Immunosuppresants

Question 1

Cyclosporine

Answer 1

MOA: binds cyclophilins and inhibits calcineurin production (a second messanger that signals IL-2 production in T cells)

Use: Suppresses organ rejection after transplant and certain autoimmune disorders

Toxicity: susceptibility to viral infection and lymphoma, nephrotoxicity, gout

Question 2

Tacrolimus

Answer 2

MOA: binds to FK-binding protein (a necessary protein needed for vesicles containing IL-2 to bind and be exocytosed from T cell membranes)

Use: immunosuppressive in organ transplants

Toxicity: nephrotoxicity, peripheral neuropathy, HTN, pleural effusion, hyperglycemia

Question 3

Sirolimus (Rapamycin)

Answer 3

MOA: inhibits mTOR (mammalian Target of Rapamycin) a protein that is activated when IL-2 binds the IL-2 receptor on T cells. Overall prevents T cell proliferation.

Use: Immunosuppression after kidney transplant (combination w/ cyclosporine and corticosteroids), also in drug-eluting stents

Toxicity: Hyperlipidemia, thrombocytopenia, leukopenia

Question 4

Daclizumab

Answer 4

MOA: monoclonal Ab that is an antagonist to CD25 of the IL-2 receptor on T cells (binding keeps the receptor inactive)

Use: Immunosuppression in kidney transplant, multiple sclerosis

Question 5

Azathioprine

Answer 5

MOA: antimetabolite precursor for 6-mercaptopurine that interferes w/ metabolism of nucleic acids in lymphocytes.

Use: kidney transplant, autoimmune disorders (glomerulonephritis, hemolytic anemia)

Toxicity: bone marrow suppression, contraindicated in patients taking allopurinol for gout

Question 6

Murmonab-CD3

Answer 6

MOA: monoclonal Ab that binds CD3 on T cells preventing signal transduction in T cells

Use: kidney transplant

Toxicity: cytokine release syndrome (binding of the medicine accidently causes massive cytokine release throughout T cells in the body causing systemic inflammation)

Question 7

Aldesleukin

Answer 7

MOA: binds and activates IL-2 receptors on T cells

Use: renal cell carcinoma, melanoma

Question 8

EPO

Answer 8

MOA: Erythropoietin analog that stimulates bone marrow

Use: anemias (especially in renal failure)

Question 9

Filgrastim

Answer 9

MOA: granulocyte-colony stimulating factor

Use: recovery of bone marrow

Question 10

Sargramostim

Answer 10

MOA: granulocyte-macrophage-colony stimulating factor

Use: recovery of bone marrow

Question 11

INF-alpha

Answer 11

MOA: signal ribonuclease production that inhibits viral protein synthesis and degrades viral mRNA

Use: Hep B and C, Kaposi sarcoma, leukemia, melanoma

Question 12

INF-beta

Answer 12

MOA: moderates ability of inflammatory cells to cross the BBB keeping inflammation of nerves to a minimum

Use: multiple sclerosis

(also has similar effects on viruses like INF-alpha but not as effective for some reason)

Question 13

INF-gamma

Answer 13

MOA: activates macrophages

Use: chronic granulomatous disease

Question 14

Oprelvekin

Answer 14

MOA: IL-11 analog which directly stimulates proliferation of hematopoietic and megakaryocytic stem cells

Use: thrombocytopenia

Question 15

Thrombopoietin

Answer 15

Use: thrombocytopenia

Question 16

Infliximab

Answer 16

MOA: monoclonal Ab against TNF-alpha that suppresses WBC recruitment, reduces vascular permeability and inflammation, decreases risk of shock (basically stops everything TNF-alpha tried to do)

Use: crohn disease, RA, psoriatic arthritis, ankylosing spondylitis

Question 17

Adalimumab

Answer 17

MOA: monoclonal Ab against TNF-alpha that suppresses WBC recruitment, reduces vascular permeability and inflammation, decreases risk of shock (basically stops everything TNF-alpha tried to do)

Use: crohn disease, RA, psoriatic arthritis, ankylosing spondylitis

Question 18

Abciximab

Answer 18

MOA: Blocks GPIIb/IIIa to prevent clot formation

Use: prevent cardiac ischemia in unstable angina and patients treated with percutaneous coronary intervention

Question 19

Trastuzumab

Answer 19

MOA: erb-B2 receptor blocker that prevents expression of the HER-2 gene

Use: breast cancer with overexpressing HER-2 genes

Question 20

Rituximab

Answer 20

MOA: binds and inhibits CD20 activation on B cells

Use: B cell non-Hodgkins lymphoma

Question 21

Omalizumab

Answer 21

MOA: binds and inhibits IgE preventing it from binding mast cells

Use: severe asthma