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.
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: Britta Stadelmann; Tatiana Küster; Sabrina Scholl; Fabienne Barna; Christian Kropf; Jennifer Keiser; David W Boykin; Chad E Stephens; Andrew Hemphill Journal: Antimicrob Agents Chemother Date: 2011-07-18 Impact factor: 5.191
Authors: Aaron Janowsky; Amy J Eshleman; Robert A Johnson; Katherine M Wolfrum; David J Hinrichs; Jongtae Yang; T Mark Zabriskie; Martin J Smilkstein; Michael K Riscoe Journal: Psychopharmacology (Berl) Date: 2014-02-02 Impact factor: 4.530
Authors: Michael W Ferenczy; Leslie J Marshall; Christian D S Nelson; Walter J Atwood; Avindra Nath; Kamel Khalili; Eugene O Major Journal: Clin Microbiol Rev Date: 2012-07 Impact factor: 26.132