11. Protein Binding of Drugs

  1. Ming Hu3 and
  2. Xiaoling Li4
  1. Antonia Kotsiou1 and
  2. Christine Tesseromatis2

Published Online: 5 JUL 2011

DOI: 10.1002/9781118067598.ch11

Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications

Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications

How to Cite

Kotsiou, A. and Tesseromatis, C. (2011) Protein Binding of Drugs, in Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications (eds M. Hu and X. Li), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118067598.ch11

Editor Information

  1. 3

    Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, 1441 Moursund Street, Houston, TX 77030, USA

  2. 4

    Department of Pharmaceutics and Medicinal Chemistry, Thomas J. Long School of Pharmacy and Health Sciences, University of the Pacific, Stockton, CA 95211, USA

Author Information

  1. 1

    Department of Pharmacology, Aretaieion University Hospital, Vas. Sophias 76, 11528, Athens, Greece

  2. 2

    Department of Pharmacology, Medical School, Athens University, M. Assias 75, 11527, Athens, Greece

Publication History

  1. Published Online: 5 JUL 2011
  2. Published Print: 15 AUG 2011

Book Series:

  1. Wiley Series in Drug Discovery and Development

Book Series Editors:

  1. Binghe Wang

ISBN Information

Print ISBN: 9780470260999

Online ISBN: 9781118067598



  • drug protein binding, physicochemical interactions - drugs, and silent transporter molecules;
  • diseases, influencing drug–protein binding - plasma proteins levels, altered in disease states;
  • protein and tissue binding, on pharmacokinetic parameters - volume of distribution


This chapter contains sections titled:

  • Introduction

  • Factors related to albumin

  • Factors related to endogenous substances

  • Factors related to exogenous substances

  • Diseases influence drug–protein binding

  • Estimation of the extent of serum protein binding

  • Tissue binding of drugs

  • Impact of protein and tissue binding on pharmacokinetic parameters

  • Pharmacological and pharmacokinetic importance of protein- and tissue-bound drug displacement interactions

  • Conclusion

  • References