Clinical Pharmacology of Carvedilol

Abstract

BACKGROUND: There is now a wealth of data supporting the use of beta-blockers in heart failure and the additional pharmacological properties of carvedilol are thought to play an important role in the therapeutic efficacy of carvedilol in this disease. METHODS AND RESULTS: Carvedilol is licensed for the treatment of essential hypertension, chronic stable angina, and mild to moderate chronic heart failure. This article provides an up-to-date review of the clinical pharmacology of carvedilol, with particular emphasis on its clinical effects in heart failure. CONCLUSION: Carvedilol is a multiple-action neurohormonal antagonist that offers nonselective beta-blockade, alpha-1 blockade, antioxidant, anti-ischemic mortality, and anti-proliferative properties. In addition to reductions in hospitalization and mortality rates, benefits of carvedilol in heart failure include dramatic improvements in left ventricular function and other parameters of cardiac remodeling.

Antioxidants: A Possible Role in Kidney Protection

“…The renoprotective activity of ß- blockers has been postulated but not yet fully proven. Carvedilol, the third-generation ß-blocker, displays powerful antioxidant properties [56]. Two experimental studies have shown favorable effects of carvedilol with regard to reduction of renal fibrosis and glomerulosclerosis, decrease in the renal expression of TGF-ß1, collagen I, III and fibronectin, which were comparable to those achieved by captopril administration [57,58].…”

Autonomic Blockade During Sinusoidal Baroreflex Activation Proves Sympathetic Modulation of Cerebral Blood Flow Velocity

“…31,32 Still, the question arises whether (1) the 0.1 Hz NS-induced increases and carvedilol-induced decreases in CBFV and in 0.1 Hz CBFV modulation also reflect an increase, respectively decrease, in sympathetic outflow in sympathetic outflow onto the cerebral vasculature; or whether (2) these changes in CBFV and 0.1 Hz CBFV powers are secondary to, and passively driven by the increases, respectively decreases, in BP and in sympathetic 0.1 Hz BP modulation.…”

Neutrophils superoxide anion generation during carvedilol therapy in patients with stable angina

“…Studies have shown that carvedilol is at least as effective as other antianginal therapies in the management of chronic stable angina [23]. The drug has beneficial effect on patients with myocardial infarction complicated by leftventricular systolic dysfunction [24]. It reduced the frequency of all-cause and cardiovascular mortality, and recurrent, non fatal myocardial infarctions.…”