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提高钙拮抗药选择性的尝试。

Attempts to improve the selectivity of calcium antagonistic drugs.

作者信息

van Zwieten P A, Pfaffendorf M, Mancia G

机构信息

Department of Pharmacotherapy, University of Amsterdam, The Netherlands.

出版信息

Blood Press Suppl. 1996;5:7-9.

PMID:8973786
Abstract

The dihydropyridine calcium antagonists differ in respect to their structures as well as their pharmacological profiles. An improved vascular selectivity has been claimed for some of the newer agents (amlodipine, felodipine, isradipine, lacidipine, lercanidipine, manidipine and nicardipine), implying that these agents exert a stronger action on the resistance and coronary arteries than on myocardial and nodal structures. By virtue of their antihypertensive effects, calcium antagonists should be considered as renal protective. Such a renal protective potential has been demonstrated in renal insufficiency and toxicity caused by cancer chemotherapy, radiocontrast agents, cyclosporine or aminoglycoside antibiotics. Furthermore, calcium antagonists may also have a protective effect on donor kidneys in kidney transplantation. Among the newer dihydropyridines, manidipine has been suggested as possessing a certain degree of renal selectivity. This claim is based mainly on animal experimental studies and has to be substantiated in the clinic. From the therapeutic point of view, the concept of renal selectivity for calcium antagonists may be of considerable interest.

摘要

二氢吡啶类钙拮抗剂在结构和药理学特性方面存在差异。一些新型药物(氨氯地平、非洛地平、伊拉地平、拉西地平、乐卡地平、马尼地平、尼卡地平)据称具有更高的血管选择性,这意味着这些药物对阻力血管和冠状动脉的作用比对心肌和窦房结结构的作用更强。由于其降压作用,钙拮抗剂应被视为具有肾脏保护作用。在由癌症化疗、放射性造影剂、环孢素或氨基糖苷类抗生素引起的肾功能不全和毒性方面,这种肾脏保护潜力已得到证实。此外,钙拮抗剂在肾移植中对供体肾脏也可能具有保护作用。在新型二氢吡啶类药物中,马尼地平被认为具有一定程度的肾脏选择性。这一说法主要基于动物实验研究,有待在临床上得到证实。从治疗角度来看,钙拮抗剂的肾脏选择性概念可能相当引人关注。

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