Reiffel James A
Department of Medicine, Division of Cardiology, Columbia University Medical Center.
J Atr Fibrillation. 2013 Apr 6;5(6):752. doi: 10.4022/jafib.752. eCollection 2013 Apr-May.
Dronedarone is a derivative of amiodarone with similar mechanisms of action (blocking calcium, potassium and sodium channels in addition to having anti-adrenergic effects). Compared to amiodarone it has fewer drug interactions (though it can interact with all current anticoagulants), more limited risk of organ toxicity, a much shorter half-life with no need for a loading regimen, but lower efficacy. Dronedarone is approved for the treatment of atrial fibrillation; has had limited studies for other arrhythmias; and has no adverse drug-ICD interactions reported. Clinical trials have resulted in only one dosing regimen (400 mg bid, to be taken with food) and have demonstrated both rate and rhythm effects in atrial fibrillation (AF). Dronedarone slows the ventricular response, can prolong the time to/reduce recurrences of/ reduce progression of AF, and reduce the incidence of hospitalization in AF patients with risk-prone markers. However, trials have also revealed an increased risk of mortality and other adverse cardiovascular outcomes from dronedarone when given to patients in heart failure. The details of these trials, additional pharmacokinetic and pharmacodynamic information, and recommendations concerning the use of dronedarone are provided in the full manuscript that follows.
决奈达隆是胺碘酮的衍生物,作用机制相似(除具有抗肾上腺素能作用外,还可阻断钙、钾和钠通道)。与胺碘酮相比,它的药物相互作用较少(尽管它可与所有目前使用的抗凝剂相互作用),器官毒性风险更有限,半衰期短得多,无需负荷给药方案,但疗效较低。决奈达隆被批准用于治疗心房颤动;对其他心律失常的研究有限;且未报告有不良的药物与植入式心脏复律除颤器(ICD)相互作用。临床试验仅得出一种给药方案(每日两次,每次400毫克,与食物同服),并已证明其对心房颤动(AF)有心率和节律方面的作用。决奈达隆可减慢心室反应,可延长房颤发生时间/减少房颤复发/降低房颤进展,降低有易患风险标志物的房颤患者的住院率。然而,试验还显示,在心力衰竭患者中使用决奈达隆时,其死亡风险及其他不良心血管结局会增加。以下完整的手稿中提供了这些试验的详细信息、更多的药代动力学和药效学信息以及有关决奈达隆使用的建议。