房颤急性转化期的新型药物:以vernakalant为重点。

Pio Cialdella, Daniela Pedicino, Pasquale Santangeli
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引用次数: 6

摘要

Vernakalant是一种新型抗心律失常药物,最近被批准用于近期发作的心房颤动的心律转复。它的作用主要是由于阻断了负责超快速延迟整流电流I(Kur)的心房选择性通道,但也与其他通道和电流有重要的相互作用,如I(Na)(向内钠电流)和I(KACh)(乙酰胆碱调节的钾电流)。由于相对选择性地阻断I(Kur),维那卡兰特延长了心房的有效不应期,而对心室的影响最小,从而将心律失常的风险降至最低。迄今为止,vernakalant已在三个安慰剂对照试验(ACT I、ACT II和ACT III)和一个胺碘酮对照研究(AVRO)中进行了测试。Vernakalant已被证明比安慰剂和胺碘酮对房颤的快速转化更有效,没有明显的不良事件。本文将对这种新型心房选择性药物的最新专利进行综述,讨论其作用机制和可能的临床应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel agents for the acute conversion of atrial fibrillation: focus on vernakalant.

Vernakalant is a novel anti-arrhythmic drug, recently approved for the cardioversion of recent-onset atrial fibrillation. Its action is mainly due to the blockade of atrial-selective channels responsible of the ultra-rapid delayed rectifier current I(Kur), but has also important interactions with other channels and currents, such as I(Na) (inward sodium current), and I(KACh) (acetylcholine-regulated potassium current). Due to the relatively selective blockade of the I(Kur), vernakalant prolongs the effective refractory period of the atria with minimal effects on the ventricles, thus minimizing the risk of proarrhythmia. Thus far vernakalant has been tested in three placebo-controlled trials (ACT I, ACT II and ACT III) and in one amiodarone-controlled study (AVRO). Vernakalant has been demonstrated more effective than both placebo and amiodarone for the rapid conversion of atrial fibrillation, without significant adverse events. This article will review the recent patents on this novel atrial-selective agent, discussing its mechanisms of action and possible clinical applications in the real-world practice.

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