokinetics:

Poor oral absorption; administered IV.
Widely distributed with high tissue concentrations.
Eliminated primarily through renal excretion.

Indications:

Complicated infections, intra-abdominal infections, CNS infections, skin and soft tissue infections, septicemia, and respiratory tract infections.

Contraindications:

Known hypersensitivity.

Side Effects:

Nausea, vomiting, diarrhea, hypersensitivity reactions, seizures, rash, headache.

Drug Interactions:

Probenecid can increase levels of carbapenems; concurrent use with valproic acid may reduce levels.

Nursing Considerations:

Monitor renal function and signs of hypersensitivity.
Educate patients about potential side effects.
Administer as a slow IV infusion.

MACROLIDES

Macrolides are a group of antibiotics derived from Streptomyces species. They exhibit primarily bacteriostatic activity but can be bactericidal against some bacteria at higher concentrations.

Mechanism of Action:

Macrolides inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit. This action disrupts the translation process, ultimately preventing the growth and replication of bacteria.

Examples of Macrolides:

Erythromycin
Azithromycin
Clarithromycin
Roxithromycin

Erythromycin

Available Preparations:

Tablet: 250 mg
Powder for Oral Suspension: 125 mg/5 mL

Dosage:

Adults: 250-500 mg
Children: 125-250 mg

Pharmacokinetics:

Absorption: Adequately absorbed from the gastrointestinal tract; optimal absorption occurs 1-2 hours after meals.
Distribution: Widely distributed in tissues; crosses the placenta and is secreted in breast milk.
Metabolism: Primarily metabolized in the liver.
Excretion: Excreted in bile.

Indications:

Pneumonia
Campylobacter enteritis
Acne vulgaris
Chancroid
Prostatitis
Acute otitis media
Sinusitis
Whooping cough
Lymphogranuloma venereum
Skin and soft tissue infections
Non-gonococcal urethritis
Bronchitis
Neonatal conjunctivitis
Pharyngitis and tonsillitis

Contraindications:

Allergy to macrolides
Porphyria
Severe hepatic impairment

Side Effects:

Nausea
Abdominal discomfort
Urticaria
Reversible hearing loss
Vomiting
Diarrhea
Skin rash
Pancreatitis

Drug Interactions:

Increases plasma concentrations of carbamazepine.
May inhibit the metabolism of dexamethasone, hydrocortisone, and prednisolone.
Increases the anticoagulant effect of warfarin.

Nursing Considerations for Erythromycin:

Administer on an empty stomach for optimal absorption unless gastrointestinal upset occurs, in which case it can be taken with food.
Inform the patient about potential drug interactions and the necessity to consult a healthcare provider before taking additional medications.
Monitor liver function, and discontinue use if severe hepatic dysfunction occurs.

Azithromycin

Available Preparations:

Capsules/Tablets: 250 mg, 500 mg
Powder for Oral Suspension: 200 mg/5 mL

Dosage:

Adults: 500 mg once daily
Children: 200 mg-500 mg once daily

Pharmacokinetics:

Absorption: Rapidly absorbed from the gut; food reduces its absorption.
Distribution: Widely distributed in body tissues.
Metabolism: Partially metabolized in the liver.
Excretion: Excreted in bile, both unchanged and as metabolites.

Indications:

Pneumonia
Skin and soft tissue infections
Typhoid fever
Pharyngitis/Tonsillitis
Trachoma
Pelvic inflammatory disease
Bronchitis
Pertussis (whooping cough)
Sinusitis
Otitis media
Traveler’s diarrhea
Mycobacterium avium complex (MAC) infections
Non-gonococcal urethritis

indications:

Known hypersensitivity to macrolides
Severe hepatic impairment

Side Effects:

Anorexia
Nausea
Vomiting
Dyspepsia
Constipation
Headache
Dizziness
Taste disturbances
Vertigo
Flatulence
Abdominal discomfort
Convulsions
Somnolence
Skin rash

Drug Interactions:

Concurrent administration of antacids containing aluminum or magnesium salts can reduce the absorption rate but not the extent of absorption.
Avoid concomitant use with lumefantrine and artemether.
Plasma concentrations of azithromycin may be increased by ritonavir.
Azithromycin increases the plasma concentration of digoxin.
Enhances the anticoagulant effect of warfarin.
The effectiveness of oral contraceptives may be reduced by azithromycin.

Nursing Considerations for Azithromycin:

Shake the suspension well before use.
Administer on an empty stomach (one hour before or two hours after meals).
Once-daily dosing is recommended due to its long half-life.

TETRACYCLINES

Tetracyclines are broad-spectrum antibacterial drugs derived from Streptomyces species. They are effective against both gram-positive and gram-negative bacteria and are active against organisms like mycoplasma, chlamydiae, spirochetes, and rickettsiae. However, due to widespread bacterial resistance, they are no longer the first-line treatment for many infections.

Mode of Action:

Bacteriostatic, inhibiting bacterial protein synthesis by reversibly binding to the 30S subunit of the bacterial ribosome.

Types of Tetracyclines:

Tetracycline
Doxycycline
Minocycline
Oxytetracycline

Tetracycline

Available Preparations:

Capsules 250mg
Eye ointment 1%
Skin ointment 3%

Pharmacokinetics:

Well absorbed but reduced by food presence.
Widely distributed to body tissues and fluids.
Partially metabolized in the liver.
Excreted unchanged in the urine.

Dose:

Adults: 250-500mg

Indications:

Brucellosis
Acne vulgaris
Trachoma
Lymphogranuloma venereum
Bronchitis
Non-gonococcal urethritis
Malaria
Gonorrhea
Shigellosis
Rosacea
Cholera
Pharyngitis
Sinusitis
Periodontal disease

Contraindications:

Children below 12 years
Pregnant and breastfeeding mothers
Known hypersensitivity to tetracyclines

Side Effects:

Anorexia
Nausea
Diarrhea
Sore throat
Photosensitivity
Epigastric distress
Vomiting
Stomatitis
Headache
Hypersensitivity reactions

Doxycycline

Available Preparations:

Capsules 100mg
Tablets 100mg

Dose:

Adults: 100mg twice daily (bd)

Pharmacokinetics:

Well absorbed orally.
Widely distributed to body tissues and fluids.
Excreted in feces.

Indications:

Acne vulgaris
Anthrax
Syphilis
Exacerbation of chronic bronchitis
Acute bacterial sinusitis
Pelvic inflammatory disease (PID)
Non-gonococcal urethritis
Malaria treatment and prevention
Recurrent aphthous ulcer

Contraindications:

Children under 8 years (causes staining and occasionally dental hypoplasia)
Pregnant and breastfeeding mothers
Hypersensitivity to tetracyclines
Porphyria

Side Effects:

Nausea
Vomiting
Loss of appetite
Esophageal irritation
Permanent staining of teeth
Vaginal candidiasis
Flushing
Diarrhea
Headache
Tinnitus
Photosensitivity

Drug Interactions:

Antacids, iron, calcium, and magnesium preparations impair absorption.
Doxycycline may increase the anticoagulant effect of oral anticoagulants.
Decreases therapeutic effect of penicillins.
May reduce the efficacy of oral contraceptives.

Nursing Considerations:

Should be taken with plenty of water to reduce esophageal irritation risk.
Avoid use in children below 12 years.
Photosensitivity may occur with prolonged sun exposure.

AMINOGLYCOSIDES

Aminoglycosides are antibacterial drugs derived from Actinomycetes species (Streptomyces and Micromonospora). They are poorly absorbed from the gastrointestinal tract, so they are administered via injection for systemic infections or topically for skin, mucous membrane, and ocular infections. Co-administration with cell wall-acting drugs like penicillins enhances their effectiveness.

Mode of Action:

Bactericidal, inhibiting protein synthesis by irreversibly binding to the 30S ribosomal subunit and causing cell membrane damage.

Types of Aminoglycosides:

Gentamicin
Streptomycin
Tobramycin
Paromomycin
Amikacin
Neomycin
Kanamycin

Gentamicin

Available Preparations:

Injection 80mg/2mL
Ear/Eye drops 0.3%
Skin ointment 0.1%

Pharmacokinetics:

Completely absorbed from IM injection sites.
Distributed to tissues and fluids, including urine (poor CSF penetration).
Excreted unchanged in urine; accumulates in renal impairment.

Dose:

Adults: 3-5 mg/kg daily (IM/IV)
Children (1 month-12 years): 2.5 mg/kg

Indications:

Urinary tract infections
Bacterial endocarditis
Pelvic inflammatory disease
Skin infections (burns, ulcers)
Surgical prophylaxis
Biliary tract infections
Otitis externa
Brucellosis
Pneumonia
Septicemia
Neonatal sepsis

Contraindications:

Hypersensitivity to aminoglycosides
Myasthenia gravis

Side Effects:

Nephrotoxicity
Ototoxicity
Headache
Rash
Nausea
Diarrhea
Blood disorders

Drug Interactions:

Increases nephrotoxicity risk with amphotericin B.
Increases ototoxicity risk with frusemide.
Vancomycin increases nephrotoxicity and ototoxicity risks.
Suxamethonium increases muscle relaxation effects.

Nursing Considerations:

Administer penicillins or cephalosporins at least one hour before or after gentamicin to avoid incompatibility.
Adjust dose in renal impairment.
Use cautiously in elderly patients due to the risk of renal and auditory impairment.

SULPHONAMIDES & TRIMETHOPRIM

Sulphonamides are a class of antibacterial agents structurally related to para-aminobenzoic acid (PABA). Their therapeutic importance has decreased due to widespread resistance. Trimethoprim is often combined with sulphonamides, specifically sulfamethoxazole, to form co-trimoxazole, increasing their effectiveness.

Mode of Action:

Sulphonamides are bacteriostatic, inhibiting bacterial folic acid synthesis.
Trimethoprim blocks bacterial dihydrofolate reductase, further inhibiting folate synthesis.

Types of Sulphonamides:

Cotrimoxazole (Trimethoprim + Sulfamethoxazole)
Sulphadiazine
Sulfasalazine
Sulphamethoxazole
Silver sulphadiazine
Sulphadoxine

Classification of Sulphonamides:

Rapidly absorbed and excreted: Sulphamethoxazole, Sulphadiazine
Poorly absorbed, active in bowel lumen: Sulfasalazine
Topical use: Silver sulphadiazine
Long-acting: Sulphadoxine

Cotrimoxazole (Trimethoprim + Sulfamethoxazole)

Available Preparations:

Tablets: 480mg, 960mg
Oral suspension: 240mg/5mL
Injection for infusion: 960mg/3mL

Dose:

Adults (oral): 960mg per dose
Children: 24mg/kg per dose

Pharmacokinetics:

Well absorbed after oral administration.
Widely distributed to tissues and fluids.
Excreted in urine.

Indications:

Urinary tract infections
Granuloma inguinale
Toxoplasmosis
Brucellosis
Shigellosis
Pneumocystis carinii pneumonia (PCP)
Pneumonia
Bronchitis
Otitis media
Traveler’s diarrhea

Contraindications:

Hypersensitivity to sulphonamides or trimethoprim
Severe renal or hepatic failure
Neonates

Side Effects:

Nausea
Headache
Skin rash
Urticaria
Anorexia
Photosensitivity reactions
Diarrhea
Itching
Renal failure
Hyperkalemia
Stomatitis

Drug Interactions:

Co-trimoxazole may increase digoxin levels.
Oral contraceptive efficacy may be reduced.
Co-trimoxazole increases the anticoagulant effect of warfarin.
May enhance the blood glucose-lowering effects of oral antidiabetics.

Nursing Considerations:

Ensure patients on co-trimoxazole take plenty of fluids to reduce crystalluria and potential kidney damage.
Monitor patients closely for life-threatening reactions and discontinue if any signs appear.

QUINOLONES

Quinolones are a class of synthetic antibacterial agents that inhibit bacterial DNA synthesis by targeting DNA gyrase and topoisomerase IV. They are bactericidal and effective against a broad range of gram-negative and some gram-positive bacteria. Quinolones are classified into generations based on their spectrum of activity.

Classification of Quinolones:

First-generation: Nalidixic acid
Second-generation: Ciprofloxacin, Norfloxacin, Ofloxacin, Pefloxacin, Lomefloxacin
Third-generation: Levofloxacin, Sparfloxacin, Gatifloxacin, Moxifloxacin

Nalidixic Acid

Available Preparations:

Tablets: 500mg

Pharmacokinetics:

Well absorbed from the gastrointestinal tract.
Concentrates in renal tissues and seminal fluid.
Metabolized in the liver to a more active form.
Excreted in urine.

Indications:

Urinary tract infections
Shigellosis

Contraindications:

Hypersensitivity
History of epilepsy
CNS lesions

Dose:

Adults: 500mg-1g every 6 hours
Children (>3 months): 15-50mg/kg every 6 hours

Side Effects:

Nausea
Dizziness
Confusion
Vomiting
Vertigo
Weakness
Skin rash
Urticaria
Headache
Cranial nerve palsy
Diarrhea
Visual disturbances
Abdominal pain
Convulsions

Drug Interactions:

Probenecid prolongs the half-life of nalidixic acid.
Increased risk of bleeding with oral anticoagulants.

Nursing Considerations:

Advise patients to take nalidixic acid on an empty stomach, preferably one hour before meals.

Ciprofloxacin

Available Preparations:

Tablets: 500mg, 1g
Injection: 200/100mL
Eye drops: 0.3% w/v

Pharmacokinetics:

Rapidly and well absorbed when taken orally, with 70-80% bioavailability.
Widely distributed throughout the body, with good tissue and bone penetration.
Metabolized in the liver.
Excreted in urine and feces.

Indications:

Urinary tract infections
Surgical prophylaxis
Chronic prostatitis
Traveler’s diarrhea
Shigellosis
Peritonitis
Gonorrhea
Respiratory tract infections
Prophylaxis of meningococcal meningitis
Septicemia
Typhoid
Chancroid
Cholera
Otitis externa
Bone and joint infections
Anthrax

Contraindications:

Breastfeeding
Pregnancy
Allergy to ciprofloxacin
Children below 18 years

Dose:

Oral (adults): 250-750mg twice daily

Side Effects:

Headache
Restlessness
Palpitations
Diarrhea
Drowsiness
Depression
Nausea and vomiting
Urticaria
Anorexia
Dizziness
Lightheadedness
Skin rash
Convulsions
Dyspepsia
Tremors
Abdominal discomfort
Insomnia

Drug Interactions:

Antacids containing aluminum and magnesium interfere with absorption.
Concomitant use with probenecid increases ciprofloxacin plasma levels.
Ciprofloxacin increases phenytoin, theophylline, and anticoagulant blood levels.
Efficacy is reduced by iron salts and sucralfate.
May increase the effects of oral anticoagulants.

Nursing Considerations:

Ciprofloxacin should be taken one hour before or two hours after meals for optimal absorption.
Advise patients to drink plenty of fluids while on ciprofloxacin.
Patients should avoid taking dairy products, antacids, iron, zinc, or calcium supplements with ciprofloxacin.
Ciprofloxacin may increase the effects of caffeine, so advise patients to reduce caffeine intake.
It may worsen seizures in epileptic patients.

NITROIMIDAZOLES

Nitroimidazoles are a class of antimicrobial agents that are primarily effective against anaerobic bacteria and protozoa. They work by disrupting DNA synthesis in these microorganisms.

Mechanism of Action: Nitroimidazoles, including metronidazole, are prodrugs that require reduction by anaerobic bacteria or protozoa to become active. The reduced form interacts with DNA, causing strand breakage and inhibiting nucleic acid synthesis, ultimately leading to cell death.

METRONIDAZOLE

Description: Metronidazole is a synthetic nitroimidazole antibiotic with antiprotozoal and antibacterial properties, particularly effective against anaerobic bacteria and certain protozoa such as Trichomonas vaginalis, Entamoeba histolytica, and Giardia lamblia.

Pharmacokinetics:

Absorption: Rapidly and well absorbed from the gastrointestinal tract; food does not significantly affect absorption.
Distribution: Widely distributed in body tissues and fluids, including the CNS and saliva.
Metabolism: Primarily metabolized in the liver.
Excretion: Excreted mainly through urine as metabolites.

Dosage:

Adult Dose: Varies based on infection; typically, 500 mg orally 2-3 times daily for infections.

Indications

Bacterial Infections: Anaerobic infections, including intra-abdominal infections, pelvic inflammatory disease, and skin and soft tissue infections.
Protozoal Infections:

Trichomoniasis
Giardiasis
Amoebic dysentery

Clostridium difficile Infection: Used in treatment of mild to moderate cases.
Surgical Prophylaxis: Particularly in colorectal surgery.
Other Uses: Treatment of H. pylori eradication in peptic ulcer disease, rosacea, and bacterial vaginosis.

Contraindications

Known Hypersensitivity: Avoid in patients with a history of hypersensitivity to metronidazole or other nitroimidazoles.
First Trimester of Pregnancy: Use with caution; avoid unless absolutely necessary.

Side Effects

Gastrointestinal: Nausea, vomiting, diarrhea, abdominal pain, metallic taste.
Neurological: Headaches, dizziness, peripheral neuropathy (with long-term use).
Dermatological: Rash, urticaria, Stevens-Johnson syndrome (rare).
Other: Darkening of urine, seizures (rare, with overdose).

Drug Interactions

Alcohol: Concurrent use can lead to a disulfiram-like reaction (flushing, nausea, vomiting).
Anticoagulants: May enhance the effects of warfarin and other anticoagulants, increasing bleeding risk.
Lithium: Metronidazole may increase lithium levels, leading to toxicity.
CYP450 Inhibitors: May interact with drugs metabolized by CYP enzymes, potentially increasing their effects.

Nursing Considerations

Administering Medication: Metronidazole can be given orally or intravenously; for intravenous administration, infuse slowly to prevent infusion reactions.
Patient Education:

Instruct patients to avoid alcohol during treatment and for at least 48 hours after discontinuation.
Advise patients about potential side effects, including gastrointestinal disturbances and metallic taste.

