title: Investigation of the in vitro gender-specific partitioning of mefloquine in malarial infected red blood cells and plasma.
abstract: The investigation of gender-specific partitioning of the antimalarial drug mefloquine to cellular and fluid blood compartments was performed using blood collected from a female and male healthy subject that were infected with Plasmodium falciparum PCM2 clone and spiked with mefloquine (0.25, 1, and 5 μM). Mefloquine concentrations in red cells of both female and male subjects were significantly higher than plasma, which suggests an intensive uptake by red cells. This was supported by a high ratio of mefloquine concentrations in the parasitized and non-parasitized red cells of about 4-fold. Gender-specific partitioning of mefloquine in parasitized blood was seen only in plasma where significantly higher concentrations were observed in female compared with male plasma. Down-adjusting the therapeutic dose of mefloquine in female patients with malaria is not advisable because mefloquine concentrations in the target cellular compartment are similar in both genders.
authors.affiliation: Chulabhorn International College of Medicine, Thammasat University, Rangsit Campus, Pathumthani, Thailand; Institute of Specific Prophylaxis and Tropical Medicine, Medical University of Vienna, Austria; Department of Clinical Product Development, Institute of Tropical Medicine, Nagasaki University, Nagasaki, Japan.
authors.forename: Nongluk
authors.initials: N
authors.lastname: Seethorn
authors.forename: Walther H
authors.initials: WH
authors.lastname: Wernsdorfer
authors.forename: Harald
authors.initials: H
authors.lastname: Noedl
authors.forename: Juntra
authors.initials: J
authors.lastname: Karbwang
authors.forename: Kesara
authors.initials: K
authors.lastname: Na-Bangchang
mesh_terms: D000962:Antimalarials / Q000737:chemistry*; D004912:Erythrocytes / Q000737:chemistry*; D005260:Female; D006801:Humans; D008297:Male; D015767:Mefloquine / Q000737:chemistry*; D010949:Plasma / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000737:chemistry*; D012737:Sex Factors
chemical_list: D000962:Antimalarials; D015767:Mefloquine