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盐酸恩卡尼和醋酸氟卡尼:两种1C类抗心律失常药。

Encainide hydrochloride and flecainide acetate: two class 1c antiarrhythmic agents.

作者信息

Chase S L, Sloskey G E

机构信息

Department of Pharmacy, Thomas Jefferson University Hospital, Philadelphia, PA 19107.

出版信息

Clin Pharm. 1987 Nov;6(11):839-50.

PMID:3119276
Abstract

The chemistry, electrophysiology, pharmacokinetics, clinical use and efficacy, adverse effects, drug interactions, and dosage of encainide hydrochloride and flecainide acetate are reviewed. Encainide and flecainide are class 1c antiarrhythmic agents that slow myocardial conduction and mildly prolong the duration of repolarization. Both agents block anterograde conduction over accessory pathways and prolong the effective refractory period of the accessory pathway. Bioavailability of encainide ranges from 7% to 82%, whereas that of flecainide is 90% to 95%. Encainide is metabolized by the liver to two major active metabolites that are slowly eliminated in the urine. About 23% of flecainide's total body clearance is dependent on renal elimination, and drug excretion is slowed in patients with renal dysfunction, requiring dosage adjustments. Both agents are effective in the suppression and prevention of ventricular arrhythmias, including premature ventricular contractions and sustained and nonsustained ventricular tachycardia. These agents may also be valuable in controlling supraventricular arrhythmias. The most common adverse effects of both agents involve the central nervous system and include dizziness, blurred vision, and headache. The potential for proarrhythmic effects is a concern with these agents. The risk is greater in patients with more severe arrhythmias, poor ventricular function, or high serum concentrations of drug. The usual initial oral dosage of encainide hydrochloride is 25 mg three times a day, with a usual dosage range of 100-200 mg/day. Flecainide acetate should be initiated at 100 mg every 12 hours and may be increased up to 400 mg/day. Encainide and flecainide could become useful therapeutic options in the treatment of a variety of arrhythmias.

摘要

本文综述了盐酸恩卡尼和醋酸氟卡尼的化学性质、电生理学、药代动力学、临床应用及疗效、不良反应、药物相互作用和剂量。恩卡尼和氟卡尼均为1c类抗心律失常药,可减慢心肌传导并轻度延长复极时间。两者均可阻断旁路的前向传导,延长旁路的有效不应期。恩卡尼的生物利用度为7%至82%,而氟卡尼为90%至95%。恩卡尼在肝脏代谢为两种主要活性代谢产物,经尿液缓慢排泄。氟卡尼约23%的全身清除率依赖于肾脏排泄,肾功能不全患者药物排泄减慢,需要调整剂量。两者均对抑制和预防室性心律失常有效,包括室性早搏、持续性和非持续性室性心动过速。这些药物在控制室上性心律失常方面也可能有价值。两者最常见的不良反应累及中枢神经系统,包括头晕、视力模糊和头痛。这些药物存在致心律失常作用的潜在风险。在心律失常更严重、心室功能差或药物血清浓度高的患者中,风险更大。盐酸恩卡尼通常的初始口服剂量为每日3次,每次25mg,常用剂量范围为100 - 200mg/天。醋酸氟卡尼应开始时每12小时100mg,可增至400mg/天。恩卡尼和氟卡尼可能成为治疗多种心律失常的有用治疗选择。

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