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钙拮抗剂之间的异同:药理学方面

Similarities and differences between calcium antagonists: pharmacological aspects.

作者信息

van Zwieten P A, Pfaffendorf M

机构信息

Department of Pharmacotherapy, Academic Medical Centre, University of Amsterdam, The Netherlands.

出版信息

J Hypertens Suppl. 1993 Mar;11(1):S3-11. doi: 10.1097/00004872-199303001-00002.

Abstract

Characteristics of three different calcium antagonist groups: Most important calcium antagonists used to treat cardiovascular disease belong to one of three main groups, phenylalkylamines, dihydropyridines and benzothiazepines. The best known drug in each group is verapamil, nifedipine and diltiazem, respectively. Dihydropyridines are predominantly vasodilators, with little or no primary cardiac activity; the tachycardia caused by these compounds is a reflex phenomenon. Verapamil and related drugs are also vasodilators, with an additional depressant effect on atrioventricular conduction, heart rate and contractility. Diltiazem's pharmacodynamic profile and side effects may be considered as intermediate between those of the dihydropyridines and verapamil. Characteristics of new calcium antagonists: Several new calcium antagonists have been introduced in the last few years, virtually all dihydropyridines. Compared with the older generation of calcium antagonists these newer drugs tend to have (1) a longer duration of action; (2) some selectivity for a specific vascular bed, such as resistance, coronary, renal or cerebral vessels; (3) a potentially useful extra component, such as diuretic or anti-atherogenic activity. Newer calcium antagonists described in this review: The newer compounds briefly characterized in this review are amlodipine, felodipine, isradipine, lacidipine, nimodipine, nisoldipine and nitrendipine. New slow-release formulations are also discussed. There is a particular emphasis on lacidipine and its potential for cardiovascular drug therapy.

摘要

三类不同钙拮抗剂的特点

用于治疗心血管疾病的最重要的钙拮抗剂属于三个主要类别之一,即苯烷基胺类、二氢吡啶类和苯并硫氮䓬类。每类中最知名的药物分别是维拉帕米、硝苯地平和地尔硫䓬。二氢吡啶类主要是血管扩张剂,基本没有或仅有微弱的原发性心脏活性;这些化合物引起的心动过速是一种反射现象。维拉帕米及相关药物也是血管扩张剂,对房室传导、心率和收缩力还有抑制作用。地尔硫䓬的药效学特征和副作用可被视为介于二氢吡啶类和维拉帕米之间。新型钙拮抗剂的特点:在过去几年中已引入了几种新型钙拮抗剂,几乎都是二氢吡啶类。与老一代钙拮抗剂相比,这些新药往往具有(1)更长的作用持续时间;(2)对特定血管床,如阻力血管、冠状动脉、肾血管或脑血管有一定选择性;(3)一种潜在有用的额外成分,如利尿或抗动脉粥样硬化活性。本综述中描述的新型钙拮抗剂:本综述中简要描述的新型化合物有氨氯地平、非洛地平、伊拉地平、拉西地平、尼莫地平、尼索地平和尼群地平。还讨论了新的缓释制剂。特别强调了拉西地平及其在心血管药物治疗方面的潜力。

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