Carvedilol: an effective antihypertensive drug with antiischemic/antioxidant cardioprotective properties.

Carvedilol is a multiple-action drug with alpha(1)- and beta-adrenergic receptor antagonistic, calcium channel blocker and antioxidant activities especially useful in the treatment of hypertension. The antioxidant activity of the drug depends on the carbazole moiety, which is unique to carvedilol and is also present in some of the metabolites lacking either the alpha(1)- or beta-adrenergic receptor blocking activity. These antioxidant properties account for the exceptional ability of carvedilol to reduce cardiac necrosis in animal models of myocardial infarction, as well as its neuroprotective activities in in vivo and in vitro models of brain ischemia. A further property of carvedilol is its ability to inhibit vascular smooth muscle cell migration and proliferation, and neointima formation, after vascular injuries. The identification of all these activities of carvedilol indicates that it is a singular multiple-action antihypertensive agent with potential for cardiovascular organ protection beyond the normalization of high blood pressure.