Nebivolol - A Review

Abstract

Hypertension is one of the major risk factor for cardiovascular disease especially ischemic heart disease and stroke. It impairs left ventricular systolic and diastolic function and thus becomes an important precursor of heart failure. A large number of cardiac death and hospitalization occurring in the elderly are due to hypertension. Pathophysiology of hypertension is characterized by endothelial dysfunction with impaired production of nitric oxide resulting in decreased vasodilatation. Nebivolol, a new highly selective beta blocker and antihypertensive agent has the potential to improve the endothelial dysfunction and improved nitric oxide production. Clinical studies have shown that it is effective and safe in controlling hypertension and chronic heart failure.Beta-blockers are frequently considered an effective and safe option for the first line treatment of hypertension. 1 However, recently they are no longer be considered for the first line therapy in uncomplicated hypertension because of unfavorable morbidity data. 2 Rather they should be used in post myocardial infarction, heart failure and atrial fibrillation and may be used in uncomplicated hypertension as a third or fourth line therapy. 3 Evidence shows that beta-blockers with or without diuretics were associated with greater number of cases of new onset diabetes mellitus than regimens based on ACE inhibitors, angiotensin receptor blockers or calcium antagonists. Nebivolol, a new third generation beta-blocker that differs from other beta-blockers such as atenolol, metoprolol or bisoprolol in that it is a highly selective beta-blocker with additional endothelial nitric oxide (NO)-mediated vasodilating activity. 6 In addition, it has anti-oxidant properties and favorable metabolic profile on both carbohydrate and lipid metabolism. 7 It significantly reduces triglycerides, total and LDL cholesterol. 8 It does not reduce insulin sensitivity like atenolol and it has no effect in the incidence of new onset of diabetes mellitus 9 . Fatigue, depression, bradycardia, erectile dysfunction worsening of cardiac contractility and bronchospasm are very low with nebivolol. 10 Nebivolol is a new beta blocker. It is a racemic mixture of dNebivolol and l-Nebivolol. The former (d-Nebivolol) has selective ß1-receptor blocking activity and the later (1-Nebivolol) has vasodilating property. Unlike other third generation ß-blockers, such as labetolol, carvedilol and bucindolol which mediate vasodilatory effect through alpha-1 adrenoreciptor antagonism, nebivolol mediate