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Information about Buprenorphine

Buprenorphine is an orally available, semisynthetic opioid analgesic, which is used as an analgesic and for management of opioid dependence.

Liver safety of Buprenorphine

Therapy with buprenorphine has not been associated with serum enzyme elevations, and clinically apparent liver injury has been reported largely with overdose and abuse (intravenous administration of the sublingual formulation).

Mechanism of action of Buprenorphine

Buprenorphine (bue" pre nor' feen) is a semisynthetic opioid that is 25 to 50 times more potent than morphine and has been used as an analgesic as well as therapy of opioid addiction. Buprenorphine is a partial µ-opioid receptor agonist and a κ-receptor antagonist accounting for its benefit for opioid deterrence. Buprenorphine competes with morphine and heroin for the µ receptor, but is only a partial agonist and has a ceiling effect.

FDA approval information for Buprenorphine

Buprenorphine was approved for treatment of opioid addiction in 2004 and is a schedule III controlled substance.

Clinical use of Buprenorphine

Current indications include treatment of moderate to severe pain (in low doses ~200 µg) and opiate addiction (in higher doses 2 to 16 mg daily).

Dosage and administration for Buprenorphine

Buprenorphine is available as 2 and 8 mg tablets for sublingual administration under the brand name Subutex, and in 1 mL ampules of 0.3 mg/mL for intravenous (iv) or intramuscular (im) injection under the brand name Buprenex. For opioid addiction, the usually recommended dose is 12 to 16 mg in a single daily dose. Buprenorphine is also available in fixed combination with naloxone for sublingual administration generically and under the brand name Suboxone. Naloxone is not absorbed orally, but provides full opioid antagonism if the combination is administer intravenously, as might occur with intentional abuse. Finally, parenteral forms of buprenorphine are used for moderate to severe pain and administered iv or im, the typical dose being 0.3 mg every 6 hours as needed.

Side effects of Buprenorphine

Common side effects of buprenorphine include headache, dizziness, fatigue, sedation, dry mouth, urinary retention, diaphoresis and withdrawal symptoms.

Substance abuse treatment agents

Cost and Coupons - Buprenorphine

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