Document Detail

Nebivolol: pharmacologic profile of an ultraselective, vasodilatory beta1-blocker.
MedLine Citation:
PMID:  18083889     Owner:  NLM     Status:  MEDLINE    
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.
L Michael Prisant
Related Documents :
23685919 - The effect of seat shape on the risk of pressure ulcers using discomfort and interface ...
6106459 - Balance of noradrenaline and sodium during chronic beta-receptor blockade in patients w...
6290019 - Beta 2-mediated hypotension and myocardial injury.
6146329 - Antihypertensive effect and degree of beta-adrenoceptor blockade after short-term and s...
426949 - Baroreflex sensitivity in hypertension during beta-adrenergic blockade.
2061869 - Hemodynamic effects of atropine, dobutamine, nitroprusside, phenylephrine, and proprano...
18698219 - Arterial function and intima-media thickness in hypertensive patients with erectile dys...
491399 - Nephron obstruction in nordihydroguaiaretic acid-induced renal cystic disease.
2822279 - Enhanced responsiveness to carotid baroreceptor unloading in conscious dogs during deve...
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    
Hypertension and Clinical Pharmacology, Medical College of Georgia, 1467 Harper Street, HB 2010, Augusta, GA 30912, USA.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Adrenergic beta-Antagonists / chemistry,  pharmacology*
Antioxidants / chemistry,  pharmacology
Benzopyrans / chemistry,  pharmacology*
Ethanolamines / chemistry,  pharmacology*
Molecular Structure
Platelet Aggregation Inhibitors / chemistry,  pharmacology
Receptors, Adrenergic, beta-1 / antagonists & inhibitors*
Vasodilator Agents / chemistry,  pharmacology*
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

Previous Document:  N-glycan modification in Aspergillus species.
Next Document:  Mitochondrial metabolism, redox signaling, and fusion: a mitochondria-ROS-HIF-1alpha-Kv1.5 O2-sensin...