Clinical pharmacology of nebivolol

Nebivolol is a novel, potent and highly selective beta(1)-adrenergic antagonist, devoid of intrinsic sympathomimetic activity, that induces endothelium-dependent arterial and venous dilatation via the L-arginine-nitric oxide pathway. Nebivolol reduces blood pressure and peripheral vascular resistance and does not depress, but rather maintains or improves, left ventricular function in healthy subjects and in patients with hypertension. It has also been shown to improve large arteries distensibility and compliance and to reduce left ventricular hypertrophy in hypertensive patients. Exercise tolerance is not affected, or may even be improved, by nebivolol treatment. In hypertensive patients, once-daily administration is effective over 24 h, with an excellent trough-to-peak ratio. The response to treatment compares favorably with diuretics, typical beta-blockers, calcium channel blockers and ACE inhibitors. The hypotensive effect is independent of age, weight, smoking, alcohol consumption and presence of diabetes. Nebivolol is effective and safe both in young and elderly patients. Nebivolol also has antianginal properties in patients with coronary artery disease and beneficial hemodynamic effects in patients with stable congestive heart failure.