Cytochrome P450 Induction

CYP induction is an increase in the activity level of a CYP enzyme due to the presence of an inducer — a compound (e.g., medication, supplement, or other substance) that can increase the number of available CYP enzymes. CYP induction can result in increased drug metabolism, leading to drug interactions that may impact treatment outcomes and side effect risk.

Summary

Cytochrome P450 (CYP) induction occurs when a compound (e.g., medication, supplement, or other substance) increases the activity level of a type of CYP enzyme. This compound would be considered an inducer. CYP induction can lead to pharmacokinetic drug interactions, ultimately causing increased drug metabolism which may alter the efficacy and safety of a medication or supplement.[1] Interestingly, not all CYP enzymes are considered inducible, including CYP2D6 and CYP2J2.[2]

Unlike CYP inhibition, which occurs due to direct interactions between an inhibitor and a CYP enzyme, CYP induction primarily occurs because the inducer causes the body to make more copies of the CYP enzyme, which translates to an increased rate of drug metabolism.

Example: CYP Induction

Medication A increases (induces) the activity of a CYP enzyme that medication B relies on for metabolism. Medication B is broken down faster than normal, leading to lower levels of medication B in the body, which could reduce its effectiveness.

Alternatively, if medication B is a prodrug that relies on the CYP enzyme for activation, more breakdown means more of the active drug, so there could be an increased risk of side effects or toxicity.

References

1.^Zhao M, Ma J, Li M, Zhang Y, Jiang B, Zhao X, Huai C, Shen L, Zhang N, He L, Qin SCytochrome P450 Enzymes and Drug Metabolism in Humans.Int J Mol Sci.(2021-Nov-26)