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β受体阻滞剂的作用持续时间及其对治疗的影响。

Beta-blocker duration of action and implications for therapy.

作者信息

Kostis J B

机构信息

Department of Medicine, University of Medicine and Dentistry, New Jersey, Robert Wood Johnson Medical School, New Brunswick 08903-0019.

出版信息

Am J Cardiol. 1990 Nov 6;66(16):60G-62G. doi: 10.1016/0002-9149(90)90399-l.

Abstract

Two studies were conducted to measure the effect of serum half-life on beta-blocker-related heart rate reduction throughout the 24-hour period. In the first study, nadolol, atenolol and pindolol were associated with significant (p less than 0.01) heart rate reduction even at 24 hours after dose. Nadolol, with a plasma half-life of 15.5 hours, had the most pronounced heart rate-lowering effect 24 hours after the daily dose compared to pindolol, which had a half-life of 5.5 hours. In a randomized, double-blind, crossover study, nadolol and atenolol had similar effects 3 to 4 hours after the daily dose. Nadolol, however, produced greater suppression of heart rate and double product (blood pressure x heart rate) than atenolol (compared to placebo) 24 hours after ingestion of the daily dose. On ambulatory electrocardiography 24 hours after medication administration, 80 to 100% of the heart rate-attenuating effect of nadolol was maintained versus only 20 to 45% of atenolol's effect. Statistically significant (p less than 0.05) reductions in heart rate were produced by nadolol, but not by atenolol, between 4 and 5 A.M., 6 and 7 A.M., 8 and 9 A.M. and 9 and 10 A.M. Furthermore, nadolol remained at 52% of peak blood level at 24 hours, whereas atenolol was at 20%. The data from these 2 studies indicate that significant differences in duration of action exist between beta blockers.

摘要

开展了两项研究,以测定血清半衰期对24小时内β受体阻滞剂相关心率降低的影响。在第一项研究中,纳多洛尔、阿替洛尔和吲哚洛尔即使在给药24小时后仍与显著(p<0.01)的心率降低相关。纳多洛尔的血浆半衰期为15.5小时,与半衰期为5.5小时的吲哚洛尔相比,其在每日给药24小时后的心率降低效果最为显著。在一项随机、双盲、交叉研究中,纳多洛尔和阿替洛尔在每日给药3至4小时后的效果相似。然而,在每日给药24小时后,纳多洛尔对心率和双乘积(血压×心率)的抑制作用比阿替洛尔(与安慰剂相比)更强。在给药24小时后的动态心电图检查中,纳多洛尔的心率衰减效果维持在80%至100%,而阿替洛尔的效果仅维持在20%至45%。在凌晨4点至5点、6点至7点、8点至9点和9点至10点期间,纳多洛尔可使心率出现具有统计学意义(p<0.05)的降低,而阿替洛尔则无此作用。此外,纳多洛尔在24小时时仍保持在峰值血药浓度的52%,而阿替洛尔则为20%。这两项研究的数据表明,β受体阻滞剂之间在作用持续时间上存在显著差异。

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