Omeprazole with Erlotinib 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 Erlotinib
- Erlotinib
- Tarceva®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 18, 2023
Interaction Effect
Reduced erlotinib exposure
Interaction Summary
Concomitant use of erlotinib (pH dependent solubility) and drugs that increase the gastric pH (proton pump inhibitors) decrease erlotinib solubility and exposure; 3 studies reported significant reductions in erlotinib exposure . Erlotinib concentrations during acute treatment of gastric bleed with pantoprazole resulted in therapeutic erlotinib levels during coadministration in a case report . Avoid concomitant use; separation of doses may not eliminate the extended affect on the pH of the upper gastrointestinal tract .
Severity
Major
Onset
Unspecified
Evidence
Established
How To Manage Interaction
The solubility of erlotinib is pH dependent and decreases as pH increases. Concomitant use of erlotinib and drugs that increase the gastric pH, such as a proton pump inhibitor, may decrease erlotinib solubility and decrease exposure. Avoid concomitant use, since separation of doses may not eliminate the extended affect on the pH of the upper gastrointestinal tract.
Mechanism Of Interaction
PH related reduction in erlotinib solubility and subsequent reduction in absorption
Literature Reports
A) Erlotinib with 250 mL of water, given 3 hours after esomeprazole 40 mg resulted in a significant decrease in erlotinib exposure (AUC(24 hours); 47% (95% CI, -57% to -34%)) and decreased Cmax by 56% (95% CI, -64% to -46%) in a pharmacokinetic study of adults with non-small cel lung cancer (N=21); when erlotinib was administered with 250 mL of cow's milk 3.9% fat, exposure to erlotinib was not significantly altered, independent of esomeprazole use .
B) Coadministration of erlotinib and proton pump inhibitors (n=12) compared with patients receiving only erlotinib (n=24) resulted in a significant decrease in the plasma-to-dose ratio of erlotinib (0.39 vs 0.51 mcg/[mL x mg x kg]) and a significant increase in erlotinib oral clearance (5.55 vs 3.95 L/hr) in a pharmacokinetic study of patients receiving erlotinib for treatment of non-small cell lung cancer. Proton pump inhibitors included lansoprazole (n=9), omeprazole (n=1), esomeprazole (n=1), or rabeprazole (n=1) .
C) Erlotinib trough concentrations were significantly reduced during coadministration of pantoprazole IV infusion, but returned to normal when the dose was reduced and pantoprazole was administered orally in a 46-year-old woman with non-small cell lung cancer requiring acute treatment of gastric bleed and ulcer. On days 16 and 17 of erlotinib 150 mg orally at least 2 hours before or 4 hours after concurrent algeldrate 800 mg/magnesium hydroxide 400 mg 4 times daily, erlotinib trough concentrations were 0.96 and 0.97 mg/L and within expected range (0.7 to 1.7 mg/L). On days 19 and 20 of erlotinib during coadministration of pantoprazole 8 mg/hour IV for 48 hours, trough levels were subtherapeutic at 0.41 and 0.52 mg/L. On days 22 and 23 of erlotinib during coadministration with pantoprazole 40 mg orally twice daily, trough levels returned to expected range at 0.87 and 0.96 mg/L. Administration times or oral pantoprazole and erlotinib were not provided .
D) In a pharmacokinetic study (N=24), administration of erlotinib 150 mg 1 hour after omeprazole 40 mg orally once daily resulted in significantly reduced erlotinib AUC by 54% and Cmax by 58% compared with erlotinib alone. Exposure to the major active metabolite, OSI-420, was similarly effected .
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.
Erlotinib Overview
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Erlotinib is used to treat certain types of non-small cell lung cancer that has spread to nearby tissues or to other parts of the body in patients who have already been treated with at least one other chemotherapy medication and have not gotten better. Erlotinib is also used in combination with another medication (gemcitabine [Gemzar]) to treat pancreatic cancer that has spread to nearby tissues or to other parts of the body and cannot be treated with surgery. Erlotinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.
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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.