The Benefits of Buprenorphine

572 WordsFeb 20, 20182 Pages
Buprenorphine is morphine-like but is 25 to 50 times more potent [15,16]. It is noteworthy that buprenorphine has very low oral bioavailability because it undergoes extensive first-pass metabolism. However, its bioavailability is substantial enough that sublingual (SL) administration makes this a feasible treatment for opioid dependence. The mean time to peak plasma concentration following SL administration varies and can range from 40 minutes to 3.5 hours. Buprenorphine is highly protein bound (96%) and has a large volume of distribution. It is metabolized extensively to norbuprenorphine by N-dealkylation, primarily through cytochrome P450 (CYP) 3A4. The half-life of buprenorphine is long, and there is considerable variation in reported values of terminal elimination, with mean values ranging from 3 to 44 hours. Most of a dose of buprenorphine is eliminated in the feces, with approximately 10–30% excreted in urine. Buprenorphine has an extremely high affinity and slow dissociation from opioid receptors, providing simultaneous opioid blockade and agonist effects. The duration of action of buprenorphine is longer than these pharmacokinetic parameters, resulting in suppression of opioid withdrawal symptoms for 2 to 3 days after cessation of use. Naloxone is added to buprenorphine for the treatment of opiate dependence and to prevent intravenous diversion [11]. However, the efficacy of buprenorphine is not affected by the combination because the half-life for buprenorphine is
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