Document Detail


Food intake increases the relative oral bioavailability of vanoxerine.
MedLine Citation:
PMID:  8471409     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Each of 12 healthy male subjects received single oral doses of 100 mg vanoxerine (GBR 12909), a dopamine reuptake inhibitor with potential antidepressant activity, on three different occasions (fasting, after a low-fat meal and after a high-fat meal) according to a randomized, cross-over design. The mean tmax value increased from 0.82 h after fasting to 1.44 h after a low-fat meal and to 2.46 h after a high-fat meal. Only modest food effects were seen on mean Cmax values (55 nM, 52 nM and 84 nM, after fasting, after the low-fat meal and after the high-fat meal, respectively) but values of AUC up to the last measurable concentration (AUC(0,t)) increased by 76% (from 110 to 194 nM h) after the low-fat meal and by 255% (from 110 to 391 nM h) after the high-fat meal compared with fasting. All of these effects were statistically significant except for the differences in tmax and Cmax between fasting and the low-fat meal. The mechanism of these changes is unclear, but it seems likely that food may lower the first-pass metabolism of vanoxerine, as has been shown for other lipophilic basic drugs.
Authors:
S H Ingwersen; T G Mant; J J Larsen
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Publication Detail:
Type:  Clinical Trial; Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  35     ISSN:  0306-5251     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  1993 Mar 
Date Detail:
Created Date:  1993-05-14     Completed Date:  1993-05-14     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  308-10     Citation Subset:  IM    
Affiliation:
Preclinical Development, Novo Nordisk A/S, Maaloev, Denmark.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Adult
Analysis of Variance
Biological Availability
Dietary Fats / administration & dosage
Eating*
Humans
Male
Neurotransmitter Uptake Inhibitors / administration & dosage,  pharmacokinetics*
Piperazines / administration & dosage,  pharmacokinetics*
Chemical
Reg. No./Substance:
0/Dietary Fats; 0/Neurotransmitter Uptake Inhibitors; 0/Piperazines; 67469-78-7/vanoxerine
Comments/Corrections

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