Stereoselective pharmacokinetics of mefloquine in young children.

OBJECTIVE

the stereospecificity of mefloquine pharmacokinetics in children has been investigated.

PATIENTS

Twelve children aged 6 to 24 months were treated for uncomplicated falciparum malaria with a single oral dose of 25 mg.kg-1 racemic mefloquine in combination with sulfadoxine and pyrimethamine.

METHODS

concentrations of mefloquine enantiomers were determined using a coupled achiral-chiral chromatographic system. Pharmacokinetic parameters were calculated using model-independent 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 the (+) enantiomer.

CONCLUSION

the stereoselectivity of mefloquine pharmacokinetics is similar to that observed in adults.