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美托洛尔渗透泵片与普萘洛尔在健康志愿者单次及连续3天给药后的中枢神经系统相关表现及血流动力学

CNS-related performance and haemodynamics of metoprolol-Oros and propranolol after single and 3 days dosing in healthy volunteers.

作者信息

van Steveninck A L, Pieters M S, Schoemaker H C, Breimer D D, Cohen A F

机构信息

Centre for Human Drug Research, University Hospital, Leiden, The Netherlands.

出版信息

Br J Clin Pharmacol. 1993 Feb;35(2):114-20. doi: 10.1111/j.1365-2125.1993.tb05676.x.

Abstract
  1. The effects of metoprolol-Oros 14/190 once daily, propranolol 80 mg twice daily and temazepam 10 mg once daily on central nervous system (CNS) related performance and haemodynamic variables were evaluated in a double-blind, randomized, placebo controlled, crossover study in 12 healthy volunteers. Drugs were administered for 3 consecutive days except for temazepam, which was administered on days 1 and 3 only. Treatment effects were evaluated at 0, 2, 5 and 8 h on days 1 and 3. 2. Neither beta-adrenoceptor blocker had significant effects in a battery of tests after single or 3 days dosing. Temazepam caused a decrease in saccadic peak velocity of 37.4 degrees s-1 (95% CI: 6.0, 68.9) at 2 h and an increase of auditory reaction times of 11.5 ms (0.2, 22.8) at 8 h on day 1. No significant effects of temazepam were detected on day 3. 3. Both beta-adrenoceptor blockers reduced exercise heart rate. Peak effects were measured at 2 h 40 min after propranolol but not metoprolol-Oros (difference, day 1:20 (11, 29) beats min-1, day 3:13 (8, 19) beats min-1). Both beta-adrenoceptor blockers significantly reduced baseline exercise heart rate on day 3. Compared with day 1, metoprolol-Oros caused larger reductions of exercise heart rate at all times on day 3. 4. Metoprolol-Oros and propranolol caused similar reductions of systolic- and diastolic blood pressure on days 1 and 3. Temazepam caused a small reduction in diastolic blood pressure at 5 h 40 min on day 1 but was otherwise devoid of haemodynamic effects.(ABSTRACT TRUNCATED AT 250 WORDS)
摘要
  1. 在一项针对12名健康志愿者的双盲、随机、安慰剂对照、交叉研究中,评估了美托洛尔控释片(每日一次,14/190规格)、普萘洛尔(每日两次,80毫克)和替马西泮(每日一次,10毫克)对中枢神经系统(CNS)相关表现及血流动力学变量的影响。除替马西泮仅在第1天和第3天给药外,其他药物均连续给药3天。在第1天和第3天的0、2、5和8小时评估治疗效果。2. 两种β-肾上腺素能受体阻滞剂在单次给药或给药3天后的一系列测试中均无显著效果。替马西泮在第1天2小时时使扫视峰值速度降低37.4度/秒(95%置信区间:6.0,68.9),在8小时时使听觉反应时间增加11.5毫秒(0.2,22.8)。在第3天未检测到替马西泮有显著效果。3. 两种β-肾上腺素能受体阻滞剂均降低运动心率。普萘洛尔给药后2小时40分钟测量到峰值效应,但美托洛尔控释片未出现(差异,第1天:20(11,29)次/分钟,第3天:13(8,19)次/分钟)。两种β-肾上腺素能受体阻滞剂在第3天均显著降低基线运动心率。与第1天相比,美托洛尔控释片在第3天的所有时间点均使运动心率降低幅度更大。4. 美托洛尔控释片和普萘洛尔在第1天和第3天对收缩压和舒张压的降低作用相似。替马西泮在第1天5小时40分钟时使舒张压略有降低,但在其他方面无血流动力学效应。(摘要截取自250字)

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