Plasma Membrane Proteins

ByJennifer Le, PharmD, MAS, BCPS-ID, FIDSA, FCCP, FCSHP, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego
Reviewed/Revised Jun 2022
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    Plasma membrane transporters affect pharmacologic activity of drugs by mediating their absorption, distribution, metabolism, and excretion (1). Drug-drug interactions arise when drugs compete to bind a drug transporter, altering drug responses and causing potentially toxic adverse effects (2, 3). The 2 major transporters are adenosine2). The expression of these drug transporters appears low during the fetal and neonatal periods, but increases after 7 years of age (4).

    (See also Overview of Pharmacokinetics.)

    References

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

    2. 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. 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. 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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