Published in:
01-06-2007 | Current Opinion
Metabolic Profile of Nebivolol, a β-Adrenoceptor Antagonist with Unique Characteristics
Authors:
Prof. Enrico Agabiti Rosei, Damiano Rizzoni
Published in:
Drugs
|
Issue 8/2007
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Abstract
β-Adrenoceptor antagonists (β-blockers) have historically been considered an effective and safe option for first-line treatment of hypertension. However, very recently, it has been proposed that β-blockers should no longer be considered suitable for first-line therapy in the patient with uncomplicated hypertension because of unfavourable morbidity and mortality data.
New evidence from recent clinical studies of nebivolol, a third-generation highly selective β1-blocker with additional endothelial nitric oxide (NO)-mediated vasodilating activity, confirms previous findings that this drug differs from other β-blockers. The combined mechanisms of β-adrenoceptor antagonism and NO-mediated vasodilation may potentiate the blood pressure-lowering effect of this agent, and confer a broader favourable metabolic profile, which may be clinically relevant for hypertensive patients. The antioxidant properties of nebivolol and its neutral or even favourable effects on both carbohydrate and lipid metabolism are well documented. These properties consistently differentiate nebivolol from nonvasodilating β-blockers such as atenolol, metoprolol or bisoprolol.
Therapeutic indications for β-blockers include a wide range of co-morbidities found in hypertensive patients, including ischaemic heart disease, tachyarrhythmias and heart failure. Given that the majority of hypertensive patients require more than one drug to control blood pressure, the multiple mechanisms of action and favourable metabolic profile of nebivolol could make it an alternative therapeutic option for hypertensive patients requiring β-adrenoceptor therapy.