Carvedilol exerts combined nonselective beta- and selective alpha-1-adrenoceptor blockade, providing beneficial hemodynamic effects for the treatment of high blood pressure.
Carvedilol's unique pharmacodynamic profile of combined beta- and alpha-blockade provides a logical approach to treating high blood pressure by reducing peripheral resistance and cardiac afterload.
The combination of a beta blocker and a vasodilator is logical in the treatment of high blood pressure. Systemic arteriolar dilatation is beneficial to reduce the elevated peripheral resistance and hence to decrease cardiac afterload. beta-Adrenoceptor blockade exerts its own antihypertensive activity and also suppresses the reflex tachycardia induced by vasodilation. The combined beta- and alpha-adrenoceptor blockade exerted by carvedilol imposes these beneficial hemodynamic effects. Carvedilol is a nonselective beta-adrenoceptor antagonist, devoid of intrinsic sympathomimetic activity and possessing selective alpha 1-adrenoceptor-blocking activity, although this is considerably weaker than its beta-adrenoceptor antagonistic activity. One isomer S(-)-carvedilol contains both the beta- and alpha-adrenoceptor activity, whereas R(+)-carvedilol is only a weak alpha blocker. Carvedilol is produced as the racemate. The hemodynamic profile is in accordance with that to be expected from the combination of beta and alpha blockade.
P. A. van Zwieten (2008) conducted a review in high blood pressure. Carvedilol was evaluated. Carvedilol exerts combined nonselective beta- and selective alpha-1-adrenoceptor blockade, providing beneficial hemodynamic effects for the treatment of high blood pressure.