Ezetimibe and Cyclosporine: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Cyclosporine
Ezetimibe
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased ezetimibe and cycloSPORINE exposure and an increased risk of ezetimibe and cycloSPORINE-related adverse effects
Interaction Deep Dive
Concomitant use of ezetimibe/simvastatin with cycloSPORINE is contraindicated because of the increased risk of myopathy and rhabdomyolysis2. Concomitant use of ezetimibe with cycloSPORINE may increase the exposure of both drugs 3. Monitor cycloSPORINE levels in patients also receiving ezetimibe. In patients treated with cycloSPORINE, the potential effects of the increased exposure to ezetimibe from concomitant use should be carefully weighed against the benefits of alterations in lipid levels provided. The degree of increase in ezetimibe exposure may be greater in patients with severe renal insufficiency 31. Additionally, avoid concomitant use of cycloSPORINE with ezetimibe/rosuvastatin 4.
Why it happens (mechanism)
Unknown
Literature reports
5 reports — tap to read
a) Ezetimibe reduced LDL-C to an unexpected level when administered concomitantly with cycloSPORINE in a 64-year-old male orthotopic heart transplant patient. The patient was receiving cycloSPORINE 100 mg twice daily and mycophenolate mofetil 1500 mg twice day and could not tolerate high-dose atorvastatin treatment to control his hypercholesterolemia. His LDL-C level was 126 mg/dL when ezetimibe 10 mg daily was initiated. After 2 months, the LDL-C level dropped an expected 60% to 51 mg/dL. The ezetimibe dose was decreased to 5 mg daily and 2 months later, the LDL-C level was 57 mg/dL 5.
b) In a pharmacokinetic study involving 8 post-renal transplant patient with normal to mildly impaired renal function (creatinine clearance >50 ml/min) concomitant exposure to ezetimibe and cycloSPORINE increased ezetimibe plasma concentrations over 3-fold. Patients received stable doses of cycloSPORINE 75 to 150 mg twice daily and experienced increases in the mean area under the concentration-time curve (AUC) and maximum concentration (Cmax) of ezetimibe of 3.4-fold (range 2.3 to 7.9-fold) and 3.9-fold (range 3.0 to 4.4-fold), respectively, compared to a historical healthy population (n=17). In a separate case study, a patient with severe renal impairment (creatinine clearance of 13.2 mL/min/1.73 (m)2) receiving multiple therapies including cycloSPORINE, had 12 times the exposure to ezetimibe compared to healthy subjects 1.
c) In a two-period crossover study, the mean AUC of cycloSPORINE increased 15% with concomitant exposure to ezetimibe as compared to cycloSPORINE alone. Twelve healthy subjects received ezetimibe 20 mg daily for 8 days with a single dose of cycloSPORINE 100 mg on day 7. The cycloSPORINE AUC increased an average of 15% (range 10% decrease to 51% increase) compared to a single dose of cycloSPORINE 100 mg alone 1.
d) In drug interaction studies, when cycloSPORINE, 100 mg single dose administered for 7 days with ezetimibe 20 mg QD for 8 days it increased AUC by 15% and increased Cmax by 10% 24.
e) In drug interaction studies, when cycloSPORINE, stable dose required 75-150 mg twice a day with ezetimibe 10 mg increased AUC by 240% and increased Cmax by 290% 4.
Common questions
Can I take Ezetimibe and Cyclosporine together?
Increased ezetimibe and cycloSPORINE exposure and an increased risk of ezetimibe and cycloSPORINE-related adverse effects Always confirm with your pharmacist or prescriber before making any change.
How serious is the Ezetimibe and Cyclosporine interaction?
It is rated contraindicated. These should generally not be used together.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Ezetimibe or Cyclosporine need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (5)
- Product Information: ZETIA(R) oral tablets, ezetimibe oral tablets. Organon LLC (per FDA), Jersey City, NJ, 2023. DailyMed
- Product Information: VYTORIN(R) oral tablets, ezetimibe simvastatin oral tablets. Organon LLC (per FDA), Jersey City, NJ, 2024. DailyMed
- Product Information: Ezetimibe oral tablets, ezetimibe oral tablets. Aurobindo Pharma USA Inc (per DailyMed), East Windsor, NJ, 2020. DailyMed
- Product Information: ROSZET oral tablets, rosuvastatin ezetimibe oral tablets. Althera Pharmaceuticals LLC (per FDA), Wilmington, DE, 2024.
- Koshman SL, Lalonde LD, Burton I, et al: Supratherapeutic response to ezetimibe administered with cyclosporine. Ann Pharmacother 2005; 39:1561-1565. PubMed
Keep reading about Cyclosporine
Keep reading about Ezetimibe
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