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.
Labeled use. Treatment of opioid dependence within a plan that includes counseling and psychosocial support.
Sources: [1]
Buprenorphine-naloxone is a first-line, office-based option for opioid use disorder, alongside methadone (dispensed through opioid treatment programs) and extended-release naltrexone. Its partial agonism gives a ceiling on respiratory depression when used alone, and the naloxone component discourages injection. Methadone may suit patients who need a full agonist or a more structured program, while naltrexone requires the patient to be opioid-free first. Buprenorphine-only products are used for induction from methadone or long-acting opioids and in moderate to severe hepatic impairment.
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.
The label does not describe a narrow therapeutic index or direct dosing by measured blood levels of the drug.
Sources: [1]
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%).
Sources: [1]
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.
Limited human data do not show an increased risk of major malformations from buprenorphine, and data on sublingual naloxone are too limited to judge. Prolonged use in pregnancy can cause neonatal opioid withdrawal syndrome, which is expected and treatable but can be life-threatening if missed, so observe newborns. Untreated opioid addiction is linked to low birth weight, preterm birth, and fetal death, and higher doses may be needed during pregnancy.
Buprenorphine and norbuprenorphine pass into breast milk at low levels, with infants exposed to less than 1% of the maternal daily dose, and no adverse reactions in breastfed infants have been shown. Oral absorption of naloxone is limited. Watch the infant for increased drowsiness and breathing difficulty.
Sources: [1]
Safety and effectiveness have not been established in children. It is not appropriate for neonatal abstinence syndrome because the naloxone is an opioid antagonist. Accidental exposure can cause severe, possibly fatal, respiratory depression in children.
Studies did not include enough patients 65 and older to show whether they respond differently. Because of possible reduced hepatic, renal, or cardiac function and other illnesses or drugs, prescribe cautiously and monitor for sedation, respiratory depression, toxicity, or overdose.