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Drug Interactions between Epitol and relugolix

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

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Interactions between your drugs

Major

carBAMazepine relugolix

Applies to: Epitol (carbamazepine) and relugolix

GENERALLY AVOID: Coadministration with potent inducers of CYP450 3A4 that also induce P-glycoprotein (P-gp) may significantly decrease the plasma concentrations of relugolix. In vitro, relugolix is metabolized primarily by CYP450 3A and, to a lesser extent, by CYP450 2C8. Relugolix is also a substrate for intestinal P-gp. When relugolix was coadministered with rifampin, a combined P-gp and potent CYP450 3A inducer, relugolix peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 23% and 55%, respectively. Reduced efficacy of relugolix may occur. By contrast, no clinically significant differences in the pharmacokinetics of relugolix were observed when coadministered with enzalutamide, a strong CYP450 3A inducer that is not known to induce P-gp.

MANAGEMENT: Concomitant use of relugolix with combined P-gp and potent CYP450 3A inducers should generally be avoided. However, when relugolix is used as monotherapy for the treatment of prostate cancer and coadministration is required, the manufacturer recommends increasing the relugolix dosage to 240 mg once daily. Therapeutic response and tolerance should be monitored more frequently. Following discontinuation of the P-gp/CYP450 3A inducer, treatment with relugolix should be resumed at the normally recommended dosage of 120 mg once daily.

References

  1. (2021) "Product Information. Orgovyx (relugolix)." Myovant Sciences, Inc.

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Drug and food interactions

Moderate

carBAMazepine food

Applies to: Epitol (carbamazepine)

GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of carbamazepine. Use in combination may result in additive central nervous system depression and/or impairment of judgment, thinking, and psychomotor skills.

In a small, randomized, crossover study, the administration of carbamazepine with grapefruit juice (compared to water) increased plasma drug concentrations by approximately 40%. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.

MANAGEMENT: Patients receiving carbamazepine should be advised to avoid or limit consumption of alcohol. Given the drug's narrow therapeutic index, patients receiving carbamazepine therapy should preferably avoid the regular consumption of grapefruits and grapefruit juice to prevent any undue fluctuations in plasma drug levels. Patients should be advised to report signs of carbamazepine toxicity (nausea, visual disturbances, dizziness, or ataxia) to their physicians.

References

  1. (2002) "Product Information. Tegretol (carbamazepine)." Novartis Pharmaceuticals
  2. Garg SK, Kumar N, Bhargava VK, Prabhakar SK (1998) "Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy." Clin Pharmacol Ther, 64, p. 286-8
  3. Bailey DG, Dresser GR, Kreeft JH, Munoz C, Freeman DJ, Bend JR (2000) "Grapefruit-felodipine interaction: Effect of unprocessed fruit and probable active ingredients." Clin Pharmacol Ther, 68, p. 468-77

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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.