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.
MUROMONAB-CD3 (OKT3) use
immunosupp after kidney transplant
MUROMONAB-CD3 (OKT3) tox
cytokine release syndrome.
hypersensitivity rxn.
recombinant cytokine: aldesleukin
IL-2 for RCC, metastatic melanoma
recombinant cytokine: erythropoietin
epoetin for anemias (esp in renal failure)
recombinant cytokine: filgrastim
granulocyte colony-stimulating factor for recovery of BM
recombinant cytokine: sargramostim
granulocyte-macrophage colony-stimulating factor for recovery of BM
recombinant cytokine: alpha interferon
for hep B and C.
Kaposi sarcoma.
leukemias.
malignant melanoma.
recombinant cytokine: beta interferon
for multiple sclerosis
recombinant cytokine: gamma interferon
for CGD
recombinant cytokine: oprelvekin
IL-11 for thrombocytopenia
recombinant cytokine: thrombopoietin
for thrombocytopenia
therapeutic Ab: muromonab CD3 (OKT3)
targets CD3 to prevent acute transplant rejection
therapeutic Ab: daclizumab
targets IL-2 receptor to prevent acute rejection of renal transplant
therapeutic Ab: digoxin immune Fab
targets digoxin as antidote for intox
therapeutic Ab: infliximab
targets TNF-a for Crohn’s disease, RA, psoriatic arthritis, ankylosing spondylitis
therapeutic Ab: adalimumab
targets TNF-a for Crohn’s disease, RA, psoriatic arthritis
therapeutic Ab: abciximab
targets GpIIb/IIIa to prevent cardiac ischemia in unstable angina and in pts treated with percutaneous coronary intervention
therapeutic Ab: trastuzumab (Herceptin)
targets erg-B2 for HER2-overexpressing breast cancer
therapeutic Ab: rituximab
targets CD20 for B cell non-Hodgkin lymphoma
therapeutic Ab: omalizumab
targets IgE for additional line of tx for severe asthma
