caa a22 4500 477056717 CHVBK 20180405111347.0 cr unu---uuuuu 170330e19961001xx s 000 0 eng 10.1007/s002280050180 doi (NATIONALLICENCE)springer-10.1007/s002280050180 Comparison between concentrations of racemic mefloquine, its separate enantiomers and the carboxylic acid metabolite in whole blood serum and plasma [Elektronische Daten] [U. Hellgren, J. Jastrebova, M. Jerling, B. Krysén, Y. Bergqvist] Objective: To compare concentrations of the separate enantiomers of mefloquine (MQ), total racemic MQ and the carboxylic acid metabolite in different blood fractions at steady state. Setting: Human volunteer laboratory, Unit of Clinical Pharmacology, Karolinska Institute. Volunteers: Ten healthy adult Caucasian volunteers. Methods: Drug concentrations were determined by high-performance liquid chromatography (HPLC). Results: Trough concentrations of the (+)RS enantiomer were higher in venous whole blood than in plasma and serum (mean ratios, 1.41 and 1.38). For the other enantiomer, (−)SR, concentrations were lower in whole blood than in plasma (mean ratio 0.89) and for the metabolite this ratio was 0.5. Conclusion: Stereoselective distribution might be important for antimalarial activity and should be considered when pharmacokinetic studies are performed. Springer-Verlag Berlin Heidelberg, 1996 Key words Mefloquine nationallicence mefloquine enantiomers nationallicence carboxylic acid metabolite nationallicence blood concentrations nationallicence pharmacokinetics nationallicence healthy volunteers nationallicence Hellgren U. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut Jastrebova J. Department of Clinical Chemistry, Falun Central Hospital, Falun, Sweden, SE aut Jerling M. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut Krysén B. Department of Clinical Chemistry, Falun Central Hospital, Falun, Sweden, SE aut Bergqvist Y. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut https://doi.org/10.1007/s002280050180 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050180 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Hellgren U. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut NATIONALLICENCE 700 1- Jastrebova J. Department of Clinical Chemistry, Falun Central Hospital, Falun, Sweden, SE aut NATIONALLICENCE 700 1- Jerling M. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut NATIONALLICENCE 700 1- Krysén B. Department of Clinical Chemistry, Falun Central Hospital, Falun, Sweden, SE aut NATIONALLICENCE 700 1- Bergqvist Y. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, SE aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer