Cyclosporine
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Cyclosporine (ciclosporin)
Sandimmune, Neoral (modified microemulsion, increased bioavailability), Gengraf, Restasis (ophthalmic)
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Summary
Common uses
Solid organ transplant rejection prevention0, Bone marrow transplant GVHD prophylaxis0, Severe psoriasis (short-term rescue)0, Refractory rheumatoid arthritis0, Dry eye disease (ophthalmic emulsion)0
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)[1]
Bioavailability
Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; Sandimmune and Neoral are NOT bioequivalent and not interchangeable[1]
Pregnancy
Used in transplant pregnancy when continued immunosuppression is required; reassuring data overall but careful monitoring needed.[citation needed]
Legal status
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[1].
References
edit- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Neoral (cyclosporine, USP) MODIFIED, Novartis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/050715s039,050716s041lbl.pdf