Pharmacokinetics of trimeprazine in children

Abstract

The pharmacokinetics of trimeprazine (alimemazine) were studied over 24 hr in six children after a recommended preanaesthetic oral dose of 3 mg.kg-1. The degree of sedation before anaesthesia was evaluated. Median maximal venous blood drug concentration was 0.357 mumols.1(-1), 1-2 hr after oral ingestion, half-life 6.8 hr and AUC0-infinity h 2.758 mumols.1(-1) hr. Assuming 100 per cent bioavailability, blood clearance was estimated to median 3.7 1.kg-1.hr-1. Trimeprazine concentrations in cerebrospinal fluid (CSF) and in venous blood were compared in three other children, measured by gas chromatography. No trimeprazine was detected in the cerebrospinal fluid. We found a rough correlation between preanaesthetic sedation and blood trimeprazine concentrations. The kinetic parameters showed substantial interindividual differences, and accordingly, major interindividual variations in drug response might be anticipated even on standardized dosage regimens.