Morton S, Lader M
Department of Psychiatry, University of London, England.
Pharmacopsychiatry. 1990 May;23 Suppl 3:120-3. doi: 10.1055/s-2007-1014547.
Alpidem, an imidazo-pyridine compound, has been evaluated as an anxiolytic in comparison with placebo and lorazepam. In the first of our normal volunteer studies, we compared single doses of alpidem, 25, 50 and 100 mg with lorazepam 2 mg and placebo on a range of cognitive, psychomotor and EEG variables. Lorazepam and the highest (100 mg) dose of alpidem impaired performance on a range of psychomotor tasks, the effects of the benzodiazepine being more severe and more prolonged. No impairment of performance was observed with the 25 and 50 mg doses. In the second study, the focus was on memory functions. Lorazepam, 2 mg, caused anterograde amnesia which was most apparent 1 h post-drug but persisted until 4 h: sedation was marked. By contrast, single doses (25, 50 mg) of alpidem had little effect on either memory or alertness. The third study compared the effects of alpidem (25, 50 mg) and lorazepam (1 mg) with placebo, each given twice-daily for 8 days to normal volunteers. On the final day, a test dose of ethanol was given. Lorazepam impaired many tests of cognitive and psychomotor function, and this impairment was enhanced by ethanol. By contrast, alpidem produced less impairment with less interaction with alcohol. In a fourth, clinical, study, 24 patients with a DSM III primary diagnosis of generalised anxiety disorder were treated, under double blind conditions, with doses adjusted according to clinical need of either alpidem 25-150 mg daily or lorazepam 1-6 mg daily.(ABSTRACT TRUNCATED AT 250 WORDS)
阿吡坦是一种咪唑并吡啶化合物,已与安慰剂和劳拉西泮进行了抗焦虑效果评估。在我们的第一项正常志愿者研究中,我们将25毫克、50毫克和100毫克的阿吡坦单剂量与2毫克劳拉西泮和安慰剂在一系列认知、精神运动和脑电图变量上进行了比较。劳拉西泮和最高剂量(100毫克)的阿吡坦在一系列精神运动任务上损害了表现,苯二氮䓬类药物的影响更严重且持续时间更长。25毫克和50毫克剂量未观察到表现受损。在第二项研究中,重点是记忆功能。2毫克劳拉西泮导致顺行性遗忘,用药后1小时最明显,但持续到4小时:镇静作用明显。相比之下,阿吡坦单剂量(25毫克、50毫克)对记忆或警觉性影响很小。第三项研究将阿吡坦(25毫克、50毫克)和劳拉西泮(1毫克)与安慰剂的效果进行了比较,每种药物每天给正常志愿者服用两次,共8天。在最后一天,给予一次乙醇测试剂量。劳拉西泮损害了许多认知和精神运动功能测试,乙醇增强了这种损害。相比之下,阿吡坦产生的损害较小,与酒精的相互作用也较小。在第四项临床研究中,对24名DSM-III原发性广泛性焦虑症患者进行了双盲治疗,根据临床需要调整剂量,每天服用25 - 150毫克阿吡坦或1 - 6毫克劳拉西泮。(摘要截断于250字)