Itraconazole and Tacrolimus: Drug Interaction Guide

Quick answer: This is a major interaction — avoid combining Itraconazole and Tacrolimus unless specifically directed by your doctor.

Interaction severity: Major — avoid combination

How Itraconazole interacts with Tacrolimus

Itraconazole strongly inhibits CYP3A4 and P-glycoprotein, dramatically reducing tacrolimus clearance and raising levels with risk of nephrotoxicity, neurotoxicity, and hyperkalemia.

What you should do

Anticipate empiric tacrolimus dose reduction of 50-66% on initiation. Monitor tacrolimus trough levels, renal function, and electrolytes closely; adjust dose again when azole is stopped.

Key facts

Severity

Major — avoid combination

Mechanism

Itraconazole strongly inhibits CYP3A4 and P-glycoprotein, dramatically reducing tacrolimus clearance and raising levels ...

Action

Anticipate empiric tacrolimus dose reduction of 50-66% on initiation. Monitor tacrolimus trough levels, renal function, ...

Important medical disclaimer: This page provides educational information about drug interactions for general reference. It is not a substitute for professional medical advice, diagnosis, or treatment. Always discuss your specific medications with a qualified healthcare provider before starting, stopping, or changing any treatment. About our editorial team.

Frequently asked questions

Can I take Itraconazole and Tacrolimus together?

No — this combination should generally be avoided. Anticipate empiric tacrolimus dose reduction of 50-66% on initiation. Monitor tacrolimus trough levels, renal function, and electrolytes closely; adjust dose again when azole is stopped.

What is the severity of this interaction?

The interaction between Itraconazole and Tacrolimus is classified as Major — avoid combination. Itraconazole strongly inhibits CYP3A4 and P-glycoprotein, dramatically reducing tacrolimus clearance and raising levels with risk of nephrotoxicity, neurotoxicity, and hyperkalemia.

What should I do if I'm prescribed both?

Anticipate empiric tacrolimus dose reduction of 50-66% on initiation. Monitor tacrolimus trough levels, renal function, and electrolytes closely; adjust dose again when azole is stopped. Always consult your prescribing clinician — do not stop or change medications without medical guidance.

Last reviewed: by iMedic Medical Editorial Team. Our editorial process.