Known brand names include Suboxone.
A film that dissolves under the tongue or inside the cheek, combining buprenorphine, a partial opioid agonist, with naloxone, an opioid blocker. It treats opioid dependence as part of a full treatment plan with counseling and support, and it is a Schedule III controlled substance.
High-alert medication. Opioids are on the ISMP acute care high-alert list, which names IV, oral, and transdermal forms. Sublingual and buccal film is not named separately and is treated here as an oral-cavity form within the opioid class.
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The label does not describe a narrow therapeutic index or direct dosing by measured blood levels of the drug.
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Naloxone, nalmefene, or another opioid overdose reversal agent can treat buprenorphine overdose, but higher than usual and repeated doses may be needed because buprenorphine binds the mu receptor tightly and acts for a long time. The first priority is restoring ventilation with an open airway and assisted breathing, plus oxygen, IV fluids, and vasopressors as needed. Monitor long enough to cover buprenorphine's long duration of action.
Doses come from the FDA label. Study tool, not for clinical decisions.
No dose adjustment is described. Buprenorphine pharmacokinetics did not differ between dialysis-dependent and healthy subjects in a small study, and the effect of renal failure on naloxone is unknown. Reduced renal function in older adults is one reason to prescribe cautiously and watch for toxicity.
Mild impairment: no adjustment. Moderate impairment: not recommended for induction because of precipitated withdrawal risk; may be used with caution for maintenance after starting on a buprenorphine-only product, watching for naloxone reducing buprenorphine's effect. Severe impairment: avoid, because naloxone exposure rises far more than buprenorphine's (naloxone AUC up about 1302%).
Buprenorphine is a mu-opioid partial agonist and kappa-opioid antagonist whose agonist effects reach a ceiling; in non-dependent opioid-experienced subjects, effects peaked between 8 mg/2 mg and 16 mg/4 mg. Naloxone is a potent mu antagonist with no clinically significant effect by the sublingual route, but given parenterally it precipitates withdrawal in people dependent on full agonists, which deters injection misuse. Buprenorphine is metabolized mainly by CYP3A4 to norbuprenorphine and by glucuronidation, with a mean half-life of 24 to 42 hours; naloxone's half-life is 2 to 12 hours.