Pharmacodynamics of Nebivolol : A Comprehensive Review of Its Biological Activities

Abstract

Nebivolol is a highly selective β1-adrenergic receptor blocker with a unique dual mechanism that combines beta-blockade with nitric oxide (NO)-mediated vasodilation, offering therapeutic benefits in the management of hypertension and heart failure. Its pharmacodynamic properties lead to reductions in heart rate, myocardial contractility, and vascular resistance while preserving endothelial function. Pharmacokinetically, nebivolol is characterized by good oral absorption, extensive first -pass metabolism via CYP2D6, high plasma protein binding, and a long half-life that supports once-daily dosing. Genetic polymorphisms in CYP2D6 and impairments in renal or hepatic function significantly influence drug metabolism and clearance, necessitating dose adjustments in certain populations. The favorable cardioselectivity and minimal impact on glucose and lipid metabolism make nebivolol a valuable option, particularly in patients with comorbid respiratory or metabolic conditions.