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Anticonvulsants

Anticonvulsants / antiepileptic drugs are a type of drugs that are used to prevent or treat seizures or convulsions by controlling abnormal electrical activity in the brain.

Common Terms

Absence seizure: type of generalized seizure that is characterized by sudden, temporary loss of consciousness, sometimes with staring or blinking for 3 to 5 seconds; formerly known as a petit mal seizure
Antiepileptic: drug used to treat the abnormal and excessive energy bursts in the brain that are characteristic of epilepsy.
Convulsion: tonic–clonic muscular reaction to excessive electrical energy arising from nerve cells in the brain.
Epilepsy: collection of various syndromes, all of which are characterized by seizures.
Generalized seizure: seizure that begins in one area of the brain and rapidly spreads throughout both hemispheres
Partial seizures: also called focal seizures; seizures involving one area of the brain that do not spread throughout the entire body.
Seizure: sudden discharge of excessive electrical energy from nerve cells in the brain
Status epilepticus: state in which seizures rapidly recur; most severe form of generalized seizure
Tonic–clonic seizure: type of generalized seizure that is characterized by serious clonic–tonic muscular reactions and loss of consciousness, with exhaustion and little memory of the event on awakening; formerly known as a grand mal seizure

A seizure is a sudden burst of uncontrolled electrical activity in the brain that occurs when neurons become excessively active.

Seizures can be generally classified into two major groups depending on where they begin in the brain;

Focal seizures affect initially only a portion of the brain typically one hemisphere and may occur with or without impairment of awareness.
Generalized seizures affect both sides of the brain at the same time and almost always cause loss of consciousness.

Seizures can be viewed as the result of an imbalance between inhibitory and excitatory processes in the brain that produces either too little inhibition or too much excitation.

Inhibition and Excitation neurotransmitters.

Excitatory. Excitatory neurotransmitters “excite” the neuron and cause it to “fire off the message,” meaning, the message continues to be passed along to the next cell. Examples of excitatory neurotransmitters include glutamate, epinephrine and norepinephrine.
Inhibitory. Inhibitory neurotransmitters block or prevent the chemical message from being passed along any farther. Gamma-aminobutyric acid (GABA), glycine and serotonin are examples of inhibitory neurotransmitters.
Modulatory. Modulatory neurotransmitters influence the effects of other chemical messengers. They “tweak” or adjust how cells communicate at the synapse. They also affect a larger number of neurons at the same time.

DRUGS FOR TREATING GENERALIZED SEIZURES

Hydantoins

Ethotoin
Fosphenytoin
Phenytoin

Barbiturates and Barbiturate-Like Drugs

Mephobarbital
Phenobarbital
Primidone

Benzodiazepines

Clonazepam
Diazepam

Succinimides

Ethosuximide
Methsuximide

Oxazolidinediones

Trimethdiaone
Paramethadione

Sulfonamides

Acetazolamide
Zonisamide

Valproates / Valproic Acid Derivatives.

Valproic acid
Sodium Valproate
Divalproex sodium

DRUGS FOR TREATING PARTIAL SEIZURES

Carboxamides

Carbamazepine
Oxcarbazepine

Gaba analogs

Pregabalin
Gabapentin

Triazines

Lamotrigine

Fructose derivatives

Topiramate

DRUGS FOR TREATING GENERALIZED SEIZURES

Drugs typically used to treat generalized seizures stabilize the nerve membranes by blocking channels in the cell membrane or altering receptor sites.

Because they work generally on the central nervous system (CNS), sedation and other CNS effects often result. Various drugs are used to treat generalized seizures, including hydantoins, barbiturates, barbiturate-like drugs, benzodiazepines, and succinimides. These drugs affect the entire brain and reduce the chance of sudden electrical
outburst.

Hydantoins

Hydantoins include ethotoin (Peganone), phenytoin (Dilantin). Because hydantoins are generally less sedating than many other antiepileptics, they may be the drugs of choice for patients who are not willing to
tolerate sedation and drowsiness. They do have significant adverse effects; thus, less toxic drugs, such as benzodiazepines, have replaced them in many situations.

Indications of Hydantoins

Treatment of tonic–clonic and psychomotor seizures.
Short-term control of status epilepticus, prevention of seizures after neurosurgery.

Dose

Phenytoin

Adult: 100 mg Orally t.d.s., up to 300–400 mg/d; 10–15 mg/kg IV
Children: 5–8 mg/kg per day Orally; 5–10 mg/kg IV in divided doses

Contraindications of Hydantoins

Presence of allergy to any of these drugs to avoid hypersensitivity reactions.
Are associated with specific birth defects and should not be used in pregnancy or lactation unless the risk of seizures outweighs the potential risk to the fetus.
Women of childbearing age should be urged to use barrier contraceptives while taking these drugs.

Adverse effects

Nystagmus
ataxia
slurred speech
depression
confusion
drowsiness
lethargy
fatigue
constipation
dry mouth
anorexia
cardiac arrhythmias and changes in blood pressure
urinary retention
loss of libido.

Barbiturates and Barbiturate-Like Drugs

The barbiturates and barbiturate-type drugs inhibit impulse conduction in the ascending reticular activating system (RAS), depress the cerebral cortex, alter cerebellar function, and depress motor nerve output. They stabilize nerve membranes throughout the CNS directly by influencing ionic channels in the cell membrane, thereby decreasing excitability and hyperexcitability to stimulation.

Indications

Treatment of tonic–clonic and absence seizures.
Are also used as anxiolytic/hypnotic agent.
Emergency control of status epilepticus and acute seizures associated with eclampsia, tetanus, and other conditions.
Treatment of cortical focal seizures

Dose

Phenobarbital

Adult: 60–100 mg/d Orally; 200–320 mg IM or IV for acute episodes, may be repeated in 6 hours; reduce dose with elderly and with renal or hepatic impairment.
Children: 3–6 mg/kg per day Orally; 4–6 mg/kg per day IM or IV; 15–20 mg/kg IV over 10–15 min for status epilepticus.

Contraindications, Adverse effects, same as hydantoins

Benzodiazepines

The benzodiazepines may potentiate the effects of GABA, an inhibitory neurotransmitter that stabilizes nerve cell membranes. These drugs, which appear to act primarily in the limbic system and the RAS, also cause muscle relaxation and relieve anxiety without affecting cortical functioning substantially. The benzodiazepines stabilize nerve membranes throughout the CNS to decrease excitability and hyperexcitability to stimulation.

Indications

Treatment of absence and myoclonic seizures.
Treatment of severe convulsions, clonic–tonic seizures, status epilepticus; treatment of alcohol withdrawal and tetanus
Relieves tension, preoperative anxiety.
Administered to patients who do not respond to succinimides.
Being studied for use in the treatment of panic attacks, restless leg movements during sleep, hyperkinetic dysarthria(where you have difficulty speaking because the muscles you use for speech are weak), acute manic episodes, multifocal tic disorders, and neuralgias.

Dose

Diazepam

Adult: 2–10 mg Orally b.d. to q.i.d.; or 0.2 mg/kg PRN, may repeat in 4–12 h, 2–20 mg IM or IV
Geriatric or debilitated patients: 2–2.5 mg, Orally b.d.; or 2–5 mg IM or IV.
Pediatric: 1–2.5 mg Orally t.d.s to q.i.d.; or 0.3–0.5 mg/kg

Contraindications and adverse effects for benzodiazepines are the same as those
discussed for hydantoins.

DRUGS FOR TREATING PARTIAL SEIZURES

Partial seizures may be simple (involving only a single muscle or reaction) or complex (involving a series of reactions or emotional changes. Drugs used in the treatment of partial seizures include carbamazepine. Some of the drugs used to treat generalized seizures have also been found to be useful in treating partial seizures

The drugs used to control partial seizures stabilize nerve membranes in either of two ways—directly, by altering sodium and calcium channels, or indirectly, by increasing the activity of GABA, an inhibitory neurotransmitter, and thereby decreasing excessive activity.

Carbamazepine and oxcarbazepine are used as monotherapy, and the
remaining drugs are used as adjunctive therapy

Carbamazepine

Indications

Drug of choice for treatment of partial seizures and tonic–clonic seizures.
Treatment of trigeminal neuralgia, bipolar disorder.

Dose

Adult: 800–1200 mg/d Orally in divided doses 6–8 hourly.
Pediatric (> 12 yr): adult doses, do not exceed 1000 mg/d
Pediatric (6–12 yr): 20–30 mg/kg per day Orally in divided doses t.d.s to q.i.d.
Pediatric (<6 yr): 35 mg/kg per day Orally

Gabapentin

Indications

Used as adjunct in treating partial seizures
Treatment of postherpetic pain in adults and children ages 3–12 yr of age, migraines, bipolar disorders
Treatment of tremors of multiple sclerosis, and nerve-generated
pain states

Dose

Adult: 900–1800 mg/d Orally in divided doses t.d.s
Pediatric (3–12 yr): 10–15 mg/kg per day Orally in divided doses.

Contraindications

Contraindications to the drugs used to control partial seizures include the following conditions:

presence of any known allergy to the drug
bone marrow suppression, which could be exacerbated by the drug effects
severe hepatic dysfunction, which could be exacerbated and could interfere with the metabolism of the drugs.
Pregnancy; Carbamazepine, clorazepate, gabapentin, and oxcarbazine have been shown to be dangerous to a fetus and should not be used during pregnancy. Women of childbearing age should be advised to use contraception.
Lactation; These drugs enter breast milk and can cause serious adverse effects in the baby. If any of these drugs is needed during lactation, another method of feeding the baby should be used.

Adverse Effects

drowsiness
fatigue
weakness
confusion
headache
insomnia
GI depression, with nausea, vomiting, and anorexia
upper respiratory infections.
can also be directly toxic to the liver and the bone marrow, causing dysfunction.

Nursing Considerations for Patients Receiving Anticonvulsants.

Assess for contraindications and cautions: any known allergies to these drugs to avoid hypersensitivity reactions,
Assess for history of bone marrow suppression or renal stones, which could be exacerbated by these drugs
History of renal or hepatic dysfunction that might interfere with drug metabolism and excretion.
Assess for current status of pregnancy or lactation, which are contraindicated or require caution when using these drugs.
Inspect the skin for color and lesions to determine evidence of possible skin effects;
Assess pulse and blood pressure and auscultate heart to evaluate for possible cardiac effects;
Assess level of orientation, affect, reflexes, and bilateral grip strength to evaluate any CNS effects;
Monitor bowel sounds and urine output to determine possible gastrointestinal or genitourinary effects.
Assess the patient’s renal and liver function, including renal and liver function tests, to determine the appropriateness of therapy and determine the need for possible dose adjustment.
Monitor the results of laboratory tests such as urinalysis and CBC with differential to identify changes in bone marrow function.

Nursing Diagnoses
Nursing diagnoses related to drug therapy might include the following:

Acute Pain related to GI and CNS effects
Disturbed Thought Processes related to CNS effects
Risk for Injury related to CNS effects
Risk for Infection related to bone marrow suppression effects
Deficient Knowledge regarding drug therapy

Implementation With Rationale

Administer the drug with food to alleviate GI irritation if GI upset is a problem.
Monitor CBC before and periodically during therapy to detect and prevent serious bone marrow suppression.
Protect the patient from exposure to infection if bone marrow suppression occurs.
Discontinue the drug if skin rash, bone marrow suppression, unusual depression, or personality changes occur to prevent further serious adverse effects.
Discontinue the drug slowly, and never withdraw the drug quickly, because rapid withdrawal may precipitate seizures.
Arrange for counseling for women of childbearing age who are taking these drugs. Because these drugs have the potential to cause serious damage to the fetus, women should understand the risk of birth defects and use barrier contraceptives to avoid pregnancy
Provide safety measures to protect the patient from injury or falls if CNS changes occur.
Provide patient teaching, including drug name and prescribed dosage, as well as measures for avoidance of adverse effects, warning signs that may indicate possible problems, and the need for periodic laboratory testing and monitoring and evaluation to enhance patient knowledge about drug therapy and to promote
compliance.

Evaluation

Monitor patient response to the drug (decrease in incidence or absence of seizures).
Monitor for adverse effects (CNS changes, GI depression, bone marrow suppression, severe dermatological reactions,
liver toxicity, renal stones).
Evaluate the effectiveness of the teaching plan (patient can give the drug name and dosage and name possible adverse effects to watch for and specific measures to prevent them; patient is aware of the risk of birth defects and the need to carry information about the diagnosis and use of this drug).
Patients being treated with antiepileptic are often on long term therapy, which requires compliance with their drug regimen and restrictions associated with their disorder and the drug effects. Educate the patients about this.

MULTIPLE CHOICE QUESTIONS

Select the best answer to the following.

When teaching a group of students about epilepsy, which of the following should the nurse include?
a. Always characterized by grand mal seizures.
b. Only a genetic problem.
c. The most prevalent neurological disorder.
d. The name given to one brain disorder.
Which of the following would the nurse be least likely to include as a type of generalized seizure?
a. Petit mal seizures.
b. Febrile seizures.
c. Grand mal seizures.
d. Complex seizures.
Which instruction would the nurse encourage a patient receiving an antiepileptic drug to do?
a. Give up his or her driver’s license.
b. Carry a Medical form identification.
c. Take antihistamines to help dry up secretions.
d. Keep the diagnosis a secret to avoid prejudice.
Drugs that are commonly used to treat grand mal seizures include;
a. barbiturates, benzodiazepines, and hydantoins.
b. barbiturates, antihistamines, and local anesthetics.
c. hydantoins, phenobarbital, and phensuximide.
d. benzodiazepines, phensuximide, and valproic acid.
The drug of choice for the treatment of partial seizures is
a. valproic acid.
b. methsuximide.
c. carbamazepine.
d. ethosuximide.
Focal or partial seizures
a. start at one point and spread quickly throughout the brain.
b. are best treated with benzodiazepines.
c. involve only part of the brain.
d. are easily diagnosed and recognized.
One drug that is used alone in the treatment of partial seizures is
a. carbamazepine.
b. topiramate.
c. lamotrigine.
d. gabapentin.
Treatment of epilepsy is directed at
a. blocking the transmission of nerve impulses into the
brain.
b. stabilizing overexcited nerve membranes
c. blocking peripheral nerve terminals.
d. thickening the meninges to dampen brain electrical activity.

