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索他洛尔抗心律失常作用的电生理基础及其与其他药物的比较。

Electrophysiologic basis for the antiarrhythmic actions of sotalol and comparison with other agents.

作者信息

Singh B N

机构信息

Department of Cardiology, Wadsworth Veterans Administration Hospital, Los Angeles, California 90073.

出版信息

Am J Cardiol. 1993 Aug 12;72(4):8A-18A. doi: 10.1016/0002-9149(93)90020-d.

DOI:10.1016/0002-9149(93)90020-d
PMID:8346731
Abstract

Although synthesized as a nonselective beta-adrenergic blocking compound, sotalol has emerged as the prototype of the so-called class III antiarrhythmic compounds. It delays cardiac repolarization by inhibiting the delayed rectifier potassium current, having a lesser effect on the inward rectifying potassium current with little or no effect on the inward calcium or sodium currents. This property of prolonging repolarization with an accompanying increase in the effective refractory period is not due to blockade of the beta-adrenergic receptors. The major electrophysiologic profile of sotalol constitutes the summed effects of beta blockade and prolonged repolarization. Sotalol exerts a potent antifibrillatory action modulated by its antiadrenergic effects. It suppresses premature ventricular contractions and nonsustained ventricular tachycardia while preventing inducible ventricular tachycardia and fibrillation in patients with advanced structural heart disease. The compound is therefore likely to exert a broad spectrum of antiarrhythmic actions in ventricular arrhythmias.

摘要

虽然索他洛尔最初是作为一种非选择性β肾上腺素能阻滞剂合成的,但它已成为所谓Ⅲ类抗心律失常化合物的原型。它通过抑制延迟整流钾电流来延迟心脏复极化,对内向整流钾电流的影响较小,对内向钙电流或钠电流几乎没有影响。这种延长复极化并伴随有效不应期增加的特性并非由于β肾上腺素能受体的阻断。索他洛尔的主要电生理特征是β受体阻断和复极化延长的综合作用。索他洛尔通过其抗肾上腺素能作用发挥强大的抗纤颤作用。它可抑制室性早搏和非持续性室性心动过速,同时预防晚期结构性心脏病患者的诱发性室性心动过速和纤颤。因此,该化合物可能对室性心律失常发挥广泛的抗心律失常作用。

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Electrophysiologic basis for the antiarrhythmic actions of sotalol and comparison with other agents.索他洛尔抗心律失常作用的电生理基础及其与其他药物的比较。
Am J Cardiol. 1993 Aug 12;72(4):8A-18A. doi: 10.1016/0002-9149(93)90020-d.
2
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Reduction of dispersion of repolarization and prolongation of postrepolarization refractoriness explain the antiarrhythmic effects of quinidine in a model of short QT syndrome.复极离散度的降低和复极后不应期的延长解释了奎尼丁在短QT综合征模型中的抗心律失常作用。
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Sotalol: a breakthrough antiarrhythmic?索他洛尔:一种突破性的抗心律失常药物?
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Pharmacologic basis of the antiarrhythmic and hemodynamic effects of sotalol.索他洛尔抗心律失常及血流动力学效应的药理学基础。
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引用本文的文献

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Molecular determinants of pro-arrhythmia proclivity of d- and l-sotalol via a multi-scale modeling pipeline.通过多尺度建模管道研究 d-和 l-索他洛尔致心律失常倾向的分子决定因素。
J Mol Cell Cardiol. 2021 Sep;158:163-177. doi: 10.1016/j.yjmcc.2021.05.015. Epub 2021 May 29.
2
d,l-Sotalol at therapeutic concentrations facilitates the occurrence of long-lasting non-stationary reentry during ventricular fibrillation in isolated rabbit hearts.治疗浓度的消旋索他洛尔可促进离体兔心在心室颤动期间出现持久的非平稳折返。
Circ J. 2009 Jan;73(1):39-47. doi: 10.1253/circj.cj-08-0540. Epub 2008 Nov 13.