Carvedilol and Relugolix: Interaction Details
AI-assisted, pharmacist-reviewed · AI content regenerated Jul 11, 2026 · Source data updated Jul 2, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Relugolix
Carvedilol
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
Here's what's going on. Relugolix (Orgovyx) is normally pumped out of your body by a protein called P-gp. Carvedilol (Coreg) can slow that pump down. When the pump slows, more relugolix stays in your body, so its levels can go up. In one study, a similar blocker raised relugolix levels by about 3 times.
Higher relugolix levels can mean more of its side effects, like hot flashes, fatigue, or joint pain. The good news is your care team can manage this by spacing the medicines apart and watching you a little more closely. Please don't stop or change either drug on your own, just check in with your pharmacist or doctor.
Mechanism: Relugolix is a P-gp substrate; carvedilol inhibits P-gp-mediated intestinal efflux, reducing relugolix clearance and increasing systemic exposure. Neither drug is a prodrug here, so this is a straightforward exposure increase.
- Direction/magnitude: Increased relugolix AUC/Cmax. Reference inhibitor (erythromycin) raised AUC ~3.5-fold and Cmax ~2.9-fold.
- Evidence: Probable; severity major.
- Management: Avoid concomitant use if possible. If unavoidable, give relugolix first, separate dosing by at least 6 hours, and monitor more frequently for relugolix adverse effects. Relugolix may be interrupted up to 2 weeks for short P-gp inhibitor courses; if held >7 days, restart with 360 mg loading dose then 120 mg daily.
What happens
Increased relugolix exposure
Interaction Deep Dive
Because relugolix is a P-gp substrate, combining it with P-gp inhibitors should be avoided, since doing so can raise relugolix exposure and thereby heighten the likelihood of relugolix-related adverse reactions. When such coadministration cannot be avoided, give relugolix or the relugolix/estradiol/norethindrone acetate combination first, allow a minimum interval of 6 hours between the two agents, and increase the frequency of monitoring for adverse reactions12. Relugolix therapy may be paused for as long as 2 weeks to accommodate a brief course of specific P-gp inhibitors, with relugolix resumed once the P-gp inhibitor has been stopped. When relugolix has been interrupted for more than 7 days, it should be reinitiated using a 360 mg loading dose on day one, followed by 120 mg once daily thereafter. A drug interaction study showed that giving relugolix (a P-gp substrate) together with erythromycin (a P-gp inhibitor) raised the AUC and Cmax of relugolix by 3.5-fold and 2.9-fold, respectively1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport of relugolix
How to manage this interaction
Keep taking both as prescribed unless your care team tells you otherwise. Here is how a team usually handles this combination:
- They may try to avoid using them together when another option exists.
- If both are needed, they often have you take relugolix first and separate the two doses by at least 6 hours.
- They will likely monitor you more closely for relugolix side effects such as hot flashes, fatigue, or joint discomfort.
- For a short course of a P-gp blocker, relugolix may be briefly paused and restarted later.
What to do: tell your pharmacist and prescriber that you take both, and report any new or worsening side effects.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a drug interaction study, giving relugolix (a P-gp substrate) together with erythromycin (a P-gp inhibitor) raised the AUC of relugolix by 3.5-fold and its Cmax by 2.9-fold 1.
Common questions
Can I take Carvedilol and Relugolix together?
Carvedilol can raise relugolix levels and its side effects; take relugolix first, separate doses by at least 6 hours, and let your care team monitor you. Do not change either medication on your own. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Carvedilol and Relugolix interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How is the Carvedilol and Relugolix interaction managed?
Keep taking both as prescribed unless your care team tells you otherwise. Here is how a team usually handles this combination: They may try to avoid using them together when another option exists. If both are needed, they often have you take relugolix first and separate the two doses by at least 6 hours. They will likely monitor you more closely for relugolix side effects such as hot flashes, fati… Management is individual — always follow your own care team's guidance.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
From our Q&A
Real reader questions about these medications, each personally answered by our pharmacist:
Questions for your pharmacist
- Does my dose of Carvedilol or Relugolix need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (2)
- Product Information: ORGOVYX oral tablets, relugolix oral tablets. Sumitomo Pharma America, Inc (per FDA), Marlborough, MA, 2025. DailyMed
- Product Information: MYFEMBREE(R) oral tablets, relugolix, estradiol, norethindrone acetate oral tablets. Myovant Sciences Inc (per FDA), Brisbane, CA, 2021. DailyMed
Keep reading about Relugolix
Keep reading about Carvedilol
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