CARDIOSELECTIVITY OF CALCIUM-ANTAGONISTS

Calcium antagonists comprise a diverse group of chemically unrelated agents that interact with voltage-operated calcium channels (L-type) and thereby inhibit smooth muscle and cardiac contractility. Although they interact with the alpha(1) subunit of voltage-operated calcium channels, all calcium antagonists are not identical pharmacological agents. They are not only different from a chemical point of view, but also because some of them exhibit tissue selectivity, being more powerful blockers of the contraction of arteries than of cardiac muscle. The current view that their major therapeutic action is related to vasodilation is an oversimplification, as their action is more complex and may be related to factors other than hemodynamic ones.