Calcineurin inhibitor
- ↓ NFAT-driven interleukin-2 transcription in T cells
- Prevents transplant rejection and treats severe autoimmunity
- Nephrotoxicity, hypertension and neurotoxicity are dose-linked
- Blocks T-cell activation — transplant rejection prophylaxis
- Nephrotoxicity, hypertension, tremor
- Narrow therapeutic index with heavy CYP3A4 interaction
Drugs with this mechanism (6)
- Cyclosporine — Calcineurin-inhibitor immunosuppressant; nephrotoxic, many interactions.
- Cyclosporine ophthalmic — Topical calcineurin inhibitor for chronic dry eye; slow but steroid-sparing.
- Pimecrolimus — Topical calcineurin inhibitor for eczema on the face and skin folds — no skin atrophy.
- Tacrolimus — Calcineurin-inhibitor immunosuppressant more potent than cyclosporine.
- Tacrolimus ointment — Steroid-sparing calcineurin-inhibitor ointment for atopic dermatitis; safe on thin skin.
- Voclosporin — Calcineurin-inhibitor immunosuppressant for lupus nephritis.
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