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Ciclosporin

Immunosuppressant

Also known as SANDIMMUNE, NEORAL, Capsorin, Capimune, Deximune

Immunosuppressant
CDSCO approved
EXCRETION
not curated
INTERACTIONS
6 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AminoglycosideSevereTextbookKDT 7e · p746
  • Amphotericin BSevereDatabaseKimi deep-research + Cla
  • CaspofunginSevereDatabaseKimi deep-research + Cla
  • EzetimibeSevereDatabaseKimi deep-research + Cla

Mechanism

Ciclosporin binds to cyclophilin, a cytoplasmic-receptor protein present in target cells. This complex binds to calcineurin, inhibiting Ca2+-stimulated dephosphorylation of the cytosolic component of NFAT. This prevents NFAT from entering the nucleus, inhibiting gene transcription and T lymphocyte activation. Cyclosporine also increases expression of transforming growth factor "β" (TGF-"β"), an inhibitor of IL-2 –stimulated T-cell proliferation and generation of cytotoxic T lymphocytes (CTLs).

Indications

Kidney transplantationLiver transplantationHeart transplantationOther organ transplantationRheumatoid arthritisPsoriasis

Dosing

Renal adjustment
No adjustments generally are necessary for dialysis or renal failure patients.
Hepatic adjustment
In the presence of hepatic dysfunction, dosage adjustments are required.

Pharmacokinetics

Bioavailability
Original soft gelatin capsule: 20-50%. Modified microemulsion formulation (Neoral): more uniform and slightly increased bioavailability.
Metabolism
Extensively metabolized in the liver by CYP3A and to a lesser degree by the GI tract and kidneys. At least 25 metabolites identified.
Excretion
Principally through the bile into the feces, with ~6% being excreted in the urine. Only 0.1% excreted unchanged in urine.

Pregnancy & lactation

Lactation

Cyclosporine is excreted in human milk.

Drug interactions

Aminoglycoside
Severe
Textbook

Increased risk of nephrotoxicity.

Avoid concurrent use.

Source: KDT 7e · p746

Amphotericin B
Severe
Database

Additive nephrotoxicity

Monitor renal function and CNI levels

Source: Kimi deep-research + Cla

Caspofungin
Severe
Database

Increased caspofungin AUC + raised transaminases

Use only if benefit outweighs risk; monitor LFTs

Source: Kimi deep-research + Cla

Ezetimibe
Severe
Database

Markedly increased ezetimibe (and ciclosporin) exposure

Monitor ciclosporin levels; use lowest ezetimibe dose, caution

Source: Kimi deep-research + Cla

Modafinil
Severe
Database

CYP3A4 induction → subtherapeutic ciclosporin

Monitor levels; adjust dose

Source: Kimi deep-research + Cla

Octreotide
Severe
Database

Reduced ciclosporin absorption → graft rejection risk

Monitor ciclosporin levels, adjust dose

Source: Kimi deep-research + Cla

Azilsartan Medoxomil
Moderate
Database

Increased risk of hyperkalemia.

Monitor serum potassium levels, especially in patients with risk factors for hyperkalemia.

Source: DDInter

Etoricoxib
Moderate
Database

Increased risk of ciclosporin-induced nephrotoxicity, leading to impaired renal function.

Avoid concomitant use if possible. If unavoidable, monitor renal function (serum creatinine, BUN) closely and ciclosporin levels. Adjust ciclosporin dose as needed.

Lornoxicam
Moderate
Database

Increased risk of renal dysfunction and nephrotoxicity.

Avoid concomitant use. If unavoidable, monitor renal function (serum creatinine, BUN) very closely. Consider alternative analgesics.

Ornidazole
Moderate
Database

Increased ciclosporin levels, leading to increased risk of nephrotoxicity and other ciclosporin-related adverse effects.

Monitor ciclosporin trough levels closely. Adjust ciclosporin dose as needed. Monitor renal function.

Roxithromycin
Moderate
Database

Increased risk of ciclosporin toxicity (nephrotoxicity, neurotoxicity, hepatotoxicity).

Monitor ciclosporin trough levels closely. Adjust ciclosporin dose as needed.

Teicoplanin
Moderate
Database

Increased risk of acute kidney injury.

Monitor renal function (serum creatinine, BUN) closely. Adjust doses of teicoplanin or ciclosporin as needed. Consider therapeutic drug monitoring for both drugs.

Related guidelines

Other Immunosuppressant drugs

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Sources: BNF·Verified: 2026-05-10 · House clinical team