Tacrolimus and Esomeprazole Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Tacrolimus
Esomeprazole Injection
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased tacrolimus exposure
Interaction Deep Dive
Tacrolimus is primarily metabolized by CYP3A3, and the coadministration of esomeprazole, a CYP3A4 and CYP2C19 substrate, may increase tacrolimus serum concentrations 2, especially in patients who are poor CYP2C19 metabolizers 3. The concurrent use of tacrolimus and esomeprazole resulted in elevated trough levels of tacrolimus in a patient who was a CYP2C19 extensive metabolizer. Concomitant administration of esomeprazole and tacrolimus may result in increased tacrolimus serum concentrations and increased risk of tacrolimus toxicity; therefore, it may be prudent to avoid coadministration. If esomeprazole and tacrolimus are used together, monitor tacrolimus levels and make dosage adjustments as necessary, and monitor for tacrolimus toxicity (eg, nephrotoxicity, myelosuppression) 1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated tacrolimus metabolism by esomeprazole
Literature reports
1 report — tap to read
a) An 18-year-old woman, diagnosed as a CYP2C19 extensive metabolizer (normal), received tacrolimus 6 mg/day and lansoprazole 30 mg/day as part of a chronic maintenance regimen post kidney transplant. Trough tacrolimus blood levels were maintained for 9 months in the target range of 5 to 8 nanograms/milliliter (ng/mL). Eight months after transplantation, the patient was switched to esomeprazole 40 mg/day and presented 1 month later with fatigue, persistent sinusitis, and a tacrolimus level of 27.4 ng/mL. The tacrolimus dose was held for 24 hours then reduced to 4 mg/day, and the tacrolimus level decreased to 9.6 ng/mL. The patient presented 10 days later with nausea, vomiting, an elevated serum creatinine, and a tacrolimus level of 13.7 ng/mL. Tacrolimus was withdrawn and the patient was switched to omeprazole 40 mg/day. Three days later, the tacrolimus level remained elevated at 20.1 ng/mL. Omeprazole was replaced with lansoprazole, and the patient became asymptomatic with a normalized tacrolimus level. The tacrolimus target concentration of 5 to 8 ng/mL was attained within 1 week, and the dose was titrated to the initial dose of 6 mg/day 1.
Common questions
Can I take Tacrolimus and Esomeprazole Injection together?
Increased tacrolimus exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Tacrolimus and Esomeprazole Injection interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Tacrolimus or Esomeprazole Injection need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (3)
- Maguire M, Franz T, & Hains DS: A clinically significant interaction between tacrolimus and multiple proton pump inhibitors in a kidney transplant recipient. Pediatr Transplant 2012; 16(6):E217-E220. PubMed
- Product Information: NEXIUM oral delayed release capsules, oral delayed release suspension, esomeprazole magnesium oral delayed release capsules, oral delayed release suspension. AstraZeneca LP (per FDA), Wilmington, DE, 2012. DailyMed
- Product Information: PROGRAF(R) oral capsules, intravenous injection, tacrolimus oral capsules, intravenous injection. Astellas Pharma US, Inc. (per FDA), Northbrook, IL, 2012. DailyMed
Keep reading about Tacrolimus
Keep reading about Esomeprazole Injection
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Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
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