Rosuvastatin with Cyclosporine Interaction Details

Brand Names Associated with Rosuvastatin

Brand Names Associated with Cyclosporine

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 10, 2023

Interaction Effect

Increased rosuvastatin exposure and an increased risk of myopathy and rhabdomyolysis

Interaction Summary

When rosuvastatin 10 mg was coadministered with cycloSPORINE in cardiac transplant patients, rosuvastatin Cmax and AUC increased by 11- and 7.1-fold, respectively. The coadministration of cycloSPORINE and rosuvastatin may result in increased risk of myopathy/rhabdomyolysis. If concomitant is required, rosuvastatin dose should not exceed 5 mg/day. The concomitant use of cycloSPORINE and rosuvastatin/ezetimibe is not recommended .

Severity

Major

Onset

Unspecified

Evidence

Probable

How To Manage Interaction

Concomitant use of cycloSPORINE, an organic anion-transporting polyprotein (OATP1B1) inhibitor, and rosuvastatin, an OATP1B1 substrate, may increase the risk of myopathy/rhabdomyolysis. If coadministration is required, the rosuvastatin dose should be limited to 5 mg once daily. The concomitant use of cycloSPORINE and rosuvastatin/ezetimibe is not recommended .

Mechanism Of Interaction

CycloSPORINE inhibition of organic anion transport protein-mediated hepatic rosuvastatin metabolism

Literature Reports

A) The concurrent administration of rosuvastatin with cycloSPORINE induced substantial increases in rosuvastatin exposure. In an open-label, historical-controlled study, cardiac transplant recipients were administered a single oral dose of rosuvastatin 10 mg followed by 10 once-daily doses of rosuvastatin 10 mg (cohort 1; n=10) or 10 once-daily doses of rosuvastatin 20 mg (cohort 2; n=5) following a single oral dose of rosuvastatin 20 mg. Each patient concurrently received a stable immunosuppressant regimen with cycloSPORINE (dose titrated to maintain whole-blood concentrations between 150 and 200 nanograms/mL), azathioprine, and prednisone. Serial blood analyses were performed over 72 hours after both the initial single dose of rosuvastatin and after the last dose given to each 10-dose regimen cohort. For subjects receiving rosuvastatin 10 mg daily, concomitant administration of cycloSPORINE provoked 10.6-fold and 7.1-fold increases in the rosuvastatin geometric mean steady-state Cmax and AUC, respectively. Compared with the rosuvastatin 10 mg cohort, additional increases in Cmax and AUC (0 to 24) were also observed in subjects receiving rosuvastatin 20 mg once daily; these increases were not directly dose proportional. The presence of rosuvastatin did not markedly alter cycloSPORINE pharmacokinetic parameters. A parallel in vitro study revealed rosuvastatin to have a substrate affinity for organic anion-transporting protein (OATP-C), while cycloSPORINE demonstrated a robust inhibitory effect upon OATP-C activity. The study authors propose that the increase in rosuvastatin serum concentrations results, at least in part, from cycloSPORINE inhibition of OATP-C-mediated hepatic rosuvastatin uptake .

B) Administration of rosuvastatin 10 mg once daily for 10 days in patients receiving cycloSPORINE (75 mg-200 mg twice daily) resulted in 7.1-fold increase in the AUC and 11-fold increase in the Cmax of rosuvastatin .

Rosuvastatin Overview

• 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.

• 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.

Cyclosporine Overview

• Cyclosporine and cyclosporine (modified) are used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system of the person who received the organ) in people who have received kidney, liver, and heart transplants. Cyclosporine (modified) is also used alone or with methotrexate (Rheumatrex) to treat the symptoms of rheumatoid arthritis (arthritis caused by swelling of the lining of the joints) in patients whose symptoms were not relieved by methotrexate alone. Cyclosporine (modified) is also used to treat psoriasis (a skin disease in which red, scaly patches form on some areas of the body) in certain patients who have not been helped by other treatments. Cyclosporine and cyclosporine (modified) are in a class of medications called immunosuppressants. They work by decreasing the activity of the immune system.

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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.