Document Detail

Metabolic profile of nebivolol, a beta-adrenoceptor antagonist with unique characteristics.
MedLine Citation:
PMID:  17521213     Owner:  NLM     Status:  MEDLINE    
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.
Enrico Agabiti Rosei; Damiano Rizzoni
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Drugs     Volume:  67     ISSN:  0012-6667     ISO Abbreviation:  Drugs     Publication Date:  2007  
Date Detail:
Created Date:  2007-05-24     Completed Date:  2007-08-10     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  7600076     Medline TA:  Drugs     Country:  New Zealand    
Other Details:
Languages:  eng     Pagination:  1097-107     Citation Subset:  IM    
Department of Medical and Surgical Sciences, Clinica Medica, University of Brescia, Brescia, Italy.
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MeSH Terms
Adrenergic beta-Antagonists / pharmacology*,  therapeutic use
Antihypertensive Agents / pharmacology*,  therapeutic use
Antioxidants / pharmacology*,  therapeutic use
Benzopyrans / pharmacology*,  therapeutic use
Blood Glucose / drug effects
Cholesterol / blood
Clinical Trials as Topic
Diabetes Mellitus / metabolism
Dyslipidemias / complications,  metabolism
Endothelium, Vascular / drug effects,  physiopathology
Ethanolamines / pharmacology*,  therapeutic use
Heart Failure / complications
Hypertension / complications,  drug therapy
Lipids / blood
Nitric Oxide / biosynthesis
Oxidative Stress / drug effects
Vasodilation / drug effects
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Antioxidants; 0/Benzopyrans; 0/Blood Glucose; 0/Ethanolamines; 0/Lipids; 10102-43-9/Nitric Oxide; 57-88-5/Cholesterol; 99200-09-6/nebivolol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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