35 out of 100
Adverse effects of Tacrolimus include all of the following EXCEPT (DNB Dec 2011)
Ans. D Hirsutism
- Tacrolimus (FK506)—It is a newer immunosuppressant chemically different from cyclosporine, but having the same mechanism of action, and is 100 times more potent.
- It binds to a different cytoplasmic immunophilin protein labeled ‘FKBP’, but the subsequent steps are the same, i.e. inhibition of helper T cells via calcineurin.
- Tacrolimus is administered orally as well as by IV infusion. Oral absorption is variable and decreased by food.
- It is metabolized by CYP3A4 and excreted in bile with a longer TVZ of 12 hour.
- Therapeutic application, clinical efficacy as well as toxicity profile are similar to cyclosporine. It is particularly valuable in liver transplantation because its absorption is not dependent on bile.
- Because of more potent action, it is also suitable for suppressing acute rejection.
- Tacrolimus is more likely to precipitate diabetes, neurotoxicity, alopecia and diarrhea. Hypertension, hirsutism and gum hyperplasia are less marked than cyclosporine;