Metabolic profile of nebivolol, a beta-adrenoceptor antagonist with unique characteristics.
beta-Adrenoceptor antagonists (beta-blockers) have historically been considered an effective and safe option for first-line treatment of hypertension. However, very recently, it has been proposed that beta-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 beta(1)-blocker with additional endothelial nitric oxide (NO)-mediated vasodilating activity, confirms previous findings that this drug differs from other beta-blockers. The combined mechanisms of beta-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 beta-blockers such as atenolol, metoprolol or bisoprolol. Therapeutic indications for beta-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 beta-adrenoceptor therapy.
Agabiti Rosei
Enrico
E
Department of Medical and Surgical Sciences, Clinica Medica, University of Brescia, Brescia, Italy. agabiti@med.unibs.it
Rizzoni
Damiano
D
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D000959:Antihypertensive Agents / Q000494:pharmacology* / Q000627:therapeutic use; D000975:Antioxidants / Q000494:pharmacology* / Q000627:therapeutic use; D001578:Benzopyrans / Q000494:pharmacology* / Q000627:therapeutic use; D001786:Blood Glucose / Q000187:drug effects; D002784:Cholesterol / Q000097:blood; D002986:Clinical Trials as Topic; D003920:Diabetes Mellitus / Q000378:metabolism; D050171:Dyslipidemias / Q000150:complications / Q000378:metabolism; D004730:Endothelium, Vascular / Q000187:drug effects / Q000503:physiopathology; D004983:Ethanolamines / Q000494:pharmacology* / Q000627:therapeutic use; D006333:Heart Failure / Q000150:complications; D006801:Humans; D006973:Hypertension / Q000150:complications / Q000188:drug therapy; D008055:Lipids / Q000097:blood; D000068577:Nebivolol; D009569:Nitric Oxide / Q000096:biosynthesis; D018384:Oxidative Stress / Q000187:drug effects; D014664:Vasodilation / Q000187:drug effects
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D000975:Antioxidants; D001578:Benzopyrans; D001786:Blood Glucose; D004983:Ethanolamines; D008055:Lipids; D000068577:Nebivolol; D009569:Nitric Oxide; D002784:Cholesterol