Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria.
PATIENTS AND METHODS: The brain disposition of the enantiomers of the antimalarial mefloquine was studied in two post-mortem human cerebral biopsies after oral administration of the racemic mixture. BACKGROUND: Mefloquine (MQ) is an effective antimalarial drug used both for prophylaxis and treatment...
| Main Authors: | , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
1999
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| Summary: | PATIENTS AND METHODS: The brain disposition of the enantiomers of the antimalarial mefloquine was studied in two post-mortem 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. |
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