Monitoring:

Monitor liver function tests, especially in patients with hepatic impairment.
Assess for signs of peripheral neuropathy, particularly with prolonged use.
Ensure patients complete the full course of therapy to prevent resistance.

Specific Anti-microbial Agents Read More »

DRUGS USED IN PAEDIATRICS

The field of pediatric pharmacology focuses on the safe and effective use of medications in children, from infancy to adolescence.

Pediatric patients require special consideration due to their developing physiology, which affects how drugs are absorbed, distributed, metabolized, and excreted. Here is an introduction to the key aspects of drugs used in pediatrics:

Nursing Considerations in Pediatric Pharmacology

1. Developmental Pharmacokinetics:

Absorption: The gastrointestinal tract of infants and young children is still developing, which can affect the absorption of oral medications.
Distribution: The distribution of drugs can vary due to differences in body composition, such as higher total body water and lower fat content in infants.
Metabolism: The liver enzymes responsible for drug metabolism are not fully mature in newborns and infants, leading to slower drug clearance.
Excretion: Renal function is also immature in newborns, affecting the excretion of drugs and their metabolites.

2. Dosing Considerations:

Dosing in pediatrics is often based on body weight or body surface area rather than fixed doses used in adults.
Growth and development can rapidly change, requiring frequent adjustments in dosing.

3. Safety and Adverse Effects:

Children are more susceptible to certain adverse effects due to their developing organs and systems.
Long-term effects of medications on growth, development, and future health must be considered.

4. Off-Label Use:

Many medications used in pediatrics are not specifically approved for use in children, leading to off-label prescribing based on clinical experience and available data.

1. Antibiotics

$\"Ampicillin\"$

Ampicillin

Dose: 50 mg/kg
Class: Beta-lactam antibiotic, specifically a penicillin derivative.
Mechanism of Action: Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins.

Indications:

Effective against Gram-positive bacteria like Streptococcus pneumoniae, Enterococcus faecalis, and some Gram-negative bacteria like Haemophilus influenzae.
Bacterial infections (e.g., pneumonia, meningitis)
Urinary tract infections
Otitis media
Sepsis
Endocarditis prophylaxis
Gastrointestinal infections
Skin and soft tissue infections

Contraindications:

Hypersensitivity to penicillin or cephalosporins
History of severe allergic reactions (anaphylaxis)
Severe renal impairment
Infectious mononucleosis (risk of rash)

Nursing Considerations:

Monitor for allergic reactions (e.g., rash, difficulty breathing).
Assess renal function prior to administration.
Administer with caution in patients with a history of seizures.
Confirm proper dosing based on weight and age.
Pharmacokinetics: Ampicillin is absorbed in the gastrointestinal tract but is susceptible to degradation by stomach acids. It has good tissue penetration and crosses the placenta.
Adverse Effects: Diarrhea, allergic reactions, including anaphylaxis in susceptible patients.

$\"Gentamicin-InjectionIntogen-2ml-scaled\"$

Gentamicin

Dose: 7.5 mg/kg
Class: Aminoglycoside antibiotic.
Mechanism of Action: Bactericidal, inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit.

Indications:

Treatment of severe infections caused by Gram-negative bacteria like E. coli and Klebsiella; also used in neonatal sepsis.
Serious bacterial infections (e.g., sepsis, pneumonia)
Urinary tract infections
Infections in immunocompromised patients
Endocarditis (in combination with other antibiotics)
Osteomyelitis
Intra-abdominal infections
Meningitis (if caused by susceptible organisms)

Contraindications:

Hypersensitivity to aminoglycosides
Pre-existing renal impairment
Myasthenia gravis
Concurrent use of other nephrotoxic or ototoxic drugs

Nursing Considerations:

Monitor renal function and drug levels (peak and trough).
Assess for signs of ototoxicity (e.g., tinnitus, dizziness).
Administer IV slowly to reduce the risk of toxicity.
Ensure hydration to minimize nephrotoxicity.
Pharmacokinetics: Poor oral absorption; given intravenously or intramuscularly. Mainly excreted through the kidneys.
Adverse Effects: Ototoxicity, nephrotoxicity, vestibular damage.

$\"\"$

Benzyl Penicillin (Penicillin G)

Dose: 50,000 IU/kg
Class: Beta-lactam antibiotic.
Mechanism of Action: Inhibits cell wall synthesis, particularly effective against Gram-positive bacteria.

Indications:

Severe infections (e.g., pneumonia, meningitis)
Syphilis
Streptococcal and staphylococcal infections
Endocarditis
Bacterial endophthalmitis
Bone and joint infections
Meningitis

Contraindications:

Hypersensitivity to penicillin
History of anaphylaxis to related antibiotics
Severe liver impairment
Caution in patients with asthma

Nursing Considerations:

Monitor for allergic reactions after administration.
Review liver and renal function tests.
Administer via appropriate route and ensure correct dilution.
Educate families on signs of allergic reactions.
Pharmacokinetics: Poor oral absorption, so it is administered intramuscularly or intravenously.
Adverse Effects: Hypersensitivity reactions, including rash and anaphylaxis.

$\"Amoxicillin\"$

Amoxicillin

Dose: Based on age.

2-12 months: 250 mg every 12 hours for 5 days
1-3 years: 500 mg every 12 hours for 5 days
3-5 years: 750 mg every 12 hours for 5 days

Class: Aminopenicillin.
Mechanism of Action: Inhibits bacterial cell wall synthesis.

Indications:

Otitis media
Lower respiratory tract infections, and bacterial sinusitis.
Pneumonia
Urinary tract infections
Skin and soft tissue infections
Gastrointestinal infections (e.g., H. pylori eradication)
Endocarditis prophylaxis

Contraindications:

Hypersensitivity to penicillin
History of jaundice or liver disease with prior amoxicillin use
Pregnant women with a history of certain liver conditions
Severe renal impairment without dosage adjustment

Nursing Considerations:

Observe for allergic reactions.
Administer with or without food (food may help with stomach upset).
Educate about the full course of treatment completion.
Assess for superinfection (e.g., oral thrush).
Pharmacokinetics: Well absorbed orally, widely distributed, and excreted in urine.
Adverse Effects: Rash, gastrointestinal disturbances like nausea and diarrhea.

$\"Ciprofloxacin\"$

Ciprofloxacin

Dose: 15 mg/kg every 12 hours for 3 days.

If using a 500 mg tablet:
Child < 6 months: ¼ tab.
Child 6 months–5 years: ½ tab.

Class: Fluoroquinolone antibiotic.
Mechanism of Action: Inhibits bacterial DNA gyrase and topoisomerase IV, inhibiting DNA replication.

Indications:

Urinary tract infections
Gastrointestinal infections (e.g., shigellosis. Gastroenteritis (certain pathogens)
Skin and soft tissue infections
Bone and joint infections
Anthrax prophylaxis
Respiratory infections
Infectious diarrhea

Contraindications:

Hypersensitivity to fluoroquinolones
History of tendon disorders related to fluoroquinolones
Myasthenia gravis
Children under 18 years (except for specific infections)

Nursing Considerations:

Monitor for signs of tendon pain or rupture.
Educate on potential side effects (e.g., gastrointestinal symptoms).
Administer with caution in patients with seizure history.
Encourage hydration to prevent crystallization in urine.
Pharmacokinetics: Well absorbed orally but may be reduced by antacids. Mainly excreted unchanged in the urine.
Adverse Effects: Tendon rupture (rare but more frequent in children), photosensitivity, nausea.

2. Antimalarials

$\"artesunate\"$

Rectal Artesunate

Dose: 10 mg/kg
Class: Antimalarial, artemisinin derivative.
Mechanism of Action: Produces reactive oxygen species that damage the parasite\’s proteins and membranes.

Indications:

Severe malaria in children unable to take oral medications
Malaria in pregnant women
Alternative for first-line treatments in specific situations
Emergency treatment for life-threatening malaria

Contraindications:

Hypersensitivity to artemisinin and derivatives
Patients with a known history of severe allergic reactions
Caution in patients with severe hepatic or renal impairment
Infants under a specific weight threshold

Nursing Considerations:

Monitor vital signs and blood glucose levels due to potential hypoglycemia.
Educate families on the administration technique.
Assess for neurologic changes or adverse reactions.
Ensure proper storage conditions for the medication.
Pharmacokinetics: Rapid absorption and action when given rectally. Metabolized in the liver.
Adverse Effects: Nausea, vomiting, dizziness, and occasional allergic reactions.

$\"Artemether$

Artemether/Lumefantrine (Coartem)

Dose: Every 12 hours for 3 days.

2-12 months: 1 tablet
1-3 years: 1 tablet
3-5 years: 2 tablets

Class: Antimalarial.
Mechanism of Action: Artemether kills rapidly, while lumefantrine has a longer half-life and helps prevent recrudescence.

Indications:

Uncomplicated malaria caused by Plasmodium falciparum
Malaria prophylaxis in certain regions
Alternative in cases of drug resistance
Combination therapy for effective treatment regimen

Contraindications:

Hypersensitivity to artemether, lumefantrine, or any excipient
History of severe allergic reactions
Severe liver dysfunction
Caution in patients with underlying cardiac arrhythmias

Nursing Considerations:

Monitor for cardiac effects (QT prolongation).
Administer with food to increase absorption.
Educate about possible side effects (nausea, headache).
Assess for resolution of malaria symptoms.
Pharmacokinetics: Oral absorption is enhanced with fatty meals.
Adverse Effects: Dizziness, weakness, and gastrointestinal disturbances.

3. Antiparasitics

$\"Mebendazole\"$

Mebendazole

Dose:

Child 1-2 years: 250 mg single dose.
Child > 2 years: 500 mg single dose.

Class: Anthelmintic.
Mechanism of Action: Inhibits the uptake of glucose by parasitic worms, leading to their immobilization and death.

Indications:

Enterobiasis (pinworm infection)
Ascariasis (roundworm infection)
Hookworm infections
Whipworm infections
Other intestinal helminthic infections
Strongyloidiasis
Preventive treatment in endemic areas

Contraindications:

Hypersensitivity to mebendazole or any excipients
Pregnancy (especially in the first trimester)
Caution in patients with liver dysfunction
Infants under 2 years (consult a physician)

Nursing Considerations:

Administer with or without food; it is often preferred to take it with food for better absorption.
Monitor for gastrointestinal side effects (e.g., diarrhea).
Educate on hygiene measures to prevent reinfection.
Assess for any signs of infection or allergic reactions.
Pharmacokinetics: Poorly absorbed from the gastrointestinal tract, primarily excreted unchanged in the feces.
Adverse Effects: Abdominal pain, diarrhea, headache.

$\"Albendazole\"$

Albendazole

Dose:

Child 1-2 years: 200 mg single dose.
Child > 2 years: 400 mg single dose.

Class: Anthelmintic.
Mechanism of Action: Inhibits glucose uptake by helminths, disrupting their energy production.

Indications:

Broad-spectrum treatment for intestinal parasites, including pinworms and roundworms.
Neurocysticercosis
Echinococcal disease (hydatid cyst disease)
Ascariasis (roundworm)
Enterobiasis (pinworm)
Hookworm infections
Whipworm infections
Giardiasis (in certain cases)

Contraindications:

Hypersensitivity to albendazole or any excipients
Pregnant women (especially in the first trimester)
Severe liver disease
Caution in patients with a history of bone marrow suppression

Nursing Considerations:

Monitor liver function tests during treatment.
Administer with food to enhance absorption.
Educate about potential side effects (e.g., headache, dizziness).
Assess for signs of hypersensitivity or allergic reactions.
Pharmacokinetics: Poor absorption; metabolized in the liver.
Adverse Effects: Nausea, vomiting, dizziness, headache.

4. Analgesics/Antipyretics

More on Opioids later.

Paracetamol (Acetaminophen)

Dose: Every 6 hours (4 doses in 24 hours).

2 months–3 years: 125 mg.
3-5 years: 250 mg.

Class: Analgesic and antipyretic.
Mechanism of Action: Inhibits prostaglandin synthesis, reducing pain and fever.
Indications: Relief of mild to moderate pain, and fever reduction.

Indications:

Fever management
Pain relief (e.g., headache, toothache)
Post-immunization fever
Musculoskeletal pain (mild to moderate)
Management of pain in children post-surgery
Fever due to infections
Rheumatic disease pain

Contraindications:

Severe liver dysfunction
Known hypersensitivity to paracetamol
Active liver disease
Caution in patients with chronic alcohol use

Nursing Considerations:

Monitor for signs of overdose (e.g., nausea, vomiting).
Educate caregivers on dosage based on weight.
Assess liver function in patients with prolonged use.
Reinforce the importance of not exceeding the recommended dose.
Pharmacokinetics: Well absorbed orally; metabolized in the liver.
Adverse Effects: Hepatotoxicity in overdose, rash, nausea.

5. Vitamins and Supplements

$\"\"$

Folic Acid

Dose: 2.5 mg daily.
Class: Vitamin, essential for DNA synthesis.
Indications: Prevents and treats folic acid deficiency anemia, often given to malnourished children or those with megaloblastic anemia.

Indications:

Megaloblastic anemia due to folate deficiency
Prevention of neural tube defects during pregnancy
Supplementation in malabsorptive conditions
Certain leukemias or malignancies
Alcoholism
Patients on methotrexate or other drugs that inhibit folate metabolism
Growth periods (infancy, adolescence)

Contraindications:

Known hypersensitivity to folate or any excipients
Untreated cobalamin deficiency (may worsen this condition)
Caution in patients overusing alcohol
Certain malignancies (without close supervision)

Nursing Considerations:

Monitor for signs of deficiency (e.g., anemia symptoms).
Educate patients about the importance of diet rich in folate.
Assess history of medication use that affects folate metabolism.
Encourage supplementation before and during pregnancy.
Pharmacokinetics: Absorbed from the small intestine, metabolized in the liver.
Adverse Effects: Rare at therapeutic doses; may cause nausea or rash.

$\"Iron$

Iron (Ferrous Sulfate)

Dose: Once daily for 14 days.

Tablet 200 mg (1/2 tablet for children 1-5 years).
Syrup 25 mg/mL (1 mL for children < 1 year).

Class: Mineral supplement.
Mechanism of Action: Replenishes iron stores for hemoglobin synthesis.
Indications: Treatment of iron deficiency anemia.

Indications:

Iron-deficiency anemia
Prevention of iron deficiency in at-risk populations (e.g., pregnant women, infants)
Chronic blood loss (e.g., GI bleeding)
Nutritional deficiency in vegetarians/vegans
Hemodialysis patients requiring iron replacement
Post-surgical patients with significant blood loss
Patients with malabsorption syndromes

Contraindications:

Hemochromatosis (iron overload)
Hemosiderosis
Known hypersensitivity to iron preparations
Certain gastrointestinal conditions (e.g., peptic ulcer disease)

Nursing Considerations:

Monitor hemoglobin and hematocrit levels during therapy.
Administer on an empty stomach to enhance absorption (unless gastrointestinal upset occurs).
Assess for gastrointestinal side effects (constipation, nausea).
Educate on dietary sources of iron and adherence to therapy.
Adverse Effects: Constipation, gastrointestinal discomfort, dark stools.

6. Antiepileptics/Anticonvulsants

Diazepam in Paediatrics

Class: Benzodiazepine
Pediatric Dose: 0.5 mg/kg (rectal)

Key Points:

Mechanism of Action: Diazepam acts on the gamma-aminobutyric acid (GABA) receptors, enhancing inhibitory neurotransmission, which results in sedation, muscle relaxation, and anti-convulsant effects.
Indications in Pediatrics: Used for febrile seizures, status epilepticus, and acute anxiety disorders in children.

Indications:

Management of anxiety disorders
Treatment of muscle spasm (e.g., from cerebral palsy)
Control of seizures (status epilepticus)
Sedation for medical procedures (preoperative sedation)
Management of acute alcohol withdrawal symptoms
Treatment of hyperactivity in specific cases
Treatment of insomnia in short-term use
Management of panic attacks

Contraindications:

Hypersensitivity to benzodiazepines
Severe respiratory insufficiency (e.g., sleep apnea)
Acute narrow-angle glaucoma
Myasthenia gravis
Pregnancy (especially during the first trimester)
Lactation (not recommended in breastfeeding mothers)
Children under six months of age (unless in severe cases)

Nursing Considerations:

Monitor vital signs (respiration, heart rate) closely during treatment.
Assess for sedation levels and degree of muscle relaxation.
Educate families about the potential for dependence and withdrawal symptoms.
Administer the drug slowly intravenously (if applicable) to prevent hypotension.
Side Effects: Sedation, dizziness, hypotension, and respiratory depression. In children, excessive drowsiness and ataxia can occur.

7. Antifungals

$\"Nystatin$

Nystatin in Pediatrics

Class: Antifungal (Polyene)
Pediatric Dose: 1 mL (oral suspension), four times daily for 7 days

Key Points:

Mechanism of Action: Nystatin binds to ergosterol in the fungal cell membrane, causing membrane disruption and leading to leakage of cellular contents, ultimately killing the fungal cells.
Indications in Pediatrics: Primarily used for oral candidiasis (thrush) and fungal infections in the gastrointestinal tract. It\’s often prescribed for neonates and young infants due to its safety profile.

Indications:

Treatment of oral thrush (candida stomatitis)
Management of esophageal candidiasis
Treatment of skin infections caused by Candida
Prophylaxis for fungal infections in immunocompromised children
Treatment of diaper dermatitis due to yeast
Treatment of vaginal candidiasis (in specific cases)
Treatment of gastrointestinal candidiasis

Contraindications:

Hypersensitivity to nystatin or any component of the formulation
Caution in patients with severe gastrointestinal disease
Topical use in patients with open wounds or burns
Not recommended for systemic fungal infections (not effective)
Caution in patients with adrenal insufficiency

Nursing Considerations:

Monitor for improvement of symptoms (e.g., resolution of thrush).
Instruct parents on proper administration techniques (oral and topical).
Assess for side effects (e.g., gastrointestinal upset).
Evaluate the necessity for concurrent antifungal medications in systemic infections.
Administration: Nystatin is given orally in the form of a suspension. For oral candidiasis, the suspension is swished in the mouth and swallowed.
Side Effects: Generally well-tolerated. Some children may experience mild gastrointestinal disturbances such as nausea, vomiting, or diarrhea. Rarely, allergic reactions like rash may occur.

