Ribociclib with Fluticasone Propionate Interaction Details

Brand Names Associated with Ribociclib

Brand Names Associated with Fluticasone Propionate

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 11, 2023

Interaction Effect

Increased fluticasone exposure

Interaction Summary

Concomitant use of fluticasone with strong CYP3A inhibitors is not recommended due to an increased risk of systemic corticosteroid adverse effects and increased cardiovascular effects may occur. Use caution during coadministration of fluticasone with strong CYP3A4 inhibitors .

Severity

Major

Onset

Unspecified

Evidence

Probable

How To Manage Interaction

Concomitant use of fluticasone ( a CYP3A4 substrate) with strong CYP3A inhibitors is not recommended due to an increased risk of systemic corticosteroid adverse effects and increased cardiovascular effects may occur. Use caution during coadministration of fluticasone with strong CYP3A4 inhibitors .

Mechanism Of Interaction

Inhibition of CYP3A4-mediated metabolism of fluticasone

Literature Reports

A) In an observational study, 10 of 12 patients with cystic fibrosis who received concomitant inhaled fluticasone and oral itraconazole had evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression, which was moderate or severe in 5 subjects. Clinical evidence of Cushing syndrome was present in 1 subject. All participants had reduced basal and peak serum cortisol levels and a blunted challenge response, particularly when compared with cystic fibrosis patients who received fluticasone but not itraconazole .

B) When orally inhaled fluticasone propionate (1000 mcg) was coadministered with ketoconazole 200 mg once daily (n=8), fluticasone AUC increased 1.9-fold and plasma cortisol AUC decreased 45%. There was no effect on urinary cortisol excretion .

C) In a drug interaction study, the fluticasone furoate AUC was increased by 36%, when coadministered with ketoconazole 400 mg compared with placebo. The increase in fluticasone furoate exposure was associated with a 27% reduction in weighted mean serum cortisol (0 to 24 hours) .

D) In a pharmacokinetic study (N=23), administration of a single midazolam 5 mg dose following multiple doses of idelalisib 150 mg orally twice daily resulted in significant increases in midazolam exposure (138% increase in Cmax and 437% increase in AUC) compared with midazolam alone .

E) Coadministration of a single dose of midazolam (a sensitive CYP3A4 substrate) following 3 weeks of ceritinib 750 mg daily under fasted conditions increased the midazolam AUC by 5.4-fold and Cmax by 1.8-fold compared to midazolam administered alone .

F) Coadministration of diazePAM and idelalisib for 10 days in a 71-year-old woman resulted in altered mental status and respiratory failure. She was receiving diazePAM 5 mg twice daily, venlafaxine XL 300 mg daily, and had initiated idelalisib 150 mg twice daily 10 days prior to presentation. The patient presented with lethargy, speaking difficulty, and progressive weakness inhibiting her ability to stand. Arterial blood gas analysis revealed respiratory acidosis and type II respiratory failure (pH 7.3, PO2 113 mmHg, PCO2 63 mmHg, and bicarbonate 31 mEq/L). Venlafaxine was reduced to 37.5 mg daily, diazePAM was changed to LORazepam 0.5 mg twice daily, and full-dose idelalisib was restarted with no further sequelae .

G) The strong CYP3A inhibitor conivaptan 40 mg/day IV increased the AUC of midazolam, a CYP3A4 substrate, by approximately 100% with a 1-mg IV dose and by 200% with a 2 mg oral dose .

H) Conivaptan 30 mg/day IV tripled the AUC of simvastatin, a CYP3A4 substrate .

I) Conivaptan 40 mg orally twice daily doubled the AUC and half-life of amLODIPine, a CYP3A4 substrate .

Ribociclib Overview

• Ribociclib is used in combination with another medication to treat a certain type of hormone receptor–positive (depends on hormones such as estrogen to grow) advanced breast cancer or that has spread to other parts of the body in women who have not experienced menopause (change of life; end of monthly menstrual periods) and in those who are close to or who have already experienced menopause. Ribociclib is also used in combination with fulvestrant (Faslodex) to treat a certain type of hormone receptor–positive advanced breast cancer or that has spread to other parts of the body as an initial treatment or in people who have not been treated successfully with other treatments in women who have already experienced menopause. Ribociclib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells.

Fluticasone Propionate Overview

• Nonprescription (over the counter) fluticasone nasal spray is used to relieve symptoms of rhinitis such as sneezing and a runny, stuffy, or itchy nose and itchy, watery eyes caused by hay fever or other allergies (caused by an allergy to pollen, mold, dust, or pets). Prescription fluticasone nasal spray is used to relieve symptoms of nonallergic rhinitis such as sneezing and runny or stuffy nose which are not caused by allergies. Prescription fluticasone nasal spray (Xhance) is used to treat nasal polyps (swelling of the lining of the nose). Fluticasone nasal spray should not be used to treat symptoms (e.g., sneezing, stuffy, runny, itchy nose) caused by the common cold. Fluticasone is in a class of medications called corticosteroids. It works by blocking the release of certain natural substances that cause allergy symptoms.

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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.