Immuno Pharm Flashcards
Cyclosporine mech
binds cyclophilins. complex blocks the differentiation & activation of T cells by inhibiting calcineurin, thus preventing the production of IL-2 and its recceptor.
Cyclosporine use
suppresses organ rejection after transplant; selected autoimmune disorders.
Cyclosporine tox
Nephrotox, HTN, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
Tacrolimus mech
(FK-506)
Similar to cyclosporine, binds FK-binding protein, inhibiting calcineurin (norm: causes secretion of IL-2 and other cytokines -> increased growth & differentiation of T cells)
Tacrolimus use
(FK-506)
Potent immunosuppressive used in organ transplants
Tacrolimus tox
(FK-506)
Similar to cyclosporine (Nephrotox, HTN, hyperlipidemia, hyperglycemia, tremor)
W/O - gingival hyperplasia, hirsutism
Sirolimus mech
(rapamycin)
Inhibits mTOR. Inhibits T-cell proliferation in response to IL-2
Sirolimus use
(rapamycin)
Immunosuppression after kidney transplant + cyclosporine & corticosteroids. Also used with drug-eluting stents.
Sirolimus tox
(rapamycin)
hyperlipidemia, thrombocytopenia, leukopenia
Azathioprine mech
antimetabolite precursor of 6-mercaptopurine that interferes w/metabolism & synth of nucleic acids. Toxic to proliferating lymphocytes.
Azathioprine use
Kidney transplant, autoimmune disorders (glomerulonephritis, hemolytic anemia)
Azathioprine tox
Bone marrow suppression. Active metabolite mercaptopurine is metabolized by xanthine oxidase -> tox increased by allopurinol
Muromonab-CD3 mech
(OKT3)
Monoclonal Ab that binds CD3 (epsilon chain) on the surface of T-cells. Blocks cellular interaction with CD3 protein responsible for T-cell transduction.
Muromonab-CD3 use
(OKT3)
immunosuppression after kidney transplant
Muromonab-CD3 tox
(OKT3)
cytokine release syndrome, hypersensitivity reaction
