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决奈达隆

Dronedarone.

作者信息

Tamargo J, López-Farré A, Caballero R, Delpón E

机构信息

Department of Pharmacology, Universidad Complutense, Madrid, Spain.

出版信息

Drugs Today (Barc). 2011 Feb;47(2):109-33. doi: 10.1358/dot.2011.47.2.1545699.

Abstract

Atrial fibrillation (AF), the most common cardiac arrhythmia, is associated with substantial morbidity and mortality. Dronedarone is an amiodarone-like benzofuran which lacks the iodine moiety and presents a methane sulfonyl group that decreases its lipophilicity, thus shortening the half-life and decreasing tissue accumulation. Like amiodarone, dronedarone blocks multiple cardiac ion channels and β-adrenoceptors, presenting electrophysiological characteristics of all four Vaughan Williams classes of antiarrhythmic drugs. In clinical trials, dronedarone has been found effective for both rhythm and rate control. Dronedarone was more effective than placebo in maintaining sinus rhythm in patients with paroxysmal and/or persistent AF and was also effective for ventricular rate control during AF recurrences, providing incremental rate control on top of standard drugs in permanent AF. Furthermore, in the ATHENA trial, dronedarone reduced the incidence of hospitalization due to cardiovascular events or death in patients with nonpermanent AF. Even when dronedarone was less effective than amiodarone in decreasing AF recurrence, it had a better safety profile, being devoid of thyroid, pulmonary and neurological toxicity. This review analyzes the electrophysiological and pharmacological properties, as well as the efficacy and safety of dronedarone in patients with atrial fibrillation.

摘要

心房颤动(AF)是最常见的心律失常,与较高的发病率和死亡率相关。决奈达隆是一种类似胺碘酮的苯并呋喃,它不含碘部分,带有一个甲磺酰基,这降低了其亲脂性,从而缩短了半衰期并减少了组织蓄积。与胺碘酮一样,决奈达隆可阻断多种心脏离子通道和β肾上腺素能受体,具有所有四类 Vaughan Williams 抗心律失常药物的电生理特性。在临床试验中,已发现决奈达隆在节律控制和心率控制方面均有效。在阵发性和/或持续性 AF 患者中,决奈达隆在维持窦性心律方面比安慰剂更有效,并且在 AF 复发期间对心室率控制也有效,在永久性 AF 中可在标准药物基础上进一步控制心率。此外,在 ATHENA 试验中,决奈达隆降低了非永久性 AF 患者因心血管事件或死亡导致的住院发生率。即使决奈达隆在减少 AF 复发方面不如胺碘酮有效,但它具有更好的安全性,没有甲状腺、肺部和神经毒性。本综述分析了决奈达隆在心房颤动患者中的电生理和药理特性,以及其疗效和安全性。

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