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Drug interactions

Istradefylline + Tacrolimus

Severity: Moderate

Istradefylline and Tacrolimus: 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

At 40 mg daily istradefylline raises exposure to CYP3A4 and P-glycoprotein substrates, and tacrolimus is both. Higher tacrolimus levels may cause toxicity, whereas this effect was not seen at 20 mg daily.

What this interaction means in plain words

Istradefylline and Tacrolimus 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.

Istradefylline belongs to Central Nervous System; Tacrolimus belongs to Miscellaneous.

Evidence level: Moderate

Why it happens

Dose-dependent inhibition of CYP3A4 and P-glycoprotein by istradefylline.

What to do

Monitor tacrolimus trough levels when istradefylline is started, especially at 40 mg daily, and reduce the tacrolimus dose as required. Prefer the 20 mg dose where clinically appropriate.

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 Istradefylline with Tacrolimus?

MediHelp rates the interaction as moderate. Istradefylline and Tacrolimus 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. At 40 mg daily istradefylline raises exposure to CYP3A4 and P-glycoprotein substrates, and tacrolimus is both. Higher tacrolimus levels may cause toxicity, whereas this effect was not seen at 20 mg daily.

How serious is the interaction between Istradefylline and Tacrolimus?

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 tacrolimus trough levels when istradefylline is started, especially at 40 mg daily, and reduce the tacrolimus dose as required. Prefer the 20 mg dose where clinically appropriate.

What other medicines interact with Tacrolimus?

MediHelp also lists interactions of Tacrolimus with, for example, Adenovirus types 4 and 7 live, Bcg vaccine live, Cidofovir. The full list is on the Tacrolimus page.

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