IMMUNO - Immunosuppressants Flashcards
Immunosuppressant general use
Block lymphocyte proliferation and activation
Decrease ACUTE graft rejection by decreasing CELLULAR immunity
Immunosuppressant general toxicity
Long-term use increases risk of infections and cancer
Cyclosporin MOA
Binds cyclophilin to inhibit calcineurin blocking NFAT dephosphorylation so NFAT can't get into nucleus so no IL-2 TC
Blocks IL-2 TC
cyclosporin use
Transplant rejection prophylaxis
Psoriasis
RA
Cyclosporin toxicity
NEPHROTOXICITY Gingival hyperplasia Hirsutism HTN hyperlipidemia neurotoxicity
Tacrolimus (FK508) MOA
Binds FKBP To inhibit calcineurin blocking NFAT dephosphorylation so NFAT can't get into nucleus so no IL-2 TC
Blocks IL-2 TC
Tacrolimus (FK508) use
transplant rejection prophylaxis
Tacrolimus (FK508) toxicity
NEPHROTOXICITY
HTN
hyperlipidemia (more risk of DM)
neurotoxicity (more risk)
Sirolimus (rapamycin) MOA
binds FKBP
to inhibit mTOR
to block T-cell activation and B-cell differentiation
Inhibits cells RESPONSE to IL-2 (IL-2 activates mTOR)
Sirolimus (rapamycin) use
KIDNEY transplant rejection prophylaxis
Sirolimus (rapamycin) toxicity
Anemia Thrombocytopenia Leukopenia Insulin resistance and hyperlipidemia *NOT nephrotoxic*
Daclizumab MOA
monoclonal Ab to block IL-2R
Daclizumab use
KIDNEY transplant rejection prophylaxis
Daclizumab toxicity
Edema
HTN
Tremor
Basiliximab MOA
monoclonal Ab to block IL-2R
Basiliximab use
KIDNEY transplant rejection prophylaxis
Basiliximab toxicity
Edema
HTN
Tremor
Azathioprine MOA
Antimetabolite: blocks NT (purine) synthesis inhibiting lymphocyte proliferation
Precursor of 6-MP.
Azathioprine use
Transplant rejection prophylaxis RA Chrons Glomerulonephritis Other autoimmunes
Azathioprine toxicities
Leukopenia
Anemia
Thrombocytopenia
*6MP degraded by XO, so increased toxicity by allopurinol