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Cyclosporin A
- uses
- mechanism
- dose and half-life
- adverse drug reactions
- contraindications and drug interactions
- metabolism and excretion
Uses
immunosupression
Mechanism
Cyclosporin blocks T cell activation through inhibition of IL-2 and IFN-γ. Molecularly, cyclosporin complexes with cyclophilin, an inhibitor of calcinurin. Calcinurin normally dephosphorylates NF-AT, promoting transcription of cytokines as mentioned above.
Cyclosporin also alters fibroblast metabolism of collagen.
Dose and Half Life
- Neoral is oral cyclosporin A
Adverse Drug Reactions
short term
Acute nephrotoxicity can result from renal vasoconstriction.
Hyperkalemia, hypomagnesemia, hypertension, hepatotoxicity, gum hyperplasia, and hirsuitism can all follow cyclosporin.
Chronic nephrotoxicity can be caused by glomerular ischemia and interstitial fibrosis.
long term
Contraindications and Drug Interactions
Drugs that induce cytochrome CYP3A4 lower drug level.
- grapefruit juice, which inhibits CYP3A4
- St John's Wort induces CYP3A4, leading to increased metabolism
Metabolism and Excretion
- metabolized by CYP 3A4