The in vivo effects of increased free fatty acid (FFA) plasma levels on the protein binding of furosemide were investigated in 30 adult-onset diabetics and 22 patients suffering from bacterial infections (gram-negative bacilli and gram-positive cocci). In diabetics, FFA were 2.43 ± 1.63 mEq/l, and in subjects with bacterial infections 1.82 ± 0.92 mEq/l. Furthermore, the percent of oleic acid and, to a very lesser extent, palmitoleic acid increased linearly with the increase of the FFA plasma level. The free furosemide fraction was about 1 % or less in subjects with a molar ratio of FFA to albumin below 4, but a displacement of the drug from the plasma proteins occurred consistently when this ratio was above 4. At a molar ratio of FFA to albumin as high as 9.34, the free furosemide was 6.7% of the total concentration (8.9 μg/ml). These results do not quantitatively agree with previous in vitro studies employing single fatty acids and human serum albumin, suggesting that in vivo plasma composition is not adequately reproduced during in vitro experiments on protein-binding displacement of drugs by FFA.

Keywords:
Diabetes, Bacterial infection, Free fatty acids, Furosemide, Human serum albumin, Linoleic acid, Oleic acid, Palmitic acid, Palmitoleic acid, Stearic acid
This content is only available via PDF.
© 1982 S. Karger AG, Basel
1982
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.