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Drug interactions

Tofacitinib + Zileuton

Severity: Moderate

Tofacitinib 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

Tofacitinib is cleared mainly by CYP3A4 with a minor CYP2C19 contribution, and zileuton may modestly raise its exposure. Higher tofacitinib levels increase the risk of infection, cytopenias and lipid changes.

What this interaction means in plain words

Tofacitinib 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.

Tofacitinib belongs to Musculoskeletal; Zileuton belongs to Respiratory.

Evidence level: Low

Why it happens

Zileuton inhibits CYP3A4 weakly to moderately, decreasing tofacitinib clearance.

What to do

No routine dose change is required with a moderate or weak CYP3A4 inhibitor alone. Monitor for infection and blood count abnormalities, and reduce the tofacitinib dose if a potent CYP2C19 inhibitor is also given.

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.

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Frequently asked questions

Can I take Tofacitinib with Zileuton?

MediHelp rates the interaction as moderate. Tofacitinib 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. Tofacitinib is cleared mainly by CYP3A4 with a minor CYP2C19 contribution, and zileuton may modestly raise its exposure. Higher tofacitinib levels increase the risk of infection, cytopenias and lipid changes.

How serious is the interaction between Tofacitinib 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: No routine dose change is required with a moderate or weak CYP3A4 inhibitor alone. Monitor for infection and blood count abnormalities, and reduce the tofacitinib dose if a potent CYP2C19 inhibitor is also given.

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.

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