Nebivolol: a Different Beta-Blocker for Hypertension

Journal of Cardiology & Current Research

Nebivolol: A Different Beta-Blocker for Hypertension

Abstract Mini Review

Beta blockers are one of the classes of antihypertensive drugs, but there Volume 5 Issue 4 - 2016 are controversies of their use as an initial therapy in treatment of arterial hypertension based on different guidelines for treatment of arterial hypertension.

University Clinic of Cardiology, Medical Faculty, University Nebivolol is a third generation, highly selective β-adrenoceptor antagonist with “Sts. Cyril and Methodius”, Macedonia antihypertensive efficacy similar to other beta blockers but with unique function improvesof increasing arterial the releasecompliance of nitric and oxide reduces (NO) peripheral via activation vascular of β3-adrenergic resistance. *Corresponding author: Otljanska Magdalena, University Nebivololreceptors highly which selective improves lipophilic endothelial B1-adrenergic function, receptor produces antagonist vasodilatation, and B3 Clinic of Cardiology, Medical Faculty, University Campus agonist has different pharmacokinetics and pharmacodynamics profile from “Mother Theresa” – Skopje, Republic of Macedonia, Tel: +389 72 231 006; Email: [email protected] like side effect profile, beta receptors blockade affinity, vasodilating properties, other beta blockers with more favourable metabolic and hemodynamic profile, Received: March 20, 2016 | Published: April 19, 2016 effective beta blocker for treatment of mild to moderate arterial hypertension as monotherapyand improvement or in combination of endothelial therapy. function. Nebivolol has been show to be

Keywords: Beta Blockers, Nebivolol, Endothelial Function, Nitric Oxide

Introduction The goals of antihypertensive treatment in hypertensive patients is the maximum reduction in long-term total risk of

pressure and treatment of all associated reversible risk factors [1]. areBeta controversies blockers of have use beenof beta used blockers widely as an since initial 1970`s therapy in cardiovascular disease, requiring a reduction in raised blood treatment of arterial hypertension and in last few years there in treatment of arterial hypertension. Beta blockers for many have many differences in pharmacokinetic and pharmacodynamic Beta blockers are heterogenic group of antihypertensive drugs who of hypertension, but the last guidelines from JNC 8 and NICE improvement of endothelial function, sympathomimetic activity, guidelinesyears have frombeen 2011established put them as infirst the line second therapy line in of managementtreatment of profile like side effect profile, maintenance of exercise tolerance, (Figure 1). beta receptor blockade affinity, vasodilating properties etc. [2] arterial hypertension. When we look at the European guidelines for treatment of hypertension from 2013, we have to choose inhibitors,from the five calcium major antagonists,antihypertensive angiotensin drugs` classesreceptor as anblockers, initial therapy in which beta blockers are one of them: diuretics, ACE ability BP reduction in hypertension but they do differ in their abilityand B-blockers. to protect They against do not overall differ cardiovascular significantly for risk their of overallcause- infarction [1]( Table 1). specific cardiovascular events, such as stroke and myocardial Table 1: are indicated. Clinical conditions in hypertensive patient when beta blockers Previous stroke Figure 1: Mechanism of action of beta blockers. Any BP lowering agent Previous MI BB, ACE-I, ARB

Angina pectoris BB, CA Essential hypertension is a condition associated with Diuretics, BB, ACE-I, ARB, antialdosterone Heart failure endothelial dysfunction which is caused by production of oxygen agents free radicals that destroy nitric oxide and impair its beneficial and BB, non-dihydropiridine CA protectiveNebivolol effects is a onthird vessel generation wall [3,4] beta (Figure blocker, 2) . highly selective permanent Atrial fibrillation, Source: ESH/ESC Guidelines for the management of arterial hypertension hypertension and heart failure (in Europe). The third-generation 2013. beta-blockersβ adrenoceptor are antagonist distinguished indicated from the for earlier treatment classes of essential of beta-

blockers by their vasodilating activity. Nebivolol in essential Because many antihypertensive drugs especially beta blockers hypertension is indicated in mild or moderate hypertension alone affect erectile function, Nebivolol may be appropriate alternative or in combination therapy. Nebivolol is beta 1 antagonist and beta

