Cyclosporine

Calcineurin inhibitor, Immunosuppressant

Cyclosporine (ciclosporin)

Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic)

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Summary

Classes

Calcineurin inhibitor, Immunosuppressant

Pharmacy

Starting dose

Transplant: 5-10 mg/kg/d divided BID, titrated to trough levels (typically 100-300 ng/mL depending on regimen and post-transplant interval); ophthalmic Restasis 0.05% one drop BID

Preparations

Sandimmune 25, 100 mg capsules; Neoral 25, 100 mg modified soft gel; 100 mg/mL oral solution; 50 mg/mL IV; Restasis 0.05% ophthalmic emulsion

US FDA Max

Transplant: regimen-specific

Pharmacology

Routes

Oral, IV, ophthalmic

Onset

Days for immunosuppressive effect

Duration

Dosing-frequency dependent

Half-life

~8-27 hours (highly variable across the population)

Bioavailability

Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; Sandimmune and Neoral are NOT bioequivalent and not interchangeable

Pregnancy

Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.^{[citation needed]}

Legal status

Rx-only in US. Carries Boxed Warning for risk of malignancy and serious infection; nephrotoxicity, hypertension, and immunosuppression-associated complications

Purported mechanism

Cyclosporine binds cyclophilin to form a complex that inhibits calcineurin, blocking the calcium-dependent phosphatase activation of NFAT and downstream IL-2 transcription; the net effect is selective inhibition of T-cell activation.▲0▼ CYP3A4 substrate with extensive drug-interaction profile (azoles, macrolides, calcium channel blockers, grapefruit) and P-glycoprotein inhibition affecting digoxin, statins, and others. Therapeutic drug monitoring is universal — trough levels (or AUC) define safe efficacy windows.