Buprenorphine for Pain and Opioid Dependence

Abstract

Naturally occurring opiates are derived from the poppy. They include morphine, codeine, and thebaine. Buprenorphine is a synthetic thebaine derivative. It is highly potent whose primary acfion is partial antagonism at the mu receptor and full antagonism at the kappa receptor. Buprenorphine has an extremely high affinity for the mu receptor; much higher than other opioids to include antagonists such as naloxone. Based on this high affinity, buprenorphine slowly dissociates from the receptor with somewhat milder withdrawal symptoms upon discontinuation in patients who are physically dependent on full agonists such as morphine, heroin, oxycodone, etc. (PsycINFO Database Record (c) 2015 APA, all rights reserved). (chapter)