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44 Cards in this Set

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cyclosporine's MOA?
Binds to cyclophilins. Complex blocks the differentiation and activation of T cells by inhibiting calcineurin, thus preventing the production of IL-2 and its receptor.
Tacrolimu (FK506) MOA?
Similar to cyclosporine; binds to FK-binding protein, inhibiting secretion of IL-2 and other cytokines
Sirolimus (rapamycin) MOA?
Inhibits mTOR. Inhibits T cell proliferation in response to IL-2
Daclizumab MOA?
Monoclonal antibody with high affinity for the IL-2 Receptor on activated T cells
Azathioprine MOA?
Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids. Toxic to proliferating lymphocytes.
Muromonab-CD3 (OKT3) MOA?
Monoclonal Ab that binds to CD3 (epsilon chain) on the surface of T cells. Blocks cellular interaction with CD3 protein responsible for T cell signal transduction.
Cyclosporine - clinical use?
1. suppresses organ rejection after transplantation
2. selected autoimmune disorders
Tacrolimus (FK506) - clinical use?
Potent immunosuppressive used in organ transplant recipients.
Sirolimus (rapamycin) - clinical use?
1. Immunosuppression after kidney transplantation in combo w/cyclosporine and corticosteroids
2. also used w/drug eluting stents
Daclizumab - clinical use?
Prevents acute rejection of renal transplant
Azathioprine - clinical use?
1. Kidney transplantation
2. Autoimmune disorders (including glomerulonephritis and hemolytic anemia)
Muromonab-CD3 (OKT3) - clinical use?
Immunosuppression after kidney transplant
Cyclosporine toxicity?
1. Predisposes patient to viral infections and lymphoma
2. nephrotoxic (preventable with mannitol diuretics)
3. gout
Tacrolimus (FK506) toxicity?
SIGNIFICANT!! (think Neil Patrick Harris, NPH... NPPHH)
1. nephrotoxicity
2. Peripheral neuropathy
3. Pleural Effusion
4. Hypertension
5. Hyperglycemia
Sirolimus (rapamycin) toxicity?
1. Hyperlipidemia
2. Thrombocytopenis
3. leukopenia
Azathiprine toxicity?
1. BM suppression
2. Active metabolite mercaptopurine is metabolized by xanthine oxidase so toxic effects may be increased by allopurinol! *
Muromonab-CD3 (OKT3) toxicity?
1. Cytokine release syndrome
2. Hypersensitivity Rxn
Aldesleukin use?
1. Renal Cell Carcinoma
2. Metastatic melanoma
Erythropoietin use?
Anemias (especially in renal failure)
Filgrastim use?
Recovery of bone marrow
Sargramostim use?
recovery of BM
alpha interferon use?
1. Hepatitis B, C
2. Kaposi's Sarcoma
3. Leukemias
4. Malignant Melanoma
beta interferon use?
Multiple sclerosis
gamma interferon use?
chronic granulomatous disease
oprelvekin (interleukin 11) use?
thrombocytopenia
Thrombopoietin use?
thrombocytopenia
Muromonab-CD3 (OKT3) target?
CD3
Muromonab-CD3 (OKT3) clinical use?
prevent acute transplant rejection
Daclizumab target?
IL-2 Receptor
Daclizumab clinical use?
prevent acute rejection of renal transplant
Digoxin Immune Fab target?
Digoxin
Digoxin Immune Fab clinical use?
antidote for digoxin toxicity
Infliximab target?
TNF-alpha
Infliximab clinical use?
1. Crohn's disease
2. rheumatoid arthritis
3. Psoriatic Arthritis
4. Ankylosing Spondylitis
Adalimumab target?
TNF-alpha
Adalimumab clinical use?
1. Crohn's disease
2. rheumatoid arthritis
3. Psoriatic Arthritis
Abciximab target?
glycoprotein 2b/3a
Abciximab clinical use?
Prevent cardiac ischemia in unstable angina and in patients treated with percutaneous coronary intervention (PCI)
Trastuzumab (Herceptin) target?
erb-B2
Trastuzumab (Herceptin) clinical use?
Her-2 - overexpressing breast cancer
Rituximab target?
CD20
Rituximab clinical use?
B-cell non-Hodgkin's lymphoma
Omalizumab target?
IgE
Omalizumab clinical use?
Additional line of Tx for severe asthma