Nebivolol is a third-generation beta-blocker that combines high beta-1 selectivity with nitric oxide-mediated vasodilation, offering effective blood pressure control with potentially fewer typical beta-blocker side effects.
May improve tolerability in select hypertensive patients; leaves open need for head-to-head RCTs.
Nebivolol is a highly selective β1 adrenoceptor blocker available clinically and is devoid of intrinsic sympathomimetic activity, inverse agonistic activity, and α1 receptor blocking properties along with peripheral vasodilatation and nitric oxide (NO) induced benefits such as antioxidant activity and reversal of endothelial dysfunction. Nebivolol is the racemic mixture of 2 isomers with 4 asymmetric centres. The d-isomer is the active b-blocking component, while the l-isomer is responsible for the release of nitric oxide. Nebivolol has a hemodynamic profile different from classic β receptor antagonists that iit acutely lowers arterial blood pressure without depressing left ventricular function, and reduces systemic vascular resistance. Nebivolol shown to inhibit platelet aggregation and thrombus formation, it has also an antiproliferative effects and reverses endothelial dysfunction in animal models of oxidative stress. Clinically, this compound has been proven to have antihypertensive and anti-ischemic effects as well as beneficial effects on hemodynamics. The tolerability of nebivolol has been shown to be superior to that of other beta blocker. Further studies are now necessary to compare the benefit of nebivolol with that of other drugs in the same class and to prove its claims of superiority and novelty of action, most importantly, its prognostic impact in patients with hypertension and its potential benefit in other comorbid conditions. Keywords- Nebivolol, β1 adrenoceptor blocker. Â
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Kumar et al. (2013) studied this question.
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