Paper II
2019 July (Supplementary) (2010 Scheme)

Question

Tacrolimus

Q73 marksShort Notes

Answer

Tacrolimus is a calcineurin inhibitor immunosuppressant.

Mechanism of action

  • Binds to FKBP (FK-binding protein, an intracellular immunophilin, distinct from cyclosporine’s cyclophilin); this complex inhibits calcineurin
  • Suppresses IL-2 gene transcription, reducing T-lymphocyte activation and proliferation
  • More potent than cyclosporine

Uses

  • Prevention of organ transplant rejection (kidney, liver, heart)
  • Topical use in atopic dermatitis

Adverse effects

  • Nephrotoxicity
  • Neurotoxicity (tremor, seizures)
  • Hyperglycaemia/diabetes (more than cyclosporine)
  • Hypertension
  • Increased susceptibility to infections/malignancy
  • (Less gingival hyperplasia/hirsutism than cyclosporine)

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