Anticonvulsants Read More »

Epilepsy

Epilepsy is a physical condition which comprises sudden depolarization of groups of cerebral neurons which may remain localized (focal) or which may spread to cause generalized seizures

OR Abnormal, spontaneous, recurrent abnormal activity in the central nervous system which may clinically manifest as motor, sensory or psychomotor experiences.

Seizure is defined as when there is a non-recurrent abnormal electric activity in the brain or central nervous system resulting in abnormal motor, sensory or psychomotor experiences.

Therefore when a person has recurrent, intermittent tendency to develop a seizure, we say he is having epilepsy.

EPILEPSY

Epilepsy is a neurological disorder in which the brain activity becomes abnormal, causing seizures or periods of unusual behaviour, sensations, and sometimes loss of awareness.

Epilepsy is the commonest neurological disorder in Uganda. it presents in different ways and this complicates the attempts of its diagnosis. However, its very important to make its clear diagnosis early to prevent neurological complications, promote good control and improve welfare and quality of life of the affected.

Anyone can develop epilepsy at any age irrespective of sex or race. It presents a significant burden of disease and remains largely untreated especially in developing countries.

Causes

Epilepsy has no identifiable cause in about half of the people with the condition.

Genetic influence especially primary epilepsy; condition runs in families
Head trauma from accidents, domestic violence etc.
brain tumors
Brain conditions such strokes or any condition that damages the brain
uncontrolled convulsions in fever during the first four years of life (febrile convulsions)
Infectious diseases such as AIDS, meningitis, encephalitis etc.
birth trauma to an infant
Prenatal injury such as infections to the mother, poor nutrition or oxygen deficiency.
Prematurity
Malnutrition
Post maturity
alcohol and drug abuse

Types of epilepsy

Grand mal epilepsy (major), (generalised tonic-clonic epilepsy)
Petit mal epilepsy (minor), (absences)
Temporal lobe epilepsy psychomotor
Jacksonian epilepsy (focal)

Grand mal epilepsy

Is a major form of epilepsy characterized by total loss of consciousness and occurrence of a fit lasting 3-5 minutes. the patient regains consciousness spontaneously and may sustain injuries during the episode.

It is characterised by a grand mal seizure which occurs in four phases

Aura phase
Tonic phase
Clonic phase
Deep sleep or post convulsive phase

Aura phase

Is a brief warning sensation which can be a sound, a flash of light, a peculiar taste in the mouth , feeling of weakness, dizziness, arm or leg numbness or a brief pain in the stomach at the onset of some seizures. It occurs in 50% of patients and it takes less than 10 seconds.

Tonic phase

It follows aura phase for those who have. There is total loss of consciousness and falling down with contraction of all muscles such that the whole body is hyperextended. There is often a cry as air is being forced through a tight and narrowed vocal cord. It lasts for about 20seconds.

Clonic phase

This is characterised by repeated contractions and relaxation of all muscles of the body. There is gross motor activity resulting into jerking of the limbs. It is at this stage that the bladder is emptied and rarely stool is released through the sphincters of the rectum.

A lot of frothy saliva comes from the mouth, sometimes its blood stained if the tongue and lips are beaten.

This lasts between 30 and 90 seconds.

Deep sleep

The patient goes into deep sleep for about two hours, upon waking up, the patient is confused for a few minutes, complains of headache as has amnesia for the entire attack.

Note; Pre ictal stage is a stage that occurs in hours, days or weeks before an episode of epilepsy. It is characterise by

Talkativeness
Violence
Irritability
Restlessness
Depression

Post ictal stage is a stage that occurs after an episode of a disease i.e

Calmness
Quietness
Isolation
Retarded mobility
Depression

Different Types of Generalized Seizures

Absence Seizures

Once known as “petit mal” seizures, these are staring spells that start suddenly and may be mistaken for simple daydreaming. The person having an absence seizure will typically stop moving and stare in one direction for 15 seconds or less.

The episode resolves on its own, and though the person may not remember what happened during the seizure, their normal state of alertness returns immediately afterward.

Atonic Seizures (Drop Attacks)

A seizure of this type involves a sudden decrease in muscle tone, causing a person’s body to go limp, slump or collapse, possibly causing injury. Atonic seizures characterize certain epilepsy syndromes such as Lennox-Gastaut syndrome.

Myoclonic Seizures

Myoclonic seizures are characterized by a sudden body “jolts” or increases in muscle tone as if the person had been jolted with electricity. A myoclonic seizure is similar to the single or multiple sudden jerks people sometimes experience as they are falling asleep. “Sleep myoclonic” jerks are benign whereas myoclonic seizures can be harmful, since the “jolts” occur in bouts.

Infantile spasms is a subtype type of myoclonic epilepsy that typically begins between the ages of 3 and 12 months of age and may persist for several years. Infantile spasms typically consist of a sudden jerk followed by stiffening. Often the child’s arms fling outward as the knees pull up and the body bends forward. Each spasm lasts only a second or two but they usually occur close together in a series. Sometimes the spasms are mistaken for colic, but the cramps of colic do not typically occur in a series. Infantile spasms are most common just after waking up or falling asleep. This particularly severe form of epilepsy can have lasting effects on a child and should be evaluated and treated promptly.

Tonic and Clonic Seizures

In a tonic seizure, the person’s muscles stiffen, and they lose consciousness. The eyes roll back in their head, and muscles of the chest, arms and legs stiffen, causing the back to arch. The contracting muscles in the chest make it hard to breathe, and the person’s lips and face may turn gray or blue. The person may make gurgling sounds while struggling to breathe.

Clonic seizures cause a person’s muscles to spasm and jerk. Muscles in the elbows, legs and neck flex and then relax in rapid succession. The jerking motion slows down as the seizure subsides, and finally stops altogether. As the jerking stops, it is common for the person to let out a deep sigh before resuming normal breathing. Tonic-clonic seizures , once known as “grand mal” or “convulsive” seizures, occur when tonic and clonic movements happen at the same time. Though witnessing a seizure can be frightening, it is a myth that a person having a seizure is in danger of swallowing their tongue, which is not anatomically possible. NEVER put anything in the mouth or forcefully open a tightly clenched jaw while the seizure is happening as this could harm the person.

A seizure typically lasts a few minutes or less, after which the person is likely to remain unconscious for a few minutes more, depending on the intensity of the seizure. This is the post-seizure or post-ictal period, and during this phase the person’s brain is extremely active as it tries to contain the abnormal electrical impulses and bring the seizure under control. People regaining consciousness after a seizure are likely to be sore, confused or frightened and very tired. Providing assurance and support is the best help an observer can offer.

Tonic for stiffness, Clonic for Jerking, Tonic-clonic, for stiffening then jerking, Atonic for loosing tone and body becomes like a lump and myoclonic for recurrent tendency for a part of the body to jerk.

PETIT MAL EPILEPSY

Is a minor form of epilepsy in which there is absence of a fit or a fall. It commonly occurs in children. There is a brief loss of awareness which lasts for about 15seconds.

The patient usually does not fall down and does not know that something unusual has happened to him or her. Slight muscle contractions may occur; bladder control is hardly lost.

It starts at childhood and disappears at adolescence or can be complicated into grand mal epilepsy.

The first indication of petit mal epilepsy is when a developing child gets short disruption in motor activity and if writing, he stops and the pen drops down or when a child drops cups, plates unknowingly. This attack may occur several times in a day and may present with poor academic performance in school

JACKSONIAN EPILEPSY

This type of epilepsy has got its point of focus in the motor sensory area in the cerebral cortex.

It disrupts the function of a particular part of the body resulting from excessive electrical discharges from a focal point in the brain that controls that part for example if the focus of epilepsy is the part of the brain that supplies the left hand, there will be twitching or tremors that can start from the thumb, fingers or the whole hand. The seizure may insidiously or gradually spread to involve the whole body as a grand mal seizure.

TEMPORAL LOBE EPILEPSY

Temporal lobe seizures begin in the temporal lobes of the brain, which process emotions and are important for short-term memory. This may occur following anoxia at birth, anatomical defect or a scar in a temporal lobe. And because of that, the temporal lobes are seen to be vulnerable to low oxygen levels.

During a temporal lobe seizure, a patient may remain aware of what is happening, but in more intense seizure, the patient might look awake but be unresponsive, lips and hands may make purposeless repetitive movements like chewing, swallowing or smacking of lips

Some symptoms of a temporal lobe seizure may be related to these functions, including having odd feelings — such as euphoria, deja vu or fear.

Temporal lobe seizures are sometimes called focal seizures with impaired awareness. Temporal lobe seizures may stem from an anatomical defect or scar in your temporal lobe, but the cause is often unknown. Temporal lobe seizures are treated with medication. For some people who don’t respond to medication, surgery may be an option.

Symptoms

An unusual sensation (aura) may precede a temporal lobe seizure, acting as a warning. Not everyone who has temporal lobe seizures has auras, and not everyone who has auras remembers them.

The aura is actually the first part of a focal seizure before consciousness is impaired. Examples of auras include:

A sudden sense of unprovoked fear or joy
A deja vu experience — a feeling that what’s happening has happened before
A sudden or strange odor or taste
A rising sensation in the abdomen

Sometimes temporal lobe seizures impair ones ability to respond to others. This type of temporal lobe seizure usually lasts 30 seconds to two minutes. Characteristic signs and symptoms include:

Loss of awareness of surroundings
Staring
Lip smacking
Repeated swallowing or chewing
Unusual finger movements, such as picking motions

After a temporal lobe seizure, patient may have:

A period of confusion and difficulty speaking
Inability to recall what occurred during the seizure
Unawareness of having had a seizure
Extreme sleepiness

In extreme cases, what starts as a temporal lobe seizure evolves into a generalized tonic-clonic (grand mal) seizure — featuring convulsions and loss of consciousness

COMPLICATIONS OF EPILEPSY

Status epilepticus

This is considered as a complication of grand mal epilepsy rather than a certain type of epilepsy.

It is both a medical and psychiatric emergency.

Status epilepticus is a single epileptic seizure lasting more than five minutes or two or more seizures within a five minute period without a person returning to normal between them. It is common in young children and the elderly.

Note, most seizures last for not more than 2 minutes. This condition is life threatening and getting treatment started fast is vital.

Management

This condition requires urgent medical treatment to lessen the chances of serious complications and death.

oxygen is administered to the patient with other support breathing
intravenous line is connected for intravenous fluids and emergency drugs
anaesthetics are used in hospitals to put a person into comma to stop the seizures.
Continuous EEG monitoring may be needed to monitor the seizures and how a person responds to treatment.
Various tests are done to find out the cause so as to give appropriate treatment.

Mental deterioration

This is another complication of epilepsy which occurs after years of uncontrolled seizures. It is a form of chronic brain syndrome in which brain damage results from repeated seizures. This is why it’s important to diagnose and treat epilepsy early enough there by keeping a number of convulsions minimum or if possible eradicate them totally.

Diagnosis

Observation of a fit
History of a fit
Neurological examination to check he reflexes
Electro encephalogram ma reveal epileptiform activity
CT scan to reveal brain function
skull X ray may indicate evidence of lessions

Triggers of an epileptic fit

fevers in childhood
sleep; convulsions during sleep may occur soon after the child wakes up from bed
daylong or overnight fast
emotional arousal e.g fear, anger, excitement etc
flickering lights
intoxication with alcohol
alcohol withdrawal
fatigue and boredom
high altitude

Treatment and management of a grand mal seizure

Management of grandma fit is divided into two parts;

Emergency management
General management

An epileptic seizure is usually sudden and time to prepare for it is not there. It can occur at any time in any place.

The occurrence of a fit with or without warning, the following should be done to

Avoid injury to the patient
To prevent complications

Emergency Management

Stay calm and speak calmly if you are to give instructions or when reassuring bystanders
Remove the person from danger or vice versa if the patient is safe, don’t move them.
Note the time the seizure starts and continue checking if it does not stop in 5 minutes, call for an ambulance.
Loosen ties, necklaces or any cloth around the neck that may make it hard to breathe
Support the head with a soft flat material under like a folded jacket so as to protect it from injury during jerking
Clear space and minimize any form of crowdness such that the patient receives fresh air.
As soon as the fit stops, Make the patient lie down in a lateral position so as to ensure he does not chock with his own saliva
Check that breathing is returning to normal if their breathing sounds difficult after the seizure has stopped call for an ambulance.
Check gently to see that nothing is blocking their airway such as false teeth.
Stay with the patient until when the patient is fully awake
After recovery, reorient the patient and reassure incase he is embarrassed.

The following should not be done;

Don’t put any hard object like spoon in the mouth this can injure teeth or jaw.
Don’t hold his limbs tightly because that prevents contraction and relaxation of muscles
Don’t give anything to eat or drink until he is fully alert
Do not try to give mouth to mouth breaths, people usually start to breath again on their own after a seizure

Drug management

Drugs do not cure epilepsy but they are intended to reduce the frequency of seizures or to eradicate them altogether.

The commonly available used drugs include

Phenobarbitone 30 to 90 mg tds daily in divided doses
Phenytoin sodium 100-300mg DDD
Sodium valproate 200-1200mg tds in divided doses
Carbamazepine 100-1200mg in 3 divided doses

Encourage the patient to review clinical progress after every 2-4 weeks till control is achieved. The maximum dose for each patient depends on control of the fit and tolerance of side effects.

GENERAL PRINCIPLES OF THE TREATMENT OF EPILEPSY

Treat the causative factors if you can identify them e.g. febrile illness like malaria, infections like meningitis, and cerebral growths such as neoplasm.
Avoidance of precipitating factors e.g. alcohol, stress, exposure to chemicals and gases especially poisonous ones.
Anticipation of natural variation of a seizure e.g. period when the seizure occurs helps in planning patient’s managements.
Appropriate and regular administration of antiepileptic drugs.

