Apixaban with Cobicistat Interaction Details
Brand Names Associated with Apixaban
- Apixaban
- Eliquis®
Brand Names Associated with Cobicistat
- Cobicistat
- Tybost®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Increased exposure of apixaban
Interaction Summary
The concomitant use of apixaban, a substrate of both CYP3A4 and P-glycoprotein (P-gp), with a combined P-gp and strong CYP3A4 inhibitor may increase the exposure of apixaban[1]. Apixaban Cmax increased 62% and AUC increased 97% when coadministered with ketoconazole [2]. Avoid concomitant use in patients receiving apixaban doses of 2.5 mg orally twice daily. Decrease higher apixaban doses (ie, 5 or 10 mg twice daily) by 50% during concomitant use with a combined P-gp and strong CYP3A4 inhibitor [1]. Monitor the patient carefully if coadministration is necessary.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
The concomitant use of apixaban, a substrate of both CYP3A4 and P-glycoprotein (P-gp), with a combined P-gp and strong CYP3A4 inhibitor may increase the exposure of apixaban. Avoid concomitant use in patients receiving apixaban doses of 2.5 mg orally twice daily. Decrease higher apixaban doses (ie, 5 or 10 mg twice daily) by 50% during concomitant use with a combined P-gp and strong CYP3A4 inhibitor[1]. Monitor the patient carefully if coadministration is necessary.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism and inhibition of P-glycoprotein-mediated efflux transport of apixaban
Literature Reports
A) Concurrent administration of apixaban and ketoconazole led to a 62% increase in apixaban Cmax and a 97% increase in apixaban AUC when compared with apixaban alone. Oral apixaban 10 mg was administered 4 days after beginning ketoconazole 400 mg once daily in 18 subjects [2].
References
1 ) Product Information: ELIQUIS(R) oral tablets, apixaban oral tablets. Bristol-Myers Squibb Company (per FDA), Princeton, NJ, 2018.
2 ) Frost CE, Byon W, Song Y, et al: Effect of ketoconazole and diltiazem on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor. Br J Clin Pharmacol 2015; 79(5):838-846.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
Apixaban Overview
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Apixaban is used help prevent strokes or blood clots in people who have atrial fibrillation (a condition in which the heart beats irregularly, increasing the chance of clots forming in the body and possibly causing strokes) that is not caused by heart valve disease. Apixaban is also used to prevent deep vein thrombosis (DVT; a blood clot, usually in the leg) and pulmonary embolism (PE; a blood clot in the lung) in people who are having hip replacement or knee replacement surgery. Apixaban is also used to treat DVT and PE and may be continued to prevent DVT and PE from happening again after the initial treatment is completed. Apixaban is in a class of medications called factor Xa inhibitors. It works by blocking the action of a certain natural substance that helps blood clots to form.
Cobicistat Overview
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Cobicistat is used to increase the amounts of atazanavir (Reyataz, in Evotaz ) in adults and children weighing at least 77 pounds (35 kg) or darunavir (Prezista, in Prezcobix ) in adults and children weighing at least 88 pounds (40 kg) in the blood when these medications are used to treat human immunodeficiency virus (HIV). Cobicistat is in a class of medications called pharmacokinetic boosters. It works by increasing the amount of atazanavir or darunavir in the body so that they can have a greater effect.
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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.