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部分激动剂活性对慢性稳定性心绞痛患者β受体阻滞剂副作用的影响。

Effect of partial agonist activity on the side effects of beta-blockade in patients with chronic stable angina.

作者信息

Chambers J, Ong M L, Akhras F, Adam G, Jackson G

机构信息

Cardiac Department, Lewisham Hospital, London, United Kingdom.

出版信息

Drugs. 1989;38 Suppl 2:39-44. doi: 10.2165/00003495-198900382-00009.

Abstract

Some side effects of the beta 1-adrenoceptor blocker atenolol may result from depression of cardiac output at rest. They may, therefore, be reduced by the use of drugs with beta 1-partial agonist activity, such as epanolol. We compared once-daily atenolol 100mg and epanolol 200mg in 20 patients reporting side effects while taking atenolol for chronic stable angina. A double-dummy, double-blind, crossover design was used to assess side effects by use of visual analogue scales and interviews, and antianginal efficacy by treadmill exercise tests and diary cards. In a comparison with atenolol, no significant differences in exercise time (686 +/- 11 seconds vs 685 +/- 10 seconds, maximum ST depression (1.02 +/- 0.09mm vs 1.07 +/- 0.08mm), time to 1mm ST depression (8.4 +/- 1.9 minutes vs 9.0 +/- 2.0 minutes), or days without angina (median 100% in both) were shown. All visual analogue scores were higher with epanolol (subjective energy 58.3 +/- 1.7 vs 54.3 +/- 1.5, well-being 61.8 +/- 1.8 vs 58.6 +/- 1.5 and warmth of extremities 68.4 +/- 3.6 vs 62.0 +/- 3.1). Although these differences did not attain statistical significance, 11 patients expressed a preference for epanolol and only 6 for atenolol. We conclude that, in this study, epanolol is as effective as atenolol as an antianginal agent for chronic stable angina. It improved the side effect profile in some but not all patients.

摘要

β1肾上腺素能受体阻滞剂阿替洛尔的某些副作用可能源于静息心输出量降低。因此,使用具有β1部分激动剂活性的药物(如依泮洛尔)可能会减少这些副作用。我们在20例因慢性稳定型心绞痛服用阿替洛尔而出现副作用的患者中,比较了每日一次服用100mg阿替洛尔和200mg依泮洛尔的效果。采用双模拟、双盲、交叉设计,通过视觉模拟量表和访谈评估副作用,并通过平板运动试验和日记卡评估抗心绞痛疗效。与阿替洛尔相比,运动时间(686±11秒对685±10秒)、最大ST段压低(1.02±0.09mm对1.07±0.08mm)、ST段压低至1mm的时间(8.4±1.9分钟对9.0±2.0分钟)或无心绞痛天数(两者中位数均为100%)均无显著差异。依泮洛尔的所有视觉模拟评分均较高(主观能量58.3±1.7对54.3±1.5,幸福感61.8±1.8对58.6±1.5,四肢温暖度68.4±3.6对62.0±3.1)。尽管这些差异未达到统计学显著性,但11例患者表示更喜欢依泮洛尔,只有6例更喜欢阿替洛尔。我们得出结论,在本研究中,依泮洛尔作为慢性稳定型心绞痛的抗心绞痛药物与阿替洛尔一样有效。它改善了部分但并非所有患者的副作用情况。

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