Document Detail


Nebivolol: pharmacologic profile of an ultraselective, vasodilatory beta1-blocker.
MedLine Citation:
PMID:  18083889     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Beta-blockers are well-established therapeutic agents in the treatment of hypertension and cardiovascular disease. However, these agents are highly heterogeneous. Beta-blockers differ in their ancillary pharmacologic properties, which are clinically important. Nebivolol is a highly selective beta(1)-adrenergic receptor blocker that induces vasodilation through stimulation of the endothelial nitric oxide/L-arginine pathway. As a racemic mixture of d- and l-enantiomers, nebivolol is highly lipophilic and rapidly absorbed. Nebivolol undergoes extensive hepatic metabolism through the cytochrome P450 2D6 (CYP2D6) system. As a result of genetic polymorphisms, CYP2D6 has variable activity, manifested by extensive and poor metabolizers of nebivolol. Time to maximum concentration is 0.5 to 2 hours, and half-life is 11 hours in extensive metabolizers; these values are about 3 times longer in poor metabolizers. Urinary and fecal excretion of unchanged nebivolol is less than 0.5% of the dose. Nebivolol has a unique hemodynamic profile of reduced systemic vascular resistance and increased left ventricular function. These properties are attributed to its vasodilating action and contrast with the hemodynamic effects of conventional beta-blockers. Nebivolol is thus a novel beta-blocker with several important pharmacologic properties that distinguish it from traditional beta-blockers. These unique properties may confer clinical benefits beyond simple blood pressure lowering.
Authors:
L Michael Prisant
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2007-12-14
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  48     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2008 Feb 
Date Detail:
Created Date:  2008-01-17     Completed Date:  2008-05-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  225-39     Citation Subset:  IM    
Affiliation:
Hypertension and Clinical Pharmacology, Medical College of Georgia, 1467 Harper Street, HB 2010, Augusta, GA 30912, USA. mprisant@mcg.edu
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MeSH Terms
Descriptor/Qualifier:
Adrenergic beta-Antagonists / chemistry,  pharmacology*
Animals
Antioxidants / chemistry,  pharmacology
Benzopyrans / chemistry,  pharmacology*
Ethanolamines / chemistry,  pharmacology*
Humans
Molecular Structure
Platelet Aggregation Inhibitors / chemistry,  pharmacology
Receptors, Adrenergic, beta-1 / antagonists & inhibitors*
Stereoisomerism
Vasodilator Agents / chemistry,  pharmacology*
Chemical
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Antioxidants; 0/Benzopyrans; 0/Ethanolamines; 0/Platelet Aggregation Inhibitors; 0/Receptors, Adrenergic, beta-1; 0/Vasodilator Agents; 99200-09-6/nebivolol

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


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