Tacrolimus/Moderate and Weak CYP3A4 Inhibitors Interactions

This information is generalized and not intended as specific medical advice. Consult your healthcare professional before taking or discontinuing any drug or commencing any course of treatment.

Medical warning:

Moderate. These medicines may cause some risk when taken together. Contact your healthcare professional (e.g. doctor or pharmacist) for more information.

How the interaction occurs:

Your other drug may slow down how quickly your body processes tacrolimus.

What might happen:

Your blood levels of tacrolimus may increase and cause toxic effects, including kidney damage and an irregular heartbeat, which may be life-threatening.

What you should do about this interaction:

Make sure your healthcare professionals (e.g. doctor or pharmacist) know that you are taking these two medicines together. Your doctor may need to check the amount of tacrolimus in your blood and adjust the dose until you have been stabilized on the combination.Contact your healthcare professional if you experience a decrease in the amount of urine you make, or any chest discomfort, irregular heartbeat, dizziness, fainting, shaking, leg cramping, swelling, or any unusual stomach upset, headache, or skin irritation.Your healthcare professionals (e.g. doctor or pharmacist) may already be aware of this interaction and may be monitoring you for it. Do not start, stop, or change the dosage of any medicine before checking with them first.

  • 1.Prograf (tacrolimus) US prescribing information. Astellas Pharma US, Inc. August, 2023.
  • 2.Drew BJ, Ackerman MJ, Funk M, Gibler WB, Kligfield P, Menon V, Philippides GJ, Roden DM, Zareba W. Prevention of torsade de pointes in hospital settings: a scientific statement from the American Heart Association and the American College of Cardiology Foundation. J Am Coll Cardiol 2010 Mar 2;55(9):934-47.
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  • 6.This information is based on an extract from the Certara Drug Interaction Database (DIDB) Platform, Copyright Certara 1999-2023..
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  • 8.Uno T, Wada K, Matsuda S, Terada Y, Terakawa N, Oita A, Yokoyama S, Kawase A, Hosomi K, Takada M. Effects of clotrimazole on tacrolimus pharmacokinetics in patients with heart transplants with different CYP3A5 genotypes. Eur J Clin Pharmacol 2019 Jan;75(1):67-75.
  • 9.Vasquez EM, Shin GP, Sifontis N, Benedetti E. Concomitant clotrimazole therapy more than doubles the relative oral bioavailability of tacrolimus. Ther Drug Monit 2005 Oct;27(5):587-91.
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  • 12.Viesselmann CW, Descourouez JL, Jorgenson MR, Radke NA, Odorico JS. Clinically Significant Drug Interaction Between Clotrimazole and Tacrolimus in Pancreas Transplant Recipients and Associated Risk of Allograft Rejection. Pharmacotherapy 2016 Mar;36(3):335-41.

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CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.