Disposition of venlafaxine enantiomers in rats with hepatic encephalopathy after chronic drug treatment.
Details
Serval ID
serval:BIB_7655A9D32B64
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Disposition of venlafaxine enantiomers in rats with hepatic encephalopathy after chronic drug treatment.
Journal
Chirality
ISSN
0899-0042 (Print)
ISSN-L
0899-0042
Publication state
Published
Issued date
2002
Peer-reviewed
Oui
Volume
14
Number
4
Pages
347-350
Language
english
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Publication Status: ppublish
Abstract
Portacaval shunted (PCS) rats, a model of hepatic encephalopathy, and control animals were administered racemic venlafaxine for 14 days (10 mg/kg). The levels of the S- and R-enantiomers and the S/R-enantiomer ratios of venlafaxine and its metabolites were assessed by an enantiomer-selective chromatographic assay in serum, brain parenchyma, and brain dialysate of both groups. Higher levels of the S- and R-enantiomers of venlafaxine were found in serum and brain of PCS vs. normal rats (median values of S- and R-venlafaxine in serum: 290 and 201 nM in PCS; 97 and 66 nM in normal rats; median values of S- and R-venlafaxine in cortex: 956 and 939 nM in PCS; 357 and 318 nM in normal rats). Interestingly, similar S/R-venlafaxine ratios were observed in PCS and normal rats both in serum (S/R = 1.4) and brain compartments (S/R = l.0-1.1). These findings may have clinical relevance for the safety of venlafaxine in chronic hepatic encephalopathy.
Keywords
Animals, Antidepressive Agents, Second-Generation/administration & dosage, Antidepressive Agents, Second-Generation/chemistry, Brain/metabolism, Cyclohexanols/administration & dosage, Cyclohexanols/chemistry, Disease Models, Animal, Hepatic Encephalopathy/drug therapy, Hepatic Encephalopathy/metabolism, Humans, Male, Portacaval Shunt, Surgical, Rats, Rats, Sprague-Dawley, Safety, Stereoisomerism
Pubmed
Web of science
Create date
10/03/2008 10:53
Last modification date
20/08/2019 14:33