$\"Griseofulvin\"$

Griseofulvin in Pediatrics

Class: Antifungal (Fungistatic)
Pediatric Dose:

10-20 mg/kg/day (depending on the type and severity of the fungal infection)

Key Points:

Mechanism of Action: Griseofulvin disrupts fungal cell mitosis by binding to microtubules, inhibiting fungal cell division.
Indications in Pediatrics: Primarily used for dermatophytosis (fungal infections of the skin, hair, and nails), such as tinea capitis (scalp ringworm) and tinea corporis (body ringworm).

Indications:

Treatment of tinea capitis (scalp ringworm)
Treatment of tinea corporis (ringworm of the body)
Treatment of tinea cruris (jock itch)
Treatment of tinea pedis (athlete\’s foot)
Onychomycosis (fungal infection of the nails)
Prophylaxis against dermatophyte infections in specific cases
Infection of the hair and nails caused by fungi

Contraindications:

Hypersensitivity to griseofulvin or any component of the formulation
Liver dysfunction or active hepatic disease
Pregnancy (known teratogenic effects)
Porphyria
Caution in patients with penicillin allergy (cross-reactivity)

Nursing Considerations:

Monitor for liver function tests periodically during therapy.
Assess for gastrointestinal side effects (nausea, vomiting).
Ensure patients comply with a full course of treatment to prevent recurrence.
Educate parents on the importance of using the medication consistently and checking for signs of fungal infection.
Administration: Administered orally. Absorption is enhanced when taken with fatty foods (e.g., milk or ice cream), which helps improve its efficacy.
Side Effects: Common side effects include gastrointestinal upset, headache, dizziness, fatigue, and skin rashes. Prolonged use may cause photosensitivity (increased sensitivity to sunlight).

Clotrimazole in Pediatrics

Class: Antifungal (Imidazole)
Pediatric Dose: 1% cream or lotion (applied topically)

Key Points:

Mechanism of Action: Clotrimazole interferes with fungal cell membrane integrity by inhibiting ergosterol synthesis, leading to fungal cell death.
Indications in Pediatrics: Topical clotrimazole is commonly used to treat fungal skin infections such as tinea pedis (athlete\’s foot), tinea corporis, and cutaneous candidiasis.

Indications:

Topical treatment of dermatophyte infections (e.g., ringworm)
Treatment of candidiasis (fungal infections) of the skin
Management of tinea pedis (athlete\’s foot)
Treatment of tinea cruris (jock itch)
Treatment of vulvovaginal candidiasis (in females)
Oral candidiasis (thrush) (topical formulations)
Prevention of fungal infections in at-risk pediatric populations

Contraindications:

Hypersensitivity to clotrimazole or any of its components
Open wounds or extensive areas of burns (topical use)
Known hepatic impairment (with caution)
Use in pregnancy (especially during the first trimester) should be monitored
Caution in pediatric patients under two years old

Nursing Considerations:

Monitor the skin for improvement of fungal infections.
Educate patients and parents on the proper application technique.
Instruct about maintaining skin hygiene to prevent recurrence of infection.
Assess for any signs of hypersensitivity reaction (rash, itching) after application.
Side Effects: Mild skin irritation, burning, and redness are the most common adverse effects

$\"\"$

OPIOID ANALGESICS

Opioid analgesics are drugs derived from opium or synthetic analogs, primarily prepared from the poppy plant (Papaver somniferum). They are the most effective pain relievers available and are commonly used as first-line therapy for the management of:

Acute severe pain
Moderate to severe chronic pain associated with cancer, AIDS, or other life-threatening conditions

Classification:

Weak opioid analgesics: e.g., codeine.
Strong opioid analgesics: e.g., morphine, pethidine, and methadone.

Mechanism of Action:
Opioids relieve pain by mimicking the effects of endogenous opioid peptides (like endorphins), primarily by binding to the mu-opioid receptors. These receptors are found in both the ascending and descending pain pathways in the brain and spinal cord. By binding to these receptors, opioids alter pain perception and can produce euphoria and relaxation, which help alleviate the stress and emotional distress that often accompanies severe pain.

Codeine

Available Preparations:

Tablets: 30 mg

Indications:

Mild to moderate pain
Cough suppression
Diarrhea

Contraindications:

Respiratory depression
Obstructive airway disease
Hypersensitivity to codeine
Acute alcoholism
Risk of paralytic ileus
Raised intracranial pressure or head injury

Dosage:

Relief of pain:

Adults: 30 mg–60 mg every 4–6 hours, maximum dose of 240 mg/day.
Children (1–12 years): 0.5 mg–1 mg/kg every 4–6 hours.

Diarrhea:

Adults: 30 mg 4–6 times daily.

Pharmacokinetics:

Well absorbed after oral administration.
Widely distributed in the body, crosses the placenta, and enters breast milk.
Metabolized in the liver and excreted primarily in urine.

Side Effects:

Constipation
Dry mouth
Facial flushing
Nausea and vomiting
Difficulty urinating
Headache and dizziness
Sweating

Drug Interactions:

Alcohol and other CNS depressants increase the sedative effects of codeine.
Rifampicin and phenytoin may increase the accumulation of codeine.
Severe cardiovascular depression may occur when used with general anesthetics.

Nursing Considerations:

Encourage increased fluid and fiber intake to prevent constipation.
Avoid alcohol during codeine therapy.
Avoid abrupt discontinuation after prolonged use to prevent withdrawal symptoms.
Codeine is not recommended for productive cough.
Administer with food to minimize nausea and GI upset.

Morphine

Type:
Strong, centrally acting opioid analgesic.

Available Preparations:

Oral solution: 5 mg/5 ml, 10 mg/5 ml, 50 mg/5 ml
Injection: 10 mg/ml, 15 mg/ml

Indications:

Severe pain (e.g., post-operative, cancer pain)
Myocardial infarction
Premedication before surgery
Sickle cell crisis
Acute pulmonary edema
Chronic pain

Contraindications:

Acute respiratory depression
Hypersensitivity to morphine
Acute alcoholism
Head injury
Acute abdominal pain
Raised intracranial pressure
Avoid injections in patients with pheochromocytoma

Pharmacokinetics:

Absorbed variably from the gastrointestinal tract (GIT).
Widely distributed throughout the body.
Metabolized mainly in the liver.
Excreted in urine and bile.

Mechanism of Action:
Morphine binds to opioid receptors in the central nervous system (CNS), altering both the perception of and emotional response to pain. It has both depressing and stimulating effects on the CNS:

Depressing effects:

Reduces the brain\’s appreciation of pain.
Depresses respiration.
Depresses the cough reflex.
Acts as a mild hypnotic, inducing sleep or drowsiness.
Causes euphoria and reduces anxiety.

Stimulating effects:

Stimulates the chemoreceptor trigger zone, causing nausea and vomiting in some patients.
Causes pupil constriction due to effects on the third cranial nerve.
Decreases bowel peristalsis, leading to constipation.

Dosage:

Acute pain (post-operative pain):

Oral: 5–20 mg every 4 hours.
Subcutaneous (SC) or intramuscular (IM):

Adults: 10 mg every 4 hours if necessary.
Children (6–12 years): 5–10 mg every 4 hours.
Children (1–5 years): 2.5–5 mg every 4 hours.
Neonates: 150 mcg/kg 4 times a day.

Chronic pain:

Adults: 10–15 mg every 4 hours.
Children (1–12 years): 200–400 mcg/kg every 4 hours.

Side Effects:

Nausea and vomiting
Constipation
Respiratory depression
Postural hypotension
Urinary retention
Euphoria or hallucinations
Sweating
Bradycardia
Decreased libido
Dependency

Drug Interactions:

Increases sedative effects when combined with antidepressants, antipsychotics, or sedating antihistamines.
May lead to severe cardiovascular depression when used with drugs metabolized by the liver (e.g., phenytoin, rifampicin).

Nursing Considerations:

Avoid alcohol during morphine therapy.
Prolonged use may lead to dependence, and abrupt discontinuation should be avoided.
Caution patients about the potential for low blood pressure and blurred vision.
Naloxone can be used to treat morphine overdose.
Watch for urinary retention, especially in patients with prostatic hypertrophy.

Pethidine

Type:
Synthetic opioid, less potent than morphine but equally effective in pain management.

Available Preparations:

Injection: 50 mg/ml, 100 mg/ml

Routes of Administration:
Intramuscular (IM), intravenous (IV), subcutaneous (SC), or oral.

Indications:

Pre-operative medication
Acute analgesia (e.g., post-operative, obstetric)
Moderate to severe acute pain

Contraindications:

Hypersensitivity to pethidine
Acute respiratory depression
Severe renal or liver disease
Head injury and raised intracranial pressure

Pharmacokinetics:

Well absorbed orally, with a bioavailability of 50%.
Onset of action: 10–15 minutes after oral administration.
Short duration of action: 2–3 hours.
Metabolized in the liver; excreted in urine.

Dosage:

Acute pain:

Adults: 50–150 mg, repeated after 4 hours if necessary.
Children: 0.5–2 mg/kg every 4 hours.

Obstetric analgesia:

50–100 mg, repeated every 1–3 hours, with a maximum dose of 400 mg/day.

Side Effects:

Nausea and vomiting
Constipation
Respiratory depression
Postural hypotension
Urinary retention
Sweating, palpitations
Dependency, hallucinations
Bradycardia

Drug Interactions:

Phenothiazines may cause severe hypotensive episodes and prolonged respiratory depression.
Alcohol and other CNS depressants potentiate respiratory depression.
Cimetidine may decrease pethidine elimination, increasing the risk of toxic effects.

Nursing Considerations:

Prolonged use may lead to physical dependence.
Use the lowest effective dose, especially in labor.
Avoid alcohol during therapy.

Opioid/Narcotic Antagonist:

Naloxone

Type:
A drug that reverses the effects of opioid analgesics.

Indications:

Opioid overdose (e.g., morphine overdose)
Neonatal asphyxia due to opioid use during labor
Diagnosis of opioid dependence (it worsens withdrawal symptoms)
Opioid-induced respiratory depression

Dosage:
0.4 mg intravenously (IV).

Mechanism of Action:
Naloxone competitively blocks the actions of opioid peptides at opioid receptors, reversing their effects.

Pharmacokinetics:

Well absorbed via IV, with an onset of action in 2–3 minutes.
Undergoes first-pass metabolism when given orally.
Metabolized in the liver, excreted in urine.
Duration of action: 3–4 hours.

Side Effects:
Rare at normal doses, but adverse effects may include:

Hypertension
Tachycardia
Hyperventilation
Nausea and vomiting

Nursing Considerations:

Monitor the patient\’s response and adjust the dose as needed.

DRUGS USED IN PAEDIATRICS Read More »

DRUGS USED IN MIDWIFERY

Drugs used in midwifery are drugs specifically used during pregnancy, labor, delivery, and postpartum care to ensure the health of the mother and baby.

They may induce labor, prevent complications, manage pain, or treat postpartum conditions.

Examples;

Oxytocics: e.g., Oxytocin (induces or augments labor), Misoprostol (induces labor or manages postpartum hemorrhage).
Tocolytics: e.g., Nifedipine, Terbutaline (delay preterm labor).
Anticoagulants: e.g., Heparin (prevents thromboembolism during pregnancy).
Antiemetics: e.g., Doxylamine + Pyridoxine (treat nausea and vomiting in pregnancy).
Analgesics/Anesthetics: e.g., Epidural anesthesia (manages labor pain).
Magnesium Sulfate: Prevents seizures in preeclampsia/eclampsia.
Rh Immunoglobulin: Prevents Rh incompatibility complications.

Clinical Use;

Inducing or augmenting labor.
Managing preterm labor.
Preventing or treating postpartum hemorrhage.
Managing pregnancy-related conditions like preeclampsia, nausea, or pain.

DRUGS USED IN LABOUR

Drugs in Labor refers to the medications that are administered to a woman during labor to manage pain, assist with the process of childbirth, or address complications. These drugs can be used for pain relief, induction or augmentation of labor, and management of medical conditions that may arise during labor.

Drugs used in labor can be grouped according to the effect they have on the uterus.

Uterine relaxants (Tocolytics): These drugs relax the uterus, slowing or stopping contractions such as Nifedipine, Magnesium Sulfate.
Uterine Stimulants/Uterine Motility drugs. (Oxytocics): These drugs stimulate the uterus to contract, helping to induce or strengthen labor, such as Oxytocin (Pitocin).

$\"Uterine-Relaxants\"$

Uterine Relaxants

Uterine relaxants, also known as tocolytics, are a group of medications used to suppress uterine contractions and delay labor.

Their primary goal is to prolong pregnancy, allowing the fetus to develop further and increasing the chances of neonatal survival. These drugs are primarily used to prevent premature labor, particularly when cervical dilation is less than 4 cm.

Types of Uterine Relaxants

Beta-adrenergic agonists (Beta-2 agonists):

Salbutamol.
Terbutaline.

Calcium channel blockers:

Nifedipine.

Magnesium sulfate

Nonsteroidal anti-inflammatory drugs (NSAIDs):

Indomethacin.

Oxytocin receptor antagonists:

Atosiban.

Corticosteroids:

Dexamethasone: (used for fetal lung maturity rather than directly for uterine relaxation but is often used in combination with tocolytics in premature labor)

$\"Salbutamol\"$

Salbutamol (A Beta-2 Adrenergic Agonist)

Legal Class: Class B controlled drugs
Medical Class: Tocolytic agent
Form: Tablets, sterile solution for injection
Dosage: Tablets 4 mg; Solution for injection 50 mg/mL

Mechanism of Action

Salbutamol stimulates beta-2 adrenergic receptors in the uterine smooth muscle, leading to increased levels of cAMP, which inhibits myosin light-chain kinase, thereby reducing uterine contractions.

Indications

Uncomplicated premature labor between 24 to 33 weeks of gestation
Asthma (as it also has bronchodilatory effects)

Contraindications

Cardiac diseases (risk of tachycardia and other arrhythmias)
Antepartum hemorrhage (APH)
Intrauterine fetal death (IUFD)
Intrauterine infections
Ruptured membranes
Eclampsia and pre-eclampsia
First and second trimester of pregnancy (risk of fetal malformations)

Dosage

Premature labor: IV infusion 10 mcg/min, gradually increase according to response at 10-minute intervals until contractions diminish, with a maximum dose of 45 mcg/min. Maintain rate for 1 hour, then gradually reduce by IV or IM injection 100-250 mg, repeated according to response, followed by oral administration of 4 mg every 6-8 hours.
Duration of use: Do not use for more than 48 hours due to the risk of maternal and fetal complications.

Side Effects

Hypoglycemia (especially in diabetic patients)
Vomiting and nausea
Sweating and tremors
Hypotension
Pulmonary edema
Maternal and fetal tachycardia
Headache and palpitations
Urticaria

Adverse Effects

Severe hypotension
Pulmonary edema
Cardiac arrhythmias
Hyperglycemia

$\"Magnesium$

Magnesium Sulfate (MgSO4)

Legal Class: Class B controlled drugs
Medical Class: Tocolytic and anticonvulsant
Form: Sterile solution for injection
Strength/Dosage: 50% of 5 grams/10 mL

Mechanism of Action

Magnesium sulfate acts as a calcium antagonist by competing with calcium for entry into the cells, which decreases the action potential in uterine smooth muscle, leading to muscle relaxation. It also stabilizes membranes by interacting with sodium and potassium channels.

USING MAGNESIUM SULPHATE (MgSO₄) TO PREVENT OR STOP SEIZURES

LOADING DOSE:

1. Give 4 g of 20% MgSO₄ solution IV over 20 min. prepared as stated below:

Take one 20 ml syringe and draw 8 ml of 50% MgSO₄ (4 g)
Add 12 ml water for injection to make 20% solution
Give IV over 20 minutes (each 2mls has 1g

2. Immediately follow this with 10 g of 50% solution deep IM as shown below:

Take two 10 ml syringes
Draw 10 ml of 50% MgSO₄ (undiluted) = 5 g into each syringe
Add 1 ml of 2% lignocaine to each syringe to reduce pain
Give 10 ml (5 g) deep IM in each buttock
Prepare to refer to a comprehensive EmOC(Emergency Obstetric Care) facility if delivery is imminent
If delivery is not imminent and mother cannot reach referral unit within 4 hours give Maintenance dose (see 3 below)

3. If fits re-occur:

Give another 4 ml = 2 g of MgSO₄, 20% IV slowly over 20 minutes

MAINTENANCE DOSE:

Give 5 g of 50% MgSO₄ deep IM in alternate buttocks every 4 hours as shown below:

Take one 10 ml syringe and draw 10 ml of 50% MgSO₄ (5 g) in each syringe
Add 1 ml of 2% lignocaine in the same syringe
Give 5 g deep IM in alternate buttocks every 4 hours
Continue treatment for 24 hours after birth or the last fit, whichever is later

TOXICITY:

Before repeating MgSO₄, always monitor for toxicity.
Withhold or delay next IM dose if any of the following occurs:
Respiratory rate <16/minute. STOP MgSO₄, and give calcium gluconate
Patellar reflexes absent. STOP MgSO₄
Urine output <30 ml/hour over preceding 4 hours

ANTIDOTE: Calcium Gluconate

Assist ventilation with mask and ambu-bag, anaesthesia apparatus, intubation
Give calcium gluconate 1 g (10 ml of 10% solution) IV slowly (over 10 minutes) until it begins to counteract the effect of MgSO₄ and respiration returns to normal
Give oxygen

Dosage

Loading Dose: 4 g of MgSO4 given slowly IV over 15 to 20 minutes, followed by 10 g IM (5 g in each buttock) with 1 mL of 2% lignocaine to reduce pain.
Maintenance Dose: 5 g of 50% MgSO4 IM on alternate buttocks every 4 hours. Treatment continues for 24 hours from the start or after the last seizure.

