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索他洛尔:现状与适应证拓展

Sotalol: Current Status and Expanding Indications.

作者信息

Singh BN

机构信息

UCLA School of Medicine, Veterans Affairs Medical Center of West Los Angeles, Los Angeles, California, USA

出版信息

J Cardiovasc Pharmacol Ther. 1999 Jan;4(1):49-65. doi: 10.1177/107424849900400108.

Abstract

BACKGROUND

The role of antiarrhythmic drug therapy continues to undergo major changes. The change is necessitated by the advent of invasive interventional procedures, such as catheter ablation of arrhythmias and the use of implantable devices for sensing and terminating life-threatening ventricular arrhythmias and symptomatically traublesome supraventricular arrhythmias. Many conventional and time-honored drugs, such as sodium channel blockers, have been found either to be ineffective or to have the potential to produce serious proarrhythmic reactions. Attention is therefore focused on compounds that prolong repolarization and reduce sympathetic stimulation. Two compounds, amiodarone and sotalol, have emerged as prototypes of drugs of the future. METHODS AND RESULTS: This review focuses on sotalol for controlling supraventricular and ventricular tachyarrhythmias. Sotalol is a major antiarrhythmic agent that combines potent class III action with nonselective beta-blocking properties. The drug's pharmacokinetics is simple. Its elimination half-life is 10-15 hours, the drug being excreted almost exclusively by the kidneys. Sotalol's pharmacokinetics allows development of optimal dosing for initiation of therapy relative to changes in creatinine clearance with further dose adjustment by monitoring the QT interval on the surface electrocardiogram. The compound exerts broad-spectrum antiarrhythmic actions in supraventricular and ventricular arrhythmias. It prevents inducible ventricular tachycardia (VT) and ventricular fibrillation (VF) in approximately 30% of patients with a higher figure for the suppression of spontaneously occurring arrhythmias documented on Holter recordings. CONCLUSIONS: The major role of sotalol is in the management of VT/VF often in conjunction with an implantable cardioverter/defibrillator, in which context it lowere the defibrillation threshold. Sotalol is superior to class I agents, especially in VT/VF and in survivors of cardiac arrest. Sotalol has emerged as a major antifibrillatory compound for the control of life-threatening ventricular arrhythmias as the main indication. Data have indicated its potential for the maintenance of stability of sinus rhythm in patients with atrial fibrillation and flutter after electrical conversion and in preventing their occurrence in a variety of clinical settings.

摘要

背景

抗心律失常药物治疗的作用仍在经历重大变革。侵入性介入手术的出现使得这种变革成为必要,例如心律失常的导管消融以及使用植入式设备来感知和终止危及生命的室性心律失常和有症状的麻烦性室上性心律失常。许多传统且久负盛名的药物,如钠通道阻滞剂,已被发现要么无效,要么有产生严重促心律失常反应的可能性。因此,注意力集中在延长复极和减少交感神经刺激的化合物上。两种化合物,胺碘酮和索他洛尔,已成为未来药物的原型。

方法与结果

本综述聚焦于索他洛尔用于控制室上性和室性快速心律失常。索他洛尔是一种主要的抗心律失常药物,兼具强效Ⅲ类作用和非选择性β受体阻断特性。该药物的药代动力学简单。其消除半衰期为10 - 15小时,药物几乎完全通过肾脏排泄。索他洛尔的药代动力学允许根据肌酐清除率的变化制定起始治疗的最佳剂量,并通过监测体表心电图的QT间期进一步调整剂量。该化合物在室上性和室性心律失常中发挥广谱抗心律失常作用。它能预防约30%患者的可诱导性室性心动过速(VT)和心室颤动(VF),对于动态心电图记录中记录到的自发性心律失常的抑制率更高。

结论

索他洛尔的主要作用在于常常与植入式心脏复律除颤器联合用于VT/VF的管理,在这种情况下它可降低除颤阈值。索他洛尔优于Ⅰ类药物,尤其是在VT/VF以及心脏骤停幸存者中。索他洛尔已成为一种主要的抗纤颤化合物,用于控制危及生命的室性心律失常作为主要适应证。数据表明其在房颤和房扑患者电复律后维持窦性心律稳定性以及在多种临床情况下预防其发生的潜力。

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