Esomeprazole with Tacrolimus Interaction Details
Brand Names Associated with Esomeprazole
- Esomeprazole
- Nexium®
- Nexium® 24HR
- Vimovo® (as a combination product containing Esomeprazole, Naproxen)
Brand Names Associated with Tacrolimus
- Astagraf XL®
- Envarsus XR®
- FK 506
- Prograf®
- Tacrolimus
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 08, 2023
Interaction Effect
Increased tacrolimus exposure
Interaction Summary
Tacrolimus is primarily metabolized by CYP3A, and the coadministration of esomeprazole, a CYP3A4 and CYP2C19 substrate, may increase tacrolimus serum concentrations , especially in patients who are poor CYP2C19 metabolizers . 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) .
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
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) .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated tacrolimus metabolism by esomeprazole
Literature Reports
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 .
Esomeprazole Overview
-
Prescription esomeprazole is used to treat the symptoms of gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and possible injury of the esophagus (the tube between the throat and stomach) in adults and children 1 year of age and older. Prescription esomeprazole is used to treat damage from GERD in adults and children 1 month of age and older. Prescription esomeprazole is used to allow the esophagus to heal and prevent further damage to the esophagus in adults with GERD. Prescription esomeprazole is also used to decrease the chance that people who are taking nonsteroidal anti-inflammatory drugs (NSAIDs) will develop ulcers (sores in the lining of the stomach or intestine) in adults. It is also used with other medications to treat and prevent the return of stomach ulcers caused by a certain type of bacteria (H. pylori) in adults. Prescription esomeprazole is also used to treat conditions in which the stomach produces too much acid such as Zollinger-Ellison syndrome in adults. Nonprescription (over-the-counter) esomeprazole is used to treat frequent heartburn (heartburn that occurs at least 2 or more days a week) in adults. Esomeprazole is in a class of medications called proton pump inhibitors. It works by decreasing the amount of acid made in the stomach.
Tacrolimus Overview
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Tacrolimus (Astagraf XL, Envarsus XR, Prograf) is used along with other medications to prevent rejection (attack of a transplanted organ by the immune system of a person receiving the organ) in people who have received a kidney transplant. Tacrolimus (Prograf) is also used along with other medications to prevent rejection in people who have received a liver, lung, or heart transplant. Tacrolimus is in a class of medications called immunosupressants. It works by decreasing the activity of the immune system to prevent it from attacking the transplanted organ.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.