A study was undertaken in seven schizophrenic patients to evaluate the tolerability and examine the pharmacokinetics of intramuscularly administered remoxipride after a single 200 mg dose and at steady state following repeated doses of 200 mg twice daily for one week. Comparisons of AUC, t1/2 and tmax using the Wilcoxon's signed rank test showed no significant difference between single dose and steady state indicating that the pharmacokinetics of intramuscular remoxipride were linear. The steady-state Cmax was found to be significantly larger than that after single dose and the increase was accounted for by the predicted accumulation factor, assuming linear kinetics. Although the inter-individual variability in plasma concentrations was large, the intra-individual variability was low as shown by the reproducibility of the single-dose and steady-state plasma curves. Remoxipride, administered intramuscularly, was well tolerated.