Trade Names:Buprenex- Injection 0.324 mg (equiv. to 0.3 mg buprenorphine)/mL
Trade Names:Subutex- Tablets, sublingual 2 mg (as base)- Tablets, sublingual 8 mg (as base)
Analgesic effect caused by binding to opiate receptors in the CNS. Antagonist effects decrease abuse potential.
C max is approximately 5.47 ng/mL (16 mg SL dose). AUC is approximately 32.63 h•ng/mL (16 mg SL dose).
Approximately 96% protein bound.
Undergoes CYP3A4-mediated N-dealkylation to norbuprenorphine (active) and glucuronidation.
30% is excreted in the urine and 69% in the feces. The t ½ is 37 h.
15 min (IM).
1 h (IM).
At least 6 h (IM).
Treatment of opioid dependence.Injection
Relief of moderate to severe pain.
SL (Use limited to health care providers who meet certain qualifications and have notified the Health and Human Services of their intent to prescribe.) 12 to 16 mg/day.InjectionAdults and children (13 yr of age and older)
IM/IV 0.3 mg deep IM or slow IV (over at least 2 min) at up to 6 h intervals, as needed. May repeat once (up to 0.3 mg) 30 to 60 min after initial dosage, if required.
Store tablets at controlled room temperature (59° to 86°F). Store injection at controlled room temperature (59° to 86°F). Avoid freezing or exposure to excessive heat (over 104°F). Protect from prolonged exposure to light.
May have additive effects with buprenorphine, increasing the respiratory and CNS effects.Benzodiazepines (eg, diazepam)
Coma and death have been associated with misuse of buprenorphine and benzodiazepines.CNS depressants (eg, alcohol, phenothiazines, sedative-hypnotics)
Increased CNS depression may occur.CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin)
May reduce buprenorphine plasma levels, decreasing the efficacy.CYP3A4 inhibitors (eg, erythromycin, ketoconazole, ritonavir)
May elevate buprenorphine plasma levels, increasing the risk of side effects.
None well documented.
Hypotension; hypertension; tachycardia; bradycardia.
Sedation; dizziness/vertigo; headache; confusion; dreaming; psychosis; euphoria; weakness/fatigue; malaise; hallucinations; depersonalization; coma; tremor; dysphoria; agitation; convulsions; lack of muscle coordination; insomnia.
Sweating; pruritus; injections site reaction; rash; pallor; urticaria.
Nausea; vomiting; constipation; dry mouth; dyspepsia; flatulence; loss of appetite; diarrhea; abdominal pain.
Hepatitis and hepatitis with jaundice.
Chronic and acute hypersensitivity; infection.
Ensure that liver enzymes and hepatic function are evaluated prior to starting therapy and periodically during treatment. Document type of opioid dependence (eg, long-, short-acting), time since last opioid use, and degree of opioid dependence prior to starting SL tablets. Monitor patient for respiratory depression. If noted, re-establish adequate ventilation with mechanical assistance and notify health care provider immediately. Naloxone may not be effective in reversing respiratory depression caused by this drug. Monitor patient for narcotic withdrawal symptoms, CNS, GI, and general body side effects. Report to health care provider if noted and significant.
Category C .
Excreted in breast milk.
Safety and efficacy not established in children under 13 yr of age.
Use with caution in elderly or debilitated patients; use with caution in patients with impaired hepatic, renal or pulmonary function, myxedema or hypothyroidism, adrenal cortical insufficiency (eg, Addison disease), CNS depression or coma, toxic psychoses, prostatic hypertrophy or urethral stricture, acute alcoholism, delirium tremens or kyphoscoliosis, biliary tract dysfunction.
May obscure diagnosis or clinical course of patients with acute abdominal conditions.
Buprenorphine has abuse potential. Psychological and physical dependence as well as tolerance may occur.
Use with caution; drug can increase CSF pressure.
Use in physically dependent individuals may result in withdrawal effects.
Respiratory depression, pinpoint pupils, sedation, hypotension, death.
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