Immunosuppressants

Question 1

Tacrolimus

Answer 1

Calcineurin inhib, binds FK506 binding protein and prevents IL2 transcription –> no T cell activation

Prevent rejection

Nephrotoxic! Increased risk of DM and neurotox relative to cyclosporine

Question 2

Sirolimus (aka?)

Answer 2

aka Rapamycin

mTOR inhib, binds FKBP (like tacrolimus)

Blocks response to IL2 –> no T cell activation or B cell differentiation

Prevent rejection

Can –> pancytopenia, insulin resistance, hyperlipidemia but NOT NEPHROTOXIC (so often used with cyclosporine), also in stents

Question 3

Daclizumab, basiliximab

Answer 3

Monoclonal antibodies that block IL-2R

Kidney transplant rejection prophylaxis

Can –> Edema, HTN, tremor

Question 4

Azathioprine

Answer 4

Precursor of 6-mercaptopurine, blocks purine synthesis and thus inhibits lymphocyte prolif

Transplant rejection, RA, Crohn disease, GN, others

Can –> pancytopenia

Question 5

Glucocorticoids

Answer 5

Inhibit NF-kappaB

Suppress B and T cell fxn by decreasing cytokine transcription

Can –> hyperglycemia, osteoporosis, central obesity, Cushing, muscle breakdown, psychosis, acne, htn, cataracts, avascular necrosis (BAD)

Question 6

Calcineurin inhibitors

Answer 6

Cyclosporine and Tacrolimus (prevent IL2 transcription)

Question 7

Cyclosporine

Answer 7

Calcineurin inhibitor, binds cyclophilin

Blocks T cell activation by preventing IL2 transcription

Prevents rejection, psoriasis, RA

nephrotoxic!! also can cause neurotox, gingival hyperplasia, hirsutism, htn