Indications

Severe eclampsia and pre-eclampsia (prevention and treatment of seizures)
Hypomagnesemia
Severe asthma
Short-term treatment of constipation (acts as a laxative)
Myocardial infarction (as an adjunct)

Contraindications

Hypermagnesemia
Hypersensitivity to MgSO4
Renal impairment
Hepatic failure
Hypotensive patients
Patients with epilepsy

Side Effects

Drop in blood pressure
Flushing of the skin
Dizziness and confusion
Muscle weakness and loss of deep tendon reflexes (e.g., knee-jerk reflex)
Prolonged bleeding time
Diarrhea

Adverse Effects

Hypermagnesemia (risk of respiratory depression, cardiac arrest, and coma)
Magnesium toxicity, leading to respiratory paralysis
Shock in hypertensive patients

$\"\"$

Nifedipine (A Calcium Channel Blocker)

Legal Class: Class B controlled drugs
Medical Class: Tocolytic and antihypertensive
Form: Tablets

Mechanism of Action

Nifedipine inhibits calcium influx through voltage-dependent calcium channels in the smooth muscle, including the uterus, which leads to relaxation and reduced contractility.

Dosage

Initial Dose: 20 mg, repeat after 30 minutes if contractions persist.
Maintenance Dose: If contractions continue after 3 hours, give 20 mg every 3-8 hours until contractions cease. The maximum dose is 160 mg/day.

Indications

Threatened abortion
Preterm labor less than 34 weeks of gestation
Hypertension (both chronic and pregnancy-induced)

Contraindications

Maternal cardiac diseases
Uncontrolled hypertension
Intrauterine infections
Conditions where prolonging pregnancy is contraindicated
Intrauterine fetal death

Side Effects

Dizziness and headache
Flushing and warmth sensation
Peripheral edema
Fatigue
Nausea

Adverse Effects

Severe hypotension
Reflex tachycardia
Congestive heart failure (CHF) exacerbation

Uterine Stimulants/Uterine Motility Drugs (Oxytocics)

Uterine motility drugs, also known as oxytocics, are agents used to stimulate uterine contractions.

These medications are primarily used to induce or augment labor, manage postpartum hemorrhage, and facilitate uterine evacuation in cases of incomplete abortion or fetal death. They are also employed as abortifacients to induce abortion.

Oxytocics

Oxytocics are drugs that stimulate uterine contractions, mimicking the action of the natural hormone oxytocin. They are used to induce or augment labor, control postpartum bleeding, and in some cases, manage incomplete or missed abortions.

Types of Oxytocics

$\"\"$

Oxytocin (Pitocin, Syntocinon)

Legal Class: Class B controlled drugs
Medical Class: Oxytocic drugs
Form: Sterile solution for injection
Strength: 10 IU per ampule

Indications of Oxytocin:

Induction of Labor: When labor is not progressing naturally.
Augmentation of Labor: To strengthen contractions when labor is slow or stalled.
Control of Postpartum Bleeding (PPH): To contract the uterus after delivery and prevent excessive bleeding.
Active Management of the Third Stage of Labor: To help deliver the placenta and reduce the risk of PPH.

Others include;

Management of hypotonic uterine contractions
Treatment of intrauterine fetal death
Prevention and treatment of postpartum hemorrhage (PPH)
Active management of the third stage of labor
Management of preeclampsia and eclampsia
Treatment of congestive heart failure secondary to fluid overload in pregnancy
Management of post-term pregnancies
Incomplete or missed abortion

Contraindications of Oxytocin.

Hypertonic Uterine Contractions: When the uterus is already contracting too strongly.
Fetal and Maternal Distress: When the baby or mother is experiencing complications.
Multiple Pregnancy: Increased risk of complications.
Trial of Labor: When a woman is attempting a vaginal delivery after a previous Cesarean section.
Malpresentation: When the baby is in a position that makes vaginal delivery difficult (e.g., breech, brow).
Cephalo Pelvic Disproportion: When the baby\’s head is too large to fit through the mother\’s pelvis.
Low Blood Pressure: Oxytocin can further lower blood pressure.

Dosage of Oxytocin

Induction/Augmentation of Labor: 5 IU in 500 mL of IV infusion, initially at 5 drops per minute, titrated as needed.
Prevention of PPH: 5 IU slow IV injection after delivery of the placenta, with an increase in rate if necessary during the third stage of labor.
PPH: 10 unit IM after delivery of placenta

Routes of Administration:

Intramuscular (IM)
Intravenous (IV), often in combination with normal saline or dextrose

Side Effects of Oxytocin

Dizziness
Nausea and vomiting
Skin rashes
Fetal bradycardia
Hypotension

Adverse Effects:

Uterine rupture, particularly in cases of hyperstimulation
Severe hypotension
Tachycardia
Fetal anoxia and hypoxia leading to birth asphyxia

Pharmacokinetics:

Absorption: Rapid following IV injection
Distribution: Distributed throughout the extracellular fluid, with some crossing into fetal circulation
Metabolism: Primarily in the liver and kidneys, with rapid metabolism and excretion in the urine

$\"Syntometrine\"$

Syntometrine

Syntometrine is a combination drug containing both ergometrine and oxytocin, designed to provide a synergistic effect in controlling postpartum bleeding.

Legal Class: Class B controlled drug
Medical Class: Oxytocic drug
Form: Sterile solution for injection
Strength: Combination of ergometrine 0.5 mg + oxytocin 5 IU (International Units)
Dosage: 1 mL as a single dose, but can be repeated if necessary if bleeding is not controlled.

Route:

Intramuscular: Injection into a muscle.
Intravenous: Injection into a vein.

Indications:

Multigravidas: Women who have had multiple pregnancies, as they are at higher risk for PPH.
History of Postpartum Hemorrhage: Women with a previous history of PPH.
Multiple or Twin Delivery: Due to the larger placental site.
Heavy Lochia: Excessive vaginal discharge after delivery.
Abortion: When the fundal height (measurement of the uterus) is less than 12 weeks.

Contraindications:

Cardiac Disease: Syntometrine can worsen heart conditions.
Preeclampsia and Eclampsia: Syntometrine can exacerbate these conditions.
Hypertension: Syntometrine can raise blood pressure.

Adverse Effects:

Retained Placenta: The placenta may not be fully expelled.
IUFD (Intrauterine Fetal Death) in Undiagnosed Second Twin: If a second twin is present and undiagnosed, Syntometrine can lead to its death.
Retained Second Twin: The second twin may not be fully expelled.
Uterine Rupture: If given during abortion after 20 weeks of gestation, especially if the products of conception are not fully expelled.
Hypoxia and Anoxia: Lack of oxygen to the fetus or mother.

Side Effects:

Nausea and Vomiting
Headache
Hypotension: Low blood pressure.
Dyspnea: Difficulty breathing.
Muscle Pain

$\"Methyl-Ergometrine\"$

Ergometrine

Ergometrine is a potent oxytocic that acts directly on the uterine muscle to cause sustained contractions.

Legal Class: Class B controlled drug

Medical Class: Oxytocic drug

Form: Tablet and sterile solution

Strength/Dosage:

Tablets: 0.25 to 0.5 mg
Injection: 200 mcg/mL or 0.5 mg/mL

Effects: Causes sudden, prolonged, intermittent uterine contractions.

Indications: Similar to Syntometrine, primarily used to control postpartum bleeding.

Contraindications: Similar to Syntometrine.

Side Effects: Similar to Syntometrine.

Dangers: Similar to Syntometrine.

$\"indomethacin\"$

Indomethacin (An NSAID)

Legal Class: Prescription-only medication
Medical Class: NSAID, tocolytic
Form: Tablets, rectal suppositories, oral suspension

Mechanism of Action

Indomethacin inhibits the cyclooxygenase (COX) enzymes, leading to reduced synthesis of prostaglandins, which are crucial for uterine contractions.

Dosage

Preterm labor: 50-100 mg rectally or orally, followed by 25-50 mg every 6-8 hours. The treatment duration is limited to 48 hours to minimize fetal side effects.

Indications

Preterm labor (especially when caused by polyhydramnios)
Patent ductus arteriosus (PDA) closure in neonates

Contraindications

Fetal distress
Intrauterine fetal death
Peptic ulcer disease
Renal impairment
Bleeding disorders

Side Effects

Gastrointestinal discomfort (nausea, vomiting, epigastric pain)
Dizziness and headache
Rash

Adverse Effects

Oligohydramnios (reduced amniotic fluid)
Premature closure of the ductus arteriosus in the fetus
Renal impairment in both mother and fetus

Abortifacients

Abortifacients are drugs that induce abortion by causing strong uterine contractions, leading to the expulsion of uterine contents. They are often used in the first and second trimesters of pregnancy for medical termination, and are often used in conjunction with other medications.

Types of Abortifacients

$\"Misoprostol\"$

Misoprostol

Legal Class: Class B controlled drugs
Medical Class: Oxytocic drugs/Cervical ripening agent
Form: Tablets
Strength: 100 mcg or 200 mcg per tablet

Indications of Misoprostol:

Induction of Labor: When labor is not progressing naturally.
Control of Postpartum Hemorrhage: Due to uterine atony.
Cervical Ripening: To soften the cervix before labor induction.
Intrauterine Fetal Death: To induce labor and expel the fetus.
Gastric and Duodenal Ulcerations: Off-label use for treating ulcers.
Medical termination of pregnancy in combination with mifepristone

Contraindications of Misoprostol:

Malpresentation: When the baby is in a position that makes vaginal delivery difficult.
Placenta Previa Grade 3 and 4: When the placenta is covering the cervix.
Multiparous Mothers: Increased risk of complications.
Cephalo Pelvic Disproportion: When the baby\’s head is too large to fit through the mother\’s pelvis.
Hypersensitivity to Misoprostol: Allergic reaction.

Dosage of Misoprostol:

Induction of Labor: 25-50 mcg vaginally every 4-6 hours until adequate uterine contractions are achieved
NSAID-Induced Ulceration: 200 mcg orally four times daily

Routes of Administration:

Sublingual: Under the tongue.
Rectal: Inserted into the rectum.
Vaginal: Inserted into the vagina.
Oral: Swallowed

Side Effects:

Headache
Dizziness
Fever and shivering
Nausea and vomiting
Uterine rupture (rare but serious)

Adverse Effects:

Fetal distress and bradycardia
Uterine hyperstimulation leading to rupture
Severe gastrointestinal disturbances

Pharmacokinetics:

Absorption: Rapidly absorbed after oral, sublingual, or vaginal administration
Distribution: Well distributed throughout the body, crossing into fetal circulation
Metabolism: Hepatically metabolized to active prostaglandin analogs
Excretion: Primarily excreted in urine.

$\"\"$

Dysmenorrhea: Drug Treatment

Dysmenorrhoea refers to pain during menstruation, caused by excessive prostaglandin production, leading to strong uterine contractions.

Dysmenorrhea, or painful menstruation, is categorized into primary and secondary types, based on the presence or absence of an identifiable underlying cause.

I. Primary Dysmenorrhea:

Cause: Unknown; believed to be related to excessive prostaglandin production leading to intense uterine contractions.
Risk Factors: Early menarche, heavy menstrual bleeding, family history of dysmenorrhea, smoking.
Signs and Symptoms: Cramping abdominal pain, headache, nausea/vomiting, diarrhea, lower back pain, loss of appetite.
Non-Pharmacological Management: Regular exercise, hot water bottles/warm baths, adequate rest and sleep, back massage, low-fat diet, nutritional supplements (Vitamin E, zinc, Vitamin B1). Educate the patient that the condition isn\’t a gynecological abnormality.
Pharmacological Management:

Non-Steroidal Anti-inflammatory Drugs (NSAIDs): Reduce prostaglandin production. Start 1-2 days before anticipated menstruation for optimal effectiveness.

Mefenamic acid: 500mg three times daily for 3-4 days.
Ibuprofen: 400mg three times daily for 3-4 days.
Indomethacin: 50mg three times daily for 3-4 days.
Diclofenac: 50mg three times daily for 3-4 days.
Aceclofenac: 100mg twice daily for 3-4 days. (Note: The provided text lists 10mg, but 100mg is a more common and appropriate dosage.)

Hormonal Therapy: Used if NSAIDs are ineffective. These suppress ovulation, reducing prostaglandin production.

Combined Oral Contraceptives (COCs): Examples include Pilplan and Microgynon.
Norethisterone (Primolut-N): A progestogen.

Antispasmodics: Relax uterine smooth muscle, providing relief from spasms. May be used alone or in combination with NSAIDs for severe cases.

Drotaverine (Nospa): 80mg three times daily for 3 days.

II. Secondary Dysmenorrhea:

Cause: Identifiable underlying condition, such as: pelvic inflammatory disease (PID), endometriosis, fibroids, ovarian cysts, intrauterine devices (IUDs).
Signs and Symptoms: Abdominal bloating, backache, pain starting 3-5 days before menstruation, pain during sexual intercourse.
Management: Treatment focuses on addressing the underlying cause. NSAIDs may provide temporary pain relief while the underlying condition is treated.

Others;

$\"Analgesics$

Analgesics and Anesthetics for Labor Pain

Purpose: Provide pain relief during labor and delivery.

Examples:

Epidural Anesthesia:

Mechanism: Local anesthetics (e.g., bupivacaine) injected into the epidural space to block pain signals.
Indications: Pain relief during labor.
Administration: Continuous infusion via epidural catheter.

Nitrous Oxide:

Mechanism: Inhaled analgesic that provides mild pain relief.
Indications: Labor pain.
Administration: Inhalation.

Opioids:

Mechanism: Bind to opioid receptors in the brain to reduce pain perception.
Examples: Fentanyl, Remifentanil.
Indications: Moderate to severe labor pain.
Administration: IV or IM.

$\"Drugs$

Drugs for Postpartum Hemorrhage (PPH)

Purpose: Prevent or treat excessive bleeding after delivery.

Examples:

Oxytocin:

Mechanism: Stimulates uterine contractions to reduce bleeding.
Indications: First-line treatment for PPH.
Administration: IV or IM.
Dosage: 10-40U in 1L normal saline infused at 200-500mL/hr.

Misoprostol:

Mechanism: Induces uterine contractions.
Indications: PPH, especially in resource-limited settings.
Administration: Oral, sublingual, or rectal.
Dosage: 800-1000 mcg PR(Per Rectal) once.

Carboprost:

A medication used after the delivery of a baby to control bleeding from the uterus that has not resolved with other treatments.

Mechanism: Strong uterine contractor.
Indications: PPH unresponsive to oxytocin.
Administration: IM.

Tranexamic Acid:

A medication used to control episodes of heavy bleeding.

Mechanism: Antifibrinolytic that reduces bleeding.
Indications: PPH.
Administration: IV.
Dosage: 1g over 10 minutes

Rh Immunoglobulin :

A medication used to prevent unwanted immune reactions in blood transfusions or pregnancy.

Human Rho(D) immune globulin is a solution of antibodies used to prevent isoimmunization of Rho(D) negative patients exposed to Rho(D) positive blood in pregnancy or transfusion.

Purpose: Prevent Rh sensitization in Rh-negative mothers.
Mechanism: Prevents the mother’s immune system from producing antibodies against Rh-positive fetal blood cells.
Indications: Rh-negative mothers with Rh-positive babies.
Administration: IM, usually at 28 weeks of pregnancy and within 72 hours of delivery.

$\"\"$

Antiemetics for Nausea and Vomiting in Pregnancy

Purpose: Manage nausea and vomiting, including hyperemesis gravidarum.

Examples:

First-Line Pharmacotherapy:

This is the initial treatment approach. Two options are presented:

Pyridoxine (Vitamin B6)

Dosage: 10-25mg orally every 6-8 hours: This is a common first-line treatment for mild NVP.

Doxylamine + Pyridoxine:

This combination therapy is often more effective than pyridoxine alone, particularly for moderate NVP.

Mechanism: Antihistamine and vitamin B6 combination.
Indications: Nausea and vomiting in pregnancy.
Administration: Oral.

If symptoms persist despite first-line treatment and dehydration occurs, proceed to:

Second-Line Pharmacotherapy:

This stage involves intravenous (IV) fluid resuscitation to correct dehydration in addition to one of the following antiemetic medications given intravenously:

Metoclopramide

Dosage: 5-10 mg every 8 hours: This medication stimulates gastric motility and can help with nausea.

Ondansetron:

Mechanism: Serotonin 5-HT3 receptor antagonist.
Indications: Severe nausea and vomiting.
Administration: 8mg every 12 hours, Oral or IV.

Promethazine

Dosage: 12.5-25mg every 4-6 hours: An antihistamine with antiemetic properties.

If vomiting remains uncontrolled (\”refractory vomiting\”) despite second-line therapy, proceed to:

Third-Line Pharmacotherapy:

This is reserved for severe, persistent cases. Again, IV fluid resuscitation is crucial, and one of the following medications is added:

Methylprednisolone

Dosage: 16mg every 8 hours orally or intravenously for 3 days (tapering over 2 weeks, continuing for a total of 6 weeks if effective): A corticosteroid with potent anti-inflammatory and antiemetic effects. The tapering schedule is crucial to minimize side effects.

Chlorpromazine

Dosage: 25-50mg intravenously or intramuscularly every 4-6 hours: A phenothiazine derivative with antiemetic and sedative properties. Use cautiously due to side effects.

Chlorpromazine

Dosage: 10-25mg orally every 4-6 hours: Oral alternative to the IV/IM route.

$\"betamethazone\"$

Corticosteroids for Fetal Lung Maturation

Purpose: Accelerate fetal lung development in preterm labor.

Examples:

Betamethasone:

Mechanism: Stimulates surfactant production in fetal lungs.
Indications: Preterm labor (24–34 weeks gestation).
Administration: Two 12 mg doses given IM 24 hours apart.

Dexamethasone:

Mechanism: Similar to betamethasone.
Indications: Preterm labor.
Administration: Four 6 mg doses given IM every 12 hours.

