Warfarin with Apalutamide Interaction Details
Brand Names Associated with Warfarin
- Coumadin®
- Jantoven®
- Warfarin
Brand Names Associated with Apalutamide
- Apalutamide
- Erleada®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Decreased exposure of warfarin
Interaction Summary
Warfarin is metabolized by CYP450 enzymes including CYP2C9 and CYP3A4[1]. Apalutamide is a strong inducer of CYP3A4 and a weak inducer of CYP2C9. The AUC of S-warfarin (a CYP2C9 substrate) was decreased by 46% when a single warfarin dose was coadministered with apalutamide [2]. Substitution for warfarin is recommended when possible, or evaluate for loss of activity if coadministration is required [2] and closely monitor INR, especially when starting, stopping, or changing the dose of coadministered CYP450 inducers [1].
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of apalutamide and warfarin may lead to decreased warfarin exposure due to induction of CYP2C9 and CYP3A4 enzymes by apalutamide. Substitution for warfarin is recommended when possible, or evaluate for loss of activity if coadministration is required[2] and closely monitor INR, especially when starting, stopping, or changing the dose of CYP450 inducers [1].
Mechanism Of Interaction
Induction of CYP2C9- and CYP3A4-mediated metabolism of warfarin by apalutamide
References
1 ) Product Information: COUMADIN(R) oral tablets, intravenous injection, warfarin sodium oral tablets, intravenous injection. Bristol-Myers Squibb Company (per FDA), Princeton, NJ, 2017.
2 ) Product Information: Erleada(TM) oral tablets, apalutamide oral tablets. Janssen Products, LP (per FDA), Horsham, PA, 2018.
Warfarin Overview
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Warfarin is used to prevent blood clots from forming or growing larger in your blood and blood vessels. It is prescribed for people with certain types of irregular heartbeat, people with prosthetic (replacement or mechanical) heart valves, and people who have suffered a heart attack. Warfarin is also used to treat or prevent venous thrombosis (swelling and blood clot in a vein) and pulmonary embolism (a blood clot in the lung). Warfarin is in a class of medications called anticoagulants ('blood thinners'). It works by decreasing the clotting ability of the blood.
Apalutamide Overview
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Apalutamide is used to treat certain types of prostate cancer (cancer in men that begins in the prostate [a male reproductive gland]) and has spread to other parts of the body or that has not spread to other parts of the body but has not been helped by other medical treatments. Apalutamide is in a class of medications called androgen receptor inhibitors. It works by blocking the effects of androgen (a male reproductive hormone) to stop the growth and 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.