Imatinib with Acetaminophen Interaction Details
Brand Names Associated with Imatinib
- Gleevec®
- Imatinib
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Feb 25, 2024
Interaction Effect
Increased acetaminophen levels
Interaction Summary
Concomitant use of chronic doses of acetaminophen with imatinib may result in increased acetaminophen levels and hepatoxicity due to inhibition of UGT-mediated metabolism of acetaminophen by imatinib. In an in-vitro pharmacokinetic study, 200 mg daily doses of imatinib coadministered with acetaminophen is predicted to result in a 22% increase in acetaminophen AUC[1]. In a case report, fatal acute liver failure occurred in a 51-year old women with chronic myeloid leukemia treated with imatinib 400 mg/day and taking chronic daily acetaminophen doses of 500 to 1000 mg. Carefully monitor liver function tests during treatment and discontinue therapy if elevation of liver function tests occurs [2] due to the possibility of hepatoxicity when acetaminophen is used chronically in a patient receiving imatinib.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Carefully monitor liver function tests during treatment and discontinue therapy if elevation of liver function tests occurs[2] due to the possibility of hepatoxicity when acetaminophen is used chronically in patients receiving imatinib.
Mechanism Of Interaction
Inhibition of UGT-mediated metabolism of acetaminophen by imatinib
Literature Reports
A) Fatal acute liver failure was reported in a 51-year old women with chronic myeloid leukemia treated with imatinib 400 mg/day and taking chronic daily acetaminophen doses of 500 to 1000 mg. Following 5 months of imatinib treatment, the patient developed asthenia and began taking acetaminophen. She presented with elevated aminotransferases and a normal bilirubin. Despite discontinuation of imatinib therapy, liver function tests worsened and jaundice and severe hepatitis with coagulopathy (prothrombin time 30% and clotting factor V level 19%) developed. Ultrasound revealed a reduced-size, homogenous liver. Viral and autoimmune hepatitis screening was negative. The patient continued to deteriorate with increased bilirubin, marked decrease of clotting factor V, and grade 3 encephalopathy and expired following cardiac arrest [2].
References
1 ) Liu Y , Ramirez J , & Ratain MJ : Inhibition of paracetamol glucuronidation by tyrosine kinase inhibitors. Br J Clin Pharmacol 2011; 71(6):917-920.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
2 ) Ridruejo E , Cacchione R , Villamil AG , et al: Imatinib-induced fatal acute liver failure. World J Gastroenterol 2007; 13(48):6608-111.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
Imatinib Overview
-
Imatinib is used to treat certain types of leukemia (cancer that begins in the white blood cells) and other cancers and disorders of the blood cells. Imatinib is also used to treat certain types of gastrointestinal stromal tumors (GIST; a type of tumor that grows in the walls of the digestive passages and may spread to other parts of the body). Imatinib is also used to treat dermatofibrosarcoma protuberans (a tumor that forms under the top layer of skin) when the tumor cannot be removed surgically, has spread to other parts of the body, or has come back after surgery. Imatinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.
Return To Our Drug Interaction Homepage
Feedback, Question Or Comment About This Information?
Ask Dr. Brian Staiger, PharmD, our medical editor, directly! He's always more than happy to assist.
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.