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Importance of P-glycoprotein for Drug–Drug Interactions

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Drug Transporters

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 201))

Abstract

P-glycoprotein (ABCB1) is one of the most extensively studied transporters regarding drug resistance and drug–drug interactions. P-glycoprotein is expressed in multiple key organs in drug disposition such as small intestine, blood–brain barrier, kidney, and liver. Therefore, P-glycoprotein mediated drug–drug interactions can occur at various organs and tissues. This chapter will mainly focus on drug–drug interactions that are mediated by the intestinal P-glycoprotein.

During the last decade, many in vitro and in vivo studies reported that the induction or inhibition of P-glycoprotein can lead to drug–drug interactions. For instance, induction of the intestinal P-glycoprotein activity can cause reduced bioavailability of orally administered drugs and decreased therapeutic efficacy. On the other hand, the inhibition of the intestinal P-glycoprotein activity can lead to increased bioavailability, thus leading to an increased risk of adverse side effects.

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Authors and Affiliations

  1. Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-University Erlangen-Nuremberg, Fahrstraße 17, 91054, Erlangen, Germany

    Hartmut Glaeser

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  1. Hartmut Glaeser
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Correspondence to Hartmut Glaeser .

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Editors and Affiliations

  1. Inst. Experimentelle und Klinische, Pharmakologie und Toxikologie, Universität Erlangen-Nürnberg, Fahrstr. 17, Erlangen, 91054, Germany

    Martin F. Fromm

  2. Division of Clinical Pharmacology, University of Western Ontario, Windmere Road 339, London, N6A 5A5, Ontario, Canada

    Richard B. Kim

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Glaeser, H. (2011). Importance of P-glycoprotein for Drug–Drug Interactions. In: Fromm, M., Kim, R. (eds) Drug Transporters. Handbook of Experimental Pharmacology, vol 201. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-14541-4_7

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