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Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses

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 adjus...

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Autores principales: Wernsdorfer, Walther H, Noedl, Harald, Rendi-Wagner, Pamela, Kollaritsch, Herwig, Wiedermann, Gerhard, Mikolasek, Andrea, Karbwang, Juntra, Na-Bangchang, Kesara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901017/
https://www.ncbi.nlm.nih.gov/pubmed/24321055
http://dx.doi.org/10.1186/1475-2875-12-443
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author Wernsdorfer, Walther H
Noedl, Harald
Rendi-Wagner, Pamela
Kollaritsch, Herwig
Wiedermann, Gerhard
Mikolasek, Andrea
Karbwang, Juntra
Na-Bangchang, Kesara
author_facet Wernsdorfer, Walther H
Noedl, Harald
Rendi-Wagner, Pamela
Kollaritsch, Herwig
Wiedermann, Gerhard
Mikolasek, Andrea
Karbwang, Juntra
Na-Bangchang, Kesara
author_sort Wernsdorfer, Walther H
collection PubMed
description 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. CONCLUSION: 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.
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spelling pubmed-39010172014-01-25 Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses Wernsdorfer, Walther H Noedl, Harald Rendi-Wagner, Pamela Kollaritsch, Herwig Wiedermann, Gerhard Mikolasek, Andrea Karbwang, Juntra Na-Bangchang, Kesara Malar J Research 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. CONCLUSION: 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. BioMed Central 2013-12-09 /pmc/articles/PMC3901017/ /pubmed/24321055 http://dx.doi.org/10.1186/1475-2875-12-443 Text en Copyright © 2013 Wernsdorfer et al.; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Research
Wernsdorfer, Walther H
Noedl, Harald
Rendi-Wagner, Pamela
Kollaritsch, Herwig
Wiedermann, Gerhard
Mikolasek, Andrea
Karbwang, Juntra
Na-Bangchang, Kesara
Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title_full Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title_fullStr Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title_full_unstemmed Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title_short Gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
title_sort gender-specific distribution of mefloquine in the blood following the administration of therapeutic doses
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3901017/
https://www.ncbi.nlm.nih.gov/pubmed/24321055
http://dx.doi.org/10.1186/1475-2875-12-443
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