A Review of Nebivolol Pharmacology and Clinical Evidence

Nebivolol is a highly selective beta(1)-adrenergic receptor antagonist with a pharmacologic profile that differs from those of other drugs in its class. In addition to cardioselectivity mediated via beta(1) receptor blockade, nebivolol induces nitric oxide-mediated vasodilation by stimulating endothelial nitric oxide synthase via beta(3) agonism. This vasodilatory mechanism is distinct from those of other vasodilatory beta-blockers (carvedilol, labetalol), which are mediated via alpha-adrenergic receptor blockade. Nebivolol is approved for the treatment of hypertension in the US, and for hypertension and heart failure in Europe. While beta-blockers are not recommended within the current US guidelines as first-line therapy for treatment of essential hypertension, nebivolol has shown comparable efficacy to currently recommended therapies in lowering peripheral blood pressure in adults with hypertension with a very low rate of side effects. Nebivolol also has beneficial effects on central blood pressure compared with other beta-blockers. Clinical data also suggest that nebivolol may be useful in patients who have experienced erectile dysfunction while on other beta-blockers. Here we review the pharmacological profile of nebivolol, the clinical evidence supporting its use in hypertension as monotherapy, add-on, and combination therapy, and the data demonstrating its positive effects on heart failure and endothelial dysfunction.