The clinical pharmacology of buprenorphine: extrapolating from the laboratory to the clinic

Drug Alcohol Depend. 2003 May 21;70(2 Suppl):S13-27. doi: 10.1016/s0376-8716(03)00056-5.


This paper will review clinical pharmacology studies on buprenorphine, a mixed opioid agonist-antagonist currently approved as a treatment for opioid dependence. The focus is on studies characterizing buprenorphine's pharmacodynamic actions, including its safety, abuse liability, withdrawal suppression and withdrawal precipitation capacity, physical dependence potential, cross-tolerance and duration of action as well as a review of the pharmacological profile of buprenorphine/naloxone combinations. The findings from these clinical pharmacology studies are synthesized and presented in a framework designed to (1) inform clinicians about the advantages and disadvantages of buprenorphine as an opioid maintenance agent, and (2) provide information about dosing procedures that may optimize the use of buprenorphine in the clinic.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Buprenorphine / pharmacology*
  • Buprenorphine / therapeutic use
  • Clinical Trials as Topic / methods
  • Clinical Trials as Topic / trends
  • Humans
  • Narcotic Antagonists / pharmacology*
  • Narcotic Antagonists / therapeutic use
  • Opioid-Related Disorders / drug therapy
  • Opioid-Related Disorders / metabolism
  • Pharmacology, Clinical / methods*
  • Pharmacology, Clinical / trends


  • Narcotic Antagonists
  • Buprenorphine