buprenorphinenaloxone

Buprenorphine-naloxone is a fixed-dose combination medication used to treat opioid use disorder. It combines buprenorphine, a partial mu-opioid receptor agonist with a ceiling effect on respiratory depression, with naloxone, an opioid antagonist intended to deter misuse. When taken sublingually as directed, naloxone has poor oral bioavailability, so the therapeutic effect mainly comes from buprenorphine. If the product is dissolved and injected, naloxone can precipitate withdrawal, reducing the appeal of injection.

Medical use is for induction and maintenance in adults with opioid dependence, aiming to reduce withdrawal symptoms, cravings, and illicit opioid use and overdose risk. It is not generally used for pain relief as a primary indication, though buprenorphine alone is used for analgesia in some settings; formulations with naloxone are designed for opioid dependence treatment and not routine pain management.

Formulations commonly include buprenorphine/naloxone tablets or sublingual films in ratios such as 4/1 mg or 8/2 mg. They are administered sublingually under supervision or by the patient as prescribed. Dosing is individualized and may require clinical induction. Prescribing requirements vary by country and may include additional training or waivers in some jurisdictions.

Safety considerations include common adverse effects such as nausea, constipation, headache, and sedation, with a risk of respiratory depression, especially when combined with other central nervous system depressants. The naloxone component helps deter injection but may precipitate withdrawal if misused by injection. Cautions include hepatic impairment and pregnancy; caution is advised when used with benzodiazepines or alcohol. Overdose management requires supportive care and, if needed, naloxone rescue.

Regulatory status varies by country. In many places, buprenorphine/naloxone is a controlled medication with specific prescribing requirements; in the United States, it is approved for opioid use disorder and may require physician certification.