Immunosuppressants 0519 Flashcards
CYCLOSPORINE mech
bind to cyclophilins-
complex blocks differentiation and activation of T cells by inhibiting CALCINEURIN, thus preventing production of IL-2 and its receptor
CYCLOSPORINE use
- suppress organ rejection after transplant.
2. selected autoimmune d/o.
CYCLOSPORINE tox
predispose to viral infx, lymphoma.
gout.
nephrotoxic.
how can nephrotoxicity of CYCLOSPORINE be prevented?
mannitol diuresis
TACROLIMUS (FK506) mech
similar to cyclosporine.
binds to FK-binding protein to inhibit secretion of IL-2 and other cytokines.
TACROLIMUS (FK506) use
potent immunosuppression in organ transplant recipients
TACROLIMUS (FK506) tox
SIGNIFICANT!! nephrotox. peripheral neuropathy. HTN. pleural effusion. hyperglycemia.
SIROLIMUS (RAPAMYCIN) mech
inhibit mTOR.
inhibit T cell prolix in response to IL-2.
SIROLIMUS (RAPAMYCIN) use
immunosupp after kidney transplant IN COMBO WITH cyclosporine and corticosteroids. also used with drug-eluting stents.
SIROLIMUS (RAPAMYCIN) tox
hyperlipidemia.
thrombocytopenia.
leukopenia.
daclizumab
monoclonal Ab with high affinity for IL-2 receptor on activated T cells
AZATHIOPRINE mech
antimetabolite precursor of 6-mercaptopurine.
interferes w/metabolism and synth of nucleic acids. toxic to proliferating lymphocytes.
AZATHIOPRINE use
kidney transplant.
autoimmune d/o, including glomerulonephritis and hemolytic anemia.
AZATHIOPRINE tox
BM suppression.
*may be increased by allopurinol bc mercaptopurine is metabolized by xanthine oxidase
MUROMONAB-CD3 (OKT3) mech
monoclonal Ab that binds CD3 epsilon chain on surface of T cells.
blocks cellular interaction with CD3 protein responsible for T cell signal transduction.