Department of Behavioral Science, College of Medicine, University of Kentucky, Lexington, KY 40536-0086, USA.
J Psychopharmacol. 2011 Nov;25(11):1469-79. doi: 10.1177/0269881110385597. Epub 2010 Oct 15.
Aripiprazole is a dopamine D(2) receptor partial agonist undergoing evaluation as a pharmacotherapy for stimulant-use disorders. Acutely administered aripiprazole attenuates the discriminative stimulus and other behavioral effects of d-amphetamine in humans; however, whether aripiprazole attenuates the effects of more commonly abused stimulants is unknown. The aim of this experiment was to assess the discriminative stimulus, subject-rated and cardiovascular effects of oral cocaine alone and following acute administration of aripiprazole in humans. Eight cocaine-dependent subjects learned to discriminate 150 mg cocaine from placebo. After acquiring the discrimination, the effects of cocaine (0, 25, 50, 100 and 200 mg) administered alone and in combination with aripiprazole (15 mg) were determined. Significant effects of cocaine were observed for the drug discrimination task, stimulant-like subject-rated effects and heart rate. Limited effects of aripiprazole were revealed. However, for most measures, fewer doses of cocaine were significantly greater than placebo when combined with aripiprazole, suggesting a reduction in the discriminative stimulus, self-reported and cardiovascular effects of cocaine. These data are consistent with previous studies that have tested acutely administered aripiprazole in combination with d-amphetamine and suggest that the ability of aripiprazole to modify stimulant effects is a function of the duration of treatment (acute vs. chronic).
阿立哌唑是一种多巴胺 D2 受体部分激动剂,正在评估作为治疗兴奋剂使用障碍的药物疗法。急性给予阿立哌唑可减弱人类中 d-苯丙胺的辨别刺激和其他行为效应;然而,阿立哌唑是否减弱更常见的滥用兴奋剂的效应尚不清楚。本实验的目的是评估单独口服可卡因和急性给予阿立哌唑后可卡因在人类中的辨别刺激、主观评分和心血管效应。8 名可卡因依赖者学会辨别 150 毫克可卡因与安慰剂。获得辨别力后,确定了单独给予可卡因(0、25、50、100 和 200 毫克)和与阿立哌唑(15 毫克)联合给予可卡因的效应。可卡因对药物辨别任务、兴奋剂样主观评分效应和心率有显著影响。阿立哌唑的影响有限。然而,对于大多数测量指标,当与阿立哌唑联合使用时,较少剂量的可卡因明显大于安慰剂,表明可卡因的辨别刺激、自我报告和心血管效应降低。这些数据与先前测试急性给予阿立哌唑与 d-苯丙胺联合使用的研究一致,并表明阿立哌唑改变兴奋剂效应的能力是治疗持续时间(急性与慢性)的函数。