in patients with erectile dysfunction [3,8]. receptors,3 agonist. improvingThis beta endothelialblocker have function, a unique producing function vasodilation, to increase Some study analyze the influence of Nebivolol on improvingthe release arterial of nitric compliance oxide (NO) and via reducing activation peripheral of β3-adrenergic vascular productionpostmenopausal and release. women, due to the possibility that some symptoms like hot flashes may be associated with decreased NO some central hemodynamic effects [5,6]. resistance. Due to its unique mechanism of action, nebivolol offers Conclusion Nebivolol is a third generation beta blocker indicated for

function to increase the release of nitric oxide (NO) via activation treatment of mild to moderate hypertension with a unique

of β3 adrenergic receptors. This unique mechanism of action may be reflected in nebivolol’s advantageous hemodynamic and othertolerability beta-blockers profile, compared and other with antihypertensive other beta-blockers. classes. Nebivolol has also demonstrated antihypertensive efficacy similar to that of References 1. Figure 2: (2013) 2013 ESH/ESC Guidelines for the management of arterial hypertension:Mancia G, Fagard the R,Task Narkiewicz Force for K, the Redón management J, Zanchetti of A,arterial et al. Endothelial dysfunction in hypertension. Nebivolol was hypertension of the European Society of Hypertension (ESH) and of first introduced in UK in 1999 for treatment of essential hypertension. the European Society of Cardiology (ESC). J Hypertens 31(7): 1281- proportions of “d” and “l” isomers. Nebivolol has 4 asymmetric 1357. centres,Nebivolol d-isomer is administered refers to (S,R,R,R)-nebivolol as a racemic mixture and l-isomer of equal to 2. (R,S,S,S)-nebivolol. Antihypertensive effects of nebivolol appear induced vasodilation. Vasc Health Risk Manag 2(3): 303-308. Weiss R (2006) Nebivolol: A Novel beta-blocker with Nitric Oxide– Nebivolol exhibits greater degree of beta 1/beta 2-receptor 3. (1994) Nitric oxide mediated to be greater with both isomers than with the d-isomer alone. venodilator effects of nebivolol. Br J Clin Pharmacol 38(3): 199-204. Bowman AJ, Chen CP, Ford GA 4. Tzemos N, Lim PO, MacDonald TM (2001) Nebivolol reverses The selectivity of Nebivolol on the beta 1-adrenergic receptor is selectivity compared with other commonly used beta-blockers. endothelial dysfunction in esential hypertension: a randomized, 321-fold higher than for beta 2-adrenergic receptor. Conventional doubleblind, crossover study. Circulation 104(5): 511-551. 5. McEniery CM, Schmitt M, Qasem A, Webb DJ, Avolio AP, et al. (2004) beta blockers are associated with unfavorable effects on metabolic Nebivolol increases arterial distensibility. Hypertension 44: 305- 310. agonisticparameters. activity Nebivolol on the has beta favorable 3 adrenoreceptor. metabolic This profile, beta withblocker no exhibitsdeleterious anti-proliferative effect on insulin and sensitivity antioxidant which properties may result [7]. from its 6. Maffei A, Lembo G (2009) Nitric oxide mechanism of Nebivolol. Ther Adv Cardiovasc Dis 3(4): 317-327. 7. bisoprololThe efficacy - Nebis and Study, tolerability metoprolol) of nebivolol and other have antihypertensive been evaluated B-adrenergic beta blocker. J Am Coll Cardiol 54(16): 1491-1499. Munzel T, Gori T (2009) Nebivolol: The Somewhat-different in comparison with placebo and other beta-blockers (atenolol, 8. Sahana GN, Sarala N, Kumar TN (2011) Nebivolol - pharmacological aspects. Int J Biol Med Res 2(2): 577-580. drugs. Nebivolol has good pressure–lowering effect in hypertensive patients (2838 pts) with type 2 diabetes mellitus-Yestono Study.

Citation: Otljanska M, Kostova N, Boshev M, Otljanski A (2016) Nebivolol: A Different Beta-Blocker for Hypertension. J Cardiol Curr Res 5(4): 00171. DOI: 10.15406/jccr.2016.05.00171