The effects of in vitro carbamylation of plasma with potassium cyanate on the binding of sulfisoxazole and diazepam have been investigated. Incubation of plasma with potassium cyanate produced varying degrees of carbamylation of plasma proteins which were associated with a decrease in the binding of sulfisoxazole (100 mg/l), a drug bound to site I on the human albumin. Scatchard plots showed that this decreased binding resulted from a decrease in affinity without changes in the number of binding sites. Similar changes were detected in uremia. Carbamylation of plasma proteins did not affect the binding of diazepam (3 mg/l), a drug bound to site II. The plasma protein binding of sulfisoxazole and diazepam was decreased in samples from uremic patients. Charcoal treatment did not modify the binding of sulfisoxazole to normal or carbamylated plasma while it reduced, but did not normalize, the binding defect in uremic plasma. On the other hand, charcoal treatment brought the binding of diazepam in uremic plasma to normal values. It seems that only drug binding site I is carbamylated in uremia, while competitive displacers bind to sites I and II.

This content is only available via PDF.
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.