Rosuvastatin with Rolapitant Interaction Details
Brand Names Associated with Rosuvastatin
- Crestor®
- Ezallor®
- Rosuvastatin
Brand Names Associated with Rolapitant
- Rolapitant
- Varubi®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 10, 2023
Interaction Effect
Increased rosuvastatin exposure
Interaction Summary
Concomitant use of oral rolapitant, a BCRP transporter inhibitor, and rosuvastatin, a BCRP substrate, should be undertaken with caution as this may increase rosuvastatin exposure and increase the risk of myopathy and rhabdomyolysis. If coadministered, use the lowest effective dose of rosuvastatin. Coadministration of a single dose of oral rolapitant with another BCRP substrate, sulfasalazine, significantly increased sulfasalazine's Cmax and AUC by 140% and 130%. Coadministration of sulfasalazine with IV rolapitant produced no significant changes.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of oral rolapitant and rosuvastatin should be undertaken with caution as this may increase rosuvastatin exposure and increase the risk of myopathy and rhabdomyolysis. If coadministered, use the lowest effective dose of rosuvastatin.
Mechanism Of Interaction
Inhibition of BCRP-mediated rosuvastatin efflux transport by oral rolapitant
Literature Reports
A) The Cmax and AUC of 500 mg of sulfasalazine, a BCRP substrate, was significantly increased by 140% and 130% when coadministered with a single oral dose of 180 mg of rolapitant, a BCRP transporter inhibitor, on day 1. On day 8, sulfasalazine's Cmax and AUC were still elevated by 17% and 32%. There was no effect on Cmax and AUC of sulfasalazine when coadministered with a single IV dose of 166.5 mg rolapitant. On day 11, sulfasalazine's Cmax and AUC decreased by 18% and 11% but this was not clinically significant .
Rosuvastatin Overview
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Rosuvastatin is used together with diet, weight-loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease. Rosuvastatin is also used to decrease the amount of cholesterol such as low-density lipoprotein (LDL) cholesterol ('bad cholesterol') and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL) cholesterol ('good cholesterol') in the blood. Rosuvastatin may also be used together with diet to decrease the amount of cholesterol and other fatty substances in the blood in children and teenagers 8 to 17 years of age who have familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Rosuvastatin is used together with diet, and alone or in combination with other medications, to decrease the amount of cholesterol and other fatty substances in the blood in adults and children and teenagers 7 to 17 years of age who have familial homozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Rosuvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
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Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats with rosuvastatin has been shown to prevent heart disease, angina (chest pain), strokes, and heart attacks.
Rolapitant Overview
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Rolapitant is used along with other medications to prevent nausea and vomiting that may occur several days after receiving certain chemotherapy medications. Rolapitant is in a class of medications called antiemetics. It works by blocking the action of neurokinin and substance P, natural substances in the brain that cause nausea and vomiting.
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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:
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.