Immunosuppressants 2

Question 1

cyclosporin

-class, mech?

Answer 1

enzyme inhibitor
-calcineurin phosphatase

binds to intracellular protein cyclophyllin on cyclosporin-cyclophyllin complex. inhibits calcineurin phosphatase, which prevents activation of NFAT. This prevents the activation of a gene coding for IL-2, IL-3, and TNF-alpha.
Therefore, T cell is not activated

Question 2

cyclosporin

-Tx, SE, contraindications?

Answer 2

-transplantation, psoriasis, and dry eye

SE: nephrotoxicity, liver toxicity, cosmetic (unwanted hair growth- hypertrichosis, gingival hyperplasia), increase cholesterol, and mild hypertension

contra: metabolized by p450 (possibility of drug interaction)

Question 3

tacrolimus

-class/mech?

Answer 3

enzyme inhibitor
-calcineusin phosphatase

binds to FK binding protein (FKBP), this complex inhibits calcineusin phosphatase, leading to inhibition of cytokine synthesis

Question 4

tacrolimus

-Tx, SE, contra?

Answer 4

-transplantation

SE: nephro/neurotoxicity
allopecia (bald)
diabetes

-contra: p450 metabolized (possibility of drug interactions)

Question 5

is cyclosporine or tacrolimus more efficacious?

Answer 5

tacrolimus