Carvedilol is a beta blocker with antihypertensive effects, used for treating patients with hypertension or heart failure.1,2 Beta blockers were introduced in the early 1960s for hypertensive patients to protect against cardiovascular morbidity and mortality and were shown to be beneficial for other heart conditions.3
Different beta blockers have differing effects on three adrenergic receptors (beta-1, beta-2, alpha).4 Carvedilol is one type of a beta blocker – a third generation, vasodilatory nonselective beta-adrenergic blocking agent.5 Unlike other beta blockers (e.g. atenolol, metoprolol, and propranolol), carvedilol acts by blocking both beta-1 and beta-2 adrenergic receptors, along with exhibiting alpha-1 adrenergic activities.5 It prevents norepinephrine from binding to beta-1, beta-2, and alpha-1 adrenergic receptors. Through these mechanisms, carvedilol lowers sympathetic nervous system-mediated cardiac stress and myocardial hypertrophy6 and lowers blood pressure by reducing systemic vascular resistance.7 These physiological changes are reflected as clinical benefits seen in patients with hypertension, heart failure, or left ventricular dysfunction post-myocardial infarction who take carvedilol.5,1,2
- Coreg [package insert]. Ciales, PR: GK Pharmaceuticals Contract Manufacturing Operations; 2008.
- Coreg CR [package insert]. Ciales, PR: GK Pharmaceuticals Contract Manufacturing Operations; 2008.
- Frishman WH. A historical perspective on the development of β-adrenergic blockers. Am J Hypertens. 2007;9(s4):19-27.
- Helfand M, Peterson K, Christensen V, Dana T, Thakurta S. Drug Class Reviews. In: Drug Class Review: Beta Adrenergic Blockers: Final Report Update 4. Portland (OR): Oregon Health & Science University, Portland, Oregon.; 2009.
- Frishman WH, Henderson LS, Lukas MA. Controlled-release carvedilol in the management of systemic hypertension and myocardial dysfunction. Vasc Health Risk Manag. 2008;4(6):1387-1400.
- Toda N. Vasodilating beta-adrenoceptor blockers as cardiovascular therapeutics. Pharmacol Ther. 2003;100(3):215-234.
- Sundberg S, Tiihonen K, Gordin A. Vasodilatory effects of carvedilol and pindolol. J Cardiovasc Pharmacol. 1987;10 Suppl 11:S76-80.