Immunosuppressants 0519 Flashcards

1
Q

CYCLOSPORINE mech

A

bind to cyclophilins-
complex blocks differentiation and activation of T cells by inhibiting CALCINEURIN, thus preventing production of IL-2 and its receptor

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2
Q

CYCLOSPORINE use

A
  1. suppress organ rejection after transplant.

2. selected autoimmune d/o.

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3
Q

CYCLOSPORINE tox

A

predispose to viral infx, lymphoma.
gout.
nephrotoxic.

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4
Q

how can nephrotoxicity of CYCLOSPORINE be prevented?

A

mannitol diuresis

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5
Q

TACROLIMUS (FK506) mech

A

similar to cyclosporine.

binds to FK-binding protein to inhibit secretion of IL-2 and other cytokines.

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6
Q

TACROLIMUS (FK506) use

A

potent immunosuppression in organ transplant recipients

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7
Q

TACROLIMUS (FK506) tox

A
SIGNIFICANT!!
nephrotox.
peripheral neuropathy.
HTN.
pleural effusion.
hyperglycemia.
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8
Q

SIROLIMUS (RAPAMYCIN) mech

A

inhibit mTOR.

inhibit T cell prolix in response to IL-2.

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9
Q

SIROLIMUS (RAPAMYCIN) use

A

immunosupp after kidney transplant IN COMBO WITH cyclosporine and corticosteroids. also used with drug-eluting stents.

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10
Q

SIROLIMUS (RAPAMYCIN) tox

A

hyperlipidemia.
thrombocytopenia.
leukopenia.

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11
Q

daclizumab

A

monoclonal Ab with high affinity for IL-2 receptor on activated T cells

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12
Q

AZATHIOPRINE mech

A

antimetabolite precursor of 6-mercaptopurine.

interferes w/metabolism and synth of nucleic acids. toxic to proliferating lymphocytes.

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13
Q

AZATHIOPRINE use

A

kidney transplant.

autoimmune d/o, including glomerulonephritis and hemolytic anemia.

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14
Q

AZATHIOPRINE tox

A

BM suppression.

*may be increased by allopurinol bc mercaptopurine is metabolized by xanthine oxidase

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15
Q

MUROMONAB-CD3 (OKT3) mech

A

monoclonal Ab that binds CD3 epsilon chain on surface of T cells.

blocks cellular interaction with CD3 protein responsible for T cell signal transduction.

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16
Q

MUROMONAB-CD3 (OKT3) use

A

immunosupp after kidney transplant

17
Q

MUROMONAB-CD3 (OKT3) tox

A

cytokine release syndrome.

hypersensitivity rxn.

18
Q

recombinant cytokine: aldesleukin

A

IL-2 for RCC, metastatic melanoma

19
Q

recombinant cytokine: erythropoietin

A

epoetin for anemias (esp in renal failure)

20
Q

recombinant cytokine: filgrastim

A

granulocyte colony-stimulating factor for recovery of BM

21
Q

recombinant cytokine: sargramostim

A

granulocyte-macrophage colony-stimulating factor for recovery of BM

22
Q

recombinant cytokine: alpha interferon

A

for hep B and C.
Kaposi sarcoma.
leukemias.
malignant melanoma.

23
Q

recombinant cytokine: beta interferon

A

for multiple sclerosis

24
Q

recombinant cytokine: gamma interferon

A

for CGD

25
Q

recombinant cytokine: oprelvekin

A

IL-11 for thrombocytopenia

26
Q

recombinant cytokine: thrombopoietin

A

for thrombocytopenia

27
Q

therapeutic Ab: muromonab CD3 (OKT3)

A

targets CD3 to prevent acute transplant rejection

28
Q

therapeutic Ab: daclizumab

A

targets IL-2 receptor to prevent acute rejection of renal transplant

29
Q

therapeutic Ab: digoxin immune Fab

A

targets digoxin as antidote for intox

30
Q

therapeutic Ab: infliximab

A

targets TNF-a for Crohn’s disease, RA, psoriatic arthritis, ankylosing spondylitis

31
Q

therapeutic Ab: adalimumab

A

targets TNF-a for Crohn’s disease, RA, psoriatic arthritis

32
Q

therapeutic Ab: abciximab

A

targets GpIIb/IIIa to prevent cardiac ischemia in unstable angina and in pts treated with percutaneous coronary intervention

33
Q

therapeutic Ab: trastuzumab (Herceptin)

A

targets erg-B2 for HER2-overexpressing breast cancer

34
Q

therapeutic Ab: rituximab

A

targets CD20 for B cell non-Hodgkin lymphoma

35
Q

therapeutic Ab: omalizumab

A

targets IgE for additional line of tx for severe asthma