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Competition between Drugs and Normal Substrates for Plasma and Tissue Binding Sites

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Concepts in Biochemical Pharmacology

Abstract

Many drugs are extensively but reversibly bound to plasma proteins (Meyer and Guttman, 1968). Albumin is particularly important in this regard since it binds a variety of substances of diverse structure and activity. In addition to drugs, various naturally occurring compounds such as bilirubin, thyroxine, fatty acids and certain steroids bind to albumin. The number of binding sites on albumin which have a relatively high affinity for drugs and hormones is limited and, under certain conditions, compounds may compete for such sites (Brodie, 1965). The rate of metabolism and excretion as well as the magnitude of the pharmacologic response is dependent, in part, upon the concentration of unbound drug. Thus, marked changes in pharmacologic activity and even toxicity may be observed when one compound is displaced by another from albumin (Brodie, 1966; Solomon, 1968). Such is particularly the case when the displaced compound is metabolized and/or excreted slowly. This review is concerned with the interaction between drugs and certain naturally occurring compounds relative to binding on plasma proteins.

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Authors
  1. H. M. Solomon
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Editors and Affiliations

  1. Department of Health, Education and Welfare, National Institutes of Health, 20014, Bethesda, MD, USA

    Bernard B. Brodie  & James R. Gillette  & 

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Solomon, H.M. (1971). Competition between Drugs and Normal Substrates for Plasma and Tissue Binding Sites. In: Brodie, B.B., Gillette, J.R., Ackerman, H.S. (eds) Concepts in Biochemical Pharmacology. Handbuch der experimentellen Pharmakologie/Handbook of Experimental Pharmacology, vol 28 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-65052-9_11

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  • DOI: https://doi.org/10.1007/978-3-642-65052-9_11

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-65054-3

  • Online ISBN: 978-3-642-65052-9

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