[Experimental pharmacology of calcium antagonists]

Calcium antagonists (calcium channel blockers) constitute a chemically heterogeneous group of drugs which block voltage-operated calcium channels of L-type. They specifically interact with the alpha 1 subunit of the calcium channel. Their mechanism of action has been demonstrated using pharmacological, electrophysiological and radiochemical techniques. Their therapeutic effects are not only related to their hemodynamic action but also to their remodeling effect in hypertrophic heart and arteries, to their anti-ischaemic action and to the preservation of vascular integrity during several pathologies. Drugs belonging to the second generation of calcium antagonists show various pharmacological profiles responsible for their tissue selectivity. The latter is a rational basis for novel therapeutic indications including atherosclerosis and cardiac failure.