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美西律:其药理特性及在心律失常治疗中的疗效综述。

Mexiletine: a review of its pharmacological properties and therapeutic efficacy in arrhythmias.

作者信息

Chew C Y, Collett J, Singh B N

出版信息

Drugs. 1979 Mar;17(3):161-81. doi: 10.2165/00003495-197917030-00003.

Abstract

Mexiletine is a new local anaesthetic antiarrhythmic agent whose chemical structure and electrophysiological properties closely resemble those of lignocaine although its anticonvulsant and pharmacokinetic properties differ from that drug. Unlike lignocaine (lidocaine) it is active following oral administration with a plasma half-life varying between 8 and 20 hours so that it can be administered twice or three times daily to sustain therapeutic plasma levels. The drug is effective when given intravenously or by the oral route in controlling ventricular arrhythmias especially following acute myocardial infarction but the side effects are greater during parenteral administration. Side effects during chronic oral therapy with mexiletine have not posed a serious problem. Mexiletine has the pharmacodynamic and pharmacokinetic properties of an agent suitable for the chronic oral prophylaxis of serious ventricular arrhythmias in patients with ischaemic heart disease.

摘要

美西律是一种新型局部麻醉抗心律失常药物,其化学结构和电生理特性与利多卡因极为相似,尽管其抗惊厥和药代动力学特性与利多卡因不同。与利多卡因不同,美西律口服后具有活性,血浆半衰期在8至20小时之间变化,因此可以每日给药两次或三次以维持治疗性血浆水平。该药物通过静脉注射或口服给药时,对于控制室性心律失常有效,尤其是在急性心肌梗死后,但胃肠外给药时副作用更大。美西律长期口服治疗期间的副作用尚未构成严重问题。美西律具有适合对缺血性心脏病患者严重室性心律失常进行长期口服预防的药物的药效学和药代动力学特性。

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