Ticagrelor with Apalutamide Interaction Details
Brand Names Associated with Ticagrelor
- Brilinta®
- Ticagrelor
Brand Names Associated with Apalutamide
- Apalutamide
- Erleada®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Decreased ticagrelor exposure and efficacy
Interaction Summary
The concomitant administration of ticagrelor and anti-epileptic strong CYP3A inducers compared with ticagrelor alone significantly increased platelet reactivity and the proportion of patients with high on-treatment reactivity (HPR) in a retrospective database study of patients with acute coronary syndrome[1]. Concomitant administration of ticagrelor and phenytoin produced platelet inhibition that was lower than expected with ticagrelor alone and that improved upon discontinuation of phenytoin in a case report of a man who received ticagrelor after percutaneous coronary intervention and reinitiation of phenytoin upon ICU admission after the procedure [2]. The AUC and Cmax of ticagrelor were significantly decreased with concomitant administration of the strong CYP3A4 inducer rifampin 600 mg once daily in a pharmacokinetic study. Avoid use of ticagrelor with strong inducers of CYP3A as concomitant administration can substantially decrease ticagrelor exposure and efficacy [3].
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Avoid use of ticagrelor with strong inducers of CYP3A as concomitant administration can substantially decrease ticagrelor exposure and efficacy[3].
Mechanism Of Interaction
Induction of CYP3A4-mediated ticagrelor metabolism
Literature Reports
A) Patients admitted with acute coronary syndrome who received ticagrelor concomitantly with an anti-epileptic CYP3A inducer (n=8) compared with those who received ticagrelor without a CYP3A inducer (n=49) had significantly higher mean steady-state VerifyNow P2Y12 reaction unit (PRU) levels (194.6 vs 26.3) in a retrospective database study. Steady-state PRUs were the first PRU measurement 48 hours or more after ticagrelor initiation. The proportion of patients with high on-treatment reactivity (HPR; PRU 208 or greater) was also significantly greater with an anti-epileptic CYP3A inducer (37.5% vs 0%). Patients who received anti-epileptic CYP3A inducers (age range, 60 to 88 years) were on ticagrelor for 2 to 7 days. Anti-epileptic CYP3A inducers were phenytoin (n=5), carbamazepine (n=1), phenytoin and carbamazepine (n=1), and phenytoin and phenobarbital (n=1). All patients received aspirin and ticagrelor 180-mg bolus followed by 90 mg twice daily [1].
B) A 71-year-old man with coronary artery disease was started on ticagrelor after percutaneous coronary intervention (PCI) and reinitiated on his home dose of phenytoin upon ICU admission after the PCI. Phenytoin was discontinued on the second day of ticagrelor therapy, and testing on postprocedure day 3 before the fifth dose of ticagrelor 90 mg showed a VerifyNow P2Y12 reaction unit (PRU) level of 228 and a platelet count of 215,000; a free phenytoin level on that day was 1.28 mcg/mL. Two days later, the phenytoin level was 0.41 mcg/mL. Four days later, platelet inhibition was 155 PRUs and platelet count was 279,000. The patient received ticagrelor 180-mg loading dose after PCI followed by 90 mg twice daily with aspirin 81 mg daily [2].
References
1 ) Pourdjabbar A, Hibbert B, Chong AY, et al: A pharmacodynamic analysis for the co-administration of inducers of CYP3A with ticagrelor: a cautionary tale in managing patients with acute coronary syndromes. Int J Cardiol 2016; 214:423-425.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
2 ) Weeks P, Sieg A, Vahdat K, et al: Improved ticagrelor antiplatelet effect on discontinuation of phenytoin. Ann Pharmacother 2014; 48(5):644-647.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
3 ) Product Information: BRILINTA(R) oral tablets, ticagrelor oral tablets. AstraZeneca Pharmaceuticals LP (per FDA), Wilmington, DE, 2020.
Ticagrelor Overview
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Ticagrelor is used to prevent a serious or life-threatening heart attack or stroke, or death in people who have had a heart attack or who have acute coronary syndrome (ACS; blockage of blood flow to the heart). It is also used to prevent blood clots from forming in people who have received coronary stents (metal tubes surgically placed in clogged blood vessels to improve blood flow) to treat ACS. Ticagrelor is used to decrease the risk of a first-time heart attack or stroke in people at risk with coronary artery disease (CAD; reduced blood flow to the heart). It is also used to decrease the risk of another more serious stroke in people who are having a mild to moderate stroke or a transient ischemic attack (TIA; ministroke). Ticagrelor is in a class of medications called antiplatelet medications. It works by preventing platelets (a type of blood cell) from collecting and forming clots that may cause a heart attack or stroke.
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.