Nebivolol for the treatment of heart failure

Dery, Allison S.; Hamilton, Leslie A.; Starr, Jessica

doi:10.2146/ajhp100309

Cited by 12 publications

(10 citation statements)

References 17 publications

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“…However, at the present time, only few studies have examined the role of cardiac β 1 - and β 2 -adrenoceptor (β-AR) subtypes in the pathogenesis of Dox-cardiotoxicity [9], [10] and only one study, at late-onset Dox-CM, assessed β 3 -AR subtype [11], which is recently described as a new target for some β-blockers such as nebivolol [12], [13]. Despite this lack in experimental data, some clinical studies investigated β-blocker therapies in Dox-CM.…”

Section: Introductionmentioning

confidence: 99%

Increased Beta2-Adrenoceptors in Doxorubicin-Induced Cardiomyopathy in Rat

et al. 2013

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BackgroundThe toxicity of doxorubicin, leading to an irreversible heart failure, limits its use as chemotherapeutic agent. The beneficial effects of early administration of β-blocker were reported in patients with heart failure due to doxorubicin, suggesting an important role of β-adrenoceptors (β-ARs). This study aimed to identify a putative target (β-AR and/or its effectors) at the early phase of a chronic doxorubicin-induced cardiomyopathy (Dox-CM) in a rat model.MethodologyDox-CM was induced by six doxorubicin injections (cumulative dose: 15 mg.kg−1) and validated by echocardiography and left ventricle (LV) catheterization. The β-AR protein expressions in LV were evaluated by western-blot at days 35 (d35) and 70 (d70) after the first doxorubicin injection. Ex vivo cardiac contractility (dP/dtmax, dP/dtmin) was evaluated on isolated heart in response to specific β-AR stimulations at d35.ResultsAt d35, Dox-CM hearts were characterized by mild LV systolic and diastolic dysfunctions, which were exacerbated at d70. In Dox-CM hearts, β3-AR expression was only decreased at d70 (-37±8%). At d35, β1-AR expression was decreased by 68±6%, but ex vivo β1-AR function was preserved due to, at least in part, an increased adenylyl cyclase response assessed by forskolin. β2-AR expression was increased both at d35 (+58±22%) and d70 (+174±35%), with an increase of ex vivo β2-AR response at d35. Inhibition of Gi protein with pertussis toxin did not affect β2-AR response in Dox-CM hearts, suggesting a decoupling of β2-AR to Gi protein.ConclusionThis study highlights the β1/β2-AR imbalance in early Dox-CM and reveals the important role that β2-AR/Gi coupling could play in this pathology. Our results suggest that β2-AR could be an interesting target at early stage of Dox-CM.

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Section: Introductionmentioning

confidence: 99%

Increased Beta2-Adrenoceptors in Doxorubicin-Induced Cardiomyopathy in Rat

et al. 2013

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“…This synthesis is catalyzed by an enzyme known as nitric oxide synthase. 14 There are three isoforms of this enzyme namely endothelial nitric oxide synthase (found in the cardiomyocytes and endothelial cells), neuronal nitric oxide synthase (found in the brain), and inducible nitric oxide synthase (found in macrophages). In this pathway, nitric oxide synthase cleaves the nitrogen from the guanidino group of arginine and subsequently form citrulline and NO.…”

Section: Dynamic Roles Of Nitric Oxide and Nebivolol As Its Potentiatormentioning

confidence: 99%

“…The production of nitric oxide by the NO synthase present in the endothelium is enhanced. 14,16 Moreover, in a study by Gauthier et al it was found that beta-3 adrenoreceptors are also present and functional in the heart and were responsible for the unexpected negative inotropic effects of epinephrine, norepinephrine, and was important in the pathophysiology of heart diseases and indeed, beta-3 receptors found to be important in the pathophysiology of different cardiovascular diseases including heart failure. 17 The effects of nebivolol actions on the heart are mediated via beta-3 receptors to release nitric oxide.…”

Section: Dynamic Roles Of Nitric Oxide and Nebivolol As Its Potentiatormentioning

confidence: 99%

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

Saini¹,

Wal²,

Verma³

et al. 2018

JYP

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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.

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“…Nevertheless, in oral drug delivery there is a need for innovative drug delivery systems due to low drug solubility, poor gastrointestinal absorption, metabolism related variability issues, continuous fluctuation of drug plasma levels and food effects [7,8]. Nebivolol is absorbed rapidly after oral administration and is not affected by food; however, it has variable absolute oral bioavailability due to its extensive first-pass metabolism [9]. Due to the low aqueous solubility and high membrane permeability, NBV is categorized as a Class II drug according to Biopharmaceutics Classification System [10].…”

Section: Introductionmentioning

confidence: 99%

Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet

Gökçe¹,

Kaynak²,

Yurdasiper³

et al. 2018

jrp

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ABSTRACT:The oral application of drugs is the most popular route for achieving systemic effects, nevertheless, it is limited by difficulties related to physicochemical properties of the drug. Solid lipid nanoparticles (SLNs) are appealing extensive notice because of showing increased solubility and improved oral bioavailability via different mechanisms. The aim of the study is to compare and peruse the in-situ permeation of nebivolol (NBV) loaded SLN and its commercial tablet formulation used for the treatment of hypertension. For this aim Single-Pass Intestinal Perfusion (SPIP) method was used for in-situ permeation studies. NBV loaded SLNs were prepared and modified with polyethylene glycol (PEG). In order to prepare SLNs by homogenization technique, compritol, lecithin and poloxamer were chosen. Particle sizes of blank and loaded SLN were 213.4±17.5 and 264.1±18.8 nm, respectively with polydispersity index values of approximately 0.3 for each. NBV loading resulted in positive electrical charge on SLNs. The encapsulation efficiency was 98.04±0.2 %. Permeability coefficient values were tripled when NBV was incorporated in SLNs and doubled when pure NBV was given separately with a blank SLN. PEG modified SLN can be used to enhance oral absorption of NBV, and SLNs alone can be used as permeation enhancer in oral drug delivery..

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Nebivolol for the treatment of heart failure

Cited by 12 publications

References 17 publications

Increased Beta2-Adrenoceptors in Doxorubicin-Induced Cardiomyopathy in Rat

Increased Beta2-Adrenoceptors in Doxorubicin-Induced Cardiomyopathy in Rat

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

Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet

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