Nebivolol: An Appealing, Awaited and Nitric Oxide Potentiator Drug for the Treatment of Heart Failure

Abstract

Nebivolol is a third generation beta-blocker that possesses the highest selectivity for beta-1 receptors than beta-2 receptors than any other beta blocker in its class. Long-term therapy of nebivolol, in clinical trials, has been found to be very effective in increasing the left ventricular ejection fraction, reducing all-cause mortality, and reducing the New York Heart Association (NYHA) class of heart failure. The novelty of nebivolol exists in its unique nitric oxide potentiating effects in the myocardial and endothelial cells by the activation of beta-3 adrenergic receptors by which it produces most of its actions. It produces many useful effects and helps to abate the disease progression and prolongs the survival. In many clinical studies, it has been found to be safe and well tolerated. A literature search was made on PubMed database with the keywords: "Heart failure" , "Nebivolol" , and "beta-blocker" . A total of 176 articles were found and were the combination of review articles and research articles. A further selection of articles was made by the exclusion of non-relevant articles to achieve the objective of this review. It is approved for the treatment of hypertension in the United States and is under review by the federal agency, United States Food and Drugs Administration for the treatment of heart failure. This article sole intention is to review all the clinically important aspects of nebivolol on the basis of which nebivolol can be definitely considered for its inclusion in the drug therapy list for heart failure which will ease the individualization of drug therapy. This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

Nebivolol in the treatment of arterial hypertension

“…are dose‐dependent, cardio‐selective (relatively β 1 ‐selective) drugs, which thereby offer a more favourable side effect profile . Third‐generation drugs (nebivolol, carvedilol, labetalol) show additionally vasodilatory properties beyond the β‐blockade, and allegedly offer a better haemodynamic profile along with fewer unfavourable metabolic side effects . The common drugs vary in several other parameters regarding pharmacokinetics, intrinsic sympathetic activity (ISA) and in anti‐arrhythmic effects (often referred as "membrane stabilizing activity" (MSA)), that can be explained by additional targeting of cardiac and/or neuronal voltage‐gated sodium channels .…”

“…A standard 5 mg/day dose of nebivolol is admitted orally and absorbed within 1.5‐4 hours, unaffected by food intake. The bioavailability of the drug varies from 12% to 98% . In the blood, approx.…”

“…The therapeutic effect of nebivolol has been reported to be independent of the varying bioavailability, which is attributed to its active metabolites . The main route of excretion is through faeces and urine.…”

Hypertension and Type 2 Diabetes—The Novel Treatment Possibilities

“…On the contrary, not all β-blockers show such adverse effects on glucose homeostasis. Carvedilol, nebivolol, labetalol and third-generation β-blockers not only block β-adrenoreceptors, but also show additional properties promoting vasodilatation and resulting in less adverse effects on metabolism [ 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 ]. The Glycemic Effects in Diabetes Mellitus: Carvedilol-Metoprolol Comparison in Hypertensives (GEMINI) trial involved patients with T2D and hypertension.…”