Chemotherapy

Clinical Reports

Single Dose Kinetics of Mefloquine in Man

Plasma Levels of the Unchanged Drug and of One of Its Metabolites

Schwartz D.E.a · Eckert G.a · Hartmann D.a · Weber B.b · Richard-Lenoble D.c · Ekue J.M.K.d · Gentilini M.e

Author affiliations

aBiological Pharmaceutical Research Department, F. Hoffmann-La Roche & Co. Ltd., Basle. Switzerland; bClinical Unit, Hoffmann-La Roche Ltd., Grenzach-Wyhlen, FRG; cUniversity Centre of Health Sciences, Libreville, Gabon; dWHO Tropical Disease Research Centre, Ndola Central Hospital, Ndola, Zambia; eDépartement de Parasitologie et Médecine Tropicale, Hôpital Pitlé-Salpêtrière, Paris, France

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Chemotherapy 1982;28:70–84

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Article / Publication Details

First-Page Preview
Abstract of Clinical Reports

Published online: September 08, 2009
Issue release date: 1982

Number of Print Pages: 15
Number of Figures: 0
Number of Tables: 0

ISSN: 0009-3157 (Print)
eISSN: 1421-9794 (Online)

For additional information: https://www.karger.com/CHE

Abstract

Oral single dose kinetics of mefloquine was investigated in 16 male volunteers, 3 Caucasians and 13 African natives. Unchanged mefloquine (= M) and one of its metabolites (= MM) were measured in the plasma. The apparent half-life of absorption of M ranged from 0.36 to 2.0 h, its terminal half-life of elimination from 15 to 33 days. Assuming complete systemic availability, an apparent volume of distribution of 14–29 liters kg-1 and a total clearance of 18–39 ml min-1 were derived. MM given orally to mice or rats showed at equal dose the same tolerance as mefloquine. Following oral administration of M to man, plasma levels of MM surpassed those of M, resulting in a 2.4–5.1 larger AUC. However, because of its much smaller apparent volume of distribution, MM may be anticipated to represent only a small percentage of the dose and therefore to contribute only to a minor extent towards the unwanted side effects of the drug.

© 1982 S. Karger AG, Basel




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Article / Publication Details

First-Page Preview
Abstract of Clinical Reports

Published online: September 08, 2009
Issue release date: 1982

Number of Print Pages: 15
Number of Figures: 0
Number of Tables: 0

ISSN: 0009-3157 (Print)
eISSN: 1421-9794 (Online)

For additional information: https://www.karger.com/CHE


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Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug.
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