Paper II
2016 February (2010 Scheme) · 40 marks · 120 min

Question

Cyclosporine

Q63 marksShort Notes

Answer

Cyclosporine is a calcineurin inhibitor immunosuppressant.

Mechanism of action

  • Binds to cyclophilin (an intracellular immunophilin), and this complex inhibits calcineurin
  • Calcineurin normally activates the transcription factor NFAT, which promotes IL-2 gene transcription
  • By inhibiting calcineurin, cyclosporine suppresses IL-2 production, reducing T-lymphocyte activation and proliferation (selective effect on cell-mediated immunity)

Uses

  • Prevention of organ transplant rejection (kidney, liver, heart)
  • Severe rheumatoid arthritis, psoriasis (refractory cases)
  • Nephrotic syndrome

Adverse effects

  • Nephrotoxicity (dose-limiting)
  • Hypertension
  • Hepatotoxicity
  • Gingival hyperplasia, hirsutism
  • Increased susceptibility to infections and malignancy (immunosuppression)
  • Tremor

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