Opie L H
Medical Research Council Ischemic Heart Disease Unit, University of Cape Town Medical School, South Africa.
Postgrad Med J. 1991;67 Suppl 5:S2-8.
The majority of second-generation calcium antagonists are dihydropyridines, some of which show vascular selectivity. Several new dihydropyridines have been developed with comparable pharmacodynamic properties to existing calcium antagonists in this class and greatly improved kinetic half-lives. Of these agents, amlodipine has by far the longest half-life (30-40 h) allowing the benefit of once-daily administration; it has the additional property of a slow association and dissociation with the calcium channel binding site. In the treatment of hypertension and myocardial ischaemia the prolonged duration of action distinguishes amlodipine from other second-generation agents.
大多数第二代钙拮抗剂是二氢吡啶类，其中一些具有血管选择性。已经开发出几种新的二氢吡啶类药物，它们具有与该类现有钙拮抗剂相当的药效学特性，并且动力学半衰期大大延长。在这些药物中，氨氯地平的半衰期最长（30 - 40小时），可实现每日一次给药；它还具有与钙通道结合位点缓慢结合和解离的特性。在高血压和心肌缺血的治疗中，氨氯地平作用持续时间延长使其有别于其他第二代药物。
