Comparison between concentrations of racemic mefloquine, its separate enantiomers and the carboxylic acid metabolite in whole blood serum and plasma.
OBJECTIVE
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.


METHODS
Human volunteer laboratory, Unit of Clinical Pharmacology, Karolinska Institute.


METHODS
Ten healthy adult Caucasian volunteers.


METHODS
Drug concentrations were determined by high-performance liquid chromatography (HPLC).


RESULTS
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.


CONCLUSIONS
Stereoselective distribution might be important for antimalarial activity and should be considered when pharmacokinetic studies are performed.
Hellgren
U
U
Unit of Tropical Pharmacology, Huddinge Hospital, Sweden.
Jastrebova
J
J
Jerling
M
M
Krysén
B
B
Bergqvist
Y
Y
D000328:Adult; D002264:Carboxylic Acids / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D008297:Male; D015767:Mefloquine / Q000097:blood*; D008875:Middle Aged; D010949:Plasma / Q000378:metabolism*; D013237:Stereoisomerism
D002264:Carboxylic Acids; D015767:Mefloquine