Narcotics

Narcotics

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:

  1. 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.
  2. 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

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

Types of opioid receptors

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

Types of narcotic drugs

Narcotics are divided into 3 classes;

  1. 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.
  2. 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.
  3. 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:

  1. Relief of moderate to severe acute pain or chronic pain
  2. Preoperative medication
  3. Component of combination therapy for severe chronic pain
  4. 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

  1. They should be informed and reassured that associated abuse with the use of narcotics in acute pain is remote.
  2. They should be educated about the importance of asking for pain medication before the pain becomes acute.
  3. Caution is advised for pregnant and lactating women because of potential adverse effects to the fetus.
  4. Narcotics used in labor include morphine, meperidine, and oxymorphone.
  5. 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

  1. They are more susceptible to drug adverse effects because of existing medical conditions.
  2. 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:

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

Adverse Effects

Use of narcotic agonists may result to these adverse effects:

  1. CNS: light-headedness, dizziness, psychoses, anxiety, fear, hallucinations, pupil constriction, impaired mental processes
  2. GI: nausea, vomiting, constipation, biliary spasm
  3. GU: ureteral spasm, urinary retention, hesitancy, loss of libido
  4. Others: sweating, physical and psychological dependence
  5. 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:

  1. Barbiturates, phenothiazines, MAOIs: increased likelihood of respiratory depression, hypotension, and sedation or coma
  2. 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
  3. 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

  1. Methadone
  2. Oxymorphone
  3. Propoxyphene
  4. 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

  1. Post-operative pain
  2. Myocardial infarction
  3. Premedication before surgery
  4. Severe pain
  5. Sickle cell crisis
  6. Acute pulmonary oedema
  7. Chronic pain (cancer)

Common Side effects

The common side effects of morphine include:

  1.  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.
  2.  Nausea and vomiting — if this occurs, give anti-emetics e.g. plasil 10mg 8 hourly.
  3.  Drowsiness — may occur in the first few days of taking morphine. If it does not improve after three days reduce the dose of morphine.
  4.  Itching — not very common but if it occurs reduce the dose of morphine

Contraindication

  1. 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.
  2. 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

  1.  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.

  2.  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.

  3.  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

  4.  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.

  5.  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.

  6.  If the pain stimulus is removed, then the dose of morphine should be decreased gradually to minimize the effects of physical dependence.

  7.  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:

  1. Relief of moderate to severe pain; pre-anesthetic medication and a supplement to surgical anesthesia
  2.  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:

  1. Barbiturates, phenothiazines,    MAOIs:    increased    likelihood    of    respiratory depression, hypotension, and sedation or coma
  2. Tripelennamine: increased hallucinogenic and euphoric effect with pentazocine (“Ts and Blues”)
  3. 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:

  1. Assess for mentioned cautions and contraindications (e.g. drug allergy, respiratory dysfunction, myocardial infarction and CAD, hepatorenal dysfunction, ) to prevent untoward complications.
  2. Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
  3. 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.
  4. 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:

  1. Impaired gas exchange related to respiratory depression
  2. Disturbed sensory perception related to CNS effects
  3. Constipation related to GI effects
  4. 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:

  1.  Perform baseline and periodic pain assessments with patient to monitor drug effectiveness and provide appropriate changes in pain management protocol as needed.
  2.  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.
  3.  Monitor timing of analgesic doses. Prompt administration may provide a more acceptable level of analgesia and lead to a quicker resolution of the pain.
  4.  Provide non-pharmacological pain measures like breathing exercises, back rubs, and stress reduction to increase drug effectiveness and reduce pain.
  5.  Provide comfort measures (e.g. small, frequent meals for GI upset) to help patient tolerate drug effects.
  6.  Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
  7.  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:

  1. Monitor patient response to therapy (relief of pain, sedation).
  2. Monitor for adverse effects (e.g. GI depression, respiratory depression, arrhythmias, etc).
  3. Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
  4. 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:

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

Indication of narcotic antagonists in different age groups:

Children

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

Adults

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

Older adults

  1. They are more susceptible to drug adverse effects because of existing medical conditions.
  2. 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:

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

Adverse Effects

Use of narcotic antagonists may result to these adverse effects:

  1. CNS: excitement, reversal of analgesia
  2. CV: tachycardia, blood pressure changes, dysrhythmias, pulmonary edema
  3. 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:

  1. Assess for mentioned cautions and contraindications (e.g. drug allergy, history of narcotic addiction, myocardial infarction, ) to prevent untoward complications.
  2. Conduct pain assessment with patient to establish baseline and evaluate effectiveness of drug therapy.
  3. 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.
  4. 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:

  1. Decreased cardiac output related to CV effects
  2. Acute pain related to withdrawal and CV effects
  3. Risk for injury related to CNS effects

Implementation with Rationale

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

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

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

Opioid infusion administration considerations

  1. 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.
  2. For rapid relief of pain (or anticipated pain), the prescribed bolus dose should be reached.
  3. The infusion rate may be adjusted by the nurse within the dose range specified, according to the patient’s level of pain.
  4. 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.
  5. Ideally the infusion rate should not be increased unless 3 boluses are required in a 1 hour period.
  6. The volume infused should be checked every hour and rate verified on the fluid balance flow chart.
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1 thought on “Narcotics”

  1. Kamba Derick

    I appreciate for the good work presented here…
    But me I would wish that if possible please make this work to be downloadable

    Reply

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