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CYP2E1 inhibitors, inducers and substrates

CYP2E1 is a liver enzyme that handles ethanol and other small molecules. It also turns a small share of acetaminophen into a toxic metabolite. Long-term heavy drinking induces it, and disulfiram is a strong inhibitor.

This is the desk's mapped set for CYP2E1, taken from the same catalog the desk uses to grade pairs. It is not a complete list. A drug that isn't listed here hasn't been cleared as safe; it just isn't on this list.

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What inhibition and induction mean

Inhibition. An inhibitor slows CYP2E1. Drugs that depend on CYP2E1 can build up, so their levels and effects can rise. Reversible inhibition starts as the inhibitor builds up and fades as it clears. Some inhibitors destroy the enzyme, and the effect lasts until the body makes more.

Induction. An inducer makes the body produce more CYP2E1. Levels of drugs that depend on CYP2E1 can fall, and so can their effect. Induction builds over days to weeks and takes about as long to fade after the inducer stops.

Substrates marked activation pathway are ones CYP2E1 turns into an active or reactive product. For these, inhibition can mean less of that product, and induction can mean more.

Strong, moderate and weak are the desk's grades for how much a perpetrator changes a sensitive substrate's exposure, in FDA's fold-change bins. FDA table of substrates, inhibitors and inducers.

Names with a solid underline open that drug's page of label-sourced pairs. Names with a dotted underline open the desk with that drug.

CYP2E1 inhibitors (3)

Strong inhibitors (1)

≥5-fold ↑ AUC of a sensitive index substrate

Moderate inhibitors (1)

≥2 to <5-fold ↑ AUC

Weak inhibitors (1)

≥1.25 to <2-fold ↑ AUC

CYP2E1 inducers (2)

Moderate inducers (1)

≥50 to <80% ↓ AUC

Weak inducers (1)

≥20 to <50% ↓ AUC

CYP2E1 substrates (4)

Major-pathway substrates (2)

CYP2E1 is one of the main routes for these.

Minor-pathway substrates (2)

CYP2E1 is a smaller route for these; other routes carry most of the load.

Educational reference only. Not FDA-cleared. The Prescribing Information governs.