PMID: 8471409Mar 1, 1993Paper

Food intake increases the relative oral bioavailability of vanoxerine

British Journal of Clinical Pharmacology
S H IngwersenJ J Larsen

Abstract

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.

References

Aug 1, 1977·Journal of Pharmacokinetics and Biopharmaceutics·P G Welling
Aug 3, 1989·European Journal of Pharmacology·P H Andersen

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Citations

Apr 5, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·E M PerssonB Abrahamsson
May 28, 2011·Journal of Cardiovascular Electrophysiology·Ivan CakulevAlbert L Waldo
Oct 13, 2009·Journal of Cardiovascular Electrophysiology·Antonio E LacerdaArthur M Brown
Oct 13, 2009·Journal of Cardiovascular Electrophysiology·Naomichi MatsumotoAlbert L Waldo
Jan 16, 2009·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Anne GardinSilke Appel-Dingemanse

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