Education of caretakers and persons with epilepsy

The following should be taught to the patient and the community at large

Epilepsy is an illness just like any other illness and on treatment a person gets better
People with epilepsy should be encouraged to enjoy as much as possible
Isolating, stigmatizing and labelling an epileptic patient is very traumatizing to the patient, family and clan members so they should be avoided
Children with epilepsy are encouraged to attend school
Teachers, school children and other school personnel should be educated about the illness so that they are enlightened
Adults with epilepsy can marry and should be encouraged to do so
Persons with epilepsy should avoid dangerous activities such as driving, climbing height, operating heavy machines, swimming
People have to be taught that epilepsy is not contagious so patients should be treated fairly like other people
Epileptic seizures can effectively be controlled if drugs are taken as prescribed.

An epileptic seizure becomes an emergency only when;

The person has never had a seizure before
The person has difficulty breathing or walking after the seizure
The seizure lasts longer than 5 minutes
The person has another seizure soon after the first one
The person is hurt during the seizure
The seizure happens in water
The person has a health condition like diabetes, heart disease or is pregnant

Prevention of epilepsy

Prevent head injury by wearing seat belts and bicycle helmets.
Seek medical help Immediately after suffering a first seizure.
Mothers should be encouraged to get good prenatal care to prevent brain damage to a developing fetus
Treatment of hypertension
Avoid excess alcohol abuse and alcohol intake
Treating high fevers in children
Treatment of any infections and proper nutrition including adequate vitamin intake.

ANTICONVULSANTS

Epilepsy Read More »

Anxiety Disorders

ANXIETY DISORDERS

All children have worries and fears from time to time. Whether it’s the monster in the closet, the big test at the end of the week, or any other thing, kids have things that make them anxious, just like adults.

But sometimes anxiety in children crosses the line from normal everyday worries to a disorder that gets in the way of the things they need to do. It can even keep them away from enjoying life as they should.

How can to tell if the child’s anxieties might be more than just passing worries and fears? Here are some questions to ask oneself:

Are they expressing worry or showing anxiety on most days, for weeks at a time?
Do they have trouble sleeping at night? If you aren’t sure (they might not tell you), do you notice that they seem unusually sleepy or tired during the day?
Are they having trouble concentrating?
Do they seem unusually irritable or easy to upset?

There are several different types of anxiety disorders that can affect children. The most common include:

Generalized Anxiety Disorder (GAD)

Children and adolescents with generalized anxiety disorder have persistent, excessive, and unrealistic worries that are not focused on a specific object or situation. A child may worry excessively about his or her;

performance at school or in activities such as sports
about personal safety and that of family members,
or about natural disasters.

Children with generalized anxiety have a hard time “turning off” their worrying, which leads to difficulty concentrating, learning, and participating in social situations. Some children may be insecure and frequently seek reassurance, while others may be self-conscious, self-doubting, or overly concerned about meeting other people’s expectations. Generalized anxiety disorder typically affects school-aged children and adolescents.

Kids with GAD may experience physical symptoms because they are so overwhelmed by their worries;

headaches
isolating themselves
avoiding school
Avoiding friends.

Panic Disorder

A panic attack is a sudden, intense episode of anxiety with no apparent outside cause.

Some children or adolescents may experience extreme discomfort or fear when in certain situations or places, resulting in a panic attack.

Symptoms may include;

shortness of breath
pounding heart
Tingling sensations throughout the body.
Child may tremble or feel dizzy or numb. (If your child is hyperventilating, try to have them breathe slowly with nice deep breaths.)

Although severe anxiety may result in a panic attack, a child with panic disorder often has symptoms of panic without any apparent trigger. Unlike the occasional, mild worries children often experience.

A panic attack may dramatically affect a child’s life by interrupting his or her normal activities. Often, a child becomes preoccupied with worry about possible future attacks. Panic disorder tends to begin during adolescence, although it may start during childhood, and sometimes runs in families.

Separation Anxiety Disorder

Most children have some level of separation anxiety as its a normal phase of development in babies and toddlers. Even older children may get clingy with their parents or caregivers occasionally, especially in new settings.

But older children who get unusually upset when leaving a parent or someone else close to them, who have trouble calming down after saying goodbye, or who get extremely homesick and upset when away from home at school, camp, or play dates, may have separation anxiety disorder.

Children with separation anxiety disorder experience significant fear and distress about being away from home or their caregivers. This fear affects a child’s ability to function socially and academically. For example, a child may have a hard time making friends or maintaining relationships because he or she refuses to go on play dates without a parent, or sleep without being near a parent or caregiver.

Social Phobia

Social phobia, also known as social anxiety disorder, is an excessive fear of being rejected, humiliated, or embarrassed in front of others. A child with social phobia feels severe anxiety and self-consciousness in normal, everyday, social situations. This is more than just shyness.

The socially anxious child is terrified that they will embarrass themselves when talking with classmates, answering a question in class, or doing other normal activities that involve interacting with others.

This fear can keep the child from participating in school and activities. Some children may even find themselves unable to talk at all in some situations.

Children and adolescents with social phobia worry about a wide range of situations, such as;

speaking in front of a group
participating in class
talking to adults or peers
starting or joining in conversations
eating in public.
They may fear unfamiliar people
have difficulty making friends
can also be limited to specific situations e.g. adolescents may fear dating and recreational events, for instance
but they may be confident in academic and work settings.

Children and teenagers with social phobia typically avoid the situations they fear—by staying home from school or shunning parties, for instance. Although the condition can occur in children as young as age four, it is more common among adolescents. The average age of onset is 13.

Obsessive-Compulsive Disorder

Children with obsessive-compulsive disorder (OCD) have obsessions ie; these are intrusive, unwanted thoughts. To relieve the anxiety associated with those thoughts, they perform compulsions, or repetitive actions, rituals, or routines.

Compulsions may involve washing, counting, organizing objects, or reading a passage of text over and over.

For children with OCD, these thoughts and behaviors significantly interfere with their daily functioning and can cause distress and embarrassment. OCD can develop at any age, but it’s most likely to occur between the ages of 8 and 12, in late adolescence, or early adulthood.

Specific Phobias

Fears are common in childhood and are usually outgrown as a child matures. For some children and teens, however, fears can become severe. If a fear is excessive and persistent it may be a phobia, or an intense irrational fear of a specific object or situation.

Phobias differ from usual fears in that they don’t decrease with reassurance, and they interfere with a child’s life. Children may develop phobias as early as age five. Specific phobias commonly involve animals, insects, heights, thunder, driving, dental or medical procedures, elevators etc.

Selective Mutism

Children with selective mutism speak freely in familiar situations but become mute in specific situations or around certain people. Some children with selective mutism may avoid eye contact and refuse to communicate with others. Others may enjoy the company of others but remain silent or have a close friend speak for them. Selective mutism typically affects preschool-aged children and those in elementary school, usually before age 10.

Management

Mental health professionals today understand much more about childhood anxiety disorders than in the past. No matter what the child’s anxiety disorder is, a professional health worker can help.

but the care giver has to be advised about the following for the child at home by being supportive and understanding.

If the child becomes upset and anxious, stay calm and talk to them through it.
Don’t punish the child for things like mistakes on schoolwork or lack of progress.
“Catch” them doing well: Praise even small accomplishments, and be specific.
Plan for transitions. If the child’s anxiety means going to school in the morning is very stressful, allow plenty of extra time.
While respecting the child’s privacy, do give their teachers and coaches information they need to help them understand what’s going on.

Above all, be available to listen when the child wants to talk to you about their anxiety. Kids with anxiety disorders often try to hide their fears because they think you won’t understand. So let the child know you’re ready to listen whenever they’re ready to talk

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Mental Retardation

Mental retardation is a generalized neurodevelopment disorder characterised by significantly impaired intellectual and adaptive disorder present before age of 18yrs.

Mental retardation refers to significantly sub-average general intellectual functioning resulting in or associated with concurrent impairments in adaptive behaviour as manifested during the developmental period

This is characterised by below mental ability and average intelligence or lack of skills necessary for day to day living. People with mental retardation can and do learn new skills, but they learn them more slowly.

People with intellectual disability have the following limitations

Intellectual functioning also known as (intelligence quotient) IQ

This refers to a person’s ability to learn reason, make decisions, and solve problems. Intelligence quotient is measured test of which the average is 100 and a person is considered intellectually disabled if the IQ is less than 70%

Adaptive behaviours

These are degrees with which the individual meets the standards of personal dependence and social responsibility expected of his age and cultural group.

These are skills necessary for day to day life such as being able to communicate effectively, interact with others and take care of one’s self.

Classification of Mental Retardation

Intelligence quotient is the ratio between mental age (MA) and chronological age (CA) where chronological age is determined from the date of birth and mental age is determined by the intelligence tests.

Mild mental retardation
Moderate mental retardation
Severe mental retardation
Profound

Mild mental retardation (educable)

These have IQ levels ranging from 50 to 69%. These children go undiagnosed until they reach school years. They are often slower to talk, walk and feed themselves as compared to other children. They can learn domestic and practical skills including reading and maths and achieve good independence in self-care like eating, washing, dressing etc. They can build social and job skills and can live on their own.

Moderate mental retardation (trainable)

These have IQ ranging from 35 to 49%.

Children with mild mental retardation show noticeable delays in developing speech and motor skills. Although they are unlikely to acquire useful academic skills, they can learn basic communication, some health and safety habits and other simple skills. They cannot learn how to read or do maths. Moderately retarded adults cannot live alone and need supervision throughout life but can do simple tasks and travel alone to familiar places.

Severe mental retardation (dependent retarded)

These have IQ ranging from 20 to 34%

This condition can be diagnosed as early as at birth or very soon after birth. By preschool age, they show delays in motor development and little or no ability to communicate. With good training, they can learn self-help skills such as how to feed or bath themselves. They usually learn to walk and gain basic understanding of speech as they get older.

Adults with severe mental retardation may be able to follow daily routines but need through supervision and to be kept in a protected environment.

Profound mental retardation (life support)

Only a few people with mental retardation have IQ below 20%.

This condition is diagnosed at birth and is associated with other medical problems which require nursing care. The children show delays in all aspects of development.

Most individuals are immobile, have limited ability to understand, are unable to care for themselves, have various neurological and physical disabilities, visual and hearing abilities are impaired and so many other associated disabilities.

Causes of Mental Retardation

Mental retardation is a complex action which may be caused by interaction of many factors and in 75% of patients, the cause is unknown.

Genetic factors

If one or both parents have mental retardation, chances that children develop this condition are high.
Sometimes mental retardation is caused by abnormalities of chromosomes rather than individual genes e.g. down syndrome where an individual has an extra chromosome in the cell.

Problems during pregnancy

Infections in pregnancy like TORCHES; toxoplasmosis, Rubella, Cytomegalovirus, Syphilis, herpes simplex.
Alcohol in pregnancy may cause mental retardation through Fetal Alcohol Syndrome FAS
Placental dysfunction like toxaemia of pregnancy, placenta previa, cord prolapse etc.
Some drugs like cocaine when taken in pregnancy may harm mental development of unborn child.
Maternal malnutrition
Exposure to radiations

Problems during birth (perinatal factors)

Prematurity
Very low birth weight
Instrumental delivery
Prolonged labour
Kernicterus
Birth asphyxia

Problems after birth (postnatal factors)

Lead or mercury poisoning
Severe malnutrition
Accidents that cause severe head injury
Diseases such as meningitis, encephalitis etc.
Untreated hypothyroidism
Brain tumours
Epilepsy

Environmental causes

Cultural deprivation
Low socio-economic status
Inadequate caretakers
Child abuse

Signs and symptoms of mental retardation

These vary greatly depending on the severity of the condition

IQ below 70%
Failure to achieve developmental milestones
Delay in oral language development
Deficit in memory skills
Difficult learning social roles
Difficult with problem solving skills
Decreased learning abilities or inabilities to meet education demands at school
Limited motor and communication skills
Visual and hearing impairments
Epilepsy always accompanies the problem
Require constant supervision
Neurological disorders are very common
Some may have psychotic or behavioural disorders
Self-care is a problem to these patients.

Diagnosis

This can be made by

IQ testing (MA/CA)X100
Taking history from the parents or care giver
Carrying out biochemical tests
Physical examination
Neurological examination
Assessing developmental milestones
Investigation

Urine and blood for metabolic disorders
Culture for biochemical studies
Amniocentesis in infant chromosomal disorders
Chorionic villi sampling
Hearing and speech evaluation
CT scan or MRI
Thyroid function tests when cretinism is suspected

X-ray

Management of Mental Retardation

Majority of the mentally retarded children and adults are cared for at home and admission is only required because of incompetent parents, psychotic behaviours, stigmatisation etc.

Aims

To enable the patient reach his or her maximum potential ability
To ensure safety of the patient.

Mentally retarded children are admitted in hospitals or any other institution with schools that offer them training and education suitable to their abilities.
Physical training, recreation, and social activities also play a part in treatment regimen
Love, attention and care are one of the most required elements for these children
Written, verbal and pictorial forms of communication as well as gestures and demonstration are very helpful to ensure mutual understanding and improve treatment adherence
Programmes that maximise speech, language, cognition, psychomotor, social, self care and occupational skills have to be encouraged
The main stay of treatment is by developing a comprehensive management plan for the condition which includes multiple disciplines like special educators, language therapists, behavioural therapists, occupational therapists and community service providers that provide social support to affected families.
On-going evaluation for overlapping psychiatric disorders such as depression, bipolar disorder and ADHD
Neuroleptics such as haloperidol are given in cases of psychotic behaviour
Analgesics are required for management of pain especially in severe mental retardation.
Family therapy to help parents develop coping skills and deal with guilt and anger
Early intervention programs for children younger than age 3 with mental retardation
Provide day schooling to train the child in basic skills such as bathing and feeding
Vocational training

Prevention of mental retardation

Preconception

Genetic counselling
Immunisation of maternal rubella
Adequate maternal nutrition
Family planning

During gestation

Adequate nutrition
Fetal monitoring
Protection from diseases
Avoidance of teratogenic substances like alcohol and exposure to radiations

At delivery

Delivery should be conducted in the hospital
Apgar scoring has to be done at 1 and 5 minutes after the birth of a child
Close monitoring of mother and child

Childhood

Improved general medical care for children
Improved nutrition for children
Proper and early treatment for childhood infections
Immunisation of children according to immunisation schedule

Mental Retardation Read More »

Substance Abuse

Substance abuse, as a disorder, refers to the abuse of illegal substances or the abusive use of legal substances. Alcohol is the most common legal drug of abuse.

