Publication: Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria
Issued Date
1999-01-28
Resource Type
ISSN
09461965
Other identifier(s)
2-s2.0-0032896317
Rights
Mahidol University
Rights Holder(s)
SCOPUS
Bibliographic Citation
International Journal of Clinical Pharmacology and Therapeutics. Vol.37, No.1 (1999), 58-61
Suggested Citation
Y. T. Pham, F. Nosten, R. Farinotti, N. J. White, F. Gimenez Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria. International Journal of Clinical Pharmacology and Therapeutics. Vol.37, No.1 (1999), 58-61. Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/25690
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Title
Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria
Author(s)
Abstract
Patients 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.