Iron and Folic Acid Supplements

Purpose: Prevent or treat anemia during pregnancy.
Mechanism: Supports red blood cell production and fetal development.
Indications: Routine supplementation during pregnancy.
Administration: Oral.

$\"Drugs$

Drugs for Hypertension in Pregnancy

Hypertension in pregnancy is a serious condition requiring careful management due to potential risks to both mother and fetus.

Types of Hypertension in Pregnancy:

Chronic Hypertension: This pre-existing condition is diagnosed before pregnancy or before 20 weeks gestation.
Gestational Hypertension: Onset occurs after 20 weeks of gestation and resolves postpartum. It\’s characterized by elevated blood pressure without proteinuria (protein in the urine).
Pre-eclampsia: A more serious condition, diagnosed after 20 weeks gestation. It involves hypertension with proteinuria, often accompanied by other symptoms like edema (swelling), headaches, visual disturbances, and abdominal pain.
Eclampsia: The most severe form, characterized by seizures in a woman with pre-eclampsia. This is a life-threatening emergency requiring immediate medical intervention.

Management Strategies:

Treatment depends heavily on the type and severity of hypertension and the presence of complications. The primary goals are to prevent seizures, reduce blood pressure to a safe level, and deliver the baby at an appropriate time.

Anticonvulsants (Primarily for Eclampsia):

Magnesium Sulfate: This is the first-line treatment for eclampsia to prevent seizures.

Dosage: A loading dose of 4g intravenously (IV) is administered over 10-15 minutes, followed by a maintenance dose of 10g intramuscularly (IM), typically divided into two 5g injections (one in each buttock). Continuous monitoring of magnesium levels is essential to prevent toxicity.
Toxicity Management: Calcium gluconate 1-2g IV is the antidote for magnesium sulfate toxicity. Symptoms of toxicity include decreased deep tendon reflexes, respiratory depression, and cardiac arrhythmias.

Diazepam: Used for immediate seizure control in eclampsia, although it\’s not the primary preventative agent like magnesium sulfate. Diazepam 10mg IV is usually administered.

Antihypertensives:

The choice of antihypertensive medication depends on several factors, including the type of hypertension, severity of blood pressure elevation, and the presence of any co-existing conditions. The goal is to gradually lower blood pressure to avoid sudden drops that could compromise placental perfusion.

Severe Hypertension (Emergency):

Hydralazine 5-10mg IV: A vasodilator that acts quickly to lower blood pressure. Careful monitoring is essential due to its potential side effects.
Nifedipine 20mg sublingual: A calcium channel blocker with rapid-onset action. It\’s typically given sublingually for fast-acting effects in hypertensive emergencies.

Chronic Hypertension (Non-Emergency):

Methyldopa 250mg twice daily to three times daily: A centrally acting alpha-2 agonist that is generally considered safe in pregnancy. The dosage is adjusted based on blood pressure response.
Nifedipine retard 20mg twice daily: A long-acting calcium channel blocker that offers sustained blood pressure control. Again, dose adjustments are necessary based on clinical monitoring.

ANTIMALARIAL DRUGS

Malaria is an acute febrile illness caused by protozoa of the genus Plasmodium. It is transmitted from person to person through the bite of a female Anopheles mosquito.

The Four Species of Malaria Parasites:

Plasmodium falciparum
Plasmodium vivax
Plasmodium ovale
Plasmodium malariae

Life Cycle of Malaria Parasites

Malaria parasites undergo both a sexual cycle (in the female Anopheles mosquito) and an asexual cycle (in humans).

Mosquito Bite: The mosquito injects sexual forms of the parasite (sporozoites) into the bloodstream.
Hepatic Cycle: Sporozoites enter liver cells, forming tissue schizonts, which rupture and release merozoites. Some sporozoites become dormant forms (hypnozoites), which may reactivate later.
Erythrocytic Cycle: Merozoites invade red blood cells (RBCs), forming blood schizonts. The schizonts rupture the RBCs, causing the clinical symptoms of malaria.
Gametocyte Formation: Some merozoites develop into male and female gametocytes. If taken up by a mosquito, they complete the life cycle, forming sporozoites.

Classification of Antimalarial Drugs

Classification I

Tissue Schizonticides: Act on malaria parasites in the liver (Primaquine, Pyrimethamine, Proguanil).
Blood Schizonticides: Act on schizonts in RBCs (Chloroquine, Amodiaquine, Proguanil, Pyrimethamine, Mefloquine, Quinine, Artemisinin).
Gametocides: Prevent transmission by destroying gametocytes (Primaquine).

Classification II

4-Aminoquinolines: Chloroquine, Amodiaquine
8-Aminoquinolines: Primaquine
4-Methanolquinolines (Quinoline Methanols): Quinine, Mefloquine
Biguanides: Proguanil
Sulphonamides: Sulfadoxine
Artemisinin Derivatives: Artemether, Artesunate, Dihydroartemisinin, Artemisinin
Antibiotics: Doxycycline, Tetracycline, Clindamycin

QUININE

Type: Alkaloid derived from the bark of the cinchona tree.
Classification: 4-Methanolquinoline
Action: Rapid blood schizonticide active against Plasmodium falciparum, vivax, ovale, malariae.
Mechanism: Inhibits haem polymerase, preventing the polymerization of haem to haemozoin.

Available Preparations:

Tablets 300 mg
Injection 300 mg/ml
Syrup 100 mg/5 ml

Pharmacokinetics:

Absorbed from the gastrointestinal tract, widely distributed, metabolized in the liver, excreted mainly in urine.

Indications:

Uncomplicated and severe malaria.

Dosage:

Oral: Adults 600 mg 8-hourly for 7 days.
IV: Adults 600 mg 8-hourly in dextrose 5%, to run for 4 hours.
Children: 10 mg/kg 8-hourly for 7 days (oral), or same dose IV in dextrose.

Contraindications:

Hypersensitivity, cardiac abnormalities (e.g., AV block), myasthenia gravis, haemoglobinuria, visual/auditory problems.

Side Effects:

Headache, blurred vision, abdominal pain, diarrhea, tinnitus, hypersensitivity reactions, nausea, hypoglycemia, \”cinchonism\” (tinnitus, dizziness, visual disturbances).

Drug Interactions:

Increases digoxin and warfarin levels.
Delayed absorption with aluminum antacids.
Cimetidine increases quinine blood levels.

SULFADOXINE WITH PYRIMETHAMINE (FANSIDAR)

Action: Synergistically inhibit folic acid synthesis in parasites.
Available Preparations: Tablets (500 mg sulfadoxine/25 mg pyrimethamine).

Pharmacokinetics:

Well absorbed, widely distributed, metabolized in the liver, and slowly excreted.

Indications:

Malaria prophylaxis and intermittent presumptive treatment (IPT) in pregnancy.

Dosage:

IPT in Pregnancy: 3 tablets during 2nd and 3rd trimesters.

Contraindications:

Hypersensitivity, severe renal failure, infants < 2 months, first trimester pregnancy.

Side Effects:

Urticaria, vomiting, diarrhea, nausea, headache, Stevens-Johnson syndrome.

Drug Interactions:

Increased antifolate effect with methotrexate and cotrimoxazole, raises phenytoin plasma concentration.

ARTEMISININ AND DERIVATIVES

Derived from Artemesia annua (Chinese herb Qinghaosu).
Action: Rapidly acting blood schizonticides effective against multidrug-resistant Plasmodium falciparum.
Derivatives: Artesunate (water-soluble), Artemether (lipid-soluble).

Artemether:

Available Forms: Injection (20 mg/ml, 40 mg/ml, 80 mg/ml).
Indications: Uncomplicated and severe malaria.
Dose: Adults 300 mg loading dose, followed by 100 mg once daily for 4 days.

Side Effects:

Nausea, vomiting, diarrhea, dizziness, tinnitus.

Contraindications:

Hypersensitivity, first trimester of pregnancy.

ARTEMETHER + LUMEFANTRINE

Available Forms: Tablets (20 mg/120 mg, 40 mg/240 mg), suspension (15 mg/90 mg/5 ml).
Indications: First-line treatment for uncomplicated malaria.

Dosage:

Weight	Age	Day 1	Day 2	Day 3
5-14 kg	4 months-3 yrs	1 tablet 12-hourly	1 tablet 12-hourly	1 tablet 12-hourly
15-24 kg	3-7 yrs	2 tablets 12-hourly	2 tablets 12-hourly	2 tablets 12-hourly
25-34 kg	7-12 yrs	3 tablets 12-hourly	3 tablets 12-hourly	3 tablets 12-hourly
≥35 kg	12+ yrs	4 tablets 12-hourly	4 tablets 12-hourly	4 tablets 12-hourly

Contraindications:

Cardiac arrhythmias, bradycardia, breastfeeding.

Side Effects:

Abdominal pain, diarrhea, nausea, headache, fatigue, skin rash.

Drug Interactions:

Avoid concurrent use with amiodarone, ciprofloxacin, fluconazole, mefloquine.

ARTESUNATE

Type: Derivative of artemisinin, water-soluble.

Classification: Blood schizonticide and gametocide, particularly effective against Plasmodium falciparum, including multidrug-resistant strains.

Mechanism of Action: Artesunate is a prodrug that is rapidly converted to dihydroartemisinin, its active form. It works by producing free radicals within the parasite\’s food vacuole, leading to the destruction of the parasite.

Available Preparations:

Tablets: 50 mg, 100 mg
Injection: 60 mg vial (for intravenous and intramuscular use)

Pharmacokinetics:

Rapidly absorbed
Widely distributed in body tissues
Metabolized in the liver to dihydroartemisinin
Excreted mainly in urine

Indications:

Severe and complicated malaria
Uncomplicated malaria (especially when caused by Plasmodium falciparum resistant to other drugs)

Dosage:

Severe malaria: Initial IV dose of 2.4 mg/kg at 0, 12, and 24 hours, then once daily.
Uncomplicated malaria: 4 mg/kg once daily for 3 days (used in combination therapy).

Contraindications:

Known hypersensitivity to artemisinin derivatives.
First trimester of pregnancy (unless the benefits outweigh the risks).

Side Effects:

Nausea
Vomiting
Dizziness
Diarrhea
Low neutrophil count (rare)
Injection site reactions (for IV/IM administration)

Drug Interactions:

Caution with drugs affecting the heart\’s electrical activity (e.g., antiarrhythmics like amiodarone).
Avoid concurrent use with drugs that prolong QT interval (e.g., quinidine, erythromycin).

DRUGS USED IN MIDWIFERY Read More »

Legal aspects and national policies

The National Drug Authority (NDA)

The National Drug Authority (NDA) is a regulatory body comprised of individuals of high integrity, tasked with overseeing the implementation of the national drug policy.

Its core objective is to ensure the availability, quality, and safe use of pharmaceuticals across the country.

The NDA plays a big role in maintaining public health by regulating drugs, pharmacies, and ensuring that essential medications are accessible to all who need them.

Functions of the National Drug Authority

The NDA\’s mandate covers various areas critical to pharmaceutical regulation and public health:

Development and Regulation of Pharmacies and Drugs: The NDA formulates policies for establishing and managing pharmacies. It also ensures that the drugs sold within the country meet regulatory standards and are safe for use.
Approving the National List of Essential Drugs: The NDA is responsible for approving the list of essential drugs that are deemed necessary for the healthcare system. They also periodically revise this list in consultation with the Minister of Health.
Estimating Drug Needs: The NDA estimates the country\’s pharmaceutical requirements to ensure that drugs are available in sufficient quantities and economically accessible to the population.
Control of Importation, Exportation, and Sale of Pharmaceuticals: The authority regulates the flow of drugs in and out of the country, ensuring that only safe and approved pharmaceuticals enter the market.
Quality Control of Drugs: It ensures that the drugs circulating in the market are of assured quality through stringent control measures such as inspections and laboratory testing.
Promotion of Local Drug Production: The NDA promotes local manufacturing of essential drugs to boost self-sufficiency and reduce reliance on imported medicines.
Encouragement of Herbal Medicine Research: It supports research and development of herbal medicines, integrating traditional medicine into the mainstream healthcare system.
Promotion of Rational Drug Use: The NDA promotes the rational use of medicines by training healthcare professionals and providing information that ensures the appropriate prescription, dispensing, and use of drugs.
Establishment of Professional Guidelines: The NDA creates and updates guidelines for healthcare professionals, ensuring they have the necessary information to prescribe and use drugs appropriately.
Advisory Role: It advises the Minister of Health and other related bodies on implementing the national drug policy.
Other Functions as Provided by Law: The NDA may take on additional roles as required by the country\’s legal framework.

The National List of Essential Drugs

The National List of Essential Drugs contains medicines that are vital to addressing the healthcare needs of the majority of the population.

This list is reviewed periodically to ensure that it remains relevant and effective in meeting public health needs.

The National Formulary is a document that contains the National List of Essential Drugs and other approved medicines. It serves as a guideline for healthcare professionals in prescribing medications.

Essential Drugs

Essential drugs are those that meet the health care needs of the majority of the population.

These drugs are selected based on disease prevalence, efficacy, safety, and cost-effectiveness.

Characteristics of Essential Drugs:

Availability: These drugs must be available at all times.
Adequate Supply: There should be sufficient quantities to meet demand.
Assured Quality: Drugs should meet stringent quality standards.
Appropriate Dosage Forms: Available in the correct forms for administration.
Affordability: Priced in a way that is affordable to individuals and the community.

Selection Criteria for Essential Drugs:

Disease Prevalence: Drugs are selected based on the most common diseases in the population.
Efficacy: There must be solid evidence of the drug\’s ability to treat the condition.
Safety: The drug must have a favorable safety profile, with acceptable risk/benefit ratios.
Cost-effectiveness: The drug must be economical for both patients and the health system.
Scientific Data: Sufficient scientific evidence regarding the drug\’s effectiveness must be available.
Safety Monitoring: Drugs should undergo continuous safety assessments.
Single Active Ingredient: Preferably, drugs should contain one active ingredient, unless combinations are required for compliance or synergy.

Essential Drugs in Uganda

Class	Drug Name(s)
Antimalarials	Artemether, Artemether/lumefantrine, Dihydroartemisinin/piperaquine, Quinine, Primaquine
Antiamoebics	Metronidazole, Tinidazole
Antibacterials	Amoxicillin, Amoxicillin + clavulanic acid, Benzathine penicillin, Benzylpenicillin, Ceftriaxone, Cefuroxime, Flucloxacillin, Cloxacillin, Chloramphenicol, Ciprofloxacin, Cotrimoxazole, Doxycycline, Gentamicin, Erythromycin
Antituberculosis	Ethambutol, Isoniazid, Pyrazinamide, Rifampicin, Streptomycin
Antifungal	Amphotericin B, Clotrimazole, Fluconazole, Griseofulvin, Ketoconazole, Miconazole, Nystatin
Antileprosy	Clofazimine, Dapsone, Rifampicin, Thalidomide
Antiepileptics/Anticonvulsants	Carbamazepine, Clonazepam, Diazepam, Ethosuximide, Magnesium sulfate injection, Phenobarbitone, Phenytoin, Valproic acid
Anthelmintics	Mebendazole, Albendazole, Ivermectin, Praziquantel, Diethylcarbamazine
Analgesics/Antipyretics	Acetylsalicylic acid (Aspirin), Diclofenac, Paracetamol (Acetaminophen)
Antigout	Allopurinol, Colchicine, Indomethacin, Probenecid
Opioid Analgesics	Codeine, Morphine, Pethidine, Dihydrocodeine
Antivirals	Acyclovir, Ganciclovir
Cardiovascular	Atenolol, Isosorbide dinitrate, Nifedipine, Propranolol, Verapamil, Captopril, Hydralazine, Methyldopa, Lisinopril, Digoxin
Dermatological	Benzoic acid + salicylic acid, Miconazole, Clotrimazole, Benzyl peroxide, Coal tar, Dithranol, Podophyllum resin, Salicylic acid (2%, 5%), Silver nitrate pencil (40%), Betamethasone cream, Calamine lotion (15%), Hydrocortisone cream/ointment (1%), Malathion lotion (0.5%), Benzyl benzoate lotion (25%), Silver sulphadiazine cream (1%), Neomycin + bacitracin ointment, Chlorhexidine cream (5%)
Antiulcer	Cimetidine, Omeprazole, Ranitidine, Magnesium trisilicate compound
Antiemetics	Domperidone, Promethazine, Metoclopramide, Cyclizine
Laxatives	Bisacodyl, Senna
Antidiabetics	Insulin, Glibenclamide, Metformin, Tolbutamide
Cytotoxic Drugs	Asparaginase, Calcium folinate, Cyclophosphamide, Cytarabine, Dacarbazine, Dactinomycin, Fluorouracil, Doxorubicin, Hydroxyurea, Mercaptopurine, Methotrexate, Mustine, Stilboestrol, Thioguanine, Vincristine

Rational Use of Medicines

Rational use of medicines means that patients receive the appropriate drug for their clinical needs, in the correct dosage, for an adequate period, and at a cost that is affordable for them and the community.

Rational Drug Use

Rational drug use aims to optimize treatment while minimizing risks.

Principle	Description
Right indication	Prescribe only when necessary, based on a proper diagnosis
Right drug	Select the most effective, safe, and cost-efficient option
Right dose	Tailor dose to patient needs, considering individual factors
Right duration/time	Administer for the correct length of time
Patient education	Inform patients about correct use, side effects, and adherence

Right patient, Right medicine, Right dosage, Right route., Right time, Right storage., Right formulation, Right disposal, Right site, Right equipment.

Irrational Use of Medicines

Irrational drug use occurs when:

Too many drugs are prescribed per patient.
Wrong drugs are chosen for specific conditions.
Inadequate doses are given.
Unnecessary use of injections instead of oral medications.
Indiscriminate use of antibiotics, such as for viral infections like the common cold or diarrhea.

