DISPOSITION OF CLEBOPRIDE AFTER INTRAVENOUS ADMINISTRATION

A pharmacokinetic study of clebopride, a new benzamide, was carried out within a phase I study. Plasma concentrations were measured using capillary gas chromatography with negative ion chemical ionisation mass spectrometry. The pharmacokinetic parameters are adequately described by a 2-compartment model with a terminal half-life of 9.5 +/- 3.9 (SD) hours and a volume of distribution in steady-state of 3.9 L/kg. The mean clearance was 5.2 ml/min/kg. The terminal half-life of the main active metabolite, N-desbenzyl-clebopride, is 1.5 +/- 1.0 (SD) hours. These results suggest that clebopride can be used as a single dose for chemotherapy-induced nausea and vomiting, due to its long half-life.