Profiles of calcium antagonists in cardiovascular disease with special reference to second-generation agents and amlodipine.
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.
Opie
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Medical Research Council Ischemic Heart Disease Unit, University of Cape Town Medical School, South Africa.
D017311:Amlodipine; D000959:Antihypertensive Agents / Q000627:therapeutic use; D001665:Binding Sites / Q000502:physiology; D002121:Calcium Channel Blockers / Q000627:therapeutic use*; D015220:Calcium Channels / Q000378:metabolism; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000378:metabolism; D004347:Drug Interactions; D006801:Humans; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D015220:Calcium Channels; D017311:Amlodipine; D009543:Nifedipine