Skip to content

Drug interactions

Pirfenidone + Zileuton

Severity: Moderate

Pirfenidone and Zileuton: moderate interaction.

Last updated

For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.

Summary

Pirfenidone is metabolized mainly by CYP1A2, and inhibitors increase its exposure and the risk of nausea, photosensitivity, rash and liver enzyme elevation. Zileuton is a weak CYP1A2 inhibitor, so the effect is smaller than with strong inhibitors.

What this interaction means in plain words

Pirfenidone and Zileuton can affect each other. The combination is often manageable, but it may need a change of dose, a change of timing, or extra checks while both are taken.

Pirfenidone belongs to Miscellaneous; Zileuton belongs to Respiratory.

Evidence level: Moderate

Why it happens

Zileuton inhibits CYP1A2, reducing pirfenidone clearance.

What to do

Monitor liver function and tolerability, and reduce the pirfenidone dose if adverse effects emerge. Consider an alternative to zileuton if effects persist.

What to ask your pharmacist

  • Should I take them at different times of day?
  • Does the dose of either medicine need to change?
  • Is there anything I should avoid, such as alcohol or certain foods, while on both?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

Pro+ members

Unlock the full page

Create an account and start a Pro+ trial to unlock the full management advice for Pirfenidone and Zileuton, the additional notes, the evidence detail and the whole-prescription interaction checker.

  • Full clinical management advice
  • Additional notes
  • Evidence detail
  • Interaction checker for a whole prescription

Try Pro+ free for 7 days on the web. No card needed.

Frequently asked questions

Can I take Pirfenidone with Zileuton?

MediHelp rates the interaction as moderate. Pirfenidone and Zileuton can affect each other. The combination is often manageable, but it may need a change of dose, a change of timing, or extra checks while both are taken. Pirfenidone is metabolized mainly by CYP1A2, and inhibitors increase its exposure and the risk of nausea, photosensitivity, rash and liver enzyme elevation. Zileuton is a weak CYP1A2 inhibitor, so the effect is smaller than with strong inhibitors.

How serious is the interaction between Pirfenidone and Zileuton?

MediHelp rates it moderate, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Monitor liver function and tolerability, and reduce the pirfenidone dose if adverse effects emerge. Consider an alternative to zileuton if effects persist.

What other medicines interact with Zileuton?

MediHelp also lists interactions of Zileuton with, for example, Fezolinetant, Pimozide, Alosetron. The full list is on the Zileuton page.

Full monographs, dosing and an interaction checker in the MediHelp app

Open the complete reference, check multi-drug interactions and use dosing tools in the MediHelp app.

Browse A–Z · Drug interactions

Get the app Sign in