Sirolimus and Cyclosporine Ophthalmic: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Sirolimus
Cyclosporine Ophthalmic
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 sirolimus exposure and an increased risk of sirolimus toxicity (anemia, leukopenia, thrombocytopenia, hypokalemia, diarrhea)
Interaction Deep Dive
Increases in sirolimus blood concentrations occur when the drug is given at the same time as cycloSPORINE. CycloSPORINE pharmacokinetics are unaffected by sirolimus. Immunosuppressive synergy has been observed with this combination347. It is recommended that sirolimus be administered four hours after cycloSPORINE oral solution or capsules 6. Coadministration of full dose-cycloSPORINE and sirolimus resulted in elevations in serum creatinine. This effect is often reversible with cycloSPORINE dose reduction 2.
Why it happens (mechanism)
Increased sirolimus bioavailability
Literature reports
3 reports — tap to read
a) In renal transplant recipients, there is no significant pharmacokinetic interaction between sirolimus and cycloSPORINE 34. In contrast, the timing of cycloSPORINE dosing affects sirolimus pharmacokinetics. Sirolimus whole-blood peak/trough levels and area under the concentration-time curve (AUC) have been significantly higher following concomitant administration of these agents compared to their administration four hours apart. Whole-blood trough levels increased by about 30% with concomitant dosing; the time to peak levels was also shorter in this group (1.8 versus 2.5 hours) 3. The most likely explanation for higher sirolimus levels during concomitant administration is an increase in sirolimus bioavailability. Clinically significant immunosuppressive synergy is observed during combined therapy with sirolimus and cycloSPORINE 5.
b) In a single dose drug interaction study, sirolimus 10 mg and cycloSPORINE 300 mg (Neoral(R)) oral soft gelatin capsules were administered either simultaneously or spaced by four hours. When given together, the sirolimus mean maximum concentration (Cmax) and area under the concentration-time curve (AUC) were increased by 116% and 230%, respectively, relative to administration of sirolimus alone. However, when sirolimus was given four hours after cycloSPORINE, the Cmax and AUC were increased by 37% and 80%, respectively, compared to administration of sirolimus alone. The mean cycloSPORINE Cmax and AUC were not significantly affected by sirolimus when given concomitantly or four hours after cycloSPORINE. After multiple-dose administration for six months of sirolimus four hours after cycloSPORINE in renal transplant recipients, the oral clearance of cycloSPORINE was reduced, and lower doses of cycloSPORINE were needed to maintain the target cycloSPORINE concentration 6.
c) In a multiple-dose study involving 150 psoriasis patients, sirolimus was given simultaneously with cycloSPORINE (Sandimmune(R)) oral solution. The average increase in sirolimus trough concentrations ranged between 67% and 86% as compared to sirolimus given alone. No significant effect of multiple-dose sirolimus on cycloSPORINE oral solution trough concentrations was seen 6.
Common questions
Can I take Sirolimus and Cyclosporine Ophthalmic together?
Increased sirolimus exposure and an increased risk of sirolimus toxicity (anemia, leukopenia, thrombocytopenia, hypokalemia, diarrhea) Always confirm with your pharmacist or prescriber before making any change.
How serious is the Sirolimus and Cyclosporine Ophthalmic interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "rapid". Effects can appear quickly, often within about 24 hours of combining the drugs.
How strong is the evidence for this interaction?
The evidence is graded "established". Well documented — supported by controlled studies or strong clinical data.
Questions for your pharmacist
- Does my dose of Sirolimus or Cyclosporine Ophthalmic 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 (7)
- Product Information: NEORAL(R) oral soft gelatin capsules oral solution, cyclosporine modified oral soft gelatin capsules oral solution. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2023. DailyMed
- Product Information: SANDIMMUNE(R) oral capsules, oral solution, intravenous injection, cyclosporine oral capsules, oral solution, intravenous injection. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2023. DailyMed
- Kaplan B, Meier-Kriesche HU, Napoli KL, et al: The effects of relative timing of sirolimus and cyclosporine microemulsion formulation coadministration on the pharmacokinetics of each agent. Clin Pharmacol Ther 1998; 63:48-53. DOI
- Ferron GM, Mishina EV, Zimmerman JJ, et al: Population pharmacokinetics of sirolimus in kidney transplant patients. Clin Pharmacol Ther 1997; 61:416-428. PubMed
- Kelly PA, Gruber SA, Behbod F, et al: Sirolimus, a new, potent immunosuppressive agent. Pharmacotherapy 1997; 17:1148-1156. DOI
- Product Information: RAPAMUNE(R) oral solution, tablets, sirolimus oral solution, tablets. Wyeth Pharmaceuticals Inc (per FDA), Philadelphia, PA, 2022.
- Johnson EM, Zimmerman J, Duderstadt K, et al: A randomized, double-blind, placebo-controlled study of the safety, tolerance, and preliminary pharmacokinetics of ascending doses of orally administered sirolimus (rapamycin) in stable renal transplant recipients. Transpl Proc 1996; 28:987.
Keep reading about Sirolimus
Keep reading about Cyclosporine Ophthalmic
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