title: Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses.
abstract: BACKGROUND
  The objectives of the study were to elucidate the gender-specific distribution of mefloquine in cellular and fluid blood compartments when given at therapeutic dosage, to assess its correlation with the occurrence of treatment-related adverse events, and to explore the necessity of adjusting treatment guidelines for females.
  
  
  METHODS
  The distribution of mefloquine following the administration of standard therapeutic doses (1,250 mg mefloquine in split dose) to 22 healthy Caucasian volunteers was assessed in whole blood, serum, plasma, red blood cells (RBCs), white blood cells, and platelets using high performance liquid chromatography.
  
  
  RESULTS
  Plasma mefloquine concentrations after 14 hours were considerably higher in female subjects than in males (2,778 vs 1,017 ng/ml at H14), concordant with a significantly higher frequency, duration, and severity of adverse reactions. However, mean drug concentrations of RBC appeared slightly higher in male volunteers (857 vs 719 ng/ml). At H48, a similar situation prevailed, and at H168 the mefloquine concentrations in plasma continued to be higher in females compared to males (1,353 vs 666 ng/ml), while the concentrations of RBC were similar in females (389 vs 375 ng/ml). Since the observations relate to healthy individuals, they do not take into account selective uptake of mefloquine by Plasmodium-infected erythrocytes as in the case of therapeutic drug use.
  
  
  CONCLUSIONS
  Although plasma mefloquine concentrations in female healthy volunteers are considerably higher and the concentrations of the RBCs are initially lower compared to males, they do not seem to justify an adjustment of treatment guidelines for mefloquine in female Caucasian individuals.
authors: Walther H
authors: WH
authors: Wernsdorfer
authors: Harald
authors: H
authors: Noedl
authors: Pamela
authors: P
authors: Rendi-Wagner
authors: Herwig
authors: H
authors: Kollaritsch
authors: Gerhard
authors: G
authors: Wiedermann
authors: Andrea
authors: A
authors: Mikolasek
authors: Juntra
authors: J
authors: Karbwang
authors: Chulabhorn International College of Medicine, Thammasat University, Rangsit Campus, Pathumthani, Thailand. kesaratmu@yahoo.com.
authors: Kesara
authors: K
authors: Na-Bangchang
mesh_terms: D000328:Adult; D000962:Antimalarials / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001773:Blood Cells / Q000737:chemistry*; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D008297:Male; D015767:Mefloquine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D008875:Middle Aged; D010949:Plasma / Q000737:chemistry*; D011247:Pregnancy; D012737:Sex Factors; D044465:White People; D055815:Young Adult
chemical_list: D000962:Antimalarials; D015767:Mefloquine