Cyclosporine

Summary

Cyclosporine is an immunosuppressant drug that is used to prevent transplant rejection and treat autoimmune diseases. It suppresses the immune system by inhibiting calcineurin, an enzyme necessary for IL-2 production. By inhibiting calcineurin, cyclosporine leads to a fall in IL-2 levels, which impairs T cell growth and activation. This results in an overall suppression of the immune response. However, cyclosporine does come with many adverse effects, of which the most important to remember are nephrotoxicity, gout or hyperuricemia, gingival hyperplasia, and hirsutism. Less important side effects include hyperlipidemia, neurotoxicity, and hypertension.

Key Points

• Cyclosporine
  • Immunosuppressant drug
    • Used for transplant rejection prophylaxis, psoriatic arthritis, rheumatoid arthritis
  • Mechanism
    • Inhibits calcineurin by forming a complex with cyclophilin
      • Blocks transcription and production of Interleukin-2 (IL-2)
    • Ultimately results in reduced lymphocyte proliferation
      • Especially signalling by Helper T-cells
  • Adverse Effects
    • Nephrotoxicity
    • Gout/Hyperuricemia
    • Gingival Hyperplasia
    • Hirsutism
    • Hypertension
    • Hyperlipidemia
    • Neurotoxicity