Disposition of venlafaxine enantiomers in rats with hepatic encephalopathy after chronic drug treatment.
(2002) In Chirality 14(4). p.347-350- 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... (More)
- 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. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/108451
- author
- Wikell, Cecilia LU ; Eap, Chin B ; Josefsson, Martin ; Apelqvist, Gustav ; Ahlner, Johan ; Baumann, Pierre and Bengtsson, Finn
- organization
- publishing date
- 2002
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Cyclohexanols : administration & dosage, Cyclohexanols : chemistry, Cyclohexanols : pharmacokinetics, Disease Models, Animal, Hepatic Encephalopathy : drug therapy, Hepatic Encephalopathy : metabolism, Human, Male, Portacaval Shunt, Rats, Surgical, Sprague-Dawley, Safety, Stereoisomerism, Brain : metabolism, Second-Generation : pharmacokinetics, Second-Generation : chemistry, Antidepressive Agents, Second-Generation : administration & dosage
- in
- Chirality
- volume
- 14
- issue
- 4
- pages
- 347 - 350
- publisher
- John Wiley & Sons Inc.
- external identifiers
-
- wos:000175043400013
- pmid:11968077
- scopus:0036226035
- ISSN
- 1520-636X
- DOI
- 10.1002/chir.10088
- language
- English
- LU publication?
- yes
- id
- 28cb06d2-45fd-4b58-8196-3e03276bd905 (old id 108451)
- alternative location
- http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11968077&dopt=Abstract
- date added to LUP
- 2016-04-01 12:10:58
- date last changed
- 2022-02-26 03:02:51
@article{28cb06d2-45fd-4b58-8196-3e03276bd905,
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.}},
author = {{Wikell, Cecilia and Eap, Chin B and Josefsson, Martin and Apelqvist, Gustav and Ahlner, Johan and Baumann, Pierre and Bengtsson, Finn}},
issn = {{1520-636X}},
keywords = {{Cyclohexanols : administration & dosage; Cyclohexanols : chemistry; Cyclohexanols : pharmacokinetics; Disease Models; Animal; Hepatic Encephalopathy : drug therapy; Hepatic Encephalopathy : metabolism; Human; Male; Portacaval Shunt; Rats; Surgical; Sprague-Dawley; Safety; Stereoisomerism; Brain : metabolism; Second-Generation : pharmacokinetics; Second-Generation : chemistry; Antidepressive Agents; Second-Generation : administration & dosage}},
language = {{eng}},
number = {{4}},
pages = {{347--350}},
publisher = {{John Wiley & Sons Inc.}},
series = {{Chirality}},
title = {{Disposition of venlafaxine enantiomers in rats with hepatic encephalopathy after chronic drug treatment.}},
url = {{http://dx.doi.org/10.1002/chir.10088}},
doi = {{10.1002/chir.10088}},
volume = {{14}},
year = {{2002}},
}