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Plasma Membrane Proteins

By

Jennifer Le

, PharmD, MAS, BCPS-ID, FIDSA, FCCP, FCSHP, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego

Last full review/revision Oct 2020| Content last modified Oct 2020
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Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1) References Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1). Drug-drug interactions arise when drugs compete... read more . Drug-drug interactions arise when drugs compete to bind a drug transporter, altering drug responses and causing potentially toxic adverse effects (2,3) References Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1). Drug-drug interactions arise when drugs compete... read more . The 2 major transporters are adenosine triphosphate (ATP)–binding cassette (ABC, also referred to as P-glycoprotein) and the solute carrier (SLC) transporters. SLC transporters include emerging clinically significant transporters called multidrug and toxin extrusion (MATE) transporters that contribute to the renal elimination of metformin and interactions of cimetidine with other drugs (2) References Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1). Drug-drug interactions arise when drugs compete... read more . The expression of these drug transporters appears low during the fetal and neonatal periods, but increases after 7 years of age (4) References Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1). Drug-drug interactions arise when drugs compete... read more .

References

  • 1. Nigam SK: What do drug transporters really do? Nat Rev Drug Discov 14(1):29-44, 2015. doi: 10.1038/nrd4461

  • 2. Hillgren KM, Keppler D, Zur AA, et al: Emerging transporters of clinical importance: An update from the International Transporter Consortium. Clin Pharmacol Ther 94(1):52-63, 2013. doi: 10.1038/clpt.2013.74

  • 3. Zamek-Gliszczynski MJ, Lee CA, Poirier A, et al: ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans. Clin Pharmacol Ther94(1):64–79, 2013. doi: 10.1038/clpt.2013.45

  • 4. Mooij MG, Nies AT, Knibbe CA, et al: Development of human membrane transporters: Drug disposition and pharmacogenetics. Clin Pharmacokinet 55(5): 507-524, 2016. doi: 10.1007/s40262-015-0328-5

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The activity of drug-metabolizing enzymes often varies widely among healthy people, making metabolism highly variable. Which of the following factors is a major contributor to this variation?
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