Cerebral uptake of mefloquine enantiomers in fatal cerebral malaria.

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.

• Authors: Y T Pham, F Nosten, R Farinotti, N J White, F Gimenez
• Journal: International journal of clinical pharmacology and therapeutics (Int J Clin Pharmacol Ther) Vol. 37 Issue 1 Pg. 58-61 (Jan 1999) ISSN: 0946-1965 [Print] Germany
• PMID: 10027484 (Publication Type: Case Reports, Comparative Study, Journal Article)

Chemical References

• Mefloquine

Topics

• Autopsy
• Brain (metabolism)
• Fatal Outcome
• Female
• Humans
• Malaria, Cerebral (metabolism)
• Male
• Mefloquine (blood, pharmacokinetics)
• Stereoisomerism