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Comparison between concentrations of racemic mefloquine, its separate enantiomers and the carboxylic acid metabolite in whole blood serum and plasma

  • PHARMACOKINETICS AND DISPOSITION
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Abstract

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.

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Authors and Affiliations

  1. Unit of Tropical Pharmacology, Division of Clinical Pharmacology and Infectious Diseases, Huddinge Hospital 73, Karolinska Institute, S-141 86 Huddinge, Sweden, , , , , , SE

    U. Hellgren, M. Jerling & Y. Bergqvist

  2. Department of Clinical Chemistry, Falun Central Hospital, Falun, Sweden, , , , , , SE

    J. Jastrebova & B. Krysén

Authors
  1. U. Hellgren
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  2. J. Jastrebova
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  3. M. Jerling
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  4. B. Krysén
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  5. Y. Bergqvist
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Additional information

Received: 12 September 1995/Accepted in revised form 26 January 1996

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Hellgren, U., Jastrebova, J., Jerling, M. et al. Comparison between concentrations of racemic mefloquine, its separate enantiomers and the carboxylic acid metabolite in whole blood serum and plasma. E J Clin Pharmacol 51, 171–173 (1996). https://doi.org/10.1007/s002280050180

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  • DOI: https://doi.org/10.1007/s002280050180

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