Fansimef® is a new antimalarial combination containing pyrimethamine, sulfadoxine and mefloquine in the weight proportions 1+20+10. It has been designed to fight plasmodia resistant to the presently used antimalarial drugs and to counter the development of new resistant forms of the parasites. In the present study tablets containing 25 mg pyrimethamine, 500 mg sulfadoxine and 250 mg mefloquine were used. Six Brazilian volunteers received a loading dose of 2 tablets followed by 20 maintenance doses of 1 tablet at a dosage interval of 7 days. The pharmacokinetic evaluation of each of the three components was based on the assumption of an open linear two-compartment model. After the last maintenance dose the following kinetic parameters were determined for pyrimethamine, sulfadoxine and mefloquine, respectively: elimination half-life = 123, 179 and 550 h; volume of distribution in the postdistributive phase = 2.5, 0.15 and 18.6 1·kg-1, and total systemic clearance = 14.0, 0.64 and 24.0 ml·h-1·kg-1. All these values agree fairly well with those measured in previous single-dose kinetic studies. At steady state, Cmin values of each of the three components generally showed small variations. No unexpected accumulation of any of the three components was observed, indicating that induction or inhibition of metabolic enzymes did not occur during the trial.

Keywords:
Fansimef®, Mefloquine, Sulfadoxine, Pyrimethamine, Kinetics, Multiple doses, Malaria
This content is only available via PDF.
© 1987 S. Karger AG, Basel
1987
Copyright / Drug Dosage / Disclaimer
Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher.
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.
Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.
You do not currently have access to this content.