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Terms in this set (42)
1. Binds to cyclophilins
2. Blocks differentiation and activation of T-cells by inhibiting calcineurin and therefore preventing production of IL-2 and its receptor
Give 2 clinical uses for cyclosporine
1. Suppress organ rejection after transplants
2. Selected auto-immune disorders
1. Nephrotoxic (give mannitol diuresis as antidote)
2. HTN, Hyperlipidemia, hyperglycemia
3. Hirsutism and gingival hyperplasia
Tacrolimus (FK-506) MOA
Similar to cyclosporine
1. Binds to FK-binding protein
2. Inhibits calcineurin + secretion of IL-2 (and other cytokines)
what are 2 clinical uses for tacrolimus?
1. potent immunosuppressive for transplant patient
2. topical for eczema
Similar to cyclosporine, but without the hirsutism and gingival hyperplasia
Sirolimus (rapamycin) MOA
binds FKBP12 intracellular protein + inhibits mTOR
inhibits T-cell proliferation in response to IL-2
what are 2 clinical uses for sirolimus?
1. immunosuppression after renal transplant in combo w/ cyclosporine and corticosteroids
2. Drug-eluting stents
3 potential toxicities associated with sirolimus?
moAb against IL-2 used as an immunosuppressant
Name 4 drugs that affect IL-2 autocrine growth factor signaling and therefore affect T-cell activation
2. Tacrolimus (FK-506)
3. Sirolimus (rapamycin)
precursor of 6-MP that interferes with the metabolism and synthesis of nucleic acids
anti-metabolite that is toxic to proliferating lymphocytes
name 2 clinical uses for azothioprine
1. kidney transplantation
2. autoimmune disorders including glomerulonephritis + hemolytic anemia
name 2 side effects of azothiprine
1. bone marrow suppression (can't grow rapidly dividing cells)
2. allopurinol increases toxic effects since the active metabolite of azothioprine, mercaptopurine, is metabolized by xanthine oxidase (XO is inhibited by allopurinol)
Muromonab-CD3 (OKT3) MOA
moAb that binds to the episilon chain of CD3, which is present on the surface of every T-cell --> blocks cellular interaction with CD3 protein that is responsible for T-cell signal transduction
what is 1 clinical use for muromonab-CD3 (OKT3)?
immunosuppressant after kidney transplant
what are 2 toxic effects of muromonab-CD3 (OKT3)?
1. cytokine release syndrome
2. hypersensitivity reaction
what are 2 clinical uses for thalidomide
1. immunosuppression for transplant, SLE, etc
Give an example of thalidomide toxicity
phocomelia = "flipper limbs" when previously used as a sedative during pregnancy
Mycophenolate mofetil MOA
inhibits inosine monophosphate (IMG) dehydrogenase = no production of guanine nucleoside
prevents rapid production of B and T cells
what are 2 clinical uses of myophenolate mofetil?
1. immunosuppression for transplants
2. lupus nephritis
Aldesleukin MOA and 2 clinical uses?
recombinant IL-2 that induces immune response
renal cell carcinoma + metastatic melanoma
Epoetin alfa MOA and its clinical use?
recombinant erythropoietin (normally made by kidneys)
used for anemias, especially in renal failure
Filagrastim MOA and clinical use
recombinant G-CSF used for bone marrow recovery
Similar to IL-3
"grastim" = stimulates granulocytes
Sargramostim MOA and clinical use
recombinant GM-CSF used for bone marrow recovery
Similar to IL-3
"gramostim" = stimulates granulocytes + macrophages
4 clinical uses of recombinant alpha-INF
1. Hep B and C
2. Kaposi's sarcoma
4. Malignant melanoma
what is a clinical use of recombinant Beta-INF?
what is a clinical use of recombinant gamma-INF?
chronic granulomatous disease = optimizes phagocytes (macrophages and PMNs) that are deficient in NADPH oxidase
what is a clinical use of oprelvekin?
recombinant IL-11 used for thrombocytopenia
what is a clinical use of thrombopoietin?
which therapeutic antibody targets CD3? what is its clinical use?
which therapeutic antibody targets IL-2?
which therapeutic antibody targets digoxin? what is its clinical use?
Digibind = Digoxin Immune Fab
Antidote for digoxin toxicity
Infliximab MOA and 4 clinical uses
anti-TNF-alpha used in some of the HLA-B27 dz's
1. Crohn's disease
3. Ankylosing spondylitis
4. Psoriatic arthritis
adalimumab MOA and and 3 clinical uses
1. Crohn's disease
3. Psoriatic arthritis
what 3 anti-TNF-alpha therapeutic antibodies?
what is the difference in terms of clinical uses between infliximab and adalimumab?
infliximab is used against ankylosing spondylitis, but adalimumab is not
Remember: "Adam already gave up one rib, so he isn't going to do any more work on the axial skeleton"
which therapeutic antibody targets glycoprotein IIb/IIIa? what is the end result? Give 2 clinical uses
Decreases platelet activation/activity
1. Prevent cardiac ischemia in unstable angina
2. Patients treated with percutaneous coronary intervention like stents or balloon angioplasty
which therapeutic antibody targets HER2? what is its clinical use?
Used in HER2-overexpressing breast cancer
which therapeutic antibody targets CD20? What is it's clinical use?
B-cell non-Hodgkin's lymphoma
which therapeutic antibody targets IgE? What is its clinical use?
Additional line of treatment for severe asthma (type I HSN)
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