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


METHODS
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.


CONCLUSIONS
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.
Tulane University School of Medicine, From the Heart and Vascular Institute, Department of Medicine , 1430 Tulane Ave, New Orleans, LA 70112 , USA tgiles4@cox.net.
Gary E
GE
Sander
Thomas D
TD
Giles
D058671:Adrenergic beta-1 Receptor Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D058667:Adrenergic beta-3 Receptor Agonists / Q000494:pharmacology / Q000627:therapeutic use*; D047228:Angiotensin II Type 1 Receptor Blockers / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D004338:Drug Combinations; D004983:Ethanolamines / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D000068577:Nebivolol; D013777:Tetrazoles / Q000494:pharmacology / Q000627:therapeutic use*; D014633:Valine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D000068756:Valsartan
D058671:Adrenergic beta-1 Receptor Antagonists; D058667:Adrenergic beta-3 Receptor Agonists; D047228:Angiotensin II Type 1 Receptor Blockers; D001578:Benzopyrans; D004338:Drug Combinations; D004983:Ethanolamines; D013777:Tetrazoles; D000068577:Nebivolol; D000068756:Valsartan; D014633:Valine
nebivolol/valsartan; renin-angiotensin-aldosterone system drugs; single-pill combination; β-blockers