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部分GABAA激动剂帕戈克隆滥用潜力的评估。

Evaluation of the abuse potential of pagoclone, a partial GABAA agonist.

作者信息

de Wit Harriet, Vicini Lisa, Haig George M, Hunt Thomas, Feltner Douglas

机构信息

Department of Psychiatry, The University of Chicago, Chicago, IL 60637, USA.

出版信息

J Clin Psychopharmacol. 2006 Jun;26(3):268-73. doi: 10.1097/01.jcp.0000218983.61683.96.

DOI:10.1097/01.jcp.0000218983.61683.96
PMID:16702891
Abstract

This study assessed the abuse potential of pagoclone, a partial agonist at the gamma-aminobutyric acid type A (GABAA) benzodiazepine receptor site, in healthy recreational drug users. Twenty-three young adults, who reported past recreational use of sedative drugs or alcohol, participated in 4 sessions during which capsules containing pagoclone (doses: 1.2 mg, the higher end of the proposed therapeutic dose range, and 4.8 mg, a 4-fold higher dose), diazepam (dose, 30 mg), or placebo were randomly administered under double-blind conditions. Subjective ratings of mood, drug effects, and psychomotor tests were completed at regular intervals after ingesting the capsules. On most of the standardized measures of abuse potential, pagoclone (dose, 4.8 mg) was rated as being similar to diazepam. Both drugs increased the ratings of good effects and drug liking. However, pagoclone also produced some adverse mood effects that might limit its potential to be used recreationally, and it produced fewer sedativelike effects on some measures. In general, the results with these doses indicate that the abuse potential of pagoclone is similar to that of diazepam, although its profile as a partial agonist suggests that differences between the drugs may emerge at higher doses.

摘要

本研究评估了阿戈克隆(一种γ-氨基丁酸A型(GABAA)苯二氮䓬受体位点的部分激动剂)在健康的消遣性药物使用者中的滥用可能性。23名报告过去有过镇静药物或酒精消遣性使用史的年轻人参加了4次试验,试验期间在双盲条件下随机给予含有阿戈克隆(剂量:1.2毫克,建议治疗剂量范围的上限,以及4.8毫克,4倍高剂量)、地西泮(剂量30毫克)或安慰剂的胶囊。在服用胶囊后的定期时间点完成情绪、药物效应的主观评分以及精神运动测试。在大多数滥用可能性的标准化测量中,阿戈克隆(剂量4.8毫克)的评分与地西泮相似。两种药物都提高了良好效应和对药物喜爱程度的评分。然而,阿戈克隆也产生了一些不良情绪效应,这可能会限制其消遣性使用的可能性,并且在某些测量中其产生的类镇静效应较少。总体而言,这些剂量的结果表明,阿戈克隆的滥用可能性与地西泮相似,尽管其作为部分激动剂的特性表明在更高剂量下药物之间可能会出现差异。

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