Ketoconazole and Tacrolimus: Drug Interaction Guide
Quick answer: This is a major interaction — avoid combining Ketoconazole and Tacrolimus unless specifically directed by your doctor.
How Ketoconazole interacts with Tacrolimus
Ketoconazole strongly inhibits CYP3A4 and P-glycoprotein, causing major increases in tacrolimus blood concentrations with risk of nephrotoxicity and neurotoxicity.
What you should do
If combination is required (sometimes used deliberately to spare cost), reduce tacrolimus dose by 50-80% and monitor trough levels every 2-3 days.
Key facts
Severity
Major — avoid combination
Mechanism
Ketoconazole strongly inhibits CYP3A4 and P-glycoprotein, causing major increases in tacrolimus blood concentrations wit...
Action
If combination is required (sometimes used deliberately to spare cost), reduce tacrolimus dose by 50-80% and monitor tro...
Frequently asked questions
Can I take Ketoconazole and Tacrolimus together?
No — this combination should generally be avoided. If combination is required (sometimes used deliberately to spare cost), reduce tacrolimus dose by 50-80% and monitor trough levels every 2-3 days.
What is the severity of this interaction?
The interaction between Ketoconazole and Tacrolimus is classified as Major — avoid combination. Ketoconazole strongly inhibits CYP3A4 and P-glycoprotein, causing major increases in tacrolimus blood concentrations with risk of nephrotoxicity and neurotoxicity.
What should I do if I'm prescribed both?
If combination is required (sometimes used deliberately to spare cost), reduce tacrolimus dose by 50-80% and monitor trough levels every 2-3 days. Always consult your prescribing clinician — do not stop or change medications without medical guidance.
Last reviewed: by iMedic Medical Editorial Team. Our editorial process.