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吡司卡尼。

Pilsicainide.

机构信息

Adis, Auckland, New Zealand.

出版信息

Drugs. 2010 Mar 5;70(4):455-67. doi: 10.2165/11204960-000000000-00000.

Abstract

Pilsicainide is a class Ic antiarrhythmic agent used for the treatment of supraventricular and ventricular tachycardia. The pharmacodynamic effects of pilsicainide are achieved via selective sodium channel blockade. In randomized, multicentre trials in patients with atrial fibrillation, restoration of sinus rhythm was achieved in significantly more patients treated with a single oral dose of pilsicainide than those who received placebo, and in a numerically higher proportion of oral pilsicainide than intravenous disopyramide recipients. In another well designed trial in patients with persistent atrial fibrillation, the proportion of patients whose arrhythmia converted to normal sinus rhythm was significantly higher among those randomized to receive 2 weeks of oral pilsicainide therapy than among patients who received placebo. Over a 1-year period, both pilsicainide and cibenzoline (another class Ic agent) were effective in preventing recurrence of atrial fibrillation in a substantial proportion of patients in a single-centre crossover trial. There were no between-group differences in the subgroup of patients with shorter-duration atrial fibrillation, but actuarial results over 1 year significantly favoured cibenzoline over pilsicainide in patients with longer-duration atrial fibrillation. Both oral and intravenous pilsicainide have demonstrated efficacy in ventricular tachyarrhythmias, including ventricular extrasystole. Clinical trial and postmarketing surveillance data indicate that pilsicainide is generally well tolerated in most patients.

摘要

吡西卡尼是一种 Ic 类抗心律失常药物,用于治疗室上性和室性心动过速。吡西卡尼的药效学作用是通过选择性钠通道阻断实现的。在房颤患者的随机、多中心试验中,与安慰剂组相比,接受单次口服吡西卡尼治疗的患者窦性心律恢复的比例显著更高,而口服吡西卡尼组的比例高于静脉注射双异丙吡胺组。在另一项针对持续性房颤患者的精心设计的试验中,与安慰剂组相比,接受 2 周口服吡西卡尼治疗的患者心律失常转为正常窦性心律的比例显著更高。在一项为期 1 年的单中心交叉试验中,吡西卡尼和西苯唑啉(另一种 Ic 类药物)均能有效预防相当一部分患者的房颤复发。在房颤持续时间较短的亚组中,两组之间没有差异,但 1 年的累积结果显著有利于西苯唑啉优于吡西卡尼在房颤持续时间较长的患者。口服和静脉注射吡西卡尼均已证明在室性心动过速心律失常(包括室性早搏)中有效。临床试验和上市后监测数据表明,吡西卡尼在大多数患者中通常具有良好的耐受性。

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