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对三种具有不同程度内在激动活性的β1-肾上腺素能受体阻断药物(美托洛尔、普拉洛尔和H 87/07)在心绞痛患者中的比较研究。

A comparative study of three beta 1-adrenoreceptor blocking drugs with different degree of intrinsic stimulating activity (metoprolol, practolol and H 87/07) in patients with angina pectoris.

作者信息

Keyriläinen O, Uusitalo A

出版信息

Ann Clin Res. 1978 Aug;10(4):185-90.

PMID:30388
Abstract

Three beta1-selective beta-blocker (metoprolol, practolol and H 87/07) were compared in 29 patients with stable angina pectoris. The main pharmacological difference between the three beta-blockers was their intrinsic stimulating activity (I.S.A.), metoprolol being devoid of I.S.A., practolol having moderate I.S.A. and H 87/07 having high I.S.A. Each drug was given in randomized order and the length of each cross-over period was 2 weeks. Daily activity was measured by an automatic step-counter, and subjective symptoms and nitroglycerin consumption were registered on a diary-card. Objective data, such as ECG changes and exercise capacity, were obtained by bicycle ergometer tests performed at the end of each period. At rest, the heart rate was significantly lower on metoprolol than on practolol or H 87/07. During exercise, the heart rate was significantly higher on H 87/07 than on practolol or metoprolol. No other haemodynamic differences were found between the three beta-blockers. No differences were found between the three test periods with regard to daily activity, expressed as the number of steps walked, while on the beta-blocker with high I.S.A., H 87/07, the attack rate and nitroglycerin consumption were significantly higher than when the patients were on metoprolol and practolol. No difference was found between the three beta-blockers with regard to total work or exercise time until 1 mm of S-T segment depression. Except for one patient who experienced a severe exanthema on practolol, the three beta-blockers were equally well tolerated.

摘要

对29例稳定型心绞痛患者比较了三种β1选择性β受体阻滞剂(美托洛尔、心得宁和H 87/07)。这三种β受体阻滞剂之间主要的药理学差异在于它们的内在激动活性(I.S.A.),美托洛尔无内在激动活性,心得宁有中度内在激动活性,H 87/07有高度内在激动活性。每种药物均按随机顺序给药,每个交叉期时长为2周。通过自动步数计数器测量日常活动量,并在日记卡上记录主观症状和硝酸甘油消耗量。客观数据,如心电图变化和运动能力,通过在每个阶段结束时进行的自行车测力计测试获得。静息时,服用美托洛尔时的心率显著低于服用心得宁或H 87/07时。运动期间,服用H 87/07时的心率显著高于服用心得宁或美托洛尔时。三种β受体阻滞剂之间未发现其他血流动力学差异。就日常活动量(以行走步数表示)而言,三个测试阶段之间未发现差异,而服用具有高度内在激动活性的β受体阻滞剂H 87/07时,发作率和硝酸甘油消耗量显著高于患者服用美托洛尔和心得宁时。在出现1毫米ST段压低之前,三种β受体阻滞剂在总功或运动时间方面未发现差异。除了一名患者在服用心得宁时出现严重皮疹外,三种β受体阻滞剂的耐受性相当。

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