Abstract
To compare concentrations of the separate enantiomers of mefloquine (MQ), total racemic MQ and the carboxylic acid metabolite in different blood fractions at steady state. Human volunteer laboratory, Unit of Clinical Pharmacology, Karolinska Institute. Ten healthy adult Caucasian volunteers. Drug concentrations were determined by high-performance liquid chromatography (HPLC). Trough concentrations of the (+)RS enantiomer were higher in venous whole blood than in plasma and serum (mean ratios, 1.41 and 1.38). For the other enantiomer, (-)SR, concentrations were lower in whole blood than in plasma (mean ratio 0.89) and for the metabolite this ratio was 0.5. Stereoselective distribution might be important for antimalarial activity and should be considered when pharmacokinetic studies are performed.
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