buprénorphine

Buprénorphine (buprenorphine) is a semi-synthetic opioid used primarily to treat opioid use disorder and, in some formulations, chronic pain. It acts as a partial agonist at the mu-opioid receptor and as an antagonist at the kappa-opioid receptor, with very high receptor affinity. This pharmacology provides relief from withdrawal and cravings with a ceiling effect on respiratory depression, reducing the risk of overdose relative to full opioid agonists.

In opioid use disorder, buprenorphine is used as a substitution therapy to stabilize patients and facilitate recovery. When combined with naloxone in sublingual products (for example, buprenorphine/naloxone), the formulation is designed to deter misuse by injection. For chronic pain, buprenorphine is provided in sublingual forms, a transdermal patch, and, in some markets, longer-acting delivery systems.

Common formulations include sublingual tablets and films, buprenorphine/naloxone combinations, a transdermal patch for pain, a monthly extended-release subcutaneous injection for opioid dependence, and, for longer-term oral or implant strategies, devices such as a six-month implant in select settings. Dosing is individualized and typically starts under medical supervision, with titration to achieve relief while minimizing withdrawal and adverse effects.

Safety considerations include the risk of dependence and withdrawal if misused, potential sedation with other central nervous system depressants, and caution in liver disease and pregnancy. Buprénorphine is a controlled medicine in many countries and is subject to regulatory guidelines and monitoring. Brand names and availability vary by region.