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
Glucocorticoids MOA
Inhibits NF-KB, inhibiting cytokine TC, suppressing B and T cell function
Random glucocorticoid toxicity:
Cushings
Psyhchosis
Cataracts
Avascular necrosis
Alemtuzumab (target)
Cancer therapy: CD52
Bevacizumab (target)
Cancer therapy: VEGF
Cetuximab (target)
Cancer therapy: EGFR
Rituximab (target)
Cancer therapy: CD20
Trastuzumab (target)
Cancer therapy: HER2/neu
Alemtuzumab (Clinical use)
Cancer therapy: CLL
Bevacizumab (Clinical use)
Cancer therapy: Colorectal cancer, renal cell carcinoma
Cetuximab (Clinical use)
Cancer therapy: Stage IV colorectal cancer, head and neck cancer
Rituximab (Clinical use)
Cancer therapy: B-cell non-hodgkin lymphoma, CLL, rheumatoid arthritis, ITP
Trastuzumab (Clinical use)
Cancer therapy: Breast cancer
Adalimumab (Target)
Autoimmune therapy: Soluble TNF-alpha
infliximab (Target)
Autoimmune therapy: Soluble TNF-alpha
Eculizumab (Target)
Autoimmune therapy: Compliment protein C5
Natalizumab (Target)
Autoimmune therapy: alpha4-integrin
Etanercept (Target)
Decoy TNF-alhpa receptor (not monoclonal ab)
Adalimumab (Clinical use)
IBD, rheumatoid arthriis, ankylosing spondylitis, psoriasis
Infliximab (Clinical use)
IBD, rheumatoid arthriis, ankylosing spondylitis, psoriasis
Eculizumab (Clinical use)
paroxysmal nocturnal hemoglobinuria
Natalizumab (Clinical use) (+AE)
Multiple sclerosis, Crohn disease
*risk of PML
ABCiximab (target)
Platelet glycoproteins IIb/IIIa
Denosumab (target)
RANKL
Digoxin immune fab (target)
digoxin
Omalizumab (target)
IgE
Palivizumab (target)
RSV F protein
Ranibizumab (target)
VEGF
ABCixumab (Clinical use)
Prevention of ischemic complications in percutaneous coronary intervention
Denosumab (Clinical use)
Osteoporosis; prevents osteoclast maturation
Omalizumab (Clinical use)
Allergic asthma; prevents IgE biding FcR1
Palivizumab (Clinical use)
RSV prophylaxis for high risk infants
Ranibizumab (Clinical use)
Neovascular age-related macular degeneration