Factors Contributing to Irrational Use of Medicines:

Heavy Patient Load: Overworked healthcare professionals may rush prescriptions without thorough evaluation.
Poor Communication Skills: Inadequate interaction between healthcare providers and patients leads to misunderstandings.
Lack of Ethics: Some health professionals may act unethically by overprescribing medications.
Misinterpretation of Lab Results: Inaccurate interpretation of diagnostic results can lead to incorrect treatment.
Poor Attitude towards Work: A lack of motivation may result in careless prescribing practices.
Patient Misconceptions: Patients may insist on injections or antibiotics due to false beliefs about their efficacy.
Inconsistent Drug Supply: Unpredictable availability of medications may force healthcare providers to prescribe alternatives.
Lack of Medicine Formulary: Absence of a formal guide for medication use can lead to inconsistent prescribing.
Misleading Promotions: Drug companies may advertise their products in ways that mislead both patients and providers.
Inadequate Regulation: Insufficient oversight can allow for substandard or unnecessary drugs to enter the market.

Consequences of Irrational Drug Use

Antibiotic Resistance: Overuse of antibiotics contributes to the development of resistant bacteria, making infections harder to treat.
Resource Wastage: Irrational drug use wastes valuable healthcare resources.
Increased Costs: Patients bear higher financial burdens due to unnecessary or inappropriate prescriptions.
Adverse Drug Reactions: Polypharmacy (the use of multiple drugs) increases the risk of harmful interactions and side effects.
Loss of Patient Confidence: Inconsistent or ineffective treatment can erode trust in the healthcare system.
Poor Health Outcomes: Patients are more likely to experience complications, delays in recovery, or even worsening of their conditions.

Legal aspects and national policies Read More »

Drug Classification

Classifications of Drugs

A drug is any substance that, when introduced into a living organism, alters its structure or function. This includes anything from medications used to treat illnesses to recreational substances. Drugs are used for various reasons:

Treatment: To cure or manage diseases and health conditions.
Prevention: To protect against illnesses (e.g., vaccines).
Diagnosis: To help identify medical conditions (e.g., contrast dyes used in medical imaging).
Symptom Relief: To ease the discomfort associated with various ailments (e.g., pain relievers).

Drug Nomenclature: The Three Names of a Drug

Each drug typically has three names:

Chemical Name: This is a complex, detailed description of the drug\’s precise chemical structure and composition. It\’s very long and complicated, rarely used in everyday practice (e.g., (+/-)-2-(p-isobutylphenyl) propionic acid).
Generic Name: This is the official, non-proprietary name assigned to a drug by a regulatory body like the FDA (Food and Drug Administration) or EMA (European Medicines Agency). It\’s simpler than the chemical name and universally recognized (e.g., ibuprofen). Doctors commonly use generic names when prescribing, and pharmacists usually use this name when dispensing medication.
Brand Name (Trade Name or Proprietary Name): This is the name under which the drug is marketed and sold by a specific pharmaceutical company. It is a copyrighted name and often includes a trademark symbol (®) (e.g., Brufen®, Advil®, Motrin® – all brand names for ibuprofen). Many different companies may produce the same drug, each with a different brand name.

Examples of Generic and Brand Names: Note that a single generic drug can have many different brand names. Similarly, some brand names may combine multiple active ingredients, while others may simply repackage an existing generic drug.

Generic Name	Brand Name(s)	Indication/Use
Amoxicillin	Amoxil®, Duramox®, Amoxapen®, and many more	Antibiotic (treats bacterial infections)
Ibuprofen	Brufen®, Advil®, Motrin®, Nurofen®, and many more	Pain reliever, anti-inflammatory
Paracetamol	Panadol®, Tylenol®, Acetaminophen®, and many more	Pain reliever, fever reducer
Propranolol	Inderal®, InnoPran XL®, and others	Treats high blood pressure, angina, and tremors
Salbutamol	Ventolin®, Proventil®, and others	Bronchodilator (treats asthma and other lung conditions)
Diazepam	Valium®, Diastat®, and others	Anti-anxiety medication, muscle relaxant
Metformin	Glucophage®, Fortamet®, and others	Treats type 2 diabetes
Lisinopril	Prinivil®, Zestril®, and others	Treats high blood pressure
Atorvastatin	Lipitor®, and others	Reduces cholesterol levels

Important Note: While brand-name and generic drugs contain the same active ingredient, there might be slight differences in inactive ingredients (fillers, binders). These differences usually don\’t affect the drug\’s efficacy, but some individuals might experience minor differences in how the medication affects them. This is usually not clinically significant, but it\’s important to be aware of.

Drug Classification

Drugs can be categorized in several ways, each serving a specific purpose in understanding their use, regulation, and pharmacological properties. The primary classifications include:

Prescription Classification
Pharmacological Classification
Legal Classification

Prescription Classification

This classification system divides drugs based on whether they require a prescription from a healthcare provider or can be obtained over the counter.These need a doctor\’s prescription because they\’re powerful, can have serious side effects if misused, or are easily abused.

Prescription-Only Medicines (POM):

These drugs necessitate a prescription due to their potential for harm if misused or self-administered. Examples include:

Antibiotics: Amoxicillin (treats bacterial infections), Ciprofloxacin (treats various bacterial infections), and others targeting specific bacterial strains. The choice of antibiotic depends heavily on the identified pathogen and its susceptibility.
Analgesics: Diclofenac (a nonsteroidal anti-inflammatory drug, NSAID, for pain and inflammation). Other NSAIDs like ibuprofen and naproxen also fall into this category, differing in their mechanisms and side-effect profiles.
Cardiovascular Medications: Nifedipine (a calcium channel blocker used to treat hypertension and angina). Numerous other cardiovascular drugs exist, targeting various aspects of the cardiovascular system, including blood pressure, heart rate, and cholesterol levels. Each drug has specific indications and contraindications.
Antidepressants: Sertraline (Zoloft), Fluoxetine (Prozac). These treat depression and other mood disorders. They should only be taken under a doctor\’s supervision due to potential side effects and the need for careful dose adjustment.
Anti-anxiety Medications: Alprazolam (Xanax), Diazepam (Valium). These are used for anxiety and panic disorders, and can be habit-forming.
Asthma Inhalers: Many inhalers containing corticosteroids or bronchodilators require a prescription to ensure appropriate use and monitoring for side effects.
Diabetes Medications: Insulin (various types), Metformin. These require careful monitoring and adjustment by a doctor to maintain blood sugar levels within a safe range.

Over-the-Counter (OTC) Drugs:

These are considered safe for self-administration when used as directed. These are considered safe enough for you to buy without a prescription. They\’re readily available in pharmacies and other retail outlets. Examples include:

Analgesics: Panadol® (paracetamol/acetaminophen), Hedex® (containing paracetamol and other ingredients). The specific formulation of OTC analgesics varies widely, influencing their effectiveness and potential side effects.
Vitamins and Minerals: Numerous vitamin and mineral supplements are sold OTC, but their efficacy and safety depend on factors like dosage, individual needs, and potential interactions with other medications or underlying health conditions.
Cough and Cold Remedies: Goodmorning syrup® (and similar products) containing ingredients intended to alleviate cough symptoms. It\’s crucial to consider the specific active ingredients and potential interactions before use.
Antacids: Tums, Rolaids. These neutralize stomach acid for heartburn relief. Overuse can be problematic.
Antihistamines: Diphenhydramine (Benadryl), Cetirizine (Zyrtec). These relieve allergy symptoms. Some can cause drowsiness.
Laxatives: Many types exist for treating constipation. Overuse can lead to dependence.

Pharmacological Classification

This system categorizes drugs based on their mechanism of action or their effect on the body. This focuses on what the drug does in the body.

By Target Body System:

Drugs are grouped according to the organ system they primarily affect. Examples include:

Cardiovascular Drugs: Affecting the heart and blood vessels (e.g., beta-blockers, ACE inhibitors, diuretics). Each class within cardiovascular drugs has specific actions and clinical applications.
Neurological Drugs: Affecting the nervous system (e.g., antidepressants, antipsychotics, anticonvulsants). The choice of neurological medication is highly individualized based on diagnosis and patient response.
Gastrointestinal Drugs: Affecting the digestive system (e.g., antacids, laxatives). Different gastrointestinal drugs target specific aspects of digestive function.
Respiratory Drugs: Affecting the lungs and airways (e.g., bronchodilators, corticosteroids). Respiratory drugs are crucial in managing conditions like asthma and COPD.

By Activity on Microorganisms:

This is particularly important for antimicrobial drugs:

Antibiotics: Targeting bacteria (e.g., penicillin, tetracycline, cephalosporins). Antibiotic classes differ in their mechanisms of action and spectrum of activity.
Antivirals: Targeting viruses (e.g., acyclovir, oseltamivir). Antiviral drugs often have highly specific targets and mechanisms.
Antifungals: Targeting fungi (e.g., fluconazole, ketoconazole). Antifungal drugs can have differing effects depending on the type of fungus being treated.

Legal Classification

Legal classification divides drugs into categories based on their potential for abuse and medical use. In otherwords, Drugs are classified based on their therapeutic use, abuse potential, and legal status.

Class A Drugs:

These include highly controlled substances such as:

Morphine
Pethidine
Cocaine (Schedule I and II)

Class B Drugs:

These include a broader range of controlled substances such as:

Phenobarbitone
Ciprofloxacin
Amoxicillin
Diazepam
Codeine
Griseofulvin
Metformin (Schedule 3, 4, and 5)

Class C Drugs:

These include over-the-counter drugs that are generally considered safe for public use without a prescription.

Class	Description	Examples
Class A	High abuse potential, controlled substances	Morphine, pethidine
Class B	Prescription required, lower abuse potential	Amoxicillin, antihypertensives
Class C	Over-the-counter, safe for self-medication	Paracetamol, aspirin

Schedule of Controlled Substances

Controlled substances are further categorized into schedules based on their potential for abuse and accepted medical uses. That is to say, this classification is based on the potential for abuse and the drug\’s medical usefulness.

Schedule I Drugs (High Abuse Potential, No Accepted Medical Use): Heroin, lysergic acid diethylamide (LSD). These are typically subject to the strictest control measures.

Examples: Heroin, Lysergide (LSD)
Characteristics: High abuse potential and no currently accepted medical use.

Schedule II Drugs (High Abuse Potential, Accepted Medical Use): Morphine, codeine, pethidine (meperidine), methadone, cocaine. These drugs are tightly regulated, requiring specific prescribing protocols and record-keeping. Their use is generally reserved for situations where the benefits outweigh the substantial risks of addiction and misuse.

Examples: Morphine, Codeine, Pethidine, Methadone, Cocaine
Characteristics: High abuse potential but accepted medical uses. These drugs can lead to severe physical and psychological dependence.

Schedule III Drugs (Moderate Abuse Potential, Accepted Medical Use): Phenobarbitone, preparations containing limited quantities of opioids (e.g., codeine combined with paracetamol/acetaminophen – co-codamol). These have less stringent control measures than Schedule I and II drugs but still require careful monitoring.

Examples: Phenobarbitone, preparations containing limited quantities of opioids, and combinations with non-controlled substances like Paracetamol with Codeine (Co-codamol)
Characteristics: Less abuse potential than Schedule I and II drugs, with accepted medical uses.

Schedule IV Drugs (Low Abuse Potential, Accepted Medical Use): Diazepam, lorazepam (benzodiazepines). While considered less prone to abuse, these can still cause dependence with prolonged use.

Examples: Diazepam, Lorazepam
Characteristics: Lower abuse potential than Schedule I-III drugs, with accepted medical uses.

Schedule V Drugs (Lowest Abuse Potential, Accepted Medical Use): Drugs for cough or diarrhea containing limited quantities of opioid substances (e.g., loperamide in some formulations, piritex with codeine syrup, kaolin). These are often available with less stringent regulatory oversight than higher scheduled drugs.

Examples: Drugs generally used for relief of cough or diarrhea, containing limited quantities of certain opioids like Loperamide, Kaolin, and Piritex with Codeine Syrup
Characteristics: Lower abuse potential due to their low strength, with accepted medical uses.

Drug Administration

Drug administration refers to how drugs are delivered to patients.

Route	Description	Advantages	Disadvantages
Enteral (Oral)	Taken by mouth	Convenient, safe	Slow onset, GI absorption variability
Parenteral (IV, IM, SC)	Injections directly into the body	Rapid effect, precise control	Requires skill, painful, risk of infection
Topical	Applied to skin or mucous membranes	Localized effect, non-invasive	Slow absorption, limited drug types
Inhalational	Inhaled gases or aerosols	Quick relief for respiratory conditions	Requires technique, potential for irritation

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Prescription Writing and Dispensing

Prescription Writing

A prescription is a legal document—a written order from a licensed healthcare professional (doctor, nurse practitioner, physician assistant, etc.) to a pharmacist or other authorized dispenser, instructing them to provide a specific medication to a patient.

The prescriber has a legal and ethical responsibility to ensure the prescription is accurate, clear, and safe.

A good prescription must include the following essential information:

1. Legibility: Written clearly in indelible ink (permanent ink that won\’t fade or smear).

2. Date: The date the prescription was written.

3. Patient Information: The patient\’s full name and address. For children, their age and weight are crucial for accurate dosing.

4. Diagnosis: The medical reason for prescribing the medication. While not always explicitly stated on every prescription, this is medically critical information used to justify the treatment and assess the appropriateness of the drug.

5. Medication Details:

Drug Name: The full name of the medication (generic name preferred for clarity).
Dosage Form: Tablet, capsule, liquid, injection, etc.
Strength: The amount of active ingredient per dosage unit (e.g., 500mg).
Quantity: The total amount of medication to be dispensed.
Duration: The length of treatment (e.g., \”take for 7 days\”).
Frequency: How often the medication should be taken (e.g., \”twice daily\”).

6. Patient Instructions: Clear, concise directions on how to take the medication, including when to take it (with or without food, at bedtime, etc.).

7. Prescriber Information: The prescriber\’s full name, address, and contact information (phone number, etc.).

8. Facility Information: The name and address of the healthcare facility where the prescription is written.

Qualities of a Good Prescriber

A good prescriber is knowledgeable, careful, and patient-centered. They:

Prescribe Only When Necessary: Avoid unnecessary medication.
Choose Appropriate Regimens: Select the most effective and safest treatment based on the patient\’s specific condition and other health factors (allergies, other medications).
Adjust Treatment as Needed: Monitor the patient\’s response to treatment and adjust the dosage or medication as needed.
Explain Treatment Clearly: Communicate effectively with the patient, explaining their condition, the medication\’s purpose, potential side effects, and how to take it properly.
Monitor Patient Progress: Follow up with the patient to assess their progress and make adjustments as needed.

The Rational Prescribing Process

Good prescribing follows a structured process:

Define the Problem: Accurately diagnose the patient\’s condition.
Specify Therapeutic Objectives: Clearly define the desired outcome of treatment (e.g., pain relief, blood pressure control).
Choose Appropriate Treatment: Select the most effective, safe, and well-tolerated medication, considering the patient\’s overall health, potential drug interactions, and cost.
Write an Accurate Prescription: Follow all the guidelines above.
Inform the Patient: Educate the patient about their condition, treatment, and potential side effects.
Review and Adjust Treatment: Regularly monitor the patient\’s response and make changes as needed.

Over-Prescribing vs. Under-Prescribing: Both are problematic:

Over-prescribing: Wastes resources, increases the risk of side effects and adverse drug reactions, and can lead to addiction and increased healthcare costs.
Under-prescribing: Leads to ineffective treatment, potentially worsening the condition, delaying recovery, and ultimately increasing the cost of treatment over time due to the need for more extensive treatment down the road.

The Dispensing Process

Dispensing is the process of providing medication to the patient as directed by the prescription.

It\’s performed by a licensed pharmacist or other authorized personnel (nurse, pharmacy technician).

Roles of a Dispenser

Medication Dispensing: Accurately filling prescriptions.
Patient Education: Providing medication information and instructions to patients.
Record Keeping: Maintaining accurate drug records.
Drug Storage: Ensuring proper storage conditions.
Consultation with Prescriber: Advising prescribers on medication issues. (in some settings)
Drug Procurement: Assisting with ordering drugs. (in some settings)

The Dispensing Procedure

Receiving the Prescription: Checking for completeness and accuracy.
Interpreting the Prescription: Understanding the instructions.
Retrieving the Medication: Obtaining the correct medication from stock.
Patient Counseling: Explaining how to take the medication and what to expect.
Packaging: Ensuring the medication is properly packaged and labeled.
Record Keeping: Documenting the dispensing process.
Providing the Medication: Giving the medication to the patient.

Knowledge Required for Dispensing

Dispensers need comprehensive knowledge of:

Drug formulations and dosages
Indications and uses of medications
Precautions and contraindications
Potential side effects
Packaging, labeling, and storage requirements
Legal requirements for controlled substances
Medication administration techniques
Basic disease processes

Prescribing Medications

Prescribing involves selecting the appropriate drug, dose, route, and duration for treatment.

Consideration	Details
Patient factors	Age, weight, sex, pregnancy status, organ function, allergies, comorbidities
Drug factors	Efficacy, safety, side effects, interactions, cost
Compliance	Ensuring patient understanding and adherence to the regimen

Prescription Requirements:

A legal prescription must include patient details, drug information, and prescriber information.

Prescription Element	Description
Patient Information	Name, age, address
Drug Details	Name, strength, dosage, quantity, instructions
Prescriber Information	Name, signature, registration number

Abbreviations Used in Drug Administration

A wide range of abbreviations are used by doctors when making a prescription. These abbreviations are utilized to save time and space on prescriptions. They are categorized as follows:

1) Abbreviations Related to Frequency of Drug Administration

Abbreviation	Meaning
OD	Once daily
BID	Twice daily
TDS	3 Times daily
QID	4 Times daily
PRN	When necessary
Stat	Immediately
Ac	Before meals
Pc	After meals

2) Abbreviations Related to Dosage Form

Abbreviation	Meaning
Caps	Capsules
Tabs	Tablets
Syr	Syrup
Gut	Eye drops
Inf.	Infusion
Pess.	Pessaries
Mist	Mixture
Iv	Intravenous

Drug Classification Read More »

Terminologies and Sources of Drugs

TERMINOLOGIES

Pharmacology: The scientific study of drugs, their origins, chemical properties, actions, and uses in the treatment, diagnosis, and prevention of disease.

