Trade Names:Suboxone- Tablets, sublingual 2 mg buprenorphine base per 0.5 mg naloxone- Tablets, sublingual 8 mg buprenorphine base per 2 mg naloxone
Analgesic effect caused by binding to opiate receptors in the CNS, while antagonist effects decrease abuse potential.Naloxone
Possibly antagonizes opioid effects by competing for the same receptor sites.
Treatment of opioid dependence.
SL Single daily dose in the range of 12 to 16 mg of buprenorphine. The dose should be adjusted in increments or decrements of 2 or 4 mg to a level that holds the patient in treatment and suppresses opioid withdrawal effects. This is likely to range between 4 and 24 mg/day.
Store tablets at controlled room temperature (59° to 86°F).
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.
Headache; insomnia; anxiety; depression; dizziness; nervousness; somnolence.
Rhinitis; pharyngitis; runny eyes.
Abdominal pain; constipation; diarrhea; nausea; vomiting; dyspepsia.
Pain; back pain; withdrawal symptoms; abscess; asthenia; chills; fever; flu syndrome; infection; accidental injury.
Document type of opioid dependence (eg, long-, short-acting), time since last opioid use, and degree of opioid dependence prior to starting therapy.
Ensure that liver enzymes and hepatic function are evaluated prior to starting therapy and periodically during treatment.
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 .
Buprenorphine is excreted in breast milk.
Safety and efficacy not established in children below the age of 16 yr of age.
Use with caution in elderly or debilitated patients; use with caution in patients with impaired hepatic, renal, or pulmonary function (eg, chronic obstructive pulmonary disease), 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, or biliary tract dysfunction.
Buprenorphine has abuse potential. Psychological and physical dependence as well as tolerance may occur.
Use with caution; drug can increase CSF pressure.
Marked and intense withdrawal symptoms are likely to occur if misused parenterally by individuals dependent on opioid agonists; sublingual use may cause opioid withdrawal symptoms if administered before the agonist effects of the opioid have subsided.
Pinpoint pupils, sedation, hypotension, respiratory depression, death.
Copyright © 2009 Wolters Kluwer Health.