Ketoconazole and Tolvaptan: Drug Interaction Guide
Quick answer: This is a major interaction — avoid combining Ketoconazole and Tolvaptan unless specifically directed by your doctor.
How Ketoconazole interacts with Tolvaptan
Ketoconazole strongly inhibits CYP3A4 metabolism of tolvaptan, increasing tolvaptan AUC up to 5-fold with risk of overly rapid aquaresis, severe hypernatremia and hepatotoxicity.
What you should do
Combination is contraindicated in autosomal dominant polycystic kidney disease; for SIADH, avoid or interrupt tolvaptan during ketoconazole therapy.
Key facts
Severity
Major — avoid combination
Mechanism
Ketoconazole strongly inhibits CYP3A4 metabolism of tolvaptan, increasing tolvaptan AUC up to 5-fold with risk of overly...
Action
Combination is contraindicated in autosomal dominant polycystic kidney disease; for SIADH, avoid or interrupt tolvaptan ...
Frequently asked questions
Can I take Ketoconazole and Tolvaptan together?
No — this combination should generally be avoided. Combination is contraindicated in autosomal dominant polycystic kidney disease; for SIADH, avoid or interrupt tolvaptan during ketoconazole therapy.
What is the severity of this interaction?
The interaction between Ketoconazole and Tolvaptan is classified as Major — avoid combination. Ketoconazole strongly inhibits CYP3A4 metabolism of tolvaptan, increasing tolvaptan AUC up to 5-fold with risk of overly rapid aquaresis, severe hypernatremia and hepatotoxicity.
What should I do if I'm prescribed both?
Combination is contraindicated in autosomal dominant polycystic kidney disease; for SIADH, avoid or interrupt tolvaptan during ketoconazole therapy. Always consult your prescribing clinician — do not stop or change medications without medical guidance.
Last reviewed: by iMedic Medical Editorial Team. Our editorial process.