Food intake increases the relative oral bioavailability of vanoxerine.

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. 1993 The British Pharmacological Society