Transporter-Based Drug–Drug Interactions and Their Effect on Distribution Volumes



Recently, drug transporters have emerged as significant modifiers of a patient’s pharmacokinetics. In cases where the functioning of drug transporters is altered, such as by drug–drug interactions, the resulting change in volume of distribution can lead to a significant change in drug effect or likelihood of toxicity, as well as a change in half-life independent of a change in clearance. Here, we discuss pharmacokinetic interactions at the transporter level that have been investigated in animals and humans and reported in literature, with a focus on the changes in distribution volume. Trends are discussed as they may be used to predict volume changes given the function of a transporter and the primary location of the interaction.


Distribution Volume Renal Tubule Central Compartment Drug Transporter Efflux Transporter 
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© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  1. 1.Department of Biopharmaceutical SciencesUniversity of CaliforniaSan FranciscoUSA
  2. 2.Department of Biopharmaceutical SciencesUniversity of California San FranciscoSan FranciscoUSA

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