Nebivolol and valsartan as a fixed-dose combination for the treatment of hypertension

Abstract

Introduction: The fixed-dose combination of nebivolol and valsartan drug has been clinically evaluated and demonstrated to represent a unique combination of nebivolol, a selective β₁-adrenoceptor antagonist and a β₃-adrenoceptor agonist; β₃ receptor activation increases endothelial nitric oxide and produces vasodilation. Valsartan is highly selective angiotensin AT₁ receptor blocker and exerts its major pharmacological effect by decreasing angiotensin II-induced vasoconstriction and production of aldosterone. The addition of nebivolol counteracts the effects of increased angiotensin II concentrations resulting from potent AT₁ blockade. This review describes a recently completed trial establishing the efficacy of the nebivolol/valsartan combination.

Areas covered: This review provides a literature search of pertinent pharmacological and clinical data that describes the mechanisms of both drugs individually and the results of a clinical trial comparing fixed-dose combinations of nebivolol with valsartan as compared with each drug as monotherapy.

Expert opinion: Fixed-dose combination drugs are intended to improve patient compliance and reduce drug costs, as well as to reduce long-term cardiovascular event rates and block counter-regulatory effects due to monotherapy. The vast majority of hypertensive patients will require at least two medications. We believe that the clinical evidence suggests that the combination of nebivolol with valsartan offers a definite clinical benefit, combining β₁-adrenoceptor and angiotensin AT₁ receptor blockade with β₃ receptor activation and resultant increase in nitric oxide and vasodilation.

Keywords:

• β-blockers
• nebivolol/valsartan
• renin-angiotensin-aldosterone system drugs
• single-pill combination

Declaration of interest

GE Sander has acted as a speaker for Forest Laboratories. Thomas Giles has received research support and consulting fees from Forest Laboratories. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

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