tacrolimus

Question 1

class + moa:

Answer 1

• Tacrolimus is a macrolide used as an immunosuppressant to prevent transplant rejection. It has a very similar action to ciclosporin:

Action of ciclosporin

• decreases clonal proliferation of T cells by reducing IL-2 release
• binds to cyclophilin forming a complex which inhibits calcineurin, a phosphotase that activates various transcription factors in T cells
• The action of tacrolimus differs in that it binds to a protein called FKBP rather than cyclophilin

Question 2

Ses

Answer 2

Tacrolimus is more potent than ciclosporin and hence the incidence of organ rejection is less.

However, nephrotoxicity and impaired glucose tolerance is more common