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Int J Clin Pharmacol Ther. 1999 Jan;37(1):58-61.

Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria.

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1
Faculté de Pharmacie, Pharmacie Clinique, Chatenay-Malabry, France.

Erratum in

  • Int J Clin Pharmacol Ther 1999 Jun;37(6):316.

Abstract

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.

PMID:
10027484
[Indexed for MEDLINE]
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