Nebivolol: vasodilator properties and evidence for relevance in treatment of cardiovascular disease

Abstract

β-adrenergic blocking agents, a pharmacologically diverse class of cardiovascular medications, are recommended as first-line treatment for patients with hypertension and concomitant structural heart disease, and for angina and heart failure. Many within-class differences exist, from pharmacokinetics and pharmacodynamics to ancillary effects, such as intrinsic sympathomimetic activity, antiarrhythmic activity, α-1 adrenergic receptor blockade affinity, and direct vasodilation. Nebivolol is a third-generation, β1 selective, long acting β-blocker, which causes direct vasodilation via endothelium-dependent nitric oxide stimulation. The vasodilatory actions of nebivolol might result in clinical effects with some distinct properties. Differences from other β-blockers might include improvement of endothelial function, enhancement of forward flow in muscular resistance arteries, maintenance of exercise tolerance, and overall improved tolerability, side effect profile, and adherence. Nebivolol has been shown to be a clinically effective β-blocker for treatment as initial or add-on therapy for systemic hypertension, as an antianginal agent, and as therapy for patients with heart failure. These properties position nebivolol as a treatment option for patients with hypertension and/or structural heart disease, although its precise role in the therapeutic armamentarium remains to be clarified.