Mechanism of action tacrolimus is ?
Ans. is 'a' i.e., Inhibition of calcineurin Tacrolimus It is a macrolide immunosuppressant agent. Its mechanism of action is similar to cyclosporine, i.e. inhibition of transcription of IL-2 and T-cell proliferation, but it binds to other immunophilin called FKBP (in contrast to cyclosporine which binds to cyclophilin). Subsequent steps are some, i.e. inhibition of calcineurin, which inhibits T cell activation. Tocrolimus is 10-100 times more potent than cyclosporine. It is also more toxic than cyclosporin. Adverse effects are nephrotoxicity (most common), neurotoxicity, hyperglycemia (DM). Mechanism of nephrotoxicity - Periglomerular afferent aeriolar vasoconstrication and reduced GFR.
Inhibition of calcineurin
Antimetabolite
mTOR inhibitor
Inhibition of DNA synthesis