SUBSTANCE ABUSE/CHEMICAL DEPENDENCE IN ADOLESCENTS

Alcohol and other drug use pose a serious threat to health of children and adolescents. In addition to health risks, substance abuse is often linked with other risk behaviors like violence, early sexual activity, truancy and academic failure.

Pediatricians and other PHC providers are in ideal positions to identify substance abuse and to provide preventive guidance and education to children, adolescents and their families.

Epidemiology

Between 1990’s and recent, the prevalence rates of alcohol and other drug abuse among adolescents are increasing. Research has found out that one of every two adolescents has tried an illicit drug by the time he completes high school. The most commonly abused drug is alcohol.

Definitions

There are different terms used to define substance-related disorders, including the following:

Substance abuse; Substance abuse refers to an illegal use of a substance leading to significant problems or distress

Such as problems might include;

failure to attend school
substance use in dangerous situations (driving a car)
substance-related legal problems
interfering with friendships and/or family relationships

Tolerance; refers to a need for increased amounts of a substance to attain the desired effect.

Substance dependence

Substance dependence refers to a compulsive use and continuous relying on a specific substance for both physical and psychological relief with an inability to stop its usage even after significant problems in everyday functioning have developed.

Signs include;

an increased tolerance
Withdrawal symptoms with decreased use
unsuccessful efforts to decrease use
increased time spent in activities to obtain substances
withdrawal from social and recreational activities
continued use of a substance even with awareness of physical or psychological problems encountered by the extent of the substance use

Alcohol intoxication; this is a temporary mental disturbance following heavy drinking so that the level of alcohol in blood is high and sufficient to affect someone’s activity, mood and level of consciousness.

Alcoholism; is a chronic condition where a person takes alcohol excessively and for long period of time thus leading to adverse physical, mental, social and psychological effects

Alcoholic; is a person who have been taking alcohol excessively and for a long period of time in whom it has cause serious mental, social, psychological and physical problems

Substances commonly abused by adolescents

Substances frequently abused by adolescents include, but are not limited to, the following:

Alcohol
Marijuana
Tobacco
Prescription drugs
Hallucinogens
Cocaine
Amphetamines
Opiates
Anabolic steroids
Inhalants
Methamphetamine

Causes of substance abuse

1. Cultural and societal norms and acceptable standards of substance use. Public laws determine the legality of the use of substances.

2. Genetic vulnerability; it tends to run in families

3. Psychological problems such as;

-anxiety
-stress and frustrations
-feelings of desire

4. Environmental stressors such as;

-failure of exams
-worry of the future
-failure to achieve a certain goal
-child abuse
-faulty upbringing
-lack of education
-large uncontrolled families
-economic constraints
-rape, incest and defilement

5. Social pressures from peers

6. Individual personality disorders

7. Psychiatric problems such as;

-depressive disorder
-suicidal intentions
-paronea

Adolescents at risk of substance abuse

Parental and peer substance use are two of the more common factors contributing to youthful decisions regarding substance use.

Some adolescents are more at risk of developing substance-related disorders, including adolescents with one or more of the following conditions present:

Children of substance abusers
Adolescents who are victims of physical, sexual, or psychological abuse
Adolescents with mental health problems, especially depressed and suicidal teens
Physically disabled adolescents
Children whose parents deal with substances for financial support

Symptoms of substance abuse

The following behaviors may indicate an adolescent is having a problem with substance abuse. However, each adolescent may experience symptoms differently. Symptoms may include:

Getting high on drugs or getting intoxicated (drunk) on a regular basis
Lying, especially about if and how much they are using or drinking
Avoiding friends and family members
Giving up activities they used to enjoy such as sports or spending time with nonusing friends
Talking a lot about using drugs or alcohol
Believing they need to use or drink in order to have fun
Pressuring others to use or drink
Getting in trouble at school or with the law
Taking risks, such as sexual risks or driving under the influence of a substance
Suspension from school for a substance-related incident
Missing school due to substance use and/or declining grades
Depressed, hopeless, or suicidal feelings

Diagnosis of substance abuse

A pediatrician, family doctor, psychiatrist, or qualified mental health professional usually diagnoses substance abuse in adolescents. However, adolescent substance abuse is believed by some to be the most commonly missed pediatric diagnosis. Adolescents who use drugs are most likely to visit a doctor’s office with no obvious physical findings. Substance abuse problems are more likely to be discovered by doctors when adolescents are injured in accidents occurring while under the influence, or when they are brought for medical services because of intentional efforts to hurt themselves.

History taking; this can reveal personal history on substance abuse
Clinical presentation; this often depend on the substance abused, the frequency of use, and the length of time since last used, and may include:

Weight loss
Constant fatigue
curly hair
Red eyes
Little concern for hygiene

use of the questionnaire of CAGE

Treatment for substance abuse

Specific treatment for substance abuse will be determined based on:

Adolescent’s age, overall health, and medical history
Extent of adolescent’s symptoms
Extent of adolescent’s dependence
The substance abused
Adolescent’s tolerance for specific medications or therapies
Expectations for the course of the condition
Opinion or preference of the care taker

A variety of treatment programs for substance abuse are available on an inpatient or outpatient basis. Programs considered are usually based on the type of substance abused.

Medical detoxification (if needed, based on the substance abused) and long-term follow-up management are important features of successful treatment.

Long-term, follow-up management usually includes formalized group meetings and age-appropriate psychosocial support systems, as well as continued medical supervision. Individual and family psychotherapy are often recommended to address the developmental, psychosocial, and family issues that may have contributed to and resulted from the development of a substance abuse disorder.

Prevention of substance abuse

There are three major approaches used to prevent adolescent substance use and abuse, including the following:

School-based prevention programs. School-based prevention programs usually provide drug and alcohol education and interpersonal and behavior skills training.
Community-based prevention programs. Community-based prevention programs usually involve the media and are aimed for parents and community groups. Programs, such as Mothers Against Drunk Driving (MADD) and Students Against Drunk Driving (SADD), are the most well-known, community-based programs.
Family-focused prevention programs. Family-focused prevention programs involve parent training, family skills training, adolescent social skills training, and family self-help groups. Research literature available suggests that components of family-focused prevention programs have decreased the use of alcohol and drugs in adolescents and improved effectiveness of parenting skills.

ALCOHOL AND DRUG ADDICTION

Alcohol and drug addiction have been a source of serious problems for thousands of years. Recent studies indicate that there are more psychoactive, psychological and social problems related to alcoholism and drug addiction than anything else which affect the individual and society emotionally.

The following are the commonly abused groups of substances;

Alcohol
Cannabis
Cocaine
Nicotine
Opioids
Sedatives-hypnotics/anxiolytics

Terms

Drug (substance); this refers to any chemical agent that once taken in the body is capable of causing physiological and psychological changes.

Alcoholic; this is a person who has been taking alcohol excessively in whom it has produced mental, social, physical and psychological problems

Substance intoxication; this is development of a reversible substance-specific syndrome due to recent ingestion of or exposure to the drug

Alcohol intoxication; a this is a temporally mental disturbance following heavy drinking so that the level of alcohol in blood is high and sufficient to affect somebody’s activity, mood and level of consciousness.

Tolerance; this is a need for more of the drug in order to achieve a similar effect realised before at a lower dose

Dependency; refers to compulsion to take the drug on a continuous basis in order to feel its effects and to further avoid the discomfort of its absence. This can both be physical or psychological. It is a bodily response to a substance e.g. relying on medications to control medical condition.

Addiction; this refers to a psychological and physical inability to stop consuming a drug or substance even though it’s causing psychological and physical harm. it involves using the drugs despite the consequences.

Misuse refers to the incorrect, excessive or non-therapeutic use of and mind-altering substances

ALCOHOLISM

Definition; alcoholism is a chronic condition occurring in individuals who have been taking alcohol excessively and for a long period of time that it has caused serious adverse effects physically, socially and mentally i.e. There is increased dependency of alcohol both physically and socially.

Causes of alcohol abuse

Availability; if alcohol is available and drinking is accepted for example as a norm in social gatherings and functions
Genetic factors; some excessive drinkers have a family history of excessive drinking
Poor coping strategies; people who are unable to face stress often resort to alcoholism
Psychiatric disorders; like depressive disorders, anxiety disorders an phobic disorders
Social disorders; like isolation, unemployment, loss or bereavement, injustice etc.
High risk groups e.g. people suffering from chronic physical illness, business executives, travelling salespersons, industrial workers, hostel students, military personnel etc.
Age; its common between late adolescence and early adulthood

Process of alcoholism

Experimental; due to peer pressure, influences or curiosity, the person starts to consume alcohol
Recreational; during weekends, or on holidays, the individual starts to enjoy and continue with it. If consumed in small quantities, alcohol may not cause a problem instead it may work to relieve tension and relax mind or sedate the brain from painful emotions and promote a sense of wellbeing and pleasure.
Compulsive; once used to drinking, some people who started drinking occasionally start drinking almost daily or drinking heavily for a period of time for pleasure or to avoid the discomfort of withdrawal symptoms.

Alcoholism goes through distinct stages;

Early stage

Increased tolerance– needing more and more of alcohol to experience the same pleasure as experienced earlier

Blackouts- inability to recollect incidents which happened under the incidence of alcohol

Preoccupation– always thinking about how, when and where to drink

Middle stage

Loss of control over amount, time and occasional drinking, Keeping away from alcohol for sometimes but going back to obsessive drinking after some period

Chronic stage

Getting drunk even on small amounts of alcohol, willing to lie, beg, borrow or steal to maintain supply of alcohol. Alcohol takes the priority over family or job.

Types of drinkers

Mild drinkers

These rarely and occasionally drink alcohol in small amounts or in large amounts but once in a while and it rarely causes problems

Moderate drinkers

These moderately consume not in excess nor large amounts and it doesn’t cause much health problems

Problem drinkers

These consume large amounts of alcohol daily and usually with high concentrations. As a result, the individual health will be impaired, affects peace of mind, disrupts family, loss of reputation, dignity, poor performance etc.

Effects and complications of alcohol

Physical or medical effects

Hepatitis and liver cirrhosis
Pancreatitis
Peptic ulcers and gastritis
Cardiomyopathies and heart failure
Epileptic-like fits (RUM fits)
Tuberculosis
Weight loss
Alcoholic dementia
Anaemia
Malnutrition
Lowered immunity

Psychiatric effects

Depression
Pathological intoxication such as maladaptive behavioural effects such as fighting, impaired judgement, slurred speech, mood changes, irritability and impaired attention
Delirium tremens
Alcoholic hallucinosis which are vivid hallucinations developing shortly after cessation or reduction of alcohol
Alcoholic psychosis this occurs after a person drinking alcohol for a long periods of time and in large quantities and thus develops psychotic disorder which resemble paranoid schizophrenia presenting with delusions, hallucinations and impairment of primary mental functions.
Alcohol amnestic disorder; there is impairment in short and long term memory with disorientation and confabulation
Alcoholic dementia; a chronic organic mental disorder that results into irreversible impairment in memory, orientation etc.
Suicide
Anxiety
Paranoia- persecutory and feelings of self-hate
Morbid or pathological jealousy e.g. a drunkard coming back at home and finds a ranch of a bicycle and begins quarrelling who has been at home
Hallucinations
Wernicke’s encephalopathy that occurs as a result of acute deficiency of vitamin B1 (Thiamine) in alcoholics
Korsakoff syndrome that occurs as a result of gradual depletion of thiamine from the body.

Social problems

Decreased work performance hence decreased productivity due to chronic absenteeism
Family problems like divorce
Increased accidents due to drunken driving
Legal effects like rape, theft etc.
Violence and aggression

Diagnosis of alcoholism

History taking i.e. upbringing, family background, period taken while bussing etc.
Clinical presentation like curly hair, swollen cheeks, red lips, poor hygiene etc.
Using the questionnaire of CAGE

C- Cut

Annoyed

G- Guilty

E- Eye opener

The questionnaire looks as below;

Have you ever felt that you should cut down your drinking?

Have people annoyed you by criticizing your drinking?

Have you ever felt guilty about your drinking?

Have you ever had a drink as a first thing in the morning as eye opener to get rid of hangover or calm your nerves?

Affirmative answers or any yes to two or more of the above is a suggestive to an alcoholic

Concentration of alcohol in blood with their effects

80-150mg of alcohol per 100mls of blood leads to intoxication
150-300mg of alcohol per 100mls of blood is fatal
300-500mg of alcohol per 100mls of blood is very fatal
500mg of alcohol per 100mls of blood and above leads to death

Note; all the above symptoms can change according to tolerance

Management of alcoholism

Aims

The following are the major goals in the management of alcoholism;

To detoxify the patient (only in acute stages)
To improve social relationships and support
Developing confidence and ability to change
Identifying reasons to change
Developing alternative activities
Learning to prevent relapse

Admission

Admission is very essential to ensure that the patient doesn’t have access to alcohol. The patient has to be hospitalised and not allowed home for about 6-8 weeks since they have tremendous for alcohol and can soon start drinking if allowed home.

