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新型催眠药Ro 41-3696与唑吡坦对健康受试者夜间给药后的比较药效学

Comparative pharmacodynamics of Ro 41-3696, a new hypnotic, and zolpidem after night-time administration to healthy subjects.

作者信息

Dingemanse J, Bury M, Bock J, Joubert P

机构信息

Department of Clinical Pharmacology, F. Hoffmann-La Roche Ltd, Basel, Switzerland.

出版信息

Psychopharmacology (Berl). 1995 Nov;122(2):169-74. doi: 10.1007/BF02246091.

Abstract

In a double-blind, six-way crossover study the effects on psychomotor performance and memory of single doses of Ro 41-3696 (1, 3, 5 and 10 mg), a novel non-benzodiazepine partial agonist at the benzodiazepine receptor, zolpidem (10 mg) and placebo were compared after night-time administration to 12 healthy young male subjects. Psychomotor performance tests (tracking and attention as part of a standardized task battery) were conducted just before and at 1.5 and 8 h after drug intake. The memory test consisted of the recall of a list of 15 words at 8 h after drug intake which had been learned at 1.5 h after intake. At 1.5 h after drug intake 10 mg zolpidem induced markedly larger psychomotor effects than any dose of Ro 41-3696. The effects of 5 and 10 mg Ro 41-3696 and zolpidem were significantly greater than those of placebo (P < 0.05). The following morning, 8 h after drug intake, the slight residual effects of 5 and 10 mg Ro 41-3696 were statistically significantly greater than placebo, whereas zolpidem effects did not differ from placebo. The results of the memory test showed that learning as well as recall were most clearly impaired by zolpidem. An influence of Ro 41-3696 on these variables was not observed for doses up to 5 mg. In conclusion, Ro 41-3696 at all doses tested induced less effects on psychomotor performance and memory than 10 mg zolpidem at 1.5 h after intake. However, the effects of Ro 41-3696 appeared to be of longer duration.

摘要

在一项双盲、六路交叉研究中,对12名健康年轻男性受试者在夜间给予单剂量的Ro 41-3696(1、3、5和10毫克)、新型苯二氮䓬受体非苯二氮䓬类部分激动剂唑吡坦(10毫克)和安慰剂后,比较了它们对精神运动表现和记忆的影响。在服药前以及服药后1.5小时和8小时进行精神运动表现测试(作为标准化任务组的一部分进行追踪和注意力测试)。记忆测试包括在服药后8小时回忆服药后1.5小时学习的15个单词列表。服药后1.5小时,10毫克唑吡坦引起的精神运动效应明显大于任何剂量的Ro 41-3696。5毫克和10毫克Ro 41-3696以及唑吡坦的效应明显大于安慰剂(P<0.05)。服药后第二天早上8小时,5毫克和10毫克Ro 41-3696的轻微残留效应在统计学上明显大于安慰剂,而唑吡坦的效应与安慰剂无差异。记忆测试结果表明,唑吡坦对学习和回忆的损害最为明显。对于高达5毫克的剂量,未观察到Ro 41-3696对这些变量的影响。总之,在所有测试剂量下,Ro 41-3696在服药后1.5小时对精神运动表现和记忆的影响均小于10毫克唑吡坦。然而,Ro 41-3696的效应似乎持续时间更长。

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