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抗焦虑药阿贝卡尼的精神运动效应:与劳拉西泮的比较。

Psychomotor effects of the anxiolytic abecarnil: a comparison with lorazepam.

作者信息

Hege S G, Ellinwood E H, Wilson W H, Helligers C A, Graham S M

机构信息

Duke University Medical Center, Durham, NC 27710, USA.

出版信息

Psychopharmacology (Berl). 1997 May;131(2):101-7. doi: 10.1007/s002130050271.

Abstract

Abecarnil is a metabolically stable beta-carboline that binds with high affinity and selectivity to central benzodiazepine receptors. The effects on cognitive and psychomotor skills of abecarnil (ZK 112-119), 2.5 mg and 5.0 mg, were compared with lorazepam 2.0 mg and placebo. Twenty-four healthy, young males participated in a double-blind, four-way Latin square design and performed batteries of behavioral tests at predrug and at 20, 40, 60, 80, 100, 120, 180, 240, 360 and 480 min after drug administration. Abecarnil 5.0 mg and lorazepam 2.0 mg displayed similar impairment profiles in tests of cognitive functions including memory encoding. Abecarnil 2.5 mg was substantially less impairing than lorazepam. Impairment levels of the abecarnil and lorazepam treatments peaked at 2-3 h after oral administration. The two abecarnil doses showed dose-dependent effects on the cognitive and psychomotor tasks. All three drug treatments were well tolerated by the subjects, with no one terminating early due to adverse events. The incidence of reported adverse events for abecarnil was dose-dependent. The most frequent, statistically significant adverse effects were drowsiness, lack of concentration and visual disturbance for abecarnil 5.0 mg; and lack of concentration and dizziness for lorazepam 2.0 mg. There were no significant differences in adverse incidence rates between abecarnil 2.5 mg and placebo.

摘要

阿贝卡尼是一种代谢稳定的β-咔啉,它能以高亲和力和选择性与中枢苯二氮䓬受体结合。将2.5毫克和5.0毫克的阿贝卡尼(ZK 112 - 119)对认知和精神运动技能的影响与2.0毫克的劳拉西泮及安慰剂进行了比较。24名健康的年轻男性参与了一项双盲、四向拉丁方设计,并在给药前以及给药后20、40、60、80、100、120、180、240、360和480分钟进行了一系列行为测试。5.0毫克的阿贝卡尼和2.0毫克的劳拉西泮在包括记忆编码在内的认知功能测试中表现出相似的损害特征。2.5毫克的阿贝卡尼造成的损害明显小于劳拉西泮。阿贝卡尼和劳拉西泮治疗的损害水平在口服给药后2 - 3小时达到峰值。阿贝卡尼的两种剂量对认知和精神运动任务显示出剂量依赖性效应。所有三种药物治疗受试者耐受性良好,没有人因不良事件提前终止试验。阿贝卡尼报告的不良事件发生率呈剂量依赖性。5.0毫克阿贝卡尼最常见且具有统计学意义的不良反应是嗜睡、注意力不集中和视觉障碍;2.0毫克劳拉西泮的不良反应是注意力不集中和头晕。2.5毫克阿贝卡尼与安慰剂之间的不良事件发生率无显著差异。

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