Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria
Pham, Y.T.; Nosten, F.; Farinotti, R.; White, N.J.; Gimenez, F.
International Journal of Clinical Pharmacology and Therapeutics 37(1): 58-61
1999
ISSN/ISBN: 0946-1965 PMID: 10027484 Document Number: 500726
The brain disposition of the enantiomers of the antimalarial mefloquine was studied in 2 post-mortem human cerebral biopsies after oral administration of the racemic mixture. Mefloquine (MQ) is an effective antimalarial drug used both for prophylaxis and treatment of chloroquine resistant Plasmodium falciparum. It is generally well tolerated although potentially serious neuropsychiatric reactions occur; the mechanism underlying this neurotoxicity is unknown, although a dose relationship is evidently involved. Mefloquine enantiomer concentrations were determined using a chiral liquid chromatographic method. Mefloquine concentrations were higher in brain compared to plasma. Examination in one patient showed that white matter concentrations were higher than grey matter concentrations. Based on the ratio brain concentration:plasma concentration, the brain penetration of the (+) enantiomer appears to be much higher than that of the (-) enantiomer.
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