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Nebivolol: Pharmacologic Profile of an Ultraselective, Vasodilatory β₁-Blocker

From the Medical College of Georgia, Augusta, Georgia.

Beta-blockers are well-established therapeutic agents in the treatment of hypertension and cardiovascular disease. However, these agents are highly heterogeneous. Beta-blockers differ in their ancillary pharmacologic properties, which are clinically important. Nebivolol is a highly selective β₁-adrenergic receptor blocker that induces vasodilation through stimulation of the endothelial nitric oxide/L-arginine pathway. As a racemic mixture of d- and l-enantiomers, nebivolol is highly lipophilic and rapidly absorbed. Nebivolol undergoes extensive hepatic metabolism through the cytochrome P450 2D6 (CYP2D6) system. As a result of genetic polymorphisms, CYP2D6 has variable activity, manifested by extensive and poor metabolizers of nebivolol. Time to maximum concentration is 0.5 to 2 hours, and half-life is 11 hours in extensive metabolizers; these values are about 3 times longer in poor metabolizers. Urinary and fecal excretion of unchanged nebivolol is less than 0.5% of the dose. Nebivolol has a unique hemodynamic profile of reduced systemic vascular resistance and increased left ventricular function. These properties are attributed to its vasodilating action and contrast with the hemodynamic effects of conventional β-blockers. Nebivolol is thus a novel β-blocker with several important pharmacologic properties that distinguish it from traditional β-blockers. These unique properties may confer clinical benefits beyond simple blood pressure lowering.

Key Words: Nebivolol • pharmacodynamics • pharmacokinetics • nitric oxide • β-blockers

Address for correspondence: L. Michael Prisant, MD, FCP, FACC, Professor of Medicine, Director of Hypertension and Clinical Pharmacology, Medical College of Georgia, 1467 Harper Street, HB 2010, Augusta, GA 30912; e-mail: mprisant{at}mcg.edu.