Induction of drug metabolism by nuclear receptor CAR: molecular mechanisms and implications for drug research

Eur J Pharm Sci. 2000 Oct;11(4):259-64. doi: 10.1016/s0928-0987(00)00112-3.


Recent findings indicate that induction of drug metabolism is regulated by activation of specific members of the nuclear receptor gene family. This minireview deals with the mechanisms by which phenobarbital and phenobarbital-type chemicals induce cytochrome P450 and other genes, and summarises the knowledge on the role of the constitutively active receptor CAR in the induction process. The potential implications of CAR-mediated induction for drug research and possible uses of CAR are also discussed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Anticonvulsants / metabolism*
  • Anticonvulsants / pharmacology
  • Aryl Hydrocarbon Hydroxylases*
  • Biopharmaceutics
  • Chemistry, Pharmaceutical
  • Constitutive Androstane Receptor
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme System / drug effects
  • Cytochrome P-450 Enzyme System / metabolism*
  • Humans
  • Oxidoreductases, N-Demethylating / drug effects
  • Oxidoreductases, N-Demethylating / metabolism
  • Phenobarbital / metabolism*
  • Phenobarbital / pharmacology
  • Receptors, Cytoplasmic and Nuclear / drug effects
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Response Elements / physiology*
  • Trans-Activators / metabolism*
  • Transcription Factors*


  • Anticonvulsants
  • Constitutive Androstane Receptor
  • Receptors, Cytoplasmic and Nuclear
  • Trans-Activators
  • Transcription Factors
  • Cytochrome P-450 Enzyme System
  • Aryl Hydrocarbon Hydroxylases
  • Cytochrome P-450 CYP3A
  • Oxidoreductases, N-Demethylating
  • Phenobarbital