Pharmacology is the scientific study of drugs and their use in medicine.
This includes pharmacokinetics (what the body does to the drug) and pharmacodynamics (what the drug does to the body).
In midwifery, pharmacology focuses on medications used during pregnancy, labor, delivery, and the postpartum period, considering the impact on both the mother and the fetus/newborn.
The study of pharmacology helps a midwife to use the drugs appropriately while caring for the pregnant mother.
Pharmacology is divided into two major branches namely;
Pharmacokinetics and Pharmacodynamics.

Pharmacokinetics: The study of the movement of drugs within the body, including absorption, distribution, metabolism, and excretion (ADME). Understanding pharmacokinetics is vital in midwifery to determine appropriate dosage and timing of medications, considering changes in maternal physiology during pregnancy and lactation.

Pharmacodynamics: The study of the biochemical and physiological effects of drugs and their mechanisms of action. This includes drug receptor interactions and the relationship between drug concentration and effect. In midwifery, pharmacodynamics helps predict a drug\’s efficacy and potential side effects in pregnant and breastfeeding women.

Drug: A substance intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease in humans or other animals.

A drug is a chemical substance which alters the functioning of the body.
Most drugs used in clinical practice are used to prevent, diagnose and treat diseases.
A drug can have more than two names : chemical name, generic name and a brand name.
The chemical names are normally used by chemists and are not used in
clinical practice because they are usually very difficult to remember and write.
This is a name given to a drug by an international body. Generic name of a drug is known worldwide. The Ministry of Health of Uganda recommends that all drug prescriptions should be written with generic names to avoid confusion. Examples include Oxytocin, Misoprostol.
A brand name also called a trade name is a name given to a drug by a manufacturing company.
All brand names begin with a capital letter and bear a symbol *. Example Amoxil*, Duramox*, Unixil*.

Medication: A drug administered for therapeutic purposes. This highlights the intentional use of a drug to achieve a specific clinical outcome.

Therapeutics: The branch of medicine concerned with the treatment of disease and the use of drugs in the prevention and treatment of disease.

In midwifery, therapeutic interventions include pain management, infection control, and management of obstetrical complications.

Toxicology: The study of poisons and the adverse effects of drugs and other chemicals on living organisms.

In midwifery, toxicology is important for understanding the potential risks of medications to the mother and fetus, including teratogenicity (the ability to cause birth defects) and fetotoxicity (harm to the fetus).

Chemotherapy: The use of chemical agents (drugs) to treat diseases.

In the context of midwifery, this might include the treatment of infections (e.g., with antibiotics) or the management of certain cancers. Specific consideration needs to be given to the potential effects on breastfeeding.

Teratogen: An agent that can cause birth defects. Many drugs are potential teratogens, and careful consideration is needed when prescribing medications during pregnancy.

Sources of Drugs

Drugs, substances used to prevent, diagnose, treat, or cure diseases, originate from different sources. These sources can be broadly categorized as natural or synthetic.

1. Natural Sources: These sources utilize naturally occurring substances extracted or purified from living organisms or minerals.

Plants: A rich source of medicinal compounds, plants have been used for centuries in traditional medicine. Many modern drugs are derived from or inspired by plant-based compounds. Examples include:

Atropine: An anticholinergic alkaloid derived from plants like Atropa belladonna (deadly nightshade) used to treat certain types of poisoning and slow heart rate.
Morphine: An opiate alkaloid extracted from the opium poppy (Papaver somniferum), a potent analgesic used to manage severe pain.
Quinine: An antimalarial alkaloid obtained from the bark of the cinchona tree (Cinchona species).
Digoxin: A cardiac glycoside extracted from the foxglove plant (Digitalis purpurea), used to treat heart failure and arrhythmias.
Pilocarpine: A cholinergic alkaloid from Pilocarpus species, used to treat glaucoma and dry mouth.
Physostigmine: A cholinesterase inhibitor from the Calabar bean (Physostigma venenosum), used to treat myasthenia gravis.

Animals: Certain animal tissues and secretions yield valuable medicinal compounds. Examples include:

Insulin: A hormone crucial for glucose metabolism, originally extracted from the pancreas of pigs and cattle, now primarily produced via recombinant DNA technology.
Adrenaline (Epinephrine): A hormone and neurotransmitter vital in the \”fight-or-flight\” response, originally extracted from adrenal glands, now synthesized.
Heparin: An anticoagulant extracted from animal tissues (e.g., pig intestines, cattle lungs), now also produced synthetically.
Gonadotropins: Hormones regulating reproductive function, originally extracted from animal pituitary glands or pregnant women\’s urine, now often produced via recombinant DNA technology.
Antitoxic Sera: Preparations containing antibodies obtained from animals immunized against specific toxins.

Minerals: Inorganic substances from the earth have also found therapeutic applications. Examples include:

Magnesium Sulfate: Used as a laxative, anticonvulsant, and in other applications.
Aluminum Hydroxide: An antacid used to neutralize stomach acid.
Iron Salts: Used to treat iron deficiency anemia.
Sulfur: Used in various topical treatments.
Radioactive Isotopes: Used in nuclear medicine for diagnostic and therapeutic purposes (e.g., iodine-131 for thyroid cancer).

Microorganisms: Bacteria and fungi are sources of several crucial antibiotics:

Penicillin: A beta-lactam antibiotic produced by Penicillium fungi.
Cephalosporins: A class of beta-lactam antibiotics derived from Cephalosporium fungi.
Tetracyclines: A broad-spectrum antibiotic class obtained from Streptomyces bacteria.

Humans: Certain human-derived substances have therapeutic applications:

Immunoglobulins: Antibodies obtained from human blood plasma, used to provide passive immunity.
Growth Hormone: A hormone regulating growth and development, originally extracted from human pituitary glands, now produced via recombinant DNA technology.
Chorionic Gonadotropin: A hormone produced during pregnancy, originally extracted from pregnant women\’s urine, now often produced synthetically.

2. Synthetic Sources: The majority of modern drugs are now produced synthetically, offering advantages such as precise control over purity, consistent quality, and scalability. These are chemically synthesized in laboratories, often mimicking or improving upon naturally occurring compounds. Examples include:

Quinolones: A class of broad-spectrum antibiotics.
Omeprazole: A proton pump inhibitor used to reduce stomach acid production.
Sulfonamides: (Sulfa drugs): A class of antibiotics.
Pancuronium: A neuromuscular blocking agent.
Neostigmine: A cholinesterase inhibitor.

Sources and Examples of Drugs

Source	Example Drug(s)
Plants	Atropine, Morphine, Quinine, Digoxin, Pilocarpine, Physostigmine
Animals	Insulin, Adrenaline, Heparin
Minerals	Magnesium Sulphate, Aluminum Hydroxide
Microorganisms	Penicillin, Cephalosporins, Tetracyclines
Humans	Immunoglobulins, Growth Hormone
Synthetic	Quinolones, Omeprazole, Sulfonamides

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Pharmacokinetics

Pharmacokinetics involves the study of how drugs move through the body, focusing on four key processes: absorption, distribution, metabolism, and excretion. In brief, it is what the body does to the drug.

Absorption

Absorption refers to how a drug enters the bloodstream from its site of administration.

Factor Influencing Absorption	Description	Impact
Route of administration	Method by which the drug is given (e.g., oral, IV)	Affects speed and efficiency of absorption
Surface area	Area available for drug absorption (e.g., intestines have a large surface area)	Larger surface areas increase absorption rate
Blood flow	Circulation at the absorption site	Higher blood flow enhances absorption
Presence of food	Interaction of food with the drug in the GI tract	Can either enhance or delay absorption
Drug formulation	Physical form of the drug (e.g., tablet, liquid)	Different forms have different absorption rates

Distribution

Distribution is how the drug is transported from the bloodstream to various tissues and organs.

Factor Influencing Distribution	Description	Impact
Protein binding	Degree to which a drug binds to plasma proteins	Only unbound drugs are active
Lipid solubility	Ability to dissolve in fats	Lipophilic drugs easily cross cell membranes
Blood circulation	Blood flow to different tissues	Organs with high blood flow receive drugs faster
Blood-brain barrier	A selective barrier protecting the brain	Only certain drugs can cross into the CNS

Bioavailability

Bioavailability is the proportion of a drug that reaches the systemic circulation and is available for therapeutic effect.

Route	Bioavailability	Notes
Intravenous (IV)	100%	Directly enters the bloodstream
Oral (PO)	Varies (20-80%)	Affected by first-pass metabolism and GI absorption
Subcutaneous (SC)	Moderate	Slower, sustained release into the bloodstream

Metabolism

Metabolism involves the biochemical alteration of a drug, primarily in the liver, into an inactive or less active form.

Factor Influencing Metabolism	Description	Impact
Age	Metabolic capacity varies with age	Neonates and elderly often metabolize drugs more slowly
Enzyme activity	Presence of drug-metabolizing enzymes	Drugs can induce or inhibit enzyme activity, affecting metabolism
Genetic factors	Individual genetic makeup	Variations can lead to differences in drug metabolism
Disease states	Conditions affecting organs	Liver diseases can impair metabolism, leading to drug accumulation

Excretion

Excretion is the removal of drugs or their metabolites from the body, mainly via the kidneys.

Route	Description	Examples
Renal (urine)	Primary route via kidneys	Most drugs and metabolites
Biliary (feces)	Excretion via bile into the intestines	Some drugs are excreted unchanged
Pulmonary (breath)	Exhalation of volatile drugs	Inhaled anesthetics
Others (sweat, saliva, breast milk)	Minor routes	Depends on drug properties

Pharmacodynamics

Pharmacodynamics involves the study of the effects of drugs on the body, including mechanisms of action, dose-response relationships, and therapeutic outcomes.

Term	Definition	Examples
Mechanism of Action	How a drug produces its effects	Inhibition of enzymes, receptor binding
Dose-Response Relationship	Relationship between dose and effect	Higher doses generally lead to greater effects
Therapeutic Index	Ratio of toxic dose to therapeutic dose	A higher index indicates a safer drug
Side Effects	Unintended drug effects at therapeutic doses	Nausea, drowsiness
Toxicity	Harmful effects from excessive dosing	Overdose leading to organ damage
Adverse Drug Reactions (ADRs)	Harmful reactions to normal doses	Allergic reactions, anaphylaxis

Application of Pharmacology to Midwifery Nursing and Patient Education

Pharmacological knowledge is important for safe and effective patient care and education. The nursing process provides a framework for applying this knowledge.

Pre-administration Assessment

The pre-administration assessment aims to:

1. Establish Goals:

Collect baseline data to evaluate both therapeutic and adverse responses. This requires understanding the medication\’s intended effects and potential side effects.
Identify high-risk patients based on factors like age, renal/hepatic function, genetic predispositions, allergies, pregnancy, and concurrent medications.
Assess the patient\’s capacity for self-care, including understanding, dexterity(ability to use hands), and cognitive abilities.

2. Collecting Baseline Data: Gathering data (vital signs, lab results, symptom assessment) before medication administration establishes a benchmark to measure therapeutic effectiveness and detect adverse effects.

3. Identifying High-Risk Patients: This involves recognizing predisposing factors such as:

Pathophysiology: Compromised liver or kidney function significantly impacts drug metabolism and excretion.
Genetic Factors: Genetic polymorphisms can alter drug metabolism and response.
Drug Allergies: A history of allergic reactions necessitates careful medication selection.
Pregnancy: Pregnancy alters physiology, impacting drug absorption, distribution, metabolism, and excretion. Fetal safety must be prioritized.
Age: Both very young and older adults often require dosage adjustments due to differences in organ function.
Comorbidities and Concurrent Medications: Interactions between multiple medications or underlying health conditions significantly impact drug response.

4. Tools for identification include patient history, physical examination, and laboratory tests. Knowledge of potential drug interactions is crucial.

Implementing the Medication Order

A. Making PRN Decisions: A PRN (pro re nata, \”as needed\”) order requires the nurse to exercise clinical judgement regarding the timing and dosage based on the patient\’s needs and assessment. The rationale for medication use must be clearly understood.

B. Managing Toxicity: Early recognition and management of drug toxicity are very key. Nurses must be familiar with the early signs of toxicity for each medication and the appropriate intervention protocols.

Application of Pharmacology in Patient Education

Patient education is paramount for safe and effective drug therapy. Essential information includes:

Drug Name and Therapeutic Category: Include both generic and trade names.
Dosage Size and Schedule: Clear instructions on how much to take and when.
Route and Technique of Administration: Detailed instructions on how to administer the medication (oral, injection, topical, etc.).
Duration of Treatment: Specify the length of therapy.
Method of Drug Storage: Instructions on proper storage to maintain drug efficacy and safety (e.g., refrigeration, protection from light).
Expected Therapeutic Response and Onset: Explain the expected benefits and when they should appear.
Non-drug Measures: Discuss complementary therapies or lifestyle modifications that can enhance treatment.
Symptoms of Major Adverse Effects: Educate patients on recognizing and reporting adverse effects. Include strategies for minimizing discomfort or harm.
Major Adverse Drug-Drug and Drug-Food Interactions: Explain potential interactions and precautions to take.
Contact Information: Provide contact information for reporting adverse effects or treatment concerns.

Application of the Nursing Process in Drug Therapy

The nursing process provides a systematic approach to medication administration and patient care:

A. Review of the Nursing Process:

Assessment: Data collection via interview, medical history, physical exam, observation, and laboratory tests.
Analysis/Nursing Diagnosis: Identifying actual and potential health problems related to medication therapy. This includes judging the appropriateness of the prescribed regimen, identifying potential drug-induced problems, and assessing the patient\’s capacity for self-care.
Planning: Defining goals, setting priorities, and identifying interventions to maximize therapeutic effects and minimize adverse effects.
Implementation (Intervention): Carrying out the planned interventions, including medication administration and patient education. This includes both independent (nurse-initiated) and collaborative (physician-ordered) interventions.
Evaluation: Determining the effectiveness of the interventions by analyzing data collected during implementation. This guides adjustments to the care plan as needed.

B. Applying the Nursing Process in Drug Therapy:

1. Pre-administration Assessment: This section summarizes essential information needed before administering a drug. It includes:

Patient History: Reviewing allergies, current medications (prescription and over-the-counter), relevant medical history (renal/hepatic function, etc.), and any potential drug interactions.
Baseline Data: Obtaining vital signs, relevant lab results, and other pertinent assessment data to establish a benchmark against which to measure therapeutic and adverse effects.
Patient Understanding: Assessing the patient\’s understanding of the medication, their ability to self-administer, and their overall capacity for adherence to the treatment regimen.

2. Implementation:

Administration: This section outlines the safe and effective administration of the medication, including:

Routes of Administration: Describing appropriate routes (oral, intravenous, intramuscular, subcutaneous, topical, etc.) and any specific techniques for each.
Dosage and Adjustment Guidelines: Summarizing appropriate dosage ranges, factors influencing dosage adjustments (e.g., age, renal function), and any special instructions for dose titration.
Special Considerations: Highlighting any unique considerations during administration (e.g., rate of infusion, injection site selection, monitoring for adverse effects during administration).

Enhancing Therapeutic Effects: This section focuses on strategies to optimize the medication\’s therapeutic effect, including:

Dietary Modifications: Describing any necessary dietary changes to enhance drug absorption or minimize interactions (e.g., taking medication with food or avoiding certain foods).
Comfort Measures: Identifying strategies to improve patient comfort and adherence (e.g., managing side effects with antiemetics or analgesics).
Adherence Strategies: Outlining methods to promote adherence, such as medication reminders, pill organizers, or support systems.

3. Ongoing Evaluation and Intervention: This section outlines the ongoing monitoring and management of both therapeutic and adverse responses to the medication.

a. Monitoring: Summarizes physiological and psychological parameters requiring monitoring to detect both therapeutic and adverse responses. This includes regular vital signs, lab tests (as appropriate), and ongoing assessments of the patient\’s subjective experience.
b. Evaluating Therapeutic Effects: Describes the criteria and procedures for evaluating the effectiveness of the medication in achieving its intended therapeutic goal. This should include specific, measurable outcomes.
c. Minimizing Adverse Effects: Summarizes major adverse reactions that should be monitored for and outlines appropriate interventions to minimize harm. This could include both pharmacological and non-pharmacological interventions.
d. Minimizing Adverse Interactions: Summarizes potential drug-drug and drug-food interactions and provides interventions to mitigate the risks.
e. Managing Toxicity: Describes the major symptoms of drug toxicity and the appropriate treatment protocols. This section is crucial for early recognition and intervention to prevent serious complications.

4. Patient Education: This section summarizes essential information to be provided to the patient to promote safe and effective use of the medication. It should include:

Medication Name and Purpose: Clearly explaining both the generic and brand name, along with its intended therapeutic use.
Dosage, Route, and Schedule: Providing clear and concise instructions for medication administration.
Expected Therapeutic Effects and Onset: Informing the patient what to expect and when to expect it.
Common Side Effects and Management Strategies: Educating the patient on potential side effects and how to manage them safely.
Adverse Reactions Requiring Immediate Attention: Clearly outlining warning signs and symptoms requiring immediate medical attention.
Medication Storage and Disposal: Instructing the patient on the proper storage and disposal methods.
Follow-up Care: Instructing the patient on any scheduled follow-up appointments or tests.

Terminologies and Sources of Drugs Read More »

Psychiatric disorders related to maternal child health

Psychiatric disorders that can affect mothers include:

Depression: A common disorder that can occur during pregnancy and the postpartum period
Anxiety: A common disorder that can occur during pregnancy and the postpartum period
Postpartum psychosis(Puerperal or postnatal psychosis) : A disorder that usually manifests as bipolar disorder
Post-traumatic stress disorder:
Schizophrenia: A disorder that can be increased by maternal viral infection

These disorders are often referred to as maternal mental health (MMH) disorders or perinatal mental illness.