Admit the patient in a psychiatric hospital in an open quiet room which is well lit to reduce fears and illusions
Establish a good nurse patient relationship
Keep potentially harmful objects away from the room since there is chance of deliberate self-harm
Keep the bed dry, clean and warm since the patient might be incontinent
Monitor vital signs every 15 minutes initially including physical and mental behaviour
Investigations such as
Urine for sugar
Blood for haemoglobin level and sugars
Alcohol level in blood have to be carried out

Medication

Administration of minor tranquilizers like anti-anxiety drugs such as Librium and diazepam are given parenterally if necessary to control anxiety, insomnia, agitation and tremors
Administer ant-convulsants if there is withdrawal seizure (rum fits)
Plenty of vitamins especially injection vitamin B1,B6 and B12 (100-300mg twice daily for seven days) and tablets of vitamin B complex and vitamin c
Antacids to relieve gastritis
Correct fluid and electrolyte imbalance by intravenous infusion and maintain a fluid balance chart
Drug Disulfiram (ant abuse therapy) which produces nausea and vomiting, intense headache, palpitation, blurred vision, hypotension and dyspnoea if alcohol is taken. It can be administered but under close patient supervision it is given 1g for one week then o.8g-0.6g-0.4g-0.2g and the patient is maintained on 0.1g for one year
Aversion therapy (Apo morphine) this is given in injectable form. It is a powerful emetic and the patient vomits whenever he smells alcohol. It is therefore discouraged for that
Yeast tablets are given two twice a day to induce appetite
Stamatil (avomine) is given 5-10mg to control vomiting
Sedation of the patient may be required
Avoid barbiturate drugs because alcoholics easily become addicted to them

General nursing care

Physical and psychological conditions or mental conditions associated with advanced alcoholism should be treated like malnutrition, vitamin deficiencies, hallucinations, delirium, gastritis or liver diseases
Nutrition; Ensure that the patient takes small frequent feeding rather than large meals and the diet should be nutritious and appetising to enable the patient ask for more
Hygiene; oral care, general body and bed hygiene has to be addressed
During the recovery and rehabilitation period, acceptance of the patient by the nurse is essential. The nurse’s acceptance and may encourage the patient to socialise and participate in planned activities. This will also reduce the patient’s feelings of inferiority and low self-esteem.
Psychiatric social workers should be involved in the social problems of the patient
Religious commitment has to be encouraged
Familial therapy; these should be encouraged to help the patient to stay away from alcohol
Patient should be encouraged to change friends and associates may be necessary to remove patient from those situations where drinking is very easy
Prepare the patient for alcoholic anonymous a self-group of ex-addicts who confront, instruct and support fellow drinkers in their efforts to stay sober one day at a time, through fellowships and acceptance.
Plan for discharge and resettlement of the patient into the community

STEPS OF ALCOHOLIC ANONYMUS

We admitted we were powerless over alcohol – that our lives had become unmanageable. AA firmly believes that individuals cannot overcome alcoholism on their own. They are unable to exercise willpower or personal strength that could prevent them from drinking
Came to believe that a Power greater than ourselves could restore us to sanity. Alcoholics Anonymous is based on the belief in a higher power. For some, this higher power may be God; for others, it may be a belief in the universe itself. The point is that recovery begins, in part, by looking to an entity greater than yourself.
Made a decision to turn our will and our lives over to the care of God as we understood Him.
Made a searching and fearless moral inventory of ourselves. During this step, many participants make a list of poor decisions or character flaws. They outline hurt they caused to others, as well as feelings, like fear and guilt, that motivated some of their past actions. Once the individual has acknowledged these issues, the issues are less likely to serve as triggers to future alcohol abuse.

Admitted to God, to ourselves and to another human being the exact nature of our wrongs. As AA members work this step, they sit down with someone – often their sponsor – and confess everything they identified in Step 4. This step requires the recovering individual to put aside their ego and pride to acknowledge shameful past behavior. The step is also empowering, as the alcoholic no longer has to hide behind guilt and lies.

Were entirely ready to have God remove all these defects of character. In this step, the recovering alcoholic acknowledges that he or she is ready to have a higher power – again, whatever that may be – take away the moral shortcomings identified in

Humbly asked Him to remove our shortcomings. This step requires the person to focus on the positive aspects of his or her character – humility, kindness, compassion and a desire for change – as well as step away from the negative defects that have been identified.

Made a list of all persons we had harmed, and became willing to make amends to them all. During this step, recovering alcoholics write down a list of all the people they have hurt. Often, this list includes people they hurt during their active alcoholism; however, it may go back further to include anyone they have hurt throughout their entire lives

Made direct amends to such people wherever possible, except when to do so would injure them or others. Paired with Step 8, Step 9 gives recovering alcoholics the opportunity to make things right with those they have hurt. One’s sponsor can be a big source of help during this process, helping the recovering alcoholic to determine the best way to go about making amends.

Continued to take personal inventory and when we were wrong promptly admitted it. Linked to Step 4, this step involves a commitment to continue to keep an eye out for any defects of character. It also involves a commitment to readily admit when one is wrong, reinforcing humility and honesty.

Sought through prayer and meditation to improve our conscious contact with God as we understood Him, praying only for knowledge of His will for us and the power to carry that out. Step 11 commits the recovering alcoholic to continued spiritual progress. For some, this may mean reading scripture every morning. For others, it may mean a daily meditation practice. Alcoholics Anonymous doesn’t have stringent rules on what form spiritual growth takes. It simply involves a commitment to take time to reassess one’s spiritual and mental state.

Having had a spiritual awakening as the result of these steps, we tried to carry this message to alcoholics and to practice these principles in all our affairs practice these principles in all our affairs. The final step involves helping others and serves as motivation for many to become sponsors themselves. By going through the 12 steps, individuals have a major internal shift and part of that shift is a desire to help others.

Nurses role in the prevention of alcohol abuse

Primary prevention

Aim to avoid the appearance of new cases of alcohol abuse by reducing alcohol consumption through health promotion especially health education

Secondary prevention

Attempt to detect cases early and to treat them before serious complications cause disability

Tertiary prevention

Aim to avoid further disabilities and to reintegrate individuals into the society who have been harmed by severe alcohol related problems

The nurse will be involved in all of these levels

Substance Abuse Read More »

Narcotics

Narcotics or Narcotic drugs are drugs that react with different type of opioid receptors, receptor sites that respond to naturally occurring peptides, enkephalins, and endorphins.

These are found in the CNS, peripheral nerves, and GI tract cells.

In the spinal cord, they integrate and relate pain information. Pain relief and side effects depend on the type of receptor site.

Pain

Pain is mostly a subjective experience of unpleasant sensation and emotional experience. People respond to pain differently because of cultural differences, learned experiences, and environmental stimuli.

A-delta and C-fibers are two sensory nerves that respond to stimulation by generating nerve impulses that produce pain sensations.

Classification of pain

Pain Classification According to Duration:

Acute Pain – is caused by tissue It is the type of pain which makes the person aware of the injury and leads him to seek for care and education about the injury and how to take care for it.
Chronic Pain – is a constant or intermittent pain that keeps occurring long past the time the area would be expected to This is the type that can interfere with activities of daily living.

Pain Classification According to Source

Nociceptive Pain – caused by direct pain receptor stimulus
Neuropathic Pain – caused by nerve injury
Psychogenic Pain – associated with emotional, psychological, or behavioral stimuli

Types of opioid receptors

Mu-receptors – primarily pain-blocking receptors; also account for respiratory depression, euphoria, and development of physical
Beta-receptors – modulate pain transmission by reacting with enkephalins in the periphery
Kappa-receptors – associated with some analgesia, pupillary constriction, sedation, and dysphoria
Sigma-receptors – pupillary dilation, hallucinations, psychoses with narcotic use.

Types of narcotic drugs

Narcotics are divided into 3 classes;

Narcotic Agonists – react with opioid receptors in the CNS; cause analgesia, sedation, or They are classified as controlled substances because they have potential for physical dependence.
Narcotic Agonists-Antagonists – stimulate certain opioid receptors but block other such They exert similar analgesic effect with that of morphine but they have less potential for abuse. However, they are associated with more psychotic like reactions.
Narcotic Antagonists – bind strongly to opioid receptors without causing receptor activation. They block opioid receptor effects as well as effects of too much opioids in the system.

Narcotic Agonists

These drugs react with opioid receptors in the CNS; cause analgesia, sedation, or euphoria.

Therapeutic Action

The desired and beneficial action of narcotic agonist is:

Narcotic agonists act as agonist to specific opioid receptors in the CNS to produce analgesia, euphoria, and sedation.

Indications

Narcotic agonists are indicated for the following medical conditions:

Relief of moderate to severe acute pain or chronic pain
Preoperative medication
Component of combination therapy for severe chronic pain
Intra-spinal to reduce intractable

Indication of narcotic agonists in different age groups

Children

1. Safety and effectiveness has not been established in
2. Narcotic agonists that have established pediatric dosage guidelines are codeine, fentanyl (except transdermal), hydrocodone, meperidine, and morphine
3. Naloxone is the antidote for narcotic overdose and reversal of narcotic

Adults

They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
They should be educated about the importance of asking for pain medication before the pain becomes acute.
Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus.
Narcotics used in labor include morphine, meperidine, and oxymorphone.
All narcotic agonists are pregnancy category B except oxycodone (category C) so it might be the drug of choice if one is needed during pregnancy.

Older adults

They are more susceptible to drug adverse effects because of existing medical conditions.
Safety measures should be established (side rails, call light, assistance to ambulate).

Contraindications and Cautions

The following are contraindications and cautions for the use of narcotic agonists:

Allergy to narcotic agonists. Prevent hypersensitivity reaction
Diarrhea caused by toxic poisons. Drug depresses GI activity and this could lead to increased absorption and toxicity
Respiratory dysfunction. Exacerbated by respiratory depression caused by drugs
Recent GI/GU surgery, acute abdomen, ulcerative colitis. Can be worsen by the GI depressive effects of the narcotics
Head injuries, alcoholism, delirium tremens, cerebral vascular disease. Can be exacerbated by
the CNS effects of the drug
Liver, renal dysfunction. Can interfere with metabolism and excretion of the drug
Pregnancy, lactation. Potential adverse effects to the fetus and the baby.

Adverse Effects

Use of narcotic agonists may result to these adverse effects:

CNS: light-headedness, dizziness, psychoses, anxiety, fear, hallucinations, pupil constriction, impaired mental processes
GI: nausea, vomiting, constipation, biliary spasm
GU: ureteral spasm, urinary retention, hesitancy, loss of libido
Others: sweating, physical and psychological dependence
Narcotic-induced respiratory center depression: respiratory depression with apnea, cardiac arrest, shock

Interactions

The following are drug-drug interactions involved in the use of narcotic agonists:

Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression, hypotension, and sedation or coma
SSRI, MAOI, TCA, Johns Wort: increased risk of potentially life-threatening serotonin syndrome if taken with tapentadol, the newest narcotic agonists that blocks norepinephrine reuptake in the CNS
Methylnaltrexone bromide (Relistor) is the treatment for opioid-induced constipation in palliative care patients who are no longer responding to traditional laxatives.

Drugs used as narcotic agonists

Drug

Indications

Dosage ranges

Key issues to note

Codeine

Analgesic, antitussive

Relief of pain

Adult: 30-60mg every 4-6 hours when necessary max dose 240mg daily.

Children: 1-12years: 0.5-1 mg/kg every 4-6hours

Diarrhoea

Adults: 30mg 3-4 times daily

1. Increase fluids and fibre intake to avoid constipation

2. Avoid alcohol during therapy with codeine

3. Avoid abrupt discontinuation after prolonged use

4. Codeine is not recommended for treatment of productive cough

5. Codeine may be administered with food to minimise nausea

and GI upset

Pethidine

1. Pre-operative medication

2. Acute analgesia

3. Post-operative pain

4. Moderate to severe acute pain Obstetric analgesia

Acute pain

Adult: SC or 1M injection; 50- 150mg repeated after 4 hours Children: O.5-2mg/kg every 4 hours

Obstetric analgesia: SC or 1M injection, 50-100mg repeated 1- 3 hours later if necessary max dose is 400mg in a day

Post-operative pain: SC/IM

injection

1. Prolonged use of Pethidine may result in physical dependence

2. Lowest effective doses are recommended especially during

labor

Adult: 25-100mg repeated every 2-3 hours if necessary

Children: 0.5-2mg/kg every 2 to

3 hours

Oxycodone

Analgesic

Oxycodone: 10–20 mg

PO q12h; 5 mg for break thru pain

Other narcotic agonist analgesic drugs

Methadone
Oxymorphone
Propoxyphene
Fentanyl

Short notes about Morphine

Morphine is the ‘gold standard’ against which other opioid analgesics are measured.

When used correctly, patients don’t become dependent, tolerance is uncommon and respiratory depression doesn’t usually occur.

The correct morphine dose is the one that gives pain relief: there is no ‘ceiling’ or maximum dose — the right dose is the one that controls the patient’s pain without side effects, however you need to increase the dose gradually.

Dosage of morphine

Morphine has no ceiling effect to the analgesia.

There is no standard dose of morphine for the treatment of chronic pain in patients with cancer and HIV/AIDS.

It must be individually titrated for each patient and the correct dose is that which controls the pain whilst causing tolerable side effects.

The dose required depends on many factors including the severity of pain, the type of pain, individual pharmacokinetic variations, the development of tolerance., and the psychosocial issues that affect the perception of pain.

Acute pain, postoperative pain:

Oral: 5-20mg every 4 hours

By SIC or 1M injection

Adult: 10 mg every 4 hours if necessary
Neonate: 150mcg 1kg every 6hours
6-12 years: 5-10mg every 4 hours
1-5years: 2.5-5mg every 4 hours
1 month -12months: 200mcg/kg every 6hours

Chronic pain: Oral ISC or 1M:

Adult: 10-15mg every 4 hours. Dose may be increased according to the response
Children: 2-12years: Initially 200-500mcg/kg every 4hours adjusted according to response
1-2years: Initially 200-400mcg/kg every 4hours adjusted according to response
1-12months: Initially 80mcg/kg every 4hours

Myocardial infarction:

By slow IV injection (2mg/ minute), 10mg followed by a further 5-10mg if necessary.
Elderly or debilitated patients, give a half a dose

Acute pulmonary oedema:

By slow IV injection (2mg/minute) 5-10mg

Action of morphine

Morphine acts on the opioid receptors in the brain and spinal cord to produce analgesia.

The perception of pain is altered both by a direct effect on the spinal cord, modulating peripheral nociceptive input, arid by activating the descending inhibitory systems from the brain stem and basal ganglia.

Morphine also acts on the limbic system and on higher centers to modify the emotional response to pain.

