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醋卡尼(N-乙酰普鲁卡因胺)。对其药效学和药代动力学特性以及在心律失常治疗中的潜力的综述。

Acecainide (N-acetylprocainamide). A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in cardiac arrhythmias.

作者信息

Harron D W, Brogden R N

机构信息

Queen's University of Belfast, Northern Ireland.

出版信息

Drugs. 1990 May;39(5):720-40. doi: 10.2165/00003495-199039050-00007.

Abstract

Acecainide (N-acetylprocainamide), the N-acetylated metabolite of procainamide, is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. In a small number of noncomparative and placebo-controlled short term therapeutic trials acecainide markedly reduced premature ventricular beats and prevented induction of ventricular tachycardia in more than 70% of patients following intravenous administration and in about 50% after oral administration. Acecainide was effective in about one-quarter of patients refractory to other antiarrhythmic drugs. Interpretation of its effectiveness following long term oral therapy is complicated by the limited number of patients, and patients discontinuing due to adverse effects or lack of efficacy. However, about 40% of the small number treated for extended periods were controlled for periods of 6 months to 3 to 4 years. Comparative studies with other antiarrhythmic drugs have not been undertaken apart from a small study in atrial flutter where acecainide was better than quinidine plus digoxin. Thus, although further clinical experience is required before the relative place of acecainide in therapy can be determined, the drug nevertheless appears to offer advantages over procainamide, particularly with respect to the reduced formation of antinuclear antibodies.

摘要

乙酰卡尼(N - 乙酰普鲁卡因胺)是普鲁卡因胺的N - 乙酰化代谢产物,属于Ⅲ类抗心律失常药物。它可以静脉给药或口服给药,主要通过肾脏排泄消除。在少数非对照和安慰剂对照的短期治疗试验中,乙酰卡尼能显著减少室性早搏,静脉给药后70%以上的患者以及口服给药后约50%的患者可预防室性心动过速的诱发。乙酰卡尼对约四分之一对其他抗心律失常药物无效的患者有效。长期口服治疗后其疗效的解读因患者数量有限以及患者因不良反应或缺乏疗效而停药而变得复杂。然而,在少数接受长期治疗的患者中,约40%的患者在6个月至3至4年的时间内病情得到控制。除了一项关于心房扑动的小型研究表明乙酰卡尼优于奎尼丁加地高辛外,尚未开展与其他抗心律失常药物的对比研究。因此,尽管在确定乙酰卡尼在治疗中的相对地位之前还需要更多的临床经验,但该药物似乎比普鲁卡因胺更具优势,尤其是在抗核抗体形成减少方面。

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