Amprenavir and Cyclosporine Ophthalmic: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Amprenavir
No brand names on recordCyclosporine 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 cycloSPORINE exposure
Interaction Deep Dive
Coadministration of cycloSPORINE (a CYP3A4 substrate) with amprenavir (a CYP3A4 inhibitor) may increase the plasma concentrations of cycloSPORINE. Adjust cycloSPORINE dosage to achieve the desired cycloSPORINE concentrations when these drugs are administered concomitantly12. A case report described significant increases in cycloSPORINE levels following concomitant administration with either amprenavir/ritonavir or fosamprenavir in 2 HIV-infected patients undergoing liver transplantation 4. Monitoring of therapeutic concentrations of the immunosuppressant is recommended 34.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated cycloSPORINE metabolism by amprenavir
Literature reports
1 report — tap to read
a) Significant increases in cycloSPORINE (CSA) levels occurred following concomitant administration with either amprenavir/ritonavir or fosamprenavir in 2 HIV-infected patients undergoing orthotopic liver transplantation (OLT). Both patients had been receiving highly active antiretroviral therapy (HAART) and required OLT following hepatitis C co-infection. The first patient, a 45-year-old man, was on a stable HAART of amprenavir 300 milligrams (mg), boosted with ritonavir, lamiVUDine, tenofovir, enfuvirtide at the time of surgery. Following OLT, immunosuppression was induced with CSA and steroids, with CSA doses of 200 to 350 mg twice daily, achieving CSA blood levels within the desired therapeutic range (200 to 300 nanograms/milliliter (ng/mL)). In the second week after OLT, re-initiation of HAART resulted in toxic CSA trough levels (greater than 1,000 ng/mL). Amprenavir and ritonavir trough levels were 5,293 and 186 ng/mL, respectively. Subsequently, CSA dose was reduced 12-fold to 25 mg twice daily. The second patient, a 43-year-old man, was on a stable HAART of fosamprenavir (1,400 mg twice daily), tenofovir, and lamiVUDine at the time of surgery. Following OLT, immunosuppression was induced with CSA, at doses of 250 to 350 milligrams (mg) twice daily, achieving CSA blood levels within 300 to 400 ng/mL. On day 12 after transplantation, HAART was resumed, and 48 hours later, CSA trough levels increased from 400 to 600 ng/mL. This prompted a 3.5-fold reduction in CSA dose to 100 mg twice daily. Fosamprenavir trough levels was 1,221 ng/mL. Inhibition of CYP3A-mediated CSA metabolism by amprenavir/ritonavir or fosamprenavir was postulated as the mechanism for this interaction 4.
Common questions
Can I take Amprenavir and Cyclosporine Ophthalmic together?
Increased cycloSPORINE exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Amprenavir 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 "delayed". Effects tend to build up gradually over days to weeks.
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 Amprenavir 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 (4)
- 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
- Product Information: Agenerase(R), amprenavir. Glaxo Wellcome Inc. Research Triangle Park, NC, 2001.
- Guaraldi G, Cocchi S, Codeluppi M, et al: Pharmacokinetic Interaction Between Amprenavir/Ritonavir and FosAmprenavir on Cyclosporine in Two Patients With Human Immunodeficiency Virus Infection Undergoing Orthotopic Liver Transplantation. Transplant Proc 2006; 38(4):1138-1140. PubMed
Keep reading about Amprenavir
Keep reading about Cyclosporine Ophthalmic
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