The system effects, including those affecting the gastrointestinal and respiratory tracts, arc partly centrally mediated via the autonomic nervous system and may partly be due to a direct effect on opioid receptors in the peripheral tissues.

Indications

Post-operative pain
Myocardial infarction
Premedication before surgery
Severe pain
Sickle cell crisis
Acute pulmonary oedema
Chronic pain (cancer)

Common Side effects

The common side effects of morphine include:

Constipation — therefore you should always give a laxative alongside morphine (unless the individual has diarrhoea) e.g. Bisacodyl 5mg at night increasing the dose to l5mg if needed.
Nausea and vomiting — if this occurs, give anti-emetics e.g. plasil 10mg 8 hourly.
Drowsiness — may occur in the first few days of taking morphine. If it does not improve after three days reduce the dose of morphine.
Itching — not very common but if it occurs reduce the dose of morphine

Contraindication

Morphine should be given with caution to patients with renal impairment, severe hepatic dysfunction, significant pulmonary disease (including acute or severe bronchial asthma), and CNS depression from any cause.
Elderly patients and those who are debilitated or cachectic should initially be treated with reduced doses.

Dose

Titrating oral Morphine into other formulations

Titrate the regular dose of morphine over several days until the patient is pain free. Either add the total daily dose and the total breakthrough dose given in 24 hours and divide by six to get the new 4hrly dose, or give 30—50% increments, e.g. 5—10—15mg etc., given as 4hrly doses. Increments of less than 30% are ineffective.
If the patient cannot swallow, use other routes, e.g. Rectal, subcutaneous, buccal, intravenous, or administer via an alternative enteral route such as a gastrostomy tube.
The ratio of morphine PO: SC is 2:1, g. 10mg oral morphine is 5mg SC morphine.
The ratio of morphine PO:IV is 2—3:1, g. 30mg oral morphine is 10mg IV morphine
Morphine is available in immediate and slow-release oral Use slow- release morphine once pain is controlled, dividing the total 24-hour dose into two to get the twice-daily dosage.

Useful tips when using morphine

Oral morphine can be absorbed through the mucosa of the buccal cavity (mouth) or of rectum, so small amounts can be given even for unconscious patients.
Even though a patient is on regular oral morphine they may have breakthrough pain, an additional dose of oral morphine may be given to control this pain. This may be a one off incidence of pain but if more frequent breakthrough doses are required this may mean the 4hourly dose needs increasing.
Pain has to be controlled before other problems can be addressed and treated, as it is not possible to have meaningful discussions about psychosocial concerns if a patient has
uncontrolled pain
Pain can be caused or aggravated by psychosocial concerns, which must be addressed before good pain control can be achieved. Where psychosocial or spiritual problems are causing or
aggravating pain, no amount of well-prescribed analgesia will relieve the pain until the responsible psychosocial issues are identified and addressed.
Oral morphine is effective for chronic severe pain and can be given for many years and the dose can keep increasing, some patients can even take up to several hundred mgs 4 hourly.
If the pain stimulus is removed, then the dose of morphine should be decreased gradually to minimize the effects of physical dependence.
Opiates can also be used as a short term analgesia: in AIDS opportunistic infections such as
cryptococcal meningitis; sickle cell crisis; burns and other painful conditions and does not cause
addiction

Narcotic Agonists-Antagonists

These drugs stimulate certain opioid receptors but block other such receptors.

Therapeutic Action

The desired and beneficial action of narcotic agonist-antagonist is:

Narcotic agonists-antagonists act on certain opioid receptors but block other such receptors. They have less potential for abuse compared to narcotic agonists but are able to exert similar analgesic effect as morphine.

Indications

Narcotic agonists-antagonists are indicated for the following medical conditions:

Relief of moderate to severe pain; pre-anesthetic medication and a supplement to surgical anesthesia
May be desirable for relieving chronic pain in patients who are susceptible to narcotic dependence.

Here are some important aspects to remember for indication of narcotic agonist-antagonists in different age groups:

Children

Safety and effectiveness has not been established in children.
Narcotic agonist-antagonist of choice for children older than age 13 is buprenorphine.
Naloxone is the antidote for narcotic overdose and reversal of narcotic effects..

Adults

They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
They should be educated about the importance of asking for pain medication before the pain becomes acute.
Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus.

Older adults

They are more susceptible to drug adverse effects because of existing medical conditions.
Safety measures should be established (side rails, call light, assistance to ambulate).

Contraindications and Cautions

The following are contraindications and cautions for the use of narcotic agonists-antagonists:

1. Allergy to narcotic agonists-antagonists. Prevent hypersensitivity reaction
2. Physical dependence on narcotics. Withdrawal symptom may be precipitated
3. COPD, other respiratory dysfunction. Can be exacerbated by respiratory depression
4. MI, CAD, hypertension. Can be exacerbated by cardiac stimulatory effects
5. Renal, hepatic dysfunction. Interfere with drug metabolism and excretion
6. Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
7. Nalbuphine is specifically contraindicated to patients who are also allergic to sulfites to prevent cross-hypersensitivity reactions.

Interactions

The following are drug-drug interactions involved in the use of narcotic agonist-antagonists:

Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression, hypotension, and sedation or coma
Tripelennamine: increased hallucinogenic and euphoric effect with pentazocine (“Ts and Blues”)
Methylnaltrexone bromide (Relistor) is the treatment for opioid-induced constipation in palliative care patients who are no longer responding to traditional laxatives.

Types of drugs used as narcotic agonists antagonist

Drug	Indications	Dosage ranges
Nalbuphine	Analgesia	10 mg/70 kg SC, IM, IV q3–6h PRN
Pentazocine	Analgesia	50–100 mg PO q3–4h PRN; up to 30 mg IM, SC, IV q3–4h PRN
Pentazocine	Analgesia	1 tablet q4h

Nursing Considerations when administering narcotic agonists and narcotic agonist-antagonists

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

Assess for mentioned cautions and contraindications (e.g. drug allergy, respiratory dysfunction, myocardial infarction and CAD, hepatorenal dysfunction, ) to prevent untoward complications.
Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
Perform thorough physical (CNS, vital signs, bowel sounds, urine output) to establish baseline status before beginning therapy, determine drug effectiveness and evaluate for any potential adverse effects.
Monitor laboratory results (liver function, kidney function) to determine need for possible dose adjustment and identify toxic drug effects.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of these drugs for therapy:

Impaired gas exchange related to respiratory depression
Disturbed sensory perception related to CNS effects
Constipation related to GI effects
Risk for injury related to CNS effects

Implementation with Rationale

These are vital nursing interventions done in patients who are taking narcotic agonists and narcotic agonists-antagonists:

Perform baseline and periodic pain assessments with patient to monitor drug effectiveness and provide appropriate changes in pain management protocol as needed.
Have a narcotic antagonist and equipment for assisted ventilation readily available when administering this drug IV to provide patient support in case of severe reaction.
Monitor timing of analgesic doses. Prompt administration may provide a more acceptable level of analgesia and lead to a quicker resolution of the pain.
Provide non-pharmacological pain measures like breathing exercises, back rubs, and stress reduction to increase drug effectiveness and reduce pain.
Provide comfort measures (e.g. small, frequent meals for GI upset) to help patient tolerate drug effects.
Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
Educate client on drug therapy to promote understanding and compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

Monitor patient response to therapy (relief of pain, sedation).
Monitor for adverse effects (e.g. GI depression, respiratory depression, arrhythmias, etc).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
Monitor patient compliance to drug therapy.

Narcotic Antagonists

They bind strongly to opioid receptors without causing receptor activation. They block opioid receptor effects as well as effects of too much opioids in the system

Therapeutic Action

The desired and beneficial action of narcotic antagonists is as follows:

Narcotic antagonists are drugs that bind strongly to opioid receptors but do not activate them. They block the opioid receptors and reverse the effects of opioids like respiratory depression and sedation.

Indications

Narcotic antagonists are indicated for the following medical conditions:

Indicated for complete or partial reversal of narcotic depression; diagnosis of suspected opioid

Indication of narcotic antagonists in different age groups:

Children

Safety and effectiveness has not been established in children.
Naloxone is the antidote for narcotic overdose and reversal of narcotic effects.

Adults

They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
They should be educated about the importance of asking for pain medication before the pain becomes acute.
Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus and the baby.

Older adults

They are more susceptible to drug adverse effects because of existing medical conditions.
Safety measures should be established (side rails, call light, assistance to ambulate).

Contraindications and Cautions

The following are contraindications and cautions for the use of narcotic antagonists:

Allergy to narcotic antagonists. Prevent hypersensitivity reaction
Pregnancy, lactation. Potential adverse effects to the fetus and the baby.
Narcotic addiction. Precipitation of a withdrawal symptom
CV disease. Exacerbated by the reversal of the depressive effects of narcotics

Adverse Effects

Use of narcotic antagonists may result to these adverse effects:

CNS: excitement, reversal of analgesia
CV: tachycardia, blood pressure changes, dysrhythmias, pulmonary edema
Acute narcotic abstinence syndrome: nausea, vomiting, sweating, tachycardia, hypertension, tremulousness, feelings of anxiety. A naloxone challenge should be administered before giving naltrexone to help to avoid acute reactions.

Interactions

There is no significant drug-drug interactions involved with narcotic antagonists.

Types of drugs used as narcotic antagonists

Drug	Indications	Dosage ranges
Nalmefene	Complete or partial reversal of opioid effects	Initial dose: 0.5 mg /170 kg IV PRN, second dose of 1 mg170 kg 2-5 min later; maximum dose, 1.5 mg /170 kg
Naltrexone	Narcotic overdose. postoperative narcotic depression	0.4-2 mg IV initially with additional doses repeated at 2-3 min intervals; smaller doses used for post- operative narcotic depression
Pentazocine	Narcotic addiction. alcohol dependence	Maintenance treatment: 50 mg PO daily or 100 mg every other day, or 150 mg PO every third day; 2 mL IV, SC

Nursing Considerations

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

Assess for mentioned cautions and contraindications (e.g. drug allergy, history of narcotic addiction, myocardial infarction, ) to prevent untoward complications.
Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
Perform thorough physical (neurological status, respiratory rate and rhythm, vital signs) to establish baseline status before beginning therapy, determine drug effectiveness and evaluate for any potential adverse effects.
Obtain an electrocardiogram as appropriate to evaluate for cardiac effects.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:

Decreased cardiac output related to CV effects
Acute pain related to withdrawal and CV effects
Risk for injury related to CNS effects

Implementation with Rationale

These are vital nursing interventions done in patients who are taking narcotic antagonists:

Maintain open airway and provide artificial ventilation and cardiac massage as needed to support the patient.
Administer vasopressors as ordered and as needed to manage narcotic overdose.
Administer naloxone challenge before giving naltrexone because of the serious risk of acute withdraw.
Provide comfort measures to help patient cope with withdrawal syndrome.
Provide safety measures (e.g. adequate lighting, raised side rails, ) to prevent injuries.
Ensure that patients receiving naltrexone have been narcotic-free for 7-10 days to prevent severe withdrawal syndrome.
Educate client on drug therapy to promote understanding and compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

Monitor patient response to therapy (reversal of opioid effects, treatment of alcohol dependence).
Monitor for adverse effects (e.g. CV changes, arrhythmias, hypertension, etc).
Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
Monitor patient compliance to drug therapy.

Opioid infusion administration considerations

Unless the patient has received a recent dose of opioid, a loading dose should be administered (according to the EPIC prescription) at the commencement of the infusion to ensure therapeutic plasma levels are quickly reached.
For rapid relief of pain (or anticipated pain), the prescribed bolus dose should be reached.
The infusion rate may be adjusted by the nurse within the dose range specified, according to the patient’s level of pain.
It takes approximately four half-lives (8hrs for morphine/hydromorphone, ~1.5hrs for fentanyl) to reach steady state plasma concentration if given as an infusion, therefore if the rate is to be increased, a bolus should be given as well.
Ideally the infusion rate should not be increased unless 3 boluses are required in a 1 hour period.
The volume infused should be checked every hour and rate verified on the fluid balance flow chart.

Narcotics Read More »

Post-traumatic stress disorder (PTSD)

Post-traumatic stress disorder (PTSD) is an anxiety disorder characterized hyper-arousal, re-experiencing of images of the stressful events and avoidance of reminders.

> It is a disorder that develops after a person sees, is involved in or hears
(experiences) of an extreme traumatic stressor.
> Is a condition occurring when an individual experiences extreme rare stressful event, the person reacts with severe anxiety, feeling of numbing and avoidance of thinking about the events which is often interrupted at times by sudden vivid and distressing recall of these events.
> It is a mental health disorder associated with torture.

PTSD may be immediate response to the stressor or may follow an interval of days or occasionally months. It usually improves within months, but may persist for years.
Post Traumatic Stress Disorder was first recognized in 1980 by American Psychiatric Association (APA). Before, it was known as:-

Shell shock
Soldiers’ heart
Rape trauma syndrome
Concentration camp syndrome.

Aetiology

1. An exceptionally stressful event in which the person was involved in directly or as a witness.
Examples of stressful events.

Wars
Floods
Earthquakes
Gang rape
Terrorism
Accidents
Fire out break

2. However there is a variation in responses depending on personal vulnerability.
3. Genes was found to be part of the vulnerability by twin studies.
4. Other predisposing factors. For example:

Uncontrolled temperament.
Age: children and old people are more vulnerable.
Gender: women are more vulnerable
History of psychiatric disorders
Previous traumatic experiences including separation from the parents and child abuse.
Differences in a way threatening events are appraised and encoded in the brain.

5. Neuroendocrine factors which include: sensitization of noradrenergic system.
Sensitization of serotonergic system. Reduction in cortisol levels.
6. Psychological factors:

Fear conditioning. Classical conditioning may be involved.
Cognitive theory: PTSD arises when the normal processing of emotionally charged information is over whelmed, so that memories persist in an unprocessed form in which they can intrude into the conscious awareness.
Psychodynamic theory: emphasizes the role of the previous experience in determining the individual variations in response to severely stressful events.

