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阿片类激动剂-拮抗剂在人体中的滥用可能性研究。

Abuse liability studies of opioid agonist-antagonists in humans.

作者信息

Preston K L, Jasinski D R

机构信息

Department of Psychiatry, Francis Scott Key Medical Center, Johns Hopkins University School of Medicine, Baltimore, Maryland 21224.

出版信息

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

DOI:10.1016/0376-8716(91)90053-2
PMID:1884671
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.

摘要

在药物进入市场之前预测其滥用可能性很复杂,因为有许多因素会影响药物的实际滥用情况。本文回顾了用于评估阿片类药物滥用可能性的人体实验室方法,并介绍了吗啡以及激动剂 - 拮抗剂阿片类药物喷他佐辛、布托啡诺、纳布啡和丁丙诺啡的说明性研究。三种评估方法,即主观效应测量、自我给药和药物辨别,提供了与测量强化效力相关的信息,强化效力是决定滥用者寻求和自我给药药物程度的主要因素。在直接成瘾和替代/抑制研究中评估了可能导致持续药物使用的身体依赖能力。撤药激发研究测量可能限制滥用的拮抗剂活性。对激动剂 - 拮抗剂阿片类药物进行测试的结果在这些不同方法中总体上是一致的,并且与这些药物的历史经验一致,这表明这些方法在预测新型阿片类药物的滥用可能性方面是有用的。

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