For the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence.
Buprenorphine's analgesic effect is due to partial agonist activity at mu-opioid receptors. Buprenorphine is also a kappa-opioid receptor antagonist. The partial agonist activity means that opioid receptor antagonists (e.g., an antidote such as naloxone) only partially reverse the effects of buprenorphine. The binding to the mu and kappa receptors results in hyperpolarization and reduced neuronal excitability.
Manifestations of acute overdose include pinpoint pupils, sedation, hypotension, respiratory depression and death.
31% bioavailability (sublingual)
37 hours
Buprenorphine, in common with morphine and other phenolic opioid analgesics, is metabolized by the liver and its clearance is related to hepatic blood flow.