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妥卡尼。对其药理特性和治疗效果的综述。

Tocainide. A review of its pharmacological properties and therapeutic efficacy.

作者信息

Holmes B, Brogden R N, Heel R C, Speight T M, Avery G S

出版信息

Drugs. 1983 Aug;26(2):93-123. doi: 10.2165/00003495-198326020-00001.

Abstract

Tocainide is an antiarrhythmic drug structurally related to lignocaine with similar electrophysiological, haemodynamic and antiarrhythmic effects. In contrast to lignocaine (lidocaine) it is well absorbed after oral administration and has a plasma half-life of about 15 hours. In several open and controlled therapeutic trials in patients with ventricular arrhythmias, often following a myocardial infarction, tocainide has been relatively effective and usually well tolerated. In treating ventricular ectopic beats and/or ventricular tachycardia tocainide has demonstrated effective suppression in 60 to 70% of patients in both open and controlled studies. It has an acute effect when infused in patients with ventricular arrhythmias complicating myocardial infarction, as well as a prophylactic effect when given orally. The majority of these studies have demonstrated tocainide to be more effective than placebo, but trials against other antiarrhythmic agents are few in number and vary in design. One study combining an infusion of tocainide with oral therapy compared to a bolus injection of lignocaine followed by a constant infusion in patients after myocardial infarction, found the two agents to be of similar efficacy. The most common adverse effects are neurological and gastrointestinal in nature, nausea and dizziness occurring most frequently. Adverse effects resulting in termination of therapy have been reported in about 16% of patients. Aggravation of pre-existing heart failure, increased ventricular arrhythmia, deterioration of conduction disturbances, convulsions, and cases of lupus erythematosus syndrome have occasionally been reported. Thus, tocainide appears to offer a worthwhile addition to the other antiarrhythmic agents available for ventricular arrhythmias. However, its relative place in therapy compared with other antiarrhythmic drugs is not yet clearly established.

摘要

妥卡尼是一种抗心律失常药物,其结构与利多卡因相关,具有相似的电生理、血流动力学和抗心律失常作用。与利多卡因不同,妥卡尼口服后吸收良好,血浆半衰期约为15小时。在几项针对室性心律失常患者(通常在心肌梗死后)的开放和对照治疗试验中,妥卡尼相对有效,且通常耐受性良好。在治疗室性早搏和/或室性心动过速时,妥卡尼在开放和对照研究中均显示对60%至70%的患者有有效抑制作用。在心肌梗死并发室性心律失常的患者中静脉输注时,妥卡尼有急性作用,口服时也有预防作用。这些研究大多表明妥卡尼比安慰剂更有效,但与其他抗心律失常药物对比的试验数量较少,设计也各不相同。一项将妥卡尼静脉输注与口服治疗相结合,并与利多卡因静脉推注后持续输注进行对比的研究发现,这两种药物在心肌梗死后患者中的疗效相似。最常见的不良反应是神经和胃肠道方面的,恶心和头晕最为常见。据报道,约16%的患者因不良反应而终止治疗。偶尔也有关于原有心力衰竭加重、室性心律失常增加、传导障碍恶化、惊厥以及红斑狼疮综合征病例的报道。因此,妥卡尼似乎是治疗室性心律失常的其他抗心律失常药物的一个有价值的补充。然而,与其他抗心律失常药物相比,其在治疗中的相对地位尚未明确确立。

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