7. Maintaining factors:

Negative appraisal of early symptoms
Avoidance of reminders which prevents deconditioning and cognitive reappraisal.
Suppression of anxious thoughts.

Diagnostic criteria signs/ symptoms

1. The child has been exposed to a very traumatic event outside the usual range of human experience and would be frightening to any one.

Could be the subject of trauma
Could be the perpetrator of the trauma.
Could be a mere observer.

2. Persistent re-experiencing of traumatic event.

Recurrent and intrusive recollections of the events. (In young children, repetitive play may occur in which themes or aspects of trauma are expressed).
Recurrent distressing dreams of events. (A child may have frightening dreams without recognizable content).
Acting or feeling as if the traumatic event were recurring. (Trauma specific re-enactment may occur)
Experience intense psychological distress at exposure to events that symbolize or resemble the traumatic event).

3. Persistent avoidance of stimuli associated with trauma

Efforts to avoid thought or feeling associated with trauma.
Avoiding activities or situations resembling the trauma.
In ability to recall important aspects of trauma.
Diminished interest in activities.
Feeling of detachment from others.
Restricted range of affect.
Sense of foreshortened future.

4. Persistent symptoms of increased arousal

Difficult in falling or staying asleep.
Irritability or out burst of anger.
Difficulty in concentrating.
Hyper-vigilance – not settled.
Exaggerated startle response.
Physiological reactivity upon exposure to events symbolizes or resembles the trauma.

5. Symptoms for at least one month.
If symptoms last for:-

Less than 3 months – acute PTSD
More than 3 months – chronic PTSD
Begin 6 months after the stressor- delayed PTSD.

Summary of symptoms of PTSD

The principle symptoms of post traumatic stress disorder includes;
Hyper-arousal

Persistent anxiety
Irritability
Insomnia
Poor concentration.

Intrusions

Difficulty in recalling stressful events at will.
Intense intrusive imagery (flash back).
Recurrent distressing dreams.

Avoidance

Avoidance of reminders of the vents
Detachment
Inability to feel emotion (numbness).
Diminished interest in activity.

Reactions

Night mares
Terrifying dreams
Vivid recall of the events (images)
Depression/ sadness
Irritable
Anxiety
Anti-social behaviors.

Management of PTSD

Treatment usually involves psychotherapy and counseling, medication, or a combination.

Assessment
Assess the following;

Nature and severity of the stressful event
The nature and duration of the symptoms
Previous psychiatric history
Previous personality
Neurological examination should be done to exclude a subdural haematoma or other forms of cerebral injury. If the event included injury like from assault or accident.

Treatment
1. Early treatment

If the response is not severe, sympathetic support and help with practical problems subsequent to disaster may suffice.
Counseling provides emotional support and discourages recall.
Facilitates working through the associated emotions.
Few doses of anxiolytic drugs may be needed to calm the person.
The person is helped to talk about and reconsider the event and express feelings about them. This may need to be done repeatedly.

2. Chronic PTSD is difficult to treat.

It requires series of interview where by the person is encouraged to recall, re-experience and work through the emotions associated with the event.
Cognitive therapy or techniques have been used to desensitize patients to reminders and images of the stressful events.

Options for psychotherapy will be specially tailored for managing trauma.

3. Cognitive processing therapy (CPT): Also known as cognitive restructuring, the patient is taught to think about things in a new way. Mental imagery of the traumatic event may help them work through the trauma, to gain control of the fear and distress.

4. Exposure therapy: Talking repeatedly about the event or confronting the cause of the fear in a safe and controlled environment may help the person feel they have more control over their thoughts and feelings.

5. Medications

Some medications can be used to treat the symptoms of PTSD.

Selective serotonin reuptake inhibitors (SSRIs), such as paroxetine, are commonly used. SSRIs also help treat depression, anxiety and sleep problems, symptoms that are often linked to PTSD.
benzodiazepines may be used to treat irritability, insomnia, and anxiety. However, the National Center for PTSD do not recommend these, because they do not treat the core symptoms and they can lead to dependency.
anxiolytics should be avoided unless other wise because of dependence after prolonged use. Antidepressants may be used in low doses for example fluoxetine could be given.

The patient has to be taught about the following self help techniques

Active coping is a key part of recovery. It enables a person to accept the impact of the event they have experienced, and take action to improve their situation.

learning about PTSD and understanding that an ongoing response is normal and that recovery takes time
accepting that healing does not necessarily mean forgetting, but gradually feeling less bothered by the symptoms and having confidence in the ability to cope with the bad memories

Other things that can help include:

finding someone to confide in
spending time with other people who know what happened
letting people know what might trigger symptoms
breaking down tasks into smaller parts, to make them easier to prioritize and complete
doing some physical exercise, such as swimming, walking ETC.
practicing relaxation, breathing, or meditation techniques
listening to quiet music or spending time in nature
understanding that it will take time for symptoms to go away
accepting that PTSD is not a sign of weakness but can happen to anyone
participating in enjoyable activities that can provide distraction

Post-traumatic stress disorder (PTSD) Read More »

ATYPICAL ANTIPSYCHOTIC

Atypical or second generation or novel

Atypical or ‘2nd generation’. These medications have been used since the 1990s. These are newer types of antipsychotics.

These are sometimes referred to as ‘atypicals’

These are newer antipsychotic drugs on the Ugandan market and are less commonly used because they are expensive. They are however the best antipsychotics because they control both negative and positive symptoms of schizophrenia. These drugs are also associated with fewer side effects compared to the typical antipsychotics. Are also called new antipsychotic drugs.

Some are also less likely to cause sexual side effects compared to first generation antipsychotics.

But second generation antipsychotics may be more likely to cause serious metabolic side effects. This may include rapid weight gain and changes to blood sugar levels, diabetes mellitus, hypercholesterolemia.

Mechanism of Action

They block 5-HT2A-receptors with lesser degree of antagonism of D2-receptor.
Have efficacy against negative effects especially clozapine
As a result, they have fewer extrapyramidal adverse effects than the older traditional agents.
Atypical agents are serotonin-dopamine 2 antagonists (SDAS)
They are considered atypical in the way they affect dopamine and serotonin neurotransmission in the four key dopamine path way in the brain.

Classes of Atypical Antipsychotics

Benzoxazoles- Risperidone
Dibenzodiazepines – Clozapine
Thienobenzodiazepine- Olanzapine
Dibenzothiazepine- Quetiapine
Imidazolidinone – Sertindole

Risperidone (Risperdal)

Available in regular tabs, I.M depot form and rapidly dissolving tablet.
Functions more like atypical antipsychotic at doses greater than 6 mg.
Increased extra pyramidal side effects (dose dependent)
Most likely atypical to induce hyperprolactinemia.
Weight gain and sedation (dose dependent)
Hypotension, fatigue, abdominal pain, nausea.

Olanzapine (Zyprexa)

Available in regular tabs, immediate release I.M, rapidly dissolving tab, depot form. Dose 5mg-20mg/ day-OD /nocte.

Side effects

Sedation, weight gain, hypotension, anti cholinergic effects, changes in liver function tests.

Quetiapine (Seroquel)

Available in a regular tablet form only.
Dose: 100-400mg bid or DDD

Side effects

Weight gain,
Most likely to cause orthostatic hypotension
Increase blood sugar-diabetes

Clozapine (Clozaril)

Available in one form-a regular tablet

Dose: 100-900mg bid or in DDD

Side effects

Sedation , weight gain
Hyper salivation

SIDE EFFECTS OF ANTI-PSYCHOTICS:

Extra pyramidal side effects:

Most of the anti-psychotic drugs may cause the imbalance of the neurotransmitters (excitatory and inhibitory) resulting into side effects known as extra pyramidal.

Acute dystonia– uncontrolled muscular spasm. Muscle from spasm many part of the body, for example:

Oculogyric: crisis-eyes rolling upwards.
Torticollis: head and neck twisted to the side

The patient may be unable to swallow or speak clearly. in extreme cases , the back may arch or the jaw dislocate.

Management:

Give artane tablets or anticholinergic drugs given orally, I.M or I.V depending on the severity of symptoms.
Benzodiazepines like diazepam.
Some times change in medication, or lowering dose.

Parkinsonian symptoms (pseudo-parkinsonism)

Tremor
Rigidity
Bradykinesia: decreased facial expression, flat monotone voice, slow body movements, inability to initiate movement.
Mask like face
Bradyphrenia
Slowed thinking
Salivation
Drooping posture.

Management

Reduce the antipsychotic dose.
Change to atypical drug (as antipsychotic monotherapy)
Prescribe an anticholinergic like Artane.

Akathisia (restlessness); A subjectively unpleasant state of inner restlessness where there is a strong desire or compulsion to move.

Foot stamping when seated.
Constantly crossing or uncrossing legs.
Rocking from foot to foot.
Constantly pacing up and down.

Management

Reduce or lower the antipsychotic dose.
Give benzodiazepines like diazepam
Give beta blockers like propranolol
Give an anti cholinergic like artane.

Tardive dyskinesia (abnormal movement): It is an irreversible extrapyramidal syndrome usually common in patients who have been on anti-psychotics for long. It is characterized by persistent involuntary movement of all oral facial muscles.

Rabbit syndrome: lip smacking or chewing type movement as of a rabbit.
Tongue protrusion: fly catching.
Choreiform hand movements (pill rolling or piano playing)

Severe orofacial movement can lead to difficulty, speaking, eating, or breathing. Movements are worse when under stress.

Management:

Stop anti-cholinergic if prescribed
Reduce dose of anti psychotic.
Change to a typical drug.

Neuroleptic malignant syndrome: It is rare but fatal (life threatening), occurs as a result of prolonged intake of anti psychotic drugs it is characterized by:

Severe mental, motor and autonomic disturbance.
Hyper tonicity increased muscle tone. There is an increased reflex to stimuli.
Generalized stiffness of the muscles affecting i.e. patient may find it unable to swallow.
Hyperpyrexia increased body temperature, because of that, they get profuse sweating, this leads to fast dehydration
There is increased blood pressure leading to tachycardia.

The mortality rate is 20 % as per global population. They need intensive medical and nursing.

For the above extra-pyramidal side effects, we use the following drugs to counter act them.

Benzhexol (artane)

We can use 2mg-4mg o.d /bid 4-5 days and then go back to PRN when acute. But otherwise, they are supposed to be given when necessary. It is under the group of anti-cholinergic drugs under the classification of drugs.

Benztropine mosylate (congetin)

It also falls under the group of anti-cholinergic.

Dose: 0.5-1mg to 4mg maximum o.d / PRN (orally)

Injection: 1mg-2mg to I.m-PRN.

N.B: Children below 5yrs should not be given chlorpromazine (Largactil). Use haloperidol.

Other side effects as per systems.

Gastro intestinal tract(GIT)

Dry mouth: Management: Rinsing of mouth with water (avoid candy ‘’sweetie’’ as carriers may result).
Excessive salvation (sialorrhea): management give antiparkinsonian like artane or stop drug.
Constipation: management: give high fibred diet, laxatives like bisacodyl
Sedation: management: give smaller dose in the morning some patients can only cope with single night-time dosing. Reduce dose if necessary.

Cardio vascular system:

Postural hypotension (orthostatic hypotension): Management: advise patient to take time when standing up or change posture gradually. Reduce dose or slow down rate of increase
Cardiac arrhythmias (ECG changes): Management: ECG monitoring, change drug.

Endocrine and metabolic system:

Weight gain: Management: dietary control, exercise, change drug.
Galactorrhea (increased lactation): Management: change the drug
Amenorrhea: Management: change the drug.
Decreased libido: Management: reduce dose or change drug.

Haemotological.

Bone marrow depression.
Obstructive jaundice.

Ocular

Blurred vision
Glaucoma- increased intraocular pressure
Retina pigmentation (may lead to blindness)

Genital and urinary systems.

Retention of urine-people can retain or pass urine
Polyuria- excessive passage of urine of low specific gravity.
Impotence.

Allergic.

Photo sensitivity.
Skin pigmentation.
Nasal congestion (thioridazine)

NURSE’S RESPONSIBILITY FOR A PATIENT RECEIVING ANTIPSYCHOTICS

Instruct patients the patient to take sips of water frequently to relieve dryness of mouth. Frequent mouth washes, use of chewing gum, applying glycerine on the lips are also helpful.
A higher fiber diet, increased fluid intake and laxatives if needed, help to reduce constipation.
Advise the patient to get up from the bed or chair slowly. Patient should sit on the edge of the bed for one full minute dangling his feet before standing up. Check BP before and after medication is given. This is an important measure to measure to prevent falls and other complications resulting from orthostatic hypotension.
Differentiate between akathisia and agitation and inform the physician. A change of drug may be necessary if side effects are severe. Administer antiparkinsonian drugs as prescribed
Observe the patient regularly for abnormal movements
Take all seizure precautions.
Patient should be warned about driving a car or operating machinery when first treated with antipsychotics. Giving the entire dose at bedtime usually eliminates any problem from sedation.
Advise the patient to use sunscreen measures (use of full sleeves, dark glasses etc) for photosensitive reactions.
Teach the importance of drug compliance, side-effects of drugs and reporting if too severe, and regular follow ups. Give reassurance and reduce unfounded fears and anxieties.
Seizure precautions should also be taken as clozapine reduces seizure threshold. The dose should be regulated carefully and the patient may also be put on anticonvulsants such as carbamazepine.

Typical Antipsychotics

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Classifications of Antipsychotics.

Classification of Antipsychotics

Typical Antipsychotics or first-generation (conventional)

Also called typical, conventional or traditional antipsychotic agents
Their antipsychotic effects reflect competitive blocking of D2 receptors
More likely to be associated with extra pyramidal side effects (EPS) or movement disorders, such as Parkinsonism, neck stiffness, protrusion of the tongue, upward eyeball rolling.
This is most common with the highly potent drugs.
Primarily improve positive symptoms of schizophrenia
Low potency typical antipsychotics have less affinity for the D2 receptors but tend to interact with non dopaminergic receptors resulting in more cardio toxic and anti-cholinergic adverse effects including sedation, hypotension.

These are the most commonly used drugs in Uganda because they are cheap and available. Typical antipsychotics are more effective in the treatment of positive symptoms than the negative symptoms.

