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氟卡尼。对其药效学特性和治疗效果的初步综述。

Flecainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.

作者信息

Holmes B, Heel R C

出版信息

Drugs. 1985 Jan;29(1):1-33. doi: 10.2165/00003495-198529010-00001.

Abstract

Flecainide is a Class I antiarrhythmic drug of the local anaesthetic type. It can be given either intravenously or orally and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration. In several open and a few controlled therapeutic trials, orally administered flecainide has brought about a greater than 90% suppression of ventricular ectopic beats in about 80% of patients. A similar percentage of patients (83%) experienced at least an 80% suppression of their ventricular tachycardia in these trials. A slightly greater response rate was reported with intravenous infusion of flecainide. Initial results in arrhythmias complicating the Wolff-Parkinson-White syndrome have been favourable. Comparative trials are few in number but flecainide has proved to be more effective than quinidine, and possibly more effective than disopyramide, mexiletine, tocainide and propafenone, in suppressing ventricular ectopic activity. The most commonly reported extracardiac adverse effects have been dizziness and visual disturbances. Proarrhythmic effects have been reported in 7 to 8% of patients, with a higher incidence in patients with serious ventricular tachycardia and reduced myocardial function. The moderate negative inotropic effects of flecainide can become clinically significant in patients with impaired ventricular function. Thus flecainide, with its convenient dose schedule and apparently low incidence of serious side effects, would appear to be a useful addition to the antiarrhythmic agents available. Further studies are needed though, to confirm its long term tolerability when used prophylactically.

摘要

氟卡尼是一种局部麻醉型的Ⅰ类抗心律失常药物。它可以静脉注射或口服给药,其药代动力学特性允许口服给药时采用相对较长(12小时)的给药间隔。在几项开放性和少数对照治疗试验中,口服氟卡尼使约80%的患者室性早搏抑制率超过90%。在这些试验中,类似比例(83%)的患者室性心动过速至少得到80%的抑制。据报道,静脉输注氟卡尼的有效率略高。在并发预激综合征的心律失常方面,初步结果是令人满意的。比较试验数量较少,但已证明氟卡尼在抑制室性异位活动方面比奎尼丁更有效,可能比丙吡胺、美西律、妥卡尼和普罗帕酮更有效。最常报告的心脏外不良反应是头晕和视觉障碍。7%至8%的患者报告有促心律失常作用,在严重室性心动过速和心肌功能减退的患者中发生率更高。氟卡尼的中度负性肌力作用在心室功能受损的患者中可能具有临床意义。因此,氟卡尼给药方案方便且严重副作用发生率明显较低,似乎是现有抗心律失常药物中的一个有用补充。不过,仍需要进一步研究以证实其预防性使用时的长期耐受性。

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