Mercaptopurine with Febuxostat Interaction Details
Brand Names Associated with Mercaptopurine
- 6-MP
- Mercaptopurine
- Purinethol®
- Purixan®
Brand Names Associated with Febuxostat
- Febuxostat
- Uloric®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 29, 2023
Interaction Effect
Increased azathioprine exposure
Interaction Summary
Concomitant use of azathioprine and febuxostat is contraindicated due to a risk of azathioprine toxicity. A drug interaction study of febuxostat and azathioprine has been conducted. Inhibition of xanthine oxidase by febuxostat caused increased plasma concentrations of 6-mercaptopurine, a metabolite of azathioprine, which may lead to toxicity. During in vivo drug interaction studies, coadministration with febuxostat (40 mg or 120 mg QD) reduced the apparent clearance of mercaptopurine, a xanthine oxidase substrate, by 83.2% to 83.8% following a single oral dose of azathioprine, a prodrug of 6-mercaptopurine. No significant differences were observed in the extent of inhibition of 6-mercaptopurine metabolism by febuxostat 40 mg and 120 mg.
Severity
Contraindicated
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of azathioprine and febuxostat is contraindicated. Concomitant use caused an inhibition of xanthine oxidase by febuxostat resulting in an increase in the exposure of 6-mercaptopurine, metabolite of azathioprine, which may lead to toxicity.
Mechanism Of Interaction
Inhibition of xanthine oxidase-mediated azathioprine metabolism by febuxostat
Literature Reports
A) During in vivo drug interaction studies, coadministration with febuxostat (40 mg or 120 mg QD) reduced the apparent clearance of mercaptopurine, a xanthine oxidase substrate, by 83.2% to 83.8% following a single oral dose of azathioprine, a prodrug of 6-mercaptopurine. No significant differences were observed in the extent of inhibition of 6-mercaptopurine metabolism by febuxostat 40 mg and 120 mg .
B) A drug interaction study of febuxostat and azathioprine has been conducted. Inhibition of xanthine oxidase by febuxostat caused increased plasma concentrations of 6-mercaptopurine, a metabolite of azathioprine, which may lead to toxicity. Drug interaction studies of febuxostat with other drugs that are metabolized by xanthine oxidase(e.g., mercaptopurine) have not been conducted .
Mercaptopurine Overview
-
Mercaptopurine is used alone or with other chemotherapy drugs to treat acute lymphocytic leukemia (ALL; also called acute lymphoblastic leukemia and acute lymphatic leukemia; a type of cancer that begins in the white blood cells). Mercaptopurine is in a class of medications called purine antagonists. It works by stopping the growth of cancer cells.
Febuxostat Overview
-
Febuxostat is used to treat gout in adults who were not treated successfully with or who are not able to take allopurinol (Aloprim, Zyloprim). Gout is a type of arthritis in which uric acid, a naturally occurring substance in the body, builds up in the joints and causes sudden attacks of redness, swelling, pain, and heat in one or more joints. Febuxostat is in a class of medications called xanthine oxidase inhibitors. It works by decreasing the amount of uric acid that is made in the body. Febuxostat is used to prevent gout attacks but not to treat them once they occur.
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.