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心脏选择性和内在拟交感活性在β受体阻滞剂治疗心血管疾病中的作用。

Role of cardioselectivity and intrinsic sympathomimetic activity in beta-blocking drugs in cardiovascular disease.

作者信息

Taylor S H

出版信息

Am J Cardiol. 1987 May 15;59(13):18F-20F. doi: 10.1016/0002-9149(87)90036-1.

DOI:10.1016/0002-9149(87)90036-1
PMID:2883872
Abstract

The significance of ancillary properties of beta blockers continues to be the focus of considerable clinical investigation. Beta 1-selective blocking agents, such as acebutolol, inhibit cardiac beta 1 receptors, but have less influence on bronchial and vascular beta 2 receptors. Certain beta 1-selective blocking drugs, including acebutolol, have intrinsic sympathomimetic activity (ISA), also termed partial agonist activity. This property produces slight cardiac stimulation, which can be blocked by propranolol. Drugs with mild or moderate ISA have proven to be as clinically effective as beta blockers lacking this property. Additionally, drugs with ISA possess potential therapeutic benefits, particularly for patients with coronary artery disease. The hemodynamic influences of cardioselectivity and ISA on left ventricular function, heart rate, cardiac output, left-sided heart filling pressure and myocardial oxygen consumption in patients with coronary artery disease are now clearly defined.

摘要

β受体阻滞剂辅助特性的重要性仍是大量临床研究的重点。β1选择性阻断剂,如醋丁洛尔,可抑制心脏β1受体,但对支气管和血管β2受体的影响较小。某些β1选择性阻断药物,包括醋丁洛尔,具有内在拟交感活性(ISA),也称为部分激动剂活性。该特性会产生轻微的心脏刺激,可被普萘洛尔阻断。已证实具有轻度或中度ISA的药物在临床上与缺乏该特性的β受体阻滞剂一样有效。此外,具有ISA的药物具有潜在的治疗益处,尤其是对于冠心病患者。目前已明确心脏选择性和ISA对冠心病患者左心室功能、心率、心输出量、左心充盈压和心肌氧耗的血流动力学影响。

相似文献

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Role of cardioselectivity and intrinsic sympathomimetic activity in beta-blocking drugs in cardiovascular disease.心脏选择性和内在拟交感活性在β受体阻滞剂治疗心血管疾病中的作用。
Am J Cardiol. 1987 May 15;59(13):18F-20F. doi: 10.1016/0002-9149(87)90036-1.
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Central hemodynamics of beta-adrenoceptor blocking drugs: beta 1 selectivity versus intrinsic sympathomimetic activity.β-肾上腺素能受体阻断药的中心血流动力学:β1选择性与内在拟交感活性
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Role of cardioselectivity and intrinsic sympathomimetic activity in beta-blocking drugs in chronic coronary artery disease.心脏选择性和内在拟交感活性在β受体阻滞剂治疗慢性冠状动脉疾病中的作用。
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Pharmacologic aspects of intrinsic sympathomimetic activity in beta-blocking drugs.β受体阻滞剂内在拟交感活性的药理学方面。
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The additional properties of beta adrenoceptor blocking drugs.β肾上腺素能受体阻断药的其他特性。
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Intravenous beta-blockade in coronary heart disease: is cardioselectivity or intrinsic sympathomimetic activity hemodynamically useful?冠心病中的静脉β受体阻滞剂:心脏选择性或内在拟交感活性在血流动力学上是否有用?
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Haemodynamic consequences of intrinsic sympathomimetic activity and cardioselectivity in beta-blocker therapy for hypertension.β受体阻滞剂治疗高血压时内在拟交感活性和心脏选择性的血流动力学后果。
Eur Heart J. 1983 Jul;4 Suppl D:31-41. doi: 10.1093/eurheartj/4.suppl_d.31.

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