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Drug interactions

Everolimus + Grapefruit

Severity: Major

Everolimus and Grapefruit: major interaction.

Last updated Sources: UK SmPC

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

Grapefruit and its juice can raise everolimus blood concentrations, increasing the risk of dose-related adverse effects such as stomatitis, infections, hyperglycemia, hyperlipidemia and myelosuppression. The size of the effect varies between patients and products.

What this interaction means in plain words

Everolimus and Grapefruit can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.

Evidence level: Moderate

Why it happens

Furanocoumarins in grapefruit inhibit intestinal CYP3A4 (and possibly P-glycoprotein), reducing first-pass metabolism of everolimus.

What to do

Advise patients to avoid grapefruit, grapefruit juice and related citrus such as pomelo and Seville orange while taking everolimus. If exposure is unavoidable, monitor everolimus trough levels and toxicity.

What to ask your pharmacist

  • Does the benefit of taking both outweigh the risk in my case?
  • Do I need any blood test, ECG or other check while on both?
  • What early warning signs should I watch for, and what should I do if they appear?

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

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References

Frequently asked questions

Can I take Everolimus with Grapefruit?

MediHelp rates the interaction as major. Everolimus and Grapefruit can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Grapefruit and its juice can raise everolimus blood concentrations, increasing the risk of dose-related adverse effects such as stomatitis, infections, hyperglycemia, hyperlipidemia and myelosuppression. The size of the effect varies between patients and products.

How serious is the interaction between Everolimus and Grapefruit?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Advise patients to avoid grapefruit, grapefruit juice and related citrus such as pomelo and Seville orange while taking everolimus. If exposure is unavoidable, monitor everolimus trough levels and toxicity.

What other medicines interact with Everolimus?

MediHelp also lists interactions of Everolimus with, for example, Bcg vaccine live, Influenza virus vaccine quadrivalent intranasal, Levoketoconazole. The full list is on the Everolimus page.

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