Pharmacokinetics and initial distribution of a new neuroleptic agent picobenzide (M-14012-4).

The pharmacokinetics of picobenzide was studied in 14 adult patients undergoing neuroleptoanalgesic sessions. The dose of picobenzide administered was 10 mg/kg by i.v. injection. The pharmacokinetic parameters obtained revealed a good distribution capacity with an average value of the apparent distribution volume at steady state of 28.29 +/- 4.98 1. The drug was also seen to be eliminated rapidly from the organism with an average value of the serum half-life of 2.05 +/- 0.42 h. The determination of the initial distribution kinetics of picobenzide shows that the use of a conventional kinetic model induces an overestimation of the initial distribution volume in turn caused by an underestimation of the initial serum concentration.