Drug–Drug Interaction: Enzyme Induction
Enzyme induction in humans may lead to drug-drug interactions. Possible pharmacokinetic consequences of enzyme induction include decreased or absent bioavailability for orally administered drugs, increased hepatic clearance, or accelerated formation of active or toxic metabolites. The “gold standard” accepted for in vitro enzyme induction assays are freshly isolated human hepatocytes. A procedure for in vitro induction studies in freshly isolated human hepatocytes is described including evaluation of CYP1A2, CYP2B6, and CYP3A4 enzyme activities and mRNA levels, and an example is given.
KeywordsHuman Hepatocyte Aryl Hydrocarbon Receptor Constitutive Androstane Receptor CYP3A4 Induction HepaRG Cell
The author would like to thank Dr. Martin Burschka for critical reading of this chapter.
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