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Diseases and Drug Protein Binding

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Abstract

In a number of pathological states a decrease in the plasma protein binding of drugs is observed. This may be due to many factors related either to the protein, or the ligand (drug), or to the binding conditions. The most important of these disease states quantitatively are probably hypoalbuminaemia, conditions resulting in modification of the albumin compartment volume and the presence on albumin binding sites of pathological inhibitors of drug binding.

A decrease in the extent of drug plasma protein binding does not necessarily lead to enhanced drug effects and therefore raises two important therapeutic questions. Firstly, does reduced protein binding have a clinically significant influence on the pharmacological effects of the drug? Secondly, if it does, is it preferable to modify the dosage regimen of the drug or to correct the plasma protein concentration prior to the administration of the drug? At present, only tentative answers can be given.

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Authors and Affiliations

  1. Department of Pharmacology, Faculty of Medicine, University of Paris Sud, 8 Rue du General-Sarrail, 94010, Creteil, France

    Jean-Paul Tillement, F. Lhoste & J. F. Giudicelli

  2. Department of Pharmacology, Faculty of Medicine Paris-Val de Marne, France

    Jean-Paul Tillement, F. Lhoste & J. F. Giudicelli

  3. Vascular Disease Research Institute, University Paris-Val de Marne, France

    Jean-Paul Tillement, F. Lhoste & J. F. Giudicelli

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  1. Jean-Paul Tillement
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  2. F. Lhoste
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  3. J. F. Giudicelli
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Tillement, JP., Lhoste, F. & Giudicelli, J.F. Diseases and Drug Protein Binding. Clin Pharmacokinet 3, 144–154 (1978). https://doi.org/10.2165/00003088-197803020-00004

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