NIDA research monograph
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NIDA research monograph · Jan 1992
ReviewAssessment of buprenorphine in a drug discrimination procedure in humans.
These studies indicate that buprenorphine shares stimulus effects with other opioid drugs and that in overall profile of effects buprenorphine is more similar to hydromorphone than are the other opioid mixed agonist-antagonists tested-pentazocine, butorphanol, and nalbuphine. This characterization is supported by the behavioral drug discrimination results and by the subjective effect self-report results. In the drug discrimination assessments buprenorphine showed a pattern of generalization that was different from that of the other opioid-mixed agonist-antagonists. ⋯ There were dose-related increases on various scales reflecting positive subjective effects, with little evidence of the dysphoric effects that are characteristic of high doses of the other mixed agonist-antagonists. These data are compatible with the view that buprenorphine is a partial agonist at the mu-receptor. Although they do not demonstrate the ceiling on magnitude of pharmacological effects that would be characteristic of a partial agonist, they do demonstrate that buprenorphine's profile of activity--both stimulus effects and subjective effects--is similar to that of the pure mu-agonist hydromorphone.