Itraconazole and Cyclosporine Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Itraconazole
Cyclosporine Injection
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 and risk of cycloSPORINE toxicity (renal dysfunction, cholestasis, paresthesias)
Interaction Deep Dive
There have been conflicting reports regarding the impact of the concurrent use of cycloSPORINE and itraconazole21. Monitor circulating cycloSPORINE levels and adjust cycloSPORINE dosage as necessary. Dose adjustments of calcineurin inhibitors, including cycloSPORINE, should be based on individual requirements and not be performed in a uniform manner as there is significant variation in the degree of interaction between itraconazole and calcineurin inhibitors 3.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated cycloSPORINE metabolism by itraconazole; inhibition of P-gp-mediated metabolism of cycloSPORINE
Literature reports
3 reports — tap to read
a) In a pharmacokinetic study, administration of itraconazole 200 mg oral solution once daily to an existing calcineurin inhibitor regimen (established steady dose of cycloSPORINE A or tacrolimus) resulted in increased calcineurin inhibitor exposure in 10 allogeneic hematopoietic stem cell transplant recipients. The calcineurin inhibitor concentration/dose (C/D; (nanograms/mL)/(mg/kg)) ratio significantly increased by 93.7% (range, 37.3% to 328.2%) 7 to 10 days after itraconazole administration. The calcineurin inhibitor C/D ratio increase was significantly correlated with itraconazole/hydroxyitraconazole plasma levels (correlation coefficient, 0.65; p less than 0.05) 3.
b) One case report describes a 59-year-old lung transplant patient maintained on multiple medications including cycloSPORINE and itraconazole, who experienced increased cycloSPORINE levels and elevated muscle enzyme blood levels. She complained of weakness, muscle pain, and nausea beginning one week prior to admission. Concentration of whole blood cycloSPORINE was 611 nanograms/mL, CPK was 14,765 Units/L (normal: 24 to 175 Units/L), lactic acid dehydrogenase (LDH) was 2120 Units/L (230 to 480 Units/L), glutamic oxalic transaminase (GOT) was 1516 Units/L (7 to 40 Units/L). Serum creatinine level was normal (0.9 mg/dL). Electromyography revealed myopathic changes. CycloSPORINE therapy was replaced with tacrolimus and with supportive measures the patient recovered 1.
c) Lung transplant recipients not receiving itraconazole had greater Cmax, percent peak-trough fluctuation, rise to Cmax, and Tmax values for cycloSPORINE compared to those receiving itraconazole 200 mg and 400 mg daily. Patients not currently receiving itraconazole (n=20) were compared to those receiving itraconazole 200 mg (n=20) and 400 mg (n=20) daily. All patients received cycloSPORINE (microemulsion), prednisone, and mycophenolate. CycloSPORINE levels were monitored at steady-state predose, 1, 2, and 4 hours (h) after the morning dose (C0, C1, C2, and C4, respectively), and levels at C0, C2 and the AUC (0 to 12 h) were comparable in all groups. In patients not receiving itraconazole, the mean cycloSPORINE Cmax was 1123 nanograms/mL (standard deviation (SD) +/- 374 nanograms/mL; range, 627 to 1925) compared with 890 nanograms/mL (SD, +/- 387; range, 367 to 1539) and 825 nanograms/mL (SD, +/- 271; range, 403 to 1322) in the itraconazole 200 mg and 400 mg group, respectively (p=0.03). In the group not receiving itraconazole, there was higher percent peak-trough fluctuation (203 +/- 70 nanograms/mL; range, 85 to 325) compared to the itraconazole 200 mg group (148 +/- 67 nanograms/mL; range, 48 to 281) and the 400 mg group (135 +/- 49 nanograms/mL; range, 62 to 253; p=0.009). Rise to Cmax was 835 nanograms/mL/h (SD, +/- 483; range, 175 to 1724) in patients not on itraconazole compared to 517 nanograms/mL/h (SD, +/- 446; range, 35 to 1376) and 387 nanograms/mL/h (SD, +/- 262; range, 56 to 955) in patients on itraconazole 200 mg and 400 mg, respectively (p=0.003). Patients not receiving itraconazole had a mean time to Cmax of 1.3 h (SD +/- 0.5 h; range, 1 to 2 h) compared to 1.9 h with patients taking daily itraconazole 200 mg (SD, +/- 1 h; range, 1 to 4 h) and 2 h in the 400 mg group (SD, +/- 0.9 h; range, 1 to 4 h; p=0.04) 2.
Common questions
Can I take Itraconazole and Cyclosporine Injection together?
Increased cycloSPORINE exposure and risk of cycloSPORINE toxicity (renal dysfunction, cholestasis, paresthesias) Always confirm with your pharmacist or prescriber before making any change.
How serious is the Itraconazole and Cyclosporine Injection 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 "established". Well documented — supported by controlled studies or strong clinical data.
From our Q&A
Real reader questions about these medications, each personally answered by our pharmacist:
Questions for your pharmacist
- Does my dose of Itraconazole or Cyclosporine Injection 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 (3)
- Cohen E, Kramer MR, Maoz C, et al: Cyclosporin drug-interaction-induced Rhabdomyolysis. A report of two cases in lung transplant recipients. Transplantation 2000; 70:119-122.
- Irani S, Fattinger K, Schmid-Mahler C, et al: Blood concentration curve of cyclosporine: impact of itraconazole in lung transplant recipients. Transplantation 2007; 83(8):1130-1133. PubMed
- Sansone-Parsons A, Krishna G, Martinho M, et al: Effect of oral posaconazole on the pharmacokinetics of cyclosporine and tacrolimus. Pharmacotherapy 2007; 27(6):825-834. DOI
Keep reading about Itraconazole
Keep reading about Cyclosporine Injection
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