Buprenorphine

Buprenorphine (Temgesic) is a mixed agonist-antagonist and a derivative of the naturally occurring opioid thebaine. Buprenorphine is highly lipophilic and is 25 to 50 times more potent than morphine as an analgesic. The sedation and respiratory depression it causes are more intense and longer lasting than those produced by morphine. Its respiratory depressant effects are not readily reversed by naloxone. It binds to the ^-receptor with high affinity and only slowly dissociates from the receptor, which may explain the lack of naloxone reversal of respiratory depression.

Buprenorphine has more agonist than antagonist effects and is often considered a partial agonist rather than a mixed agonist-antagonist, although it precipitates withdrawal in opioid-dependent patients. Its pharmacological effects are similar to those produced by both morphine and pentazocine. Indications for its use are similar to those of pentazocine, that is, for moderate to severe pain. Sublingual preparations are available, but have a slow onset and erratic absorption.

The abuse potential of buprenorphine is low. While high doses of the drug are perceived by addicts as being morphinelike, it does reduce the craving for morphine and for the stimulant cocaine. Thus, buprenorphine is a potential new therapy for the treatment of addiction to both classes of drugs.

Drug interactions and contraindications are similar to those described for pentazocine and morphine.

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