Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2002 Winter;36(1):67-81.

Emerging significance of P-glycoprotein in understanding drug disposition and drug interactions in psychopharmacology

Stanley W Carson  1 , Aliou D Ousmanou, Sheri L Hoyler
Affiliations
  • PMID: 12397848
Review

Emerging significance of P-glycoprotein in understanding drug disposition and drug interactions in psychopharmacology

Stanley W Carson et al. Psychopharmacol Bull. 2002 Winter.

Abstract

P-glycoprotein (P-gp) is a member of the superfamily of energy-dependent efflux protein pumps involved in the transport of a wide variety of endogenous and exogenous substrates. The role of P-gp has been extensively studied in the development of multidrug resistance (MDR) in cancer cells during chemotherapy. However, recent data suggest that P-gp is also present in normal tissue, such as the gut, blood-brain barrier, lymphocytes, liver, kidney, and other organs, where it plays a role in the absorption, distribution, metabolism, and elimination of a multitude of drugs. Psychotropic drugs, as well as many other drugs, act as substrates, inhibitors, or inducers of P-gp function. While there is a growing interest in developing inhibitors of this transporter as an approach to increasing drug bioavailability, the utility of exploiting inducers of the protein is less clear. Changes in P-gp transport activity have recently been linked to clinically significant drug-drug and drug-herb interactions. Because of its wide tissue distribution and its effect on drug disposition, clinicians should recognize the potential impact of P-gp modulation on the therapeutic efficacy and adverse events of psychopharmacologic agents that are substrates for this transporter. More research is needed in the field of psychopharmacology to classify central nervous system-active P-gp substrates and to characterize the utility of modulating P-gp activity at the blood-brain barrier.

PubMed Disclaimer

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

Publication types

MeSH terms

Substances

LinkOut - more resources

-