Tehran University of Medical Sciences Acta Medica Iranica 0044-6025 36 2 1998 12 15 133 137 E. Souri. H. Farsam F. Jamali 2015 09 28 Stereoselectivity of mefloquine enantiomers were studied in rats after oral administration of a single 50mg/Kg dose of the racemate. Pharmacokinetic parameters of (+)-(RS)-MFQ in blood and plasma showed no significant difference. The concentration, AUC , CLIF and VdlF of (+)-(RS)-enantiomerin blood were significantly higher than those for the (-)-(SR)-enantiomer. Tlie results obtained from this study showed a reverse stereoselectivity of MFQ as compared with what reported for human. A very low amount of enantiomers excreted in urine and the excretion was not stereoselective. A preliminary study in different blood fractions showed that the accumulation of MFQ enantiomers in blood cells is stereoselective with a tendency of ( + )-(RS)-enatiomer for leukocytes and (-)-(SR)-enantiomer for erythrocytes. https://acta.tums.ac.ir/index.php/acta/article/view/1758 https://acta.tums.ac.ir/index.php/acta/article/download/1758/1751