Role of Protein Binding in Pharmacokinetics

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This article describes the learning resources that are available to pharmacy students during a lecture on the role of protein binding in pharmacokinetics and pharmacodynamics as part of a clinical pharmacokinetics course. The activities are designed to enable students to predict the effects of changes in the blood (or plasma) protein binding of drugs on kinetic parameters and to recommend dosage regimen modifications, if necessary. Using these resources, students realize that the effect of protein-binding alterations on drug clearance and volume of distribution is dependent on the extent of initial extraction ratio and volume of distribution of the drug, respectively. Further, they learn that the interpretation of the total drug concentrations in blood or plasma in relation to the pharmacologic effects requires a clear understanding of the kinetics of the drug and the underlying physiologic changes leading to the altered protein binding.


This article was originally published in American Journal of Pharmaceutical Education, volume 69, issue 5, in 2005.


American Association of Colleges of Pharmacy