Immunosuppressants

Question 1

Cyclosporine MOA

Answer 1

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

Question 2

Cyclosporine Clinical Use

Answer 2

Suppresses organ rejection after transplantation, selected autoimmune disorders

Question 3

Cyclosporine Toxicity

Answer 3

Nephrotoxicity
HTN
Hyperlipidemia
Hyperglycemia
Tremor
Gingival hyperplasia
Hirsutism

Question 4

Tacrolimus MOA

Answer 4

Similar to Cyclosporine

Binds to FK-binding protein, inhibiting calcineurin and secretion of IL-2 and other cytokines

Question 5

Tacrolimus Clinical Use

Answer 5

Potent immunosuppressive use in organ transplant recipients

Question 6

Tacrolimus Toxicity

Answer 6

Nephrