Abuse liability studies of opioid agonist-antagonists in humans

Drug Alcohol Depend. 1991 Jun;28(1):49-82. doi: 10.1016/0376-8716(91)90053-2.

Abstract

Prediction of the abuse liability of a drug before it reaches the market is complicated by the fact that there are many factors that influence the actual abuse of a drug. Laboratory methods used in humans to assess the abuse liability of the opioids are reviewed and illustrative studies of morphine and the agonist-antagonist opioids, pentazocine, butorphanol, nalbuphine and buprenorphine, are presented. Three assessment methods, subjective effect measurement, self-administration and drug discrimination, provide information relevant to measuring reinforcing efficacy, a major determinant of the degree to which a drug is sought and self-administered by abusers. Physical dependence capacity, which can contribute to sustained drug use, is evaluated in direct addiction and substitution/suppression studies. Withdrawal precipitation studies measure antagonist activity which might limit abuse. The results of testing the agonist-antagonist opioids are generally consistent across these various methods and consistent with historical experience with these drugs, suggesting that these methods are useful in predicting abuse liability of novel opioids.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Arousal / drug effects
  • Humans
  • Illicit Drugs* / adverse effects
  • Narcotic Antagonists* / adverse effects
  • Narcotics* / adverse effects
  • Self Administration / psychology
  • Substance Withdrawal Syndrome / etiology
  • Substance Withdrawal Syndrome / psychology
  • Substance-Related Disorders / etiology*
  • Substance-Related Disorders / psychology

Substances

  • Illicit Drugs
  • Narcotic Antagonists
  • Narcotics