title: A Review of Nebivolol Pharmacology and Clinical Evidence.
abstract: Nebivolol is a highly selective β1-adrenergic receptor antagonist with a pharmacologic profile that differs from those of other drugs in its class. In addition to cardioselectivity mediated via β1 receptor blockade, nebivolol induces nitric oxide-mediated vasodilation by stimulating endothelial nitric oxide synthase via β3 agonism. This vasodilatory mechanism is distinct from those of other vasodilatory β-blockers (carvedilol, labetalol), which are mediated via α-adrenergic receptor blockade. Nebivolol is approved for the treatment of hypertension in the US, and for hypertension and heart failure in Europe. While β-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 β-blockers. Clinical data also suggest that nebivolol may be useful in patients who have experienced erectile dysfunction while on other β-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.
authors.affiliation: Tufts Medical Center, 800 Washington St., Boston, MA, 02111, USA.
authors.forename: Justin
authors.initials: J
authors.lastname: Fongemie
authors.forename: Erika
authors.initials: E
authors.lastname: Felix-Getzik
mesh_terms: D058665:Adrenergic beta-1 Receptor Agonists / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D003362:Cost-Benefit Analysis; D016527:Drug Costs; D004359:Drug Therapy, Combination; D006333:Heart Failure / Q000175:diagnosis / Q000188:drug therapy* / Q000191:economics / Q000503:physiopathology; D006801:Humans; D006973:Hypertension / Q000175:diagnosis / Q000188:drug therapy* / Q000191:economics / Q000503:physiopathology; D000068577:Nebivolol / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016896:Treatment Outcome; D014665:Vasodilator Agents / Q000009:adverse effects / Q000191:economics / Q000493:pharmacokinetics / Q000627:therapeutic use*
chemical_list: D058665:Adrenergic beta-1 Receptor Agonists; D000959:Antihypertensive Agents; D014665:Vasodilator Agents; D000068577:Nebivolol