Mechanism of Action

Predominantly block dopamine D2 receptors in the mesolimbic system of the brain. Also blocks:

Muscarinic acetylcholine receptors
Histamine H1 receptors
Αlpha adrenoreceptors

The binding affinity of the typical is very strongly correlated with clinical antipsychotic and extrapyramidal potency: the typical antipsychotic drugs must be given in sufficient doses to achieve 60% occupancy of striatal D2 receptors

Classes of Typical Antipsychotics

Phenothiazines.
Butyrophenones.
Thioxanthones.

Phenothiazines

Chlorpromazine (Thorazine)(Largactil)
Fluphenazine (Prolixin)
Perphenazine (Trilafon)
Prochlorperazine (Compazine)
Thioridazine (Mellaril)
Trifluoperazine (Stelazine)
Mesoridazine
Promazine
Triflupromazine (Vesprin)
Levomepromazine (Nozinan)
Promethazine (Phenergan)

Chlorpromazine (Largactil)

Chlorpromazine it is in a phenothiazine group. It has high sedating properties but with low extra pyramidal side effects. It is absorbed in the jejunum (in alimentary canal) and metabolized in the liver. Anti- depressants reduces metabolism of chlorpromazine. Chlorpromazine works as a competitor for relevant enzymes.

Indications

Schizophrenia (psychotic disorders).
Mania.
Agitation in the elders.
Alcohol related problems (where there are no antipsychotic drugs i.e. haloperidol and thioridazine).
Intractable hiccups.
Nausea and vomiting
It can also control spasms in small doses i.e. in tetanus.

Contra-indications:

Liver diseases e.g. liver cirrhosis, bone marrow depletion, in glaucoma (increased pressure in the eye.)

N.B: Chlorpromazine can induce seizures it lowers the threshold of a seizure, so a fit chart should be put to observe that.

Dosage

Orally: Depending on the severity of psychosis, dosages can range from 100mg-1500mg in daily divided doses (DDD) as per prescription.

Injectables: This may range from 25-200mg IM. This may be given start depending on the severity of the condition. Or: It may be given continuous i.e. (continuous narcosis) i.e. 8 hourly or 12hourly, until the patient calms down, then oral treatment can be continued with.

Rectal suppository : Each suppository is of 100mg, this may be OD, BD, or TDS. It may be used in children above 5 years who cannot take drugs orally.

Syrups: This is 25mg/5mls. Suspension is also 100mg/5mls

Note: haloperidol and stelazine may be preferable in epileptic patients.

Piperazine e.g. Trifluoperazine (stelazine)

It is a neuroleptic of phenothiazine group. It has high extra pyramidal side effects and less sedating effects. It also has high properties of anti-hallucigenesis.

Indications:

Schizophrenia
Mania
Organic brain syndrome
Mental retardation with psychosis
Agitation in the elderly.
Severe anxiety.

Note: It’s a good drug in schizophrenic patients with negative features such as apathy, social with draw, lack of self drive.

Dosages

Oral tablets: 5-45mg in divided doses (DDD)

Injectable: 1-3mg IM. the maximum is usually 6mg, this may be given PRN.

Piperidine e.g. Thioridazine (melleril)

It is a neuroleptics in phenothiazine group. It has moderate sedating effects and less extra pyramidal side effects, but with high anti-cholinergic effects.

Indications:

Schizophrenia.
Mania.
Agitation in the elderly (moderate side effects)

N.B: Their regular blood pressure should be monitored.

Behavioral disorders associated with psychosis
Severe anxiety (it has also anxiolytic effect)

Contra-indications

As for chlorpromazine.

Dosage:

Give 100-1000mg in divided doses (DDD) depending on the severity of the condition.
Can also be given 1mg/kg body weight in children

Butyrophenones

Haloperidol (Haldol)
Pimozide (Orap)
Melperone
Benperidol
Triperidol

Haloperidol (haldol).

Generally, it has high extra pyramidal side effects but less sedating effects,

Indications

Mania (drug of choice)
Schizophrenia
Alcohol related problems.
Organic brain syndrome of any cause
Mental retardation with psychosis and agitation.
Nausea & vomiting
Hiccup

Contra indications:

As for chlorpromazine.

Dosage: 5-30mg is divided doses; the maximum dose can be 60mg DDD.

It is in tablets form: 0.1, 0.5, 1mg, 5mg, and 10mg

Injectables: 5mg-20mg IM start or continued narcosis i.e. 2hrly, 6hrly and 8hrly.

Dosage range for children: 25-50microgram.

Trifluperidol (triperidol)

Dose: 6-8mg OD/BD or TDS

Benperidol

It is very good in patients with deviant behavior (anti-social personality disorders)

Dose: 0.25-1.5mg OD, BD or TDS.

BLACKBOX WARNING

WARNING

See full prescribing information for complete Boxed Warning.

Increased Mortality in Elderly Patients with Dementia-Related Psychosis:

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Analyses of seventeen placebo-controlled trials (modal duration of 10 weeks), largely in patients taking atypical antipsychotic drugs, revealed a risk of death in drug-treated patients of between 1.6 to 1.7 times the risk of death in placebo-treated patients. Over the course of a typical 10-week controlled trial, the rate of death in drug-treated patients was about 4.5%, compared to a rate of about 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotics drugs, treatment with conventional antipsychotic drugs may increase mortality. The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. Haloperidol is not approved for the treatment of patients with dementia-related psychosis (see WARNINGS).

Thioxanthones.

Chlorprothixene
Flupentixol (Depixol and Fluanxol)
Thiothixene (Navane)
Zuclopenthixol (Clopixol and Acuphase)

Thioxanthines are psychotropic drugs in the neuroleptics group. They were the first neuroleptics to come into use.

They are noted to have very gross side effects. With production of new neuroleptics drugs, the use of thioxanthines has reduced.

Indications:

Schizophrenia (chronic)
Mania
And other psychotic associated conditions.

Flupentixol (depixal)

Dose: 3mg-9mg. The maximum dose can be 18mg in divided doses

N.B: avoid giving neuroleptic injectables by I.V route for the fear of postural hypotension.

ANTIPSYCHOTIC DEPOT INJECTIONS (LONG ACTING)

These are antipsychotics given by injection I.M. They are oily in nature and therefore, slowly released and metabolized over a period of 2 weeks up to 4 weeks.

Indications

Chronic schizophrenia
Cases of persistent mania
Where there is total lack of oral medication compliancy in a psychotic patient.
When it can be consistently be maintained.

Give it concurrently with other oral treatment. However, it can be given alone as a maintained treatment.

Haloperidol decanoate (haldol decamate).

Dose: 50mg, 100mg-150mg (maximum) I.M. This is given monthly (4weeks).

Fluphenazine decanoate (modecate)

Initially with 12.5mg I.M stat if he is starting then 25mg-50mg for 2-4weeks

Fluspirilence (redeptin) 2mg/ml.

Give 2-4mg which is equivalent to 2mls. We can give 2mg in alternative days or weekly for one month (½) or 2months

Flupentixol decanoate (depixol)

It is very useful in patients with negative feature of schizophrenia. It has mood elevating effects.

Dose: Initially 20mg I.M, then after 10 days, increased to 40mg I.M 2-4 weekly.

Note:

Give a quarter or half stated doses in elderly.
After test dose, wait 4-10days before starting titration to maintenance therapy
Dose range is given in mg/week for convenience only avoid using shorter dose intervals than those recommended except in exceptional circumstances e.g. long interval necessitates high volume ( >3-4ml) injection.

Advice on prescribing depot injection/ medication:

Give a test dose.
Begin with the lowest therapeutic dose.
Administer at the longest possible licensed interval
Adjust doses only after an adequate period of assessment

ATYPICAL ANTIPSYCHOTIC

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Groups, Types or Classifications of Antipsychotics.

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Typical >>>

Atypical >>>

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Classifications of Antipsychotics. Read More »

Antipsychotics

Antipsychotics are a type of psychiatric medication which are available on prescription to treat psychosis.

Anti psychotic drugs are psychiatric drugs used in treatment of mental disorders that are characterized by disturbance of reality and perception, impaired cognitive functioning, and diminished mood

They are licensed to treat certain types of mental health problem whose symptoms include psychotic experiences.

Antipsychotics, also known as neuroleptics, are a class of psychotropic medication primarily used to manage psychosis, mainly schizophrenia but also in a range of other psychotic disorders such as manic states with psychotic symptoms

They are also used together with mood stabilizers in the treatment of bipolar disorder, and they are also used in management of other psychosis associated with depression and manic depressive illness and psychosis associated with Alzheimer’s disease.

Introduction to Psychosis

The term psychosis refers to a variety of mental disorders characterized by one or more of the following symptoms:

Diminished and distorted capacity to process information and draw logical conclusions
Hallucinations, usually auditory or visual, but sometimes tactile or olfactory
Delusions (false believes)
Incoherence or marked loosening of associations
Catatonic or disorganized behavior
Aggression or violence

Antipsychotic drugs lessen these symptoms regardless of the underlying cause or causes ;

Conditions characterized with psychosis include

schizophrenia,
mania,
bipolar disorder,
schizoaffective disorder,
depression,
alcohol withdraw syndrome,
and delirium.

Factors that may lead to psychosis.

Genetic factors
Alcoholism
Brain tumor
Brain injures
Central nervous system stimulants eg cocaine.

Psychosis-Producing Drugs

Levodopa
CNS stimulants like

Cocaine
Amphetamines
Khat, cathinone, methcathinone

3. Apomorphine ,Phencyclidine

Neurotransmitters

Excitatory: dopamine, adrenaline, nor adrenaline, serotonin (5-HT-5-hydroxy tryptamine)
Inhibitory: Gama Amino Butyric acid (GABA)

SCHIZOPHRENIA

Schizophrenia is a chronic mental disorder (psychotic) characterized by disordered thinking and loss of touch with reality.

In other words, it is a mental disorder characterized by;

change in personality leading to inability to relate to others ,
disturbed mood ,
impaired appreciation and interpretation of environment

The onset of symptoms usually occurs during adolescence and early adulthood.

Schizophrenia is thought to be caused by excessive release of dopamine which leads to over stimulation of the brain cells resulting into abnormal behavior.

DOPAMINE

it’s a neurotransmitter found in brain

Effects of Dopamine

Dopamine (DA) plays a critical role in initiation of movement.
Controls reinforcement and cognitive function.
Regulates prolactin release
Plays a major role in vomiting
Regulates temperature
Reduces appetite

Signs and symptoms

Symptoms of schizophrenia are classified into two namely positive symptoms (due to distorted function) and negative symptoms (due to diminished function).

Positive and negative symptoms of schizophrenia

Positive symptoms	Negative symptoms
Hallucinations( Hearing voices, seeing things)	Social withdrawal
Delusions( False belief)	Emotional withdrawal
Disorganized speech	Lack of motivation
Agitations	Poverty of speech
	Flat mood
	Poor self – care

The positive symptons are due to stimulation. If you want to reduce these effects you would use a depressant drug which would worsen the negative symptoms.
The negative symptoms are due to depression. If you want to treat them, we would use a stimulant drug which would potentiate the positive symptoms.
The clinical phenotype varies greatly, particularly with respect to the balance between negative and positive symptoms
The positive symptoms are associated with increase in Dopamine pathway activation whereas the negative symptoms are associated with a decrease in serotonin pathway activation.

Key path ways affected by dopamine in the Brain.

Meso-cortical: – projects from the brain stem to the cerebral cortex. This path way is felt to be where the negative symptoms and cognitive disorders (lack of executive function) arise. Problem here for a psychotic patient, is too little dopamine.
Meso-limbic: – projects from the dopaminergic cell bodies in the ventral tegmentum (brain stem) to the limbic system. This pathway is where the positive symptoms come from (hallucinations, delusions and thought disorders). Problem here in a psychotic patient, there is too much dopamine.
Nigro striatal: – projects from dopaminergic cell bodies in the substantia nigra to the basal ganglia. This pathway is involved in movement regulation. Remember that dopamine suppresses acetylcholine activity. Dopamine hypo activity: can cause parkinsonian movements i.e. rigidity, brady kinesia, tremors, akathisia and dystonia
Tuberoinfundibular: projects from the hypothalamus to the anterior pituitary. Remember that the dopamine release inhibits or regulates prolactin release. Blocking dopamine in this way will predispose your patient to hyper prolactinemia (gynecomastia/galactorrhea/decreased libido/ menstrual dysfunction).

General mechanisms of action antipsychotics

Blocking the action of dopamine receptors and path ways. Some scientists believe that some psychotic experiences are caused by the brain producing too much of a chemical called dopamine. Dopamine is a neurotransmitter, which passes messages around the brain. Most antipsychotic drugs are known to block some of the dopamine receptors in the brain.
This reduces the flow of these messages, which can help to reduce psychotic symptoms. By blocking these pathways antipsychotics can produce both therapeutic and adverse effects.

Blockade of dopamine and /or 5HT2 receptors in mesolimbic system.

Blockade of 5HT2 receptor (like the α2 receptors in ANS), which allows constant release of serotonin.

Many of these agents also block cholinergic, adrenergic, and histaminergic receptors. The undesirable side effects of these agents are often a result of actions at these other receptors

Absorption and Distribution

Most antipsychotics are readily but incompletely absorbed.
Significant first-pass metabolism.
Bioavailability is 25-65%.
Most are highly lipid soluble.
Most are highly protein bound (92-98%).
High volumes of distribution (>7 L/Kg).
Slow elimination.

**Duration of action longer than expected, metabolites are present and relapse occurs, weeks after discontinuation of drug.**

Metabolism

Most antipsychotics are almost completely metabolized.
Most have active metabolites, although not important in therapeutic effect, with one exception. The metabolite of thioridazine, mesoridazine, is more potent than the parent compound and accounts for most of the therapeutic effect.

Excretion

• Antipsychotics are almost completely metabolized and thus, very little is eliminated unchanged. Elimination half-life is 10-24 hrs.

Groups, Types or Classifications of Antipsychotics.

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Antipsychotics Read More »