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Drug interactions

Brexpiprazole + Itraconazole

Severity: Major

Brexpiprazole and Itraconazole: major interaction.

Last updated Sources: EMA 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

Itraconazole raises brexpiprazole exposure, which may increase sedation, akathisia, orthostatic hypotension and other adverse effects. The effect is larger if a CYP2D6 inhibitor is also present or the patient is a poor CYP2D6 metabolizer.

What this interaction means in plain words

Brexpiprazole and Itraconazole 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.

Brexpiprazole belongs to Central Nervous System; Itraconazole belongs to Anti Fungals.

Evidence level: High

Why it happens

Itraconazole inhibits CYP3A4, a main metabolic pathway of brexpiprazole.

What to do

Give half the usual brexpiprazole dose with itraconazole, and a quarter of the dose if a strong or moderate CYP2D6 inhibitor is also given. Return to the usual dose after itraconazole is stopped.

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 Brexpiprazole with Itraconazole?

MediHelp rates the interaction as major. Brexpiprazole and Itraconazole 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. Itraconazole raises brexpiprazole exposure, which may increase sedation, akathisia, orthostatic hypotension and other adverse effects. The effect is larger if a CYP2D6 inhibitor is also present or the patient is a poor CYP2D6 metabolizer.

How serious is the interaction between Brexpiprazole and Itraconazole?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Give half the usual brexpiprazole dose with itraconazole, and a quarter of the dose if a strong or moderate CYP2D6 inhibitor is also given. Return to the usual dose after itraconazole is stopped.

What other medicines interact with Itraconazole?

MediHelp also lists interactions of Itraconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Itraconazole page.

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