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抗心律失常药物分类。对其历史、现状及临床相关性的批判性评价。

Antiarrhythmic drug classifications. A critical appraisal of their history, present status, and clinical relevance.

作者信息

Nattel S

机构信息

Department of Medicine, Montreal Heart Institute, Québec, Canada.

出版信息

Drugs. 1991 May;41(5):672-701. doi: 10.2165/00003495-199141050-00002.

DOI:10.2165/00003495-199141050-00002
PMID:1712704
Abstract

Classifications of antiarrhythmic drugs have developed because of a need to organize the large number of agents available according to pharmacological properties of clinical relevance. The current classification is a hybrid of classification systems developed in the early 1970s. It subdivides drugs according to 4 major pharmacological actions: (a) depression of phase 0 sodium current; (b) antagonism of adrenergic effects on the heart; (c) prolongation of of action potential duration; and (d) calcium channel blockade. Further subdivision of sodium channel blockers is based on the kinetics of sodium channel blockade and drug effects on action potential duration. A critical analysis of selected aspects of the clinical actions of antiarrhythmic drugs indicates the value of the current classification, as well as some limitations in its ability to separate drugs into distinct groups with characteristic clinical properties. The strengths of the current classification are due to the clinical importance of the pharmacological properties on which it is based. These results in electrophysiological actions, indications, and adverse effects that are typical for each group of drugs. The limitations of the current system relate to the propensity of individual drugs to have actions of more than one class simultaneously, the way that the various actions of a given drug are dependent on concentration, rate, and tissue type, and to problems in subclass definition. Some of these shortcomings could be alleviated by returning to the concept, originally put forward by Singh and Vaughan Williams, of classes of drug action rather than classes of drug per se. This approach would be pharmacologically more realistic than trying to assign each antiarrhythmic agent to a single unique class, would be better able to incorporate the complexities of drug action, and would potentially be more flexible. The wide use of antiarrhythmic drug classifications attests to their value, and suggests that they are likely to continue to be important in the future.

摘要

抗心律失常药物的分类得以发展,是因为需要根据具有临床相关性的药理学特性来整理大量现有的药物。当前的分类是20世纪70年代初开发的分类系统的混合体。它根据4种主要药理作用对药物进行细分:(a)0期钠电流的抑制;(b)肾上腺素能对心脏作用的拮抗;(c)动作电位持续时间的延长;以及(d)钙通道阻滞。钠通道阻滞剂的进一步细分基于钠通道阻滞的动力学以及药物对动作电位持续时间的影响。对抗心律失常药物临床作用的选定方面进行的批判性分析表明了当前分类的价值,以及在将药物分为具有特征性临床特性的不同组方面其能力的一些局限性。当前分类的优势在于其基于的药理学特性的临床重要性。这导致了每组药物典型的电生理作用、适应证和不良反应。当前系统的局限性涉及个别药物同时具有不止一种类别的作用的倾向、给定药物的各种作用依赖于浓度、速率和组织类型的方式,以及亚类定义方面的问题。通过回归最初由辛格和沃恩·威廉姆斯提出的药物作用类别而非药物本身类别的概念,可以缓解其中一些缺点。这种方法在药理学上比试图将每种抗心律失常药物归为单一独特类别更现实,能够更好地纳入药物作用的复杂性,并且可能更灵活。抗心律失常药物分类的广泛使用证明了它们的价值,并表明它们在未来可能会继续重要。

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