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Drug Interactions between aprepitant and eplerenone

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Major

eplerenone aprepitant

Applies to: eplerenone and aprepitant

ADJUST DOSE: Coadministration with inhibitors of CYP450 3A4 may increase the plasma concentrations of eplerenone, which is primarily metabolized by the isoenzyme. In pharmacokinetic studies, administration of a single 100 mg dose of eplerenone in combination with the potent CYP450 3A4 inhibitor ketoconazole (200 mg twice a day) resulted in a 1.7-fold increase in eplerenone peak plasma concentration (Cmax) and a 5.4-fold increase in systemic exposure (AUC), while administration with moderate inhibitors (erythromycin 500 mg twice daily; verapamil 240 mg once daily; saquinavir 1200 mg three times daily; fluconazole 200 mg once daily) resulted in increases in eplerenone Cmax ranging from 1.4- to 1.6-fold and AUC from 2.0- to 2.9-fold.

MANAGEMENT: When used with moderate CYP450 3A4 inhibitors, the initial dosage of eplerenone should be reduced to 25 mg once daily for the treatment of hypertension. Patients already on eplerenone who start treatment with a moderate CYP450 3A4 inhibitor should have serum potassium and creatinine checked in 3 to 7 days.

References (1)
  1. (2002) "Product Information. Inspra (eplerenone)." Searle

Drug and food interactions

Major

eplerenone food

Applies to: eplerenone

GENERALLY AVOID: Coadministration with grapefruit juice may increase the plasma concentrations of eplerenone. The primary mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits. Inhibition of hepatic CYP450 3A4 may also contribute. In drug interaction studies, administration of a single 100 mg dose of eplerenone in combination with grapefruit juice resulted in a 25% increase in eplerenone systemic exposure (AUC). High blood levels of eplerenone can increase the risk of side effects including hyperkalemia. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

MANAGEMENT: It may be advisable for patients to avoid the consumption of grapefruit, grapefruit juice, or supplements that contain grapefruit during treatment with eplerenone.

References (3)
  1. (2002) "Product Information. Inspra (eplerenone)." Searle
  2. (2021) "Product Information. Eplerenone (eplerenone)." MSN Laboratories Europe Ltd
  3. (2023) "Product Information. Eplerenone (Apotex) (eplerenone)." Apotex Pty Ltd

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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