Pharmacodynamic profile of carvedilol.
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.
van Zwieten
P A
PA
Department of Pharmacotherapy, University of Amsterdam, The Netherlands.
D000317:Adrenergic alpha-Antagonists / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000319:Adrenergic beta-Antagonists / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000077261:Carvedilol; D016166:Free Radical Scavengers; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D011412:Propanolamines / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D014665:Vasodilator Agents / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D002227:Carbazoles; D016166:Free Radical Scavengers; D011412:Propanolamines; D014665:Vasodilator Agents; D000077261:Carvedilol