Abiraterone Acetate with Repaglinide Interaction Details

Brand Names Associated with Abiraterone Acetate

Brand Names Associated with Repaglinide

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Feb 25, 2024

Interaction Effect

Increased repaglinide plasma concentrations

Interaction Summary

Concomitant administration of repaglinide and a CYP2C8 inhibitor may increase exposure to repaglinide. In a study of healthy volunteers, concomitant use of repaglinide and deferasirox 30 mg/kg/day resulted in increases in repaglinide AUC and Cmax of 2.3-fold[1] and in a case report, severe hypoglycemia requiring hospitalization was reported when repaglinide was given with abiraterone, a strong CYP2C8 inhibitor [2]. Reduce the dose of repaglinide and increase the frequency of glucose monitoring if concurrent use is clinically indicated [3].

Severity

Moderate

Onset

Unspecified

Evidence

Probable

How To Manage Interaction

Concomitant administration of repaglinide and a CYP2C8 inhibitor may increase exposure to repaglinide. Reduce the dose of repaglinide and increase the frequency of glucose monitoring if concurrent use is clinically indicated[3].

Mechanism Of Interaction

Inhibition of CYP2C8-mediated repaglinide metabolism

Literature Reports

A) Coadministration of deferasirox and repaglinide increased repaglinide exposure in a study with 24 healthy participants. In the study, deferasirox 30 mg/kg was administered once daily for 3 days; on the fourth day participants received a single oral dose of repaglinide 0.5 mg. Results showed that coadministration with deferasirox increased AUC and mean Cmax values of repaglinide by 2.3-fold. Glucose AUC decreased from 63.6 mmol x hr/L to 62 mmol x hr/L with concomitant administration [1].

B) A 79-year-old man receiving repaglinide 4 mg/day for type 2 diabetes mellitus experienced severe hypoglycemia (less than 30 mg/dL) requiring hospitalization, 5 days following initiation of abiraterone plus prednisone as third-line treatment for metastatic castration-resistant prostate cancer. Interruption and subsequent reinitiation of abiraterone coadministered with repaglinide given at a 50% dosage reduction caused a severe hypoglycemia event to reoccur. Repaglinide was discontinued and the patient was initiated on insulin [2].

References

1 ) Skerjanec A, Wang J, Maren K, et al: Investigation of the pharmacokinetic interactions of deferasirox, a once-daily oral iron chelator, with midazolam, rifampin, and repaglinide in healthy volunteers. J Clin Pharmacol 2010; 50(2):205-213.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

2 ) Tucci M, Roca E, Ferrari L, et al: Abiraterone and prednisone therapy may cause severe hypoglycemia when administered to prostate cancer patients with type 2 diabetes receiving glucose-lowering agents. Endocrine 2019; 64(3):724-726.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

3 ) Product Information: PRANDIN(R) oral tablets, repaglinide oral tablets. Novo Nordisk Inc. (per FDA), Plainsboro, NJ, 2017.

Abiraterone Acetate Overview

• Abiraterone is used in combination with prednisone to treat a certain type of prostate cancer that has spread to other parts of the body. Abiraterone is in a class of medications called androgen biosynthesis inhibitors. It works by decreasing the amount of certain hormones in the body.

Repaglinide Overview

• Repaglinide is used to treat type 2 diabetes (condition in which the body does not use insulin normally and, therefore, cannot control the amount of sugar in the blood). Repaglinide helps your body regulate the amount of glucose (sugar) in your blood. It decreases the amount of glucose by stimulating the pancreas to release insulin.

• Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems.Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.

• This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

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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:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

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.