Y. T. PhamF. NostenR. FarinottiN. J. WhiteF. GimenezUniversite Paris-Sud XIShoklo Malaria Research UnitMahidol UniversityJohn Radcliffe HospitalHopital Necker Enfants Malades2018-09-072018-09-071999-01-28International Journal of Clinical Pharmacology and Therapeutics. Vol.37, No.1 (1999), 58-61094619652-s2.0-0032896317https://repository.li.mahidol.ac.th/handle/20.500.14594/25690Patients and methods: The brain disposition of the enantiomers of the antimalarial mefloquine was studied in two postmortem human cerebral biopsies after oral administration of the racemic mixture. Background: Mefloquine (MQ) is an effective antimalarial drug used both for prophylaxis and treatment of chloroquine resistant Plasmodium falciparum. MQ is generally well tolerated in treatment. Minor side-effects have been described. Potentially serious neuropsychiatric reactions occur. The mechanism underlying the neurotoxicity is unknown, although a dose relationship is evidently involved. Results: Mefloquine enantiomer concentrations were determined using a chiral liquid chromatographic method. Mefloquine concentrations were higher in brain compared to plasma. Studied in one patient, white matter concentrations were higher compared to grey matter concentrations. Conclusion: Based on the ratios brain concentration/plasma concentration, the brain penetration of the (+) enantiomer is much higher than that of the (-) enantiomer.Mahidol UniversityMedicinePharmacology, Toxicology and PharmaceuticsArticleSCOPUS