Therapeutic Uses

Buprenorphine (buprenex; subutex) is used as an analgesic and as a maintenance drug for opioid-dependent subjects. The usual intramuscular or intravenous dose for analgesia is 0.3 mg given every 6 hours. Sublingual doses of 0.4-0.8 mg also produce effective analgesia. Buprenorphine is metabolized to norbuprenorphine by CYP3A4. Thus, care should be taken in treating patients who also are taking known inhibitors of CYP3A4 (e.g., azole antifungals, macrolide antibiotics, and HIV protease inhibitors) or drugs that induce CYP3A4 activity (e.g., anticonvulsants and rifampin).

Buprenorphine is approved by the FDA for the treatment of opioid addiction. Treatment is initiated with buprenorphine alone administered sublingually, followed by maintenance therapy with a combination of buprenorphine and naloxone (suboxone) to minimize abuse potential. The partial agonist properties of buprenorphine limit its usefulness for the treatment of addicts who require high maintenance doses of opioids. However, conversion to maintenance treatment with higher doses of methadone, a full agonist, is possible.

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