CYP450 Induction and Inhibition

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The page below is a sample from the LabCE course Pharmacology for the Clinical Chemist: Therapeutic Drug Monitoring and Pharmacogenomics. Access the complete course and earn ASCLS P.A.C.E.-approved continuing education credits by subscribing online.

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CYP450 Induction and Inhibition

PGx is not the only factor to consider when thinking about variation in drug responses among different people. Although polymorphisms of drug-metabolizing enzymes are a big player, other big players influence drug metabolism.
For example, many drugs can induce the expression of CYP450 enzymes (i.e., they cause cells to produce more of a particular enzyme). Also, CYP450s can be inhibited by a variety of substances. For example, CYP2D6 can be inhibited by cimetidine (Tagamet) and fluoxetine (Prozac). Substances in food can also affect CYP450 expression or may compete with a drug for metabolism. An example is grapefruit. Several organic compounds found in grapefruit have an inhibitory action on CYP3A4.
Since many patients are on multiple medications and dietary and environmental factors can change, CYP450 expression levels cannot be solely predicted based on their genotype.
Some CYP450 inducers and inhibitors are listed in the table on the following page.