Generic
Pentazocine Hydrochloride
2 brands available in the market
At a glance
Pentazocine Hydrochloride is an opioid analgesic used for the relief of moderate to severe pain. It may also be used for preoperative or preanesthetic medication and as a supplement to surgical anesthesia.
Description
Pentazocine is an opioid (narcotic) analgesic that works in the brain and nervous system to decrease pain. It produces analgesia by an agonistic effect at the kappa receptor and weakly antagonizes effects of opiates at the μ-receptor.
Indications
- Moderate to severe pain
- Preoperative or preanesthetic medication
- Supplement to surgical anesthesia
- Labor pain
Therapeutic class
Opioid analgesics
Pharmacological class
Opioid Agonist-Antagonist
Pharmacology
Pentazocine is a benzomorphan derivative with mixed opioid agonist and antagonist actions. It alters perception of and response to pain and produces generalized CNS depression by binding to opiate receptors in the CNS and acting as a partial agonist/antagonist.
Mechanism of action
Acts as an agonist at kappa receptors and a weak antagonist at mu receptors to relieve pain.
Dosage
Adult Dose:
- Oral (Moderate to severe pain): 50-100 mg every 3-4 hours; max 600 mg/day
- IV/IM/SC (Anesthesia & pain): 30 mg every 3-4 hours; max 360 mg/day; doses >30 mg IV or 60 mg IM/SC not recommended
- Labor pain: 30 mg IM once OR 20 mg IV, 2-3 times at 2-3 hour intervals
- Renal impairment: CrCl 10-50: 75% normal dose; CrCl <10: 50% normal dose
- Hepatic impairment: Reduce dose or avoid in liver disease
Pediatric Dose (>1 year):
- Oral (6-12 years): 25 mg every 3-4 hours
- IM: 0.5 mg/kg
Administration
- Administered by doctor or nurse; do not self-administer
- Oral: Swallow tablet whole; do not chew, crush or break
- Follow the prescribed dose and duration
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Nausea
- Dizziness or light-headedness
- Vomiting
- Euphoria
- Headache
- Drowsiness
- Fatigue
- Constipation
- Dry mouth
- Increased sweating
Precautions & warnings
- May impair driving ability; do not drive if drowsy or dizzy
- Avoid alcohol (may cause excessive sleepiness)
- Caution and low dosage in respiratory depression
- Caution in renal or hepatic impairment
- Caution in patients prone to seizures (seizures may occur)
- Withdrawal symptoms may occur in opioid-dependent patients
Contraindications
- Hypersensitivity to pentazocine
- Head injury
- Narcotic dependence
- Respiratory depression
- Raised intracranial pressure
- Myocardial infarction
- Heart failure
- Arterial or pulmonary hypertension
- Porphyria
- Pregnancy (prolonged use or high doses at term)
Drug interactions
- Alcohol, CNS depressants: Depressant effects potentiated
- Fluoxetine: Diaphoresis, ataxia, flushing, and tremor (serotonin syndrome)
Food interactions
Alcohol consumption with Pentazocine Hydrochloride is unsafe.
Use in pregnancy
Use in Pregnancy: May be unsafe during pregnancy; animal studies have shown harmful effects. Pregnancy Category C.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk. No data on excretion into human milk.
Pediatric use
Safety not established in children under 1 year.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; CrCl 10-50: 75% normal dose; CrCl <10: 50% normal dose.
Hepatic Impairment: Caution in liver disease; reduce dose or avoid; consult your doctor.
Overdose effects
Clinical experience with overdosage is insufficient. Treatment: Oxygen, IV fluids, vasopressors, supportive measures; for respiratory depression, parenteral naloxone is a specific and effective antagonist.
Storage conditions
Keep away from light and store below 25°C; do not freeze; keep out of reach of children.
Chemical structure
Pentazocine Hydrochloride