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
Author(s)
Wikell C., Eap C.B., Josefsson M., Apelqvist G., Ahlner J., Baumann P., Bengtsson F.
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
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
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