STEREOSELECTIVE PHARMACOKINETICS OF MEFLOQUINE IN YOUNG-CHILDREN

Objective: the stereospecificity of mefloquine pharmacokinetics in chi ldren has been investigated. Patients: Twelve children aged 6 to 24 mo nths were treated for uncomplicated falciparum malaria with a single o ral dose of 25 mg . kg(-1) racemic mefloquine in combination with sulf adoxine and pyrimethamine. Methods: concentrations of mefloquine enant iomers were determined using a coupled achiral-chiral chromatographic system. Pharmacokinetic parameters were calculated using model-indepen dent analysis. Results: Maximum plasma concentrations, areas under the curve and apparent plasma elimination half-lives were higher for the (-) enantiomer than its antipode. In contrast, the apparent volume of distribution (V/f) and total clearance (Cl/f) values were higher for t he (+) enantiomer. Conclusion: the stereoselectivity of mefloquine pha rmacokinetics is similar to that observed in adults.