Pharmacological basis for use of calcium channel antagonists in hypertension.

The major mechanism of antihypertensive action of Ca2+ channel antagonists is the inhibition of Ca2+ entry into the vascular smooth muscle cell. Ca2+ channels are stabilized by these drugs in a mode unavailable for opening. The inhibition of Ca2+ entry leads to vasodilatation and lowering of arterial pressure. The advantages of Ca2+ channel antagonists in hypertension include improvement of blood supply to vital organs, diuretic activity, coronary vasodilatation, reduction in heart size and vascular cytoprotective effect.