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普萘洛尔单次口服剂量对人体的中枢作用。

Central effects of single oral doses of propranolol in man.

作者信息

Salem S A, McDevitt D G

出版信息

Br J Clin Pharmacol. 1984 Jan;17(1):31-6. doi: 10.1111/j.1365-2125.1984.tb04995.x.

Abstract

The central effects of propranolol, a lipophilic beta-adrenoceptor antagonist, were investigated in six healthy male volunteers using two flash fusion threshold (2FFT), simple reaction time (SRT), digital copying test (DCT), symbol digit modalities test (SDMT), Gibson spiral maze test (GSMT) and mood rating scales for tension, alertness, depression, detachment and anxiety. Compared to placebo, 2FFT was prolonged by propranolol 40, 80 and 160 mg at one or more times tested but not by propranolol 320 mg: the largest effect was seen at 3 h after 40 mg, and the effects of 40, 80 and 160 mg were significantly greater than 320 mg at 2 h. SRTs were significantly prolonged by all doses of propranolol at 2 and 3 h and by 40 and 80 mg doses at 5 h. DCT was lowered by 40 and 80 mg at 2 and 3 h by 80 mg at 5 h, and by 320 mg at 2 h, but the 160 mg dose had no effect. Propranolol impaired the expected retest gain of the SDMT with all doses except 320 mg and at 2 h after 40, 80 and 160 mg, performance was actually worsened. Mood rating scales showed increased detachment with 40 mg and decreased alertness with 80 and 320 mg. The results show that propranolol has central effects in man: the effects appeared to be greater with lower doses, 40 and 80 mg, than with higher doses, 160 and 320 mg.

摘要

在六名健康男性志愿者中,使用两种闪光融合阈值(2FFT)、简单反应时间(SRT)、数字抄写测试(DCT)、符号数字模式测试(SDMT)、吉布森螺旋迷宫测试(GSMT)以及紧张、警觉、抑郁、超脱和焦虑情绪评定量表,研究了亲脂性β肾上腺素能受体拮抗剂普萘洛尔的中枢效应。与安慰剂相比,在一次或多次测试中,40、80和160 mg的普萘洛尔可延长2FFT,但320 mg的普萘洛尔则无此作用:最大效应出现在40 mg给药后3小时,40、80和160 mg在2小时时的效应显著大于320 mg。所有剂量的普萘洛尔在2小时和3小时以及40和80 mg剂量在5小时时均显著延长SRT。40和80 mg在2小时和3小时以及80 mg在5小时和320 mg在2小时时降低了DCT,但160 mg剂量无作用。除320 mg外,所有剂量的普萘洛尔均损害了SDMT预期的重测增益,在40、80和160 mg给药后2小时,实际表现变差。情绪评定量表显示,40 mg时超脱感增加,80和320 mg时警觉性降低。结果表明,普萘洛尔对人体有中枢效应:较低剂量(40和80 mg)的效应似乎大于较高剂量(160和320 mg)。

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