Pentazocine

Indications
 Oral
Moderate to severe pain
Adult: 50-100 mg every 3-4 hrs; max 600 mg daily.
Child: 6-12 yr: As hydrochloride: 25 mg every 3-4 hr.
CrCl (ml/min)Dosage Recommendation
10-5075% normal dose.
<1050% normal dose.
Hepatic impairment: Reduce dose or avoid in liver disease.
Parenteral
Moderate to severe pain
Adult: 30-60 mg SC, IM or IV Inj given every 3-4 hr.
Child: >1 yr: up to 1 mg/kg SC, IM; up to 500 mcg/kg IV every 3-4 hr.
CrCl (ml/min)Dosage Recommendation
10-5075% normal dose.
<10 50% normal dose.
Hepatic impairment: Reduce dose or avoid in liver disease.
Rectal
Moderate to severe pain
Adult: 50 mg supp up to 4 times daily.
Child: Not recommended.
CrCl (ml/min)Dosage Recommendation
10-5075% normal dose
< 1050% normal dose
Hepatic impairment: Reduce dose or avoid in liver disease.

Incompatibility: At Y site: Nafcillin; when admixed: aminophylline, amobarbital, pentobarbital, phenobarbital, sodium bicarbonate; in syringe: glycopyrrolate, heparin, phenobarbital.
Contraindications
 Head injury; narcotic dependence; respiratory depression; raised intracranial pressure; MI; heart failure; arterial or pulmonary hypertension; porphyria; pregnancy (prolonged use or high doses at term).
Warnings / Precautions
 May precipitate withdrawal in narcotic addicts. Impaired respiratory, renal and hepatic function; morbidly obese patients; thyroid dysfunction; prostatic hyperplasia or urinary stricture; biliary tract impairment; adrenal insufficiency (including Addison's disease); abdominal conditions. Elderly or debilitated patients; seizure-prone patients; children and infants (safety and efficacy not established in <1 yr); lactation. May impair ability to drive or operate machinery. Administer IM rather than SC (when frequent inj are needed) and inj sites should be varied.
Adverse Reactions
 Physical dependence; sedation, dizziness, euphoria, lightheadedness, alterations of mood; respiratory depression; visual hallucinations, disorientation, confusion; hypertension, tachycardia, circulatory depression; shock; hypotension; nausea, vomiting, constipation; seizures, diaphoresis; rash; blood dyscrasias; local tissue damages (SC), muscle fibrosis (IM).
Potentially Fatal: Respiratory depression, hypotension, circulatory failure, deepening coma, convulsions.
Overdose Reactions
 Symptoms: respiratory depression, cardiovascular, CNS effects. Treatment: empty stomach by lavage or emesis (lavage in comatose patients or those without gag reflex must have an endotracheal tube). For respiratory depression: parenteral naloxone and supportive treatment such as oxygen, IV fluids and vasopressors.
Drug Interactions
 Depressant affects potentiated by alcohol, CNS depressants; concurrent use with fluoxetine may lead to diaphoresis, ataxia flushing and tremor associated with serotonin syndrome.
See Below for More pentazocine Drug Interactions
Mechanism of Actions
 Pentazocine is a benzomorphan derivative with mixed opioid agonist and antagonist actions. It alters perception of and response to pain and produces generalised CNS depression by binding to opiate receptors in the CNS and acting as a partial agonist/antagonist.
Onset: Oral, IM, SC: 15-30 minutes; IV 2-3 minutes.
Duration: Oral: 4-5 hr; parenteral: 2-3 hr.
Absorption: Absorbed from the GI tract (oral), through the muscles (IM); peak plasma concentrations after 1-3 hr (oral), 15 min-1 hr (IM). Oral bioavailability: approx 20% (60-70% in cirrhosis).
Distribution: Crosses the placenta. Protein-binding: 60%
Metabolism: Hepatic; via oxidative and glucuronide conjugation pathways; extensive 1st pass.
Excretion: Elimination half life: 2-3 hr; prolonged in hepatic impairment; excretion via urine (small amounts as unchanged drug).
ATC Classification
 N02AD01 - pentazocine ; Belongs to the class of benzomorphan derivative opioids. Used to relieve pain.
Available As
  • Pentazocine 15 mg
  • Pentazocine 25 mg
  • Pentazocine 30 mg

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