Immunosuppressants 0519

Question 1

CYCLOSPORINE mech

Answer 1

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

Question 2

CYCLOSPORINE use

Answer 2

1. suppress organ rejection after transplant.

2. selected autoimmune d/o.

Question 3

CYCLOSPORINE tox

Answer 3

predispose to viral infx, lymphoma.
gout.
nephrotoxic.

Question 4

how can nephrotoxicity of CYCLOSPORINE be prevented?

Answer 4

mannitol diuresis

Question 5

TACROLIMUS (FK506) mech

Answer 5

similar to cyclosporine.

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

Question 6

TACROLIMUS (FK506) use

Answer 6

potent immunosuppression in organ transplant recipients

Question 7

TACROLIMUS (FK506) tox

Answer 7

SIGNIFICANT!!
nephrotox.
peripheral neuropathy.
HTN.
pleural effusion.
hyperglycemia.

Question 8

SIROLIMUS (RAPAMYCIN) mech

Answer 8

inhibit mTOR.

inhibit T cell prolix in response to IL-2.

Question 9

SIROLIMUS (RAPAMYCIN) use

Answer 9

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

Question 10

SIROLIMUS (RAPAMYCIN) tox

Answer 10

hyperlipidemia.
thrombocytopenia.
leukopenia.

Question 11

daclizumab

Answer 11

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

Question 12

AZATHIOPRINE mech

Answer 12

antimetabolite precursor of 6-mercaptopurine.

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

Question 13

AZATHIOPRINE use

Answer 13

kidney transplant.

autoimmune d/o, including glomerulonephritis and hemolytic anemia.

Question 14

AZATHIOPRINE tox

Answer 14

BM suppression.

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

Question 15

MUROMONAB-CD3 (OKT3) mech

Answer 15

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

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

Question 16

MUROMONAB-CD3 (OKT3) use

Answer 16

immunosupp after kidney transplant

Question 17

MUROMONAB-CD3 (OKT3) tox

Answer 17

cytokine release syndrome.

hypersensitivity rxn.

Question 18

recombinant cytokine: aldesleukin

Answer 18

IL-2 for RCC, metastatic melanoma

Question 19

recombinant cytokine: erythropoietin

Answer 19

epoetin for anemias (esp in renal failure)

Question 20

recombinant cytokine: filgrastim

Answer 20

granulocyte colony-stimulating factor for recovery of BM

Question 21

recombinant cytokine: sargramostim

Answer 21

granulocyte-macrophage colony-stimulating factor for recovery of BM

Question 22

recombinant cytokine: alpha interferon

Answer 22

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

Question 23

recombinant cytokine: beta interferon

Answer 23

for multiple sclerosis

Question 24

recombinant cytokine: gamma interferon

Answer 24

for CGD

Question 25

recombinant cytokine: oprelvekin

Answer 25

IL-11 for thrombocytopenia

Question 26

recombinant cytokine: thrombopoietin

Answer 26

for thrombocytopenia

Question 27

therapeutic Ab: muromonab CD3 (OKT3)

Answer 27

targets CD3 to prevent acute transplant rejection

Question 28

therapeutic Ab: daclizumab

Answer 28

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

Question 29

therapeutic Ab: digoxin immune Fab

Answer 29

targets digoxin as antidote for intox

Question 30

therapeutic Ab: infliximab

Answer 30

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

Question 31

therapeutic Ab: adalimumab

Answer 31

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

Question 32

therapeutic Ab: abciximab

Answer 32

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

Question 33

therapeutic Ab: trastuzumab (Herceptin)

Answer 33

targets erg-B2 for HER2-overexpressing breast cancer

Question 34

therapeutic Ab: rituximab

Answer 34

targets CD20 for B cell non-Hodgkin lymphoma

Question 35

therapeutic Ab: omalizumab

Answer 35

targets IgE for additional line of tx for severe asthma