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β1 选择性激动活性是否会干扰β1 选择性阻断剂的降压疗效?

Does beta 1-selective agonistic activity interfere with the antihypertensive efficacy of beta 1-selective blocking agents?

作者信息

Leonetti G, Sampieri L, Cuspidi C, Terzoli L, Rupoli L, Fruscio M, Gradnik R, Zanchetti A

机构信息

Istituto di Clinica Medica Generale e Terapia Medica di Milano, Ospedale Maggiore, Italy.

出版信息

J Hypertens Suppl. 1985 Dec;3(3):S243-5.

PMID:2908819
Abstract

In order to investigate whether addition of beta 1-selective agonism can interfere with the antihypertensive efficacy of beta 1-selective adrenoceptor blockers, two separate studies were carried out to evaluate the effects on blood pressure and heart rate of three beta 1-selective blockers with or without varying degree of beta 1-selective agonism. In hypertensive patients at rest, the greatest blood pressure reduction and bradycardia were found with atenolol, a beta 1-selective blocker without any agonistic activity; a consistently smaller effect on blood pressure and heart rate was observed with Visacor (ICI 141 292), a beta 1-selective blocker with moderate beta 1-selective agonism, whereas no clinically relevant decrease in blood pressure occurred with Corwin (ICI 118 587), the beta 1-selective blocker with high beta 1-selective agonism. In contrast, during exercise-induced sympathetic activation, all three compounds reduced systolic blood pressure and heart rate to a similar degree.

摘要

为了研究添加β1选择性激动作用是否会干扰β1选择性肾上腺素能受体阻滞剂的降压疗效,开展了两项独立研究,以评估三种具有或不具有不同程度β1选择性激动作用的β1选择性阻滞剂对血压和心率的影响。在静息的高血压患者中,发现无任何激动活性的β1选择性阻滞剂阿替洛尔可使血压降幅最大且引起心动过缓;中度β1选择性激动作用的β1选择性阻滞剂Visacor(ICI 141 292)对血压和心率的作用始终较小,而具有高β1选择性激动作用的β1选择性阻滞剂Corwin(ICI 118 587)未引起具有临床意义的血压下降。相反,在运动诱发的交感神经激活期间,所有三种化合物均可使收缩压和心率降低至相似程度。

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