← Search & browse all drugs
NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Benzomorphan derivatives
pentazocine and naloxone
N02AD51
Forms & Strengths
- Tablet: pentazocine hydrochloride 50 mg equivalent to base / naloxone hydrochloride 0.5 mg
Adult Dosing
- 1 tablet orally every 3 to 4 hours as needed for pain
- Maximum daily dose: 12 tablets (600 mg pentazocine)
Pediatric Dosing
- Safety and efficacy in pediatric patients below 12 years of age have not been established
Indications
- Management of moderate to severe pain where the use of an opioid analgesic is appropriate
Mechanism of Action
- Pentazocine is a partial agonist/antagonist opioid acting mainly at mu and kappa opioid receptors in the central nervous system
- Naloxone is a potent opioid antagonist included orally to deter abuse by precipitating withdrawal in opioid-dependent individuals when injected
Contraindications
- Hypersensitivity to pentazocine, naloxone, or any component
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting or absence of resuscitative equipment
- Known or suspected gastrointestinal obstruction, including paralytic ileus
Adverse Reactions
- Dizziness, lightheadedness, sedation, euphoria, dysphoria, hallucinations
- Nausea, vomiting, constipation
- Respiratory depression
- Hypotension, tachycardia
- Sweating, flushing, pruritus
- Physical dependence and withdrawal symptoms upon abrupt cessation
Drug Interactions
- CNS depressants (alcohol, sedatives, hypnotics, tranquilizers) increase risk of respiratory depression, hypotension, and profound sedation
- Mixed agonist/antagonist opioids may precipitate withdrawal symptoms in patients physically dependent on full opioid agonists
- Monoamine oxidase inhibitors (MAOIs) may manifest unpredictable potentiation
Curated Content: Needs Vetting Before Put to Clinical Use