Omeprazole with Cyclosporine Interaction Details
Brand Names Associated with Omeprazole
- Omeprazole
- Prilosec®
- Prilosec® OTC
- Talicia (as a combination product containing Amoxicillin, Omeprazole, Rifabutin)
- Zegerid® (as a combination product containing Omeprazole, Sodium Bicarbonate)
- Zegerid® OTC (as a combination product containing Omeprazole, Sodium Bicarbonate)
Brand Names Associated with Cyclosporine
- Cyclosporine
- Gengraf®
- Neoral®
- Sandimmune® Capsules
- Sandimmune® Oral Solution
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 05, 2023
Interaction Effect
Altered cycloSPORINE concentrations and increased omeprazole exposure
Interaction Summary
Monitor patients to determine if it is necessary to adjust the dosage of cycloSPORINE when taken concomitantly with omeprazole. The effect of omeprazole on cycloSPORINE concentrations is unclear. Controlled studies have reported no significant alterations or increased cycloSPORINE serum concentrations . In case reports, both increased and decreased cycloSPORINE levels have been found .
Severity
Moderate
Onset
Delayed
Evidence
Theoretical
How To Manage Interaction
Monitor patients to determine if it is necessary to adjust the dosage of cycloSPORINE when taken concomitantly with omeprazole.
Mechanism Of Interaction
Altered cycloSPORINE metabolism; inhibition of CYP3A-mediated metabolism of omeprazole
Literature Reports
A) Interactions have been reported between cycloSPORINE and omeprazole; patients should be monitored and doses adjusted accordingly . Omeprazole may increase the metabolism of cycloSPORINE, causing decreased cycloSPORINE blood levels .
B) Whole-blood cycloSPORINE concentrations became substantially elevated in a patient (approximately doubled) when omeprazole was given concurrently . CycloSPORINE levels had remained constant for 6 months prior to omeprazole therapy; following a reduction in cycloSPORINE dose, the cycloSPORINE levels returned to normal range, and remained in that range through 4 months of concurrent therapy.
C) A bone marrow transplant patient experienced reduced cycloSPORINE serum concentrations (from 254 ng/mL to 81 ng/mL) when omeprazole IV 40 mg/day was added to cycloSPORINE . Following withdrawal of omeprazole, cycloSPORINE levels returned to 270 ng/mL.
D) CycloSPORINE serum concentrations were analyzed in a crossover, placebo-controlled study involving 10 stable renal transplant patients . Mean whole blood trough concentrations of cycloSPORINE were 102 mcg/L during concurrent omeprazole use (20 mg/day) compared with 100 mcg/L when placebo was used. Changes in serum levels of less than 30% were considered insufficient to achieve clinical significance and differences were less than 30% in this study. Although both drugs are metabolized in the liver by the cytochrome P450 system, it was suggested that cycloSPORINE is metabolized substantially by the P4503A4 enzyme and omeprazole by the P4502C18 enzyme, so competitive inhibition may not be a factor.
Omeprazole Overview
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Prescription omeprazole is used alone or with other medications 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 omeprazole is used to treat damage from GERD in adults and children 1 month of age and older. Prescription omeprazole is used to allow the esophagus to heal and prevent further damage to the esophagus in adults and children 1 year of age and older with GERD. Prescription omeprazole is also used to treat conditions in which the stomach produces too much acid such as Zollinger-Ellison syndrome in adults. Prescription omeprazole is also used to treat ulcers (sores in the lining of the stomach or intestine) and it is also used with other medications to treat and prevent the return of ulcers caused by a certain type of bacteria (H. pylori) in adults. Nonprescription (over-the-counter) omeprazole is used to treat frequent heartburn (heartburn that occurs at least 2 or more days a week) in adults. Omeprazole is in a class of medications called proton-pump inhibitors. It works by decreasing the amount of acid made in the stomach.
Cyclosporine Overview
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Cyclosporine and cyclosporine (modified) are used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system of the person who received the organ) in people who have received kidney, liver, and heart transplants. Cyclosporine (modified) is also used alone or with methotrexate (Rheumatrex) to treat the symptoms of rheumatoid arthritis (arthritis caused by swelling of the lining of the joints) in patients whose symptoms were not relieved by methotrexate alone. Cyclosporine (modified) is also used to treat psoriasis (a skin disease in which red, scaly patches form on some areas of the body) in certain patients who have not been helped by other treatments. Cyclosporine and cyclosporine (modified) are in a class of medications called immunosuppressants. They work by decreasing the activity of the immune system.
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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.