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Drug Metabolism and Personalized Therapy

Official journal of the European Society of Pharmacogenomics and Personalised Therapy

Editor-in-Chief: Llerena, Adrián

Editorial Board Member: Benjeddou, Mongi / Chen, Bing / Dahl, Marja-Liisa / Devinsky, Ferdinand / Hirata, Rosario D. C. / Hubacek, Jaroslav A. / Ingelman-Sundberg, Magnus / Maitland-van der Zee, Anke-Hilse / Manolopoulos, Vangelis G. / Marc, Janja / Melichar, Bohuslav / Meyer, Urs A. / Nair, Sujit / Nofziger, Charity / Peiro, Ana / Sadee, Wolfgang / Salazar, Luis A. / Simmaco, Maurizio / Turpeinen, Miia / Schaik, Ron / Shin, Jae-Gook / Visvikis-Siest, Sophie / Zanger, Ulrich M.

SCImago Journal Rank (SJR) 2015: 0.447
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P-Glycoprotein- and cytochrome P-450-mediated herbal drug interactions

Yamsani Shravan Kumar1 / Devandla Adukondalu1 / Dharani Sathish1 / Yamsani Vamshi Vishnu1 / Gannu Ramesh1 / Athukuri Bharagavi Latha1 / Palem Chinna Reddy1 / Manda Sarangapani1 / 1

1Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, AP, India

Corresponding author: Y. Madhusudan Rao, Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009, AP, India Phone: +91-870-3091323, Fax: +91-870-2453508

Citation Information: Drug Metabolism and Drug Interactions. Volume 25, Issue 1-4, Pages 3–16, ISSN (Online) 2191-0162, ISSN (Print) 0792-5077, DOI: 10.1515/DMDI.2010.006, January 2011

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P-Glycoprotein (P-gp), the most extensively studied ATP-binding cassette transporter, functions as a biological barrier by extruding toxic substances and xenobiotics out of cells. Drug efflux pumps such as P-gp play a functional role in determining the pharmacokinetics of drugs administered by oral and parenteral routes. Determining the activity of drug efflux transport proteins has important implications in the identification of substrates and/or inhibitors. The significant role of the small intestine in reducing the oral bioavailability of drugs is due to metabolic enzymes and efflux transporters. The role of cytochrome P-450 3A (CYP3A) and P-gp in intestinal drug disposition has been highlighted. This review examines the structure, localisation and functional role of P-gp, the mechanism of drug efflux and drug-herb interactions.

Keywords: cytochrome P-450 3A; inhibitors; in vitro; in vivo; P-glycoprotein

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