Amiodarone with Relugolix Interaction Details
Brand Names Associated with Amiodarone
- Amiodarone
- Cordarone®
- Pacerone®
Brand Names Associated with Relugolix
- Orgovyx®
- Relugolix
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Feb 27, 2024
Interaction Effect
Increased plasma concentrations of relugolix; increased risk of QT-interval prolongation
Interaction Summary
Concomitant use of relugolix (a P-gp substrate) and a P-gp inhibitor may increase relugolix exposure, which may increase the risk of adverse reactions associated with relugolix. Additionally coadministration of relugolix with other QT-interval prolonging drugs may result in additive effects on the QT interval[1]. Coadministration of relugolix with erythromycin (P-gp and moderate CYP3A inhibitor) increased the AUC and Cmax of relugolix by 6.2-fold, and coadministration of relugolix or relugolix/estradiol/norethindrone acetate and oral P-gp inhibitors should be avoided. If coadministration with a P-gp inhibitor that also prolongs QT-interval is unavoidable, administer relugolix-containing medication first, separate dosing by at least 6 hours, monitor for adverse reactions more frequently [2][3], correct electrolyte abnormalities, and consider periodic monitoring of ECGs and electrolytes. Treatment with relugolix may be interrupted for up to 2 weeks for a short course of P-gp inhibitor treatment. If relugolix is interrupted for more than 7 days, resume administration with a 360-mg loading dose on the first day followed by 120 mg once daily [1].
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Use caution with coadministration of relugolix with QT-interval prolonging drugs, as additive effects on the QT interval may occur[1]. Additionally, concomitant use of relugolix (a P-gp substrate) and a P-gp inhibitor may increase relugolix exposure, which may increase the risk of adverse reactions associated with relugolix. Avoid coadministration of relugolix or relugolix/estradiol/norethindrone acetate and oral P-gp inhibitors. If coadministration with a P-gp inhibitor that also prolongs the QT-interval is unavoidable, administer relugolix-containing medication first, separate dosing by at least 6 hours, and monitor for adverse reactions more frequently [1][3], correct electrolyte abnormalities, and consider periodic monitoring of ECGs and electrolytes. Treatment with relugolix may be interrupted for up to 2 weeks for a short course of treatment with certain P-gp inhibitors. If treatment with relugolix is interrupted for more than 7 days, resume administration with a 360-mg loading dose on the first day followed by 120 mg once daily [1].
Mechanism Of Interaction
Inhibition of P-gp-mediated efflux transport of relugolix and additive effects on the QT interval
Literature Reports
A) Coadministration of relugolix (P-gp substrate) with erythromycin (P-gp and moderate CYP3A inhibitor) increased the AUC and Cmax of relugolix by 6.2-fold [2].
References
1 ) Product Information: ORGOVYX oral tablets, relugolix oral tablets. Myovant Sciences Inc (per FDA), Brisbane, CA, 2023.
2 ) Product Information: ORGOVYX oral tablets, relugolix oral tablets. Myovant Sciences Inc (per FDA), Brisbane, CA, 2020.
3 ) Product Information: MYFEMBREE(R) oral tablets, relugolix, estradiol, norethindrone acetate oral tablets. Myovant Sciences Inc (per FDA), Brisbane, CA, 2021.
Amiodarone Overview
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Amiodarone is used to treat and prevent certain types of serious, life-threatening ventricular arrhythmias (a certain type of abnormal heart rhythm when other medications did not help or could not be tolerated. Amiodarone is in a class of medications called antiarrhythmics. It works by relaxing overactive heart muscles.
Relugolix Overview
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Relugolix is used to treat advanced prostate cancer (cancer that begins in the prostate [a male reproductive gland]) in adult men. Relugolix is in a class of medications called gonadotropin-releasing hormone (GnRH) receptor antagonists. It works by decreasing the amount of testosterone (a male hormone) produced by the body. This may slow or stop the spread of prostate cancer cells that need testosterone to grow.
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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.