A Review of Nebivolol Pharmacology and Clinical Evidence

Drugs. 2015 Aug;75(12):1349-71. doi: 10.1007/s40265-015-0435-5.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adrenergic beta-1 Receptor Agonists / adverse effects
  • Adrenergic beta-1 Receptor Agonists / economics
  • Adrenergic beta-1 Receptor Agonists / pharmacokinetics
  • Adrenergic beta-1 Receptor Agonists / therapeutic use*
  • Animals
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / economics
  • Antihypertensive Agents / pharmacokinetics
  • Antihypertensive Agents / therapeutic use*
  • Blood Pressure / drug effects
  • Cost-Benefit Analysis
  • Drug Costs
  • Drug Therapy, Combination
  • Heart Failure / diagnosis
  • Heart Failure / drug therapy*
  • Heart Failure / economics
  • Heart Failure / physiopathology
  • Humans
  • Hypertension / diagnosis
  • Hypertension / drug therapy*
  • Hypertension / economics
  • Hypertension / physiopathology
  • Nebivolol / adverse effects
  • Nebivolol / economics
  • Nebivolol / pharmacokinetics
  • Nebivolol / therapeutic use*
  • Treatment Outcome
  • Vasodilator Agents / adverse effects
  • Vasodilator Agents / economics
  • Vasodilator Agents / pharmacokinetics
  • Vasodilator Agents / therapeutic use*


  • Adrenergic beta-1 Receptor Agonists
  • Antihypertensive Agents
  • Vasodilator Agents
  • Nebivolol