Rr. Ruffolo et al., RECENT OBSERVATIONS WITH BETA-ADRENOCEPTOR BLOCKADE - BENEFICIAL-EFFECTS IN HYPERTENSION AND HEART-FAILURE, American journal of hypertension, 11(1), 1998, pp. 9-14
Carvedilol is a third-generation vasodilating beta-blocker initially a
pproved for the treatment of hypertension. It lowers systemic arterial
blood pressure without causing reflex tachycardia and preserves renal
function, More recently, carvedilol has been shown to reduce morbidit
y and mortality in patients with congestive heart failure. This reduct
ion may occur in part via beta-blockade and alpha(1)-adrenoceptor bloc
kade, the latter resulting in vasodilation. Importantly, carvedilol an
d several of its metabolites are potent antioxidants that may inhibit
the oxidation of norepinephrine and the subsequent formation of toxic
intermediates, such as reactive free radicals in the myocardium. As a
result, carvedilol inhibits the expression of certain genes involved i
n myocardial damage, such as intracellular adhesion molecule-1, free-r
adical-induced activation of transcription factors, and programmed cel
l death or apoptosis. In this respect, carvedilol represents a new the
rapy for the treatment of hypertension and congestive heart failure an
d combines, ire one molecule, a number of potentially beneficial prope
rties. (C) 1998 American Journal of Hypertension, Ltd.