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Drug interactions

Tacrolimus + Zafirlukast

Severity: Moderate

Tacrolimus and Zafirlukast: 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

Tacrolimus has a narrow therapeutic index and is a CYP3A4 substrate, so zafirlukast may increase its concentrations. Elevated levels risk nephrotoxicity, neurotoxicity and hyperglycemia.

What this interaction means in plain words

Tacrolimus and Zafirlukast 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.

Tacrolimus belongs to Miscellaneous; Zafirlukast belongs to Respiratory.

Evidence level: Low

Why it happens

Inhibition of CYP3A4-mediated tacrolimus metabolism by zafirlukast.

What to do

Measure tacrolimus trough levels and renal function after starting or stopping zafirlukast. Adjust the tacrolimus dose according to levels.

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 Tacrolimus with Zafirlukast?

MediHelp rates the interaction as moderate. Tacrolimus and Zafirlukast 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. Tacrolimus has a narrow therapeutic index and is a CYP3A4 substrate, so zafirlukast may increase its concentrations. Elevated levels risk nephrotoxicity, neurotoxicity and hyperglycemia.

How serious is the interaction between Tacrolimus and Zafirlukast?

MediHelp rates it moderate, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Measure tacrolimus trough levels and renal function after starting or stopping zafirlukast. Adjust the tacrolimus dose according to levels.

What other medicines interact with Zafirlukast?

MediHelp also lists interactions of Zafirlukast with, for example, Pimozide, Lomitapide, Nilotinib. The full list is on the Zafirlukast page.

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

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