On the mechanism of action of calcium antagonists

A short review is given of possible mechanisms of action of the organic "calcium antagonists". Calcium antagonists comprise a chemically heterogenous group of drugs, and the term may be used to denote agents that inhibit Ca2+-dependent processes or regulatory mechanisms without acting at other sites. Such drugs may be subdivided into those that decrease the availability of Ca2+ to the myoplasm, and those that decrease the cellular effects of Ca2+ without lowering the intracellular Ca2+ concentration. Accordingly, calcium channel blockers, such as verapamil, nifedipine, and diltiazem, form a subgroup of calcium availability inhibitors, as they block influx of extracellular calcium through ion selective channels in the membrane both in cardiac and smooth muscle. However, it cannot be excluded that some of these drugs, particularly in smooth muscle, may have additional sites of action, which must be taken into consideration when they are used as investigational tools.