They can have negative effects on both the mother and the child, including:

Adverse birth outcomes,
Impaired mother-infant attachment,
Breastfeeding difficulties,
Infant care difficulties, and
Increased risk of neuropsychiatric disorders in later life.

Risk factors for MMH disorders include:

Poverty
Migration
Extreme stress
Exposure to violence
Emergency and conflict situations
Natural disasters
Low social support

A. Puerperal Blues (Postpartum \”Baby Blues\”):

A transient mood disorder characterized by emotional lability, tearfulness, anxiety, irritability, and insomnia. It usually begins 2-3 days postpartum and resolves within 2 weeks.

Postpartum blues, also known as baby blues and maternity blues, is a very common but self-limited condition that begins shortly after childbirth and can present with a variety of symptoms such as mood swings, irritability, and tearfulness.

Prevalence: Affects approximately 50% of postpartum women.
Causes: The exact etiology is unknown, but likely involves hormonal shifts (particularly a drop in estrogen and progesterone), sleep deprivation, and the psychological stress of adjusting to motherhood. Altered neurotransmitter function (implied by lowered tryptophan levels) is suspected.
Predisposing Factors: While relatively common, pre-existing anxiety or mood disorders may increase the intensity and duration.
Antepartum/Intrapartum Predisposing Factors: Difficult labor, unplanned pregnancy, and lack of social support can exacerbate the symptoms.
Assessment: Diagnosis is primarily clinical, based on the presence of characteristic symptoms. No specific investigations are usually required.

B. Postpartum Depression (PPD):

A more severe and persistent mood disorder characterized by depressed mood, loss of interest or pleasure, fatigue, changes in appetite and sleep, feelings of worthlessness or guilt, difficulty concentrating, and recurrent thoughts of death or suicide. Symptoms typically emerge more gradually over the first 4-6 months postpartum, but onset can be earlier.

Prevalence: Affects 10-20% of postpartum women.
Causes: A complex interplay of hormonal changes (hypothalamic-pituitary-adrenal axis dysregulation), genetic predisposition, stressful life events, and lack of social support.
Predisposing Factors: History of depression or anxiety, family history of mood disorders, stressful life events, lack of social support, young maternal age, and difficult pregnancy or delivery.
Antepartum/Intrapartum Predisposing Factors: Cesarean delivery, difficult labor, neonatal complications, and unmet expectations about motherhood contribute to risk.
Assessment: Diagnosis is clinical, based on the DSM-5 criteria for major depressive disorder. Investigations are typically not necessary unless other medical conditions are suspected.

C. Postpartum Psychosis:

A rare but serious condition characterized by the sudden onset of psychotic symptoms such as hallucinations, delusions, disorganized thinking, and mood disturbances (mania or depression). It can include significant risk of self-harm or harm to the infant.

Prevalence: Affects 0.14-0.26% of postpartum women.
Causes: Likely involves a combination of hormonal changes, genetic predisposition (strong family history of psychosis), and possibly peripartum infections (Although direct microbial involvement is not definitive).
Predisposing Factors: Pre-existing psychotic disorder (e.g., schizophrenia, bipolar disorder), family history of psychosis, and history of postpartum psychosis.
Antepartum/Intrapartum Predisposing Factors: Pregnancy-related stress can exacerbate existing vulnerabilities.
Assessment: Diagnosis is clinical, based on the presence of psychotic symptoms. Investigations may include blood tests to rule out other medical conditions.
Microbes: While not directly causative, infections during pregnancy may contribute to the risk in some individuals by altering immune responses and interacting with hormonal changes, though this is not consistently established.

Management:

Aims of Management:

To alleviate symptoms and improve the mother\’s psychological well-being.
To ensure the safety of the mother and infant.
To promote bonding and attachment between mother and infant.
To provide support and education to the family.

Maternity Centre (Initial Management):

Puerperal Blues: Reassurance, emotional support, and education about the transient nature of the condition. Encourage adequate rest, healthy diet, and social support.
PPD: Assess symptom severity and provide appropriate psychological interventions (psychotherapy, support groups). Consider referral to a psychiatrist or mental health professional for pharmacotherapy (e.g., SSRIs like fluoxetine or paroxetine) if symptoms are severe or do not improve.
Postpartum Psychosis: Immediate referral to a psychiatrist and hospitalization are crucial.

Referral:

Referral to a psychiatrist or mental health professional is indicated for:

PPD with severe or persistent symptoms.
Postpartum psychosis.
Suicidal or infanticidal ideation.
Any concerns about the mother\’s or infant\’s safety.

Hospital Management:

Postpartum Psychosis: Hospitalization for stabilization, medication management (e.g., antipsychotics like chlorpromazine, possibly estradiol or other medications), and close monitoring. ECT may be considered in refractory cases. Lithium may be used for manic episodes, but breastfeeding would be contraindicated. Temporary separation of mother and infant may be necessary for safety.
Severe PPD: Hospitalization may be required for stabilization, medication management, and close observation.

Nursing Care:

Monitor vital signs, mood, and behavior.
Provide emotional support and education.
Administer medications as prescribed.
Facilitate bonding and attachment between mother and infant.
Educate the family about the condition and its management.
Assess for risk of self-harm or harm to the infant.

Complications:

Untreated PPD: Can lead to chronic depression, relationship problems, impaired parenting, and increased risk of suicide.
Postpartum Psychosis: Can result in significant functional impairment, long-term mental health problems, and potentially harm to the mother or infant.

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Postpartum Psychosis

Postpartum psychosis is a severe mental illness affecting women after childbirth or abortion.

It\’s a psychiatric emergency requiring immediate intervention. While it can emerge anytime within the first three months postpartum, the most common onset is within the first two to three weeks, sometimes as early as 3-10 days after delivery or within several weeks.

Epidemiology:

Incidence: Affects a small percentage of women, estimated at less than 1-2 per 1000 deliveries. This means that for every 1000 women who give birth, fewer than 2 will experience postpartum psychosis.
Risk Factors: While relatively rare, certain factors increase the risk. Being a first-time mother (primiparous) increases the likelihood compared to mothers who have delivered previously (multiparous).
Onset and Prognosis: The onset is abrupt and dramatic, often progressing rapidly. Fortunately, with appropriate and timely treatment, most women make a full recovery.

Etiology (Causes):

The exact cause remains unclear, but a combination of factors likely contributes:

1. Genetic Predisposition: A family history of mood disorders (such as bipolar disorder or schizophrenia) significantly increases the risk. Specific genetic links, such as those involving chromosome 16, are being investigated.

2. Hormonal Fluctuations: The dramatic hormonal shifts following childbirth—the sharp decrease in estrogen and progesterone levels—are thought to play a big role. These hormonal changes can affect neurotransmitter levels in the brain, potentially triggering psychotic symptoms.

3. Family/Personal History: Of depressive episodes or mental illness.

4. Psychological and Social Factors: Stressful life events, lack of social support, relationship difficulties, history of depression or anxiety, unwanted pregnancy, and difficulties with infant care are strong risk factors. These stressors can exacerbate underlying vulnerabilities. Low self-esteem related to body image or perceived maternal inadequacy can also contribute.

Lack of support
Death of a loved one
Low self-esteem (related to postpartum appearance or feeling inadequate as a mother)
Financial problems
Major life changes (moving, new job)
Poor marital relationship
Single parenthood
Childcare stress
Prenatal anxiety
Low socioeconomic status
Prenatal depression
Unplanned/unwanted pregnancy
Infant temperament problems
Substance abuse

5. Organic Factors (Physical Illnesses): In some cases, postpartum psychosis may be triggered or exacerbated by underlying medical conditions, such as:

Neurological Events: Stroke (ischemic or hemorrhagic) affecting brain regions regulating mood and cognition.
Electrolyte Imbalances: Severe disturbances in sodium, potassium, or other electrolytes can disrupt brain function, leading to psychotic symptoms.
Metabolic Issues: Hypo/hyperglycemia (low/high blood sugar) or thyroid abnormalities (hypo/hyperthyroidism) can impact brain chemistry.
Nutritional Deficiencies: Deficiencies in B vitamins (B12, folate, thiamine) can affect neurotransmitter production.
Infections: Severe infections (sepsis) can trigger a wide range of psychiatric symptoms.
Medication Side Effects: Certain medications can have psychiatric side effects.

Signs and Symptoms:

Symptoms vary but generally involve a mix of psychotic and mood-related features:

1. Psychotic Symptoms: These involve a break from reality:

Hallucinations: Experiencing things that aren\’t real, most commonly auditory (hearing voices, often commanding harmful actions towards the baby).
Delusions: Fixed, false beliefs, such as believing the baby is evil or has special powers.
Disorganized Thinking: Difficulty with coherent thought processes, leading to confused and illogical speech.

2. Mood Symptoms: These reflect extreme emotional disturbances:

Rapid Mood Swings: Switching abruptly between euphoria (intense happiness) and depression.
Severe Anxiety and Agitation: Intense fear, restlessness, and difficulty relaxing.
Insomnia: Difficulty sleeping, sometimes to the point of complete sleep deprivation.
Irritability: Easily angered or frustrated.
Depression: Overwhelming sadness, hopelessness, and loss of interest in activities.
Guilt and Self-Blame: Excessive feelings of guilt and inadequacy related to their role as a mother.
Depersonalization/Derealization: Feeling detached from oneself or one\’s surroundings, experiencing the world as unreal.

3. Other Symptoms: Confusion, memory problems, disorientation, difficulty recognizing loved ones, and even catatonia (immobility). These can severely impact the mother\’s ability to care for her infant. Mutism, Stupor, Misrecognition (e.g., not recognizing partner or mistaking others for them)

Complications:

Untreated postpartum psychosis poses significant risks:

Suicide: A high risk, as intense despair and hopelessness can be overwhelming.
Infanticide: Tragically, in rare cases, mothers experiencing hallucinations or delusions may harm their infant.
Neglect: The mother’s inability to care for the infant due to severe symptoms.
Impaired Mother-Infant Bonding: The severe emotional and psychological disturbances hinder the ability to form a secure attachment with the baby.
Relationship Strain: The illness impacts relationships with partners and family members.

Management:

Treatment is crucial and typically involves a multidisciplinary approach:

Immediate Hospitalization: Usually required for safety, particularly if there\’s a risk of self-harm or harm to the infant.
Medication (Pharmacotherapy): Antipsychotic medications to address psychotic symptoms, antidepressants to manage mood disorders, and anxiolytics (anti-anxiety medications) to reduce anxiety.
Psychotherapy: Individual and family therapy to provide support, coping skills, and address underlying psychological issues.
Education and Support: For the mother, family, and support network. Support groups can be beneficial.
Social Support: Crucial in aiding the mother\’s recovery, involving family, friends, and support groups.
Child Protection Services: May be involved if there are concerns about the infant\’s safety.
ECT (Electroconvulsive Therapy): Reserved for severe cases where other treatments are ineffective.
Other Interventions: Rest, adequate nutrition.
Post-Discharge Care: Continued monitoring and support are crucial to prevent relapse.

Breastfeeding and Medication:

Breastfeeding is often discouraged during treatment due to the potential risks of medication to the infant. While some antipsychotics are excreted in breast milk, the levels are often low. However, close monitoring is essential. Lithium is strictly contraindicated due to its potential toxicity for the infant. Clozapine is also contraindicated due to the risk of agranulocytosis in the infant (Harding, 2015). The decision regarding breastfeeding should be made in consultation with a physician and lactation consultant. The benefits and risks need to be carefully weighed.

Nursing Care Plan for Puerperal Psychosis

Assessment	Nursing Diagnosis	Goals/Expected Outcomes	Interventions	Rationale	Evaluation
Subjective Data: – Patient or family reports sudden mood swings and unusual behavior – Complaints of confusion or hallucinations Objective Data: – Observed symptoms of agitation, confusion, and hallucinations – Signs of severe mood swings or psychotic episodes – Patient appears disoriented or detached from reality	Risk for Injury related to impaired judgment and altered thought processes as evidenced by hallucinations, confusion, and impaired reality orientation	The patient will remain free from self-harm or injury during hospitalization and achieve improved orientation to reality	– Provide a safe and structured environment by removing harmful objects from the patient’s surroundings – Assign close supervision, including 1:1 observation if needed – Administer prescribed medications, such as antipsychotics or mood stabilizers, as directed – Educate family members on the importance of monitoring and safe practices – Assess risk factors regularly and modify interventions accordingly	– A safe environment reduces the risk of harm due to impaired judgment or psychotic behaviors – Close supervision ensures prompt intervention if self-harming or aggressive behaviors occur – Medication helps stabilize mood and manage psychotic symptoms, aiding in the patient’s safety – Family education enhances support at home and improves safety awareness – Continuous assessment ensures proactive adjustments to the care plan for patient safety	– Patient remains injury-free and demonstrates increased awareness of their surroundings
Subjective Data: – Family reports difficulty coping with patient’s unpredictable behavior – Patient displays emotional distress Objective Data: – Patient exhibits emotional instability and fear – Family members express concern and distress	Excessive anxiety related to sudden onset of psychiatric symptoms and altered mental status as evidenced by emotional instability and fear.	The patient will demonstrate decreased anxiety levels and express feelings of safety within 3 days	– Establish rapport with the patient by providing a calm, supportive presence – Use therapeutic communication techniques to listen actively and validate feelings – Involve the patient in care planning decisions as appropriate to provide a sense of control – Encourage family involvement in supportive care – Provide brief, clear explanations to the patient regarding interventions	– Establishing rapport builds trust and reduces feelings of isolation and anxiety – Validation helps the patient feel understood and supported – Involvement in care promotes a sense of control and reduces helplessness – Family support reinforces emotional stability and helps reduce anxiety – Clear communication helps ease confusion and minimizes distress	– Patient verbalizes decreased anxiety and reports feeling supported and safe
Subjective Data: – Patient appears unaware of her condition and the need for treatment Objective Data: – Non-compliance with prescribed treatments – Expressions of denial or lack of insight regarding her condition	Inadequate health Knowledge related to lack of understanding about puerperal psychosis and need for treatment as evidenced by expressions of denial or lack of insight regarding her condition	The patient and family will verbalize an understanding of puerperal psychosis and the importance of ongoing treatment by discharge	– Educate the patient and family about puerperal psychosis, including its causes, symptoms, and treatment options – Provide written materials for reference on symptoms, management, and coping strategies – Use simple language and repeat important information to reinforce understanding – Encourage family members to attend counseling sessions if available – Collaborate with mental health professionals to facilitate ongoing therapy or support groups post-discharge	– Knowledge empowers the patient and family to recognize symptoms and understand the importance of treatment – Written materials provide additional support for retention of information – Simple language reduces confusion and improves learning – Counseling sessions support coping and improve family understanding of patient care – Continued mental health support ensures long-term management of symptoms	– Patient and family verbalize an understanding of the condition and demonstrate willingness to engage in ongoing care
Subjective Data: – Patient exhibits inappropriate emotional responses or appears indifferent to her newborn Objective Data: – Limited interaction with her infant – Displays signs of impaired bonding with her child	Impaired Parenting related to psychotic symptoms and emotional instability as evidenced by signs of impaired bonding with her child	The patient will begin to engage positively with her newborn and show interest in developing a mother-infant bond within 7 days	– Facilitate safe, supervised mother-infant bonding sessions as appropriate – Encourage skin-to-skin contact or gentle interaction when the patient is calm and receptive – Educate the patient on the importance of mother-infant bonding for both her and the baby\’s well-being – Provide emotional support and reassurance to reduce fear of interaction with the infant – Involve family in infant care to offer support and positive reinforcement	– Structured bonding sessions enhance maternal confidence and promote a connection with the infant – Skin-to-skin contact fosters maternal-infant bonding and reduces stress – Education on bonding importance helps motivate the patient toward positive interactions – Emotional support decreases fear and enhances confidence in parenting – Family involvement provides a supportive environment, strengthening the mother’s sense of security	– Patient demonstrates improved interest in bonding with the newborn and engages in positive interactions
Subjective Data: – Family expresses concern over patient’s behavior and ability to care for herself and the newborn Objective Data: – Family shows signs of emotional exhaustion and distress – Limited understanding of the patient’s mental health condition	Caregiver Role Strain related to the demands of supporting a family member with puerperal psychosis as evidenced by the family showing signs of emotional exhaustion and distress.	The family will express improved coping skills and demonstrate understanding of the patient’s needs and condition	– Provide emotional support to family members, acknowledging their concerns and challenges – Educate family on puerperal psychosis, emphasizing it is treatable and not due to personal failure – Encourage family to seek respite care or delegate caregiving tasks to prevent burnout – Refer family to support groups or mental health resources – Encourage regular communication with the healthcare team to address concerns	– Emotional support validates the family’s experience, helping them feel understood – Education reduces stigma and enhances understanding of the condition – Respite care prevents caregiver burnout and enhances family resilience – Support groups provide an outlet for emotional expression and advice – Ongoing communication keeps the family informed and involved in patient care	– Family reports improved understanding of the condition, demonstrates coping strategies, and shows reduced signs of emotional distress

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Conversion disorder

Conversion disorder, also known as functional neurological disorder (FND), is a psychiatric condition that causes physical symptoms that cannot be explained by a medical or neurological condition.

These symptoms are real to the person experiencing them, but are not intentional or under their conscious control.

Clinical Presentation

Conversion disorder is a medical problem involving the function of the nervous system; specifically, the brain and body\’s nerves are unable to send and receive signals properly. As a result of this communication problem, patients with conversion disorders may have difficulty moving their limbs or have problems with one or more of their senses.

	Symptoms
Movement	Weakness, paralysis, tremors, twitching, difficulty walking, drop attacks
Senses	Blindness, double vision, hearing problems, deafness, loss of sense of smell or touch
Speech	Inability to speak, slurred speech, stuttering, speaking in a whisper
Other	Difficulty swallowing, incontinence, balance problems, hallucinations, psychogenic non-epileptic seizures (PNES)
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Management of Conversion Disorder

Conversion disorder is usually treatable through therapy, such as cognitive behavioural therapy, stress reduction and distraction techniques, or physiotherapy or occupational therapy.

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Psychiatric disorders related to maternal child health Read More »