Induction of drug-metabolizing enzymes: Mechanisms and consequences

Allan B. Okey, Eve A. Roberts, Patricia A. Harper, Michael S. Denison

Research output: Contribution to journalArticlepeer-review

78 Scopus citations


The activity of many enzymes that carry out biotransformation of drugs and environmental chemicals can be substantially increased by prior exposure of humans or animals to a wide variety of foreign chemicals. Increased enzyme activity is due to true enzyme induction mediated by increased synthesis of mRNAs which code for specific drug-metabolizing enzymes. Several species of cytochrome P-450 are inducible as are certain conjugating enzymes such as glutathione S-transferases, glucuronosyl transferases, and epoxide hydrolases. Induction of drug-metabolizing enzymes has been shown in several instances to alter the efficacy of some therapeutic agents. Induction of various species of cytochrome P-450 also is known to increase the rate at which potentially toxic reactive metabolic intermediates are formed from drugs or environmental chemicals. Overall, however, induction of drug-metabolizing enzymes appears to be a beneficial adaptive response for organisms living in a "chemically-hostile" world.

Original languageEnglish (US)
Pages (from-to)132-141
Number of pages10
JournalClinical Biochemistry
Issue number2
StatePublished - 1986
Externally publishedYes


  • biotransformation
  • carcinogenesis
  • cytochrome P-450
  • environmental exposure
  • enzyme induction
  • metabolic detoxication drug
  • polycyclic hydrocarbons
  • receptor drug

ASJC Scopus subject areas

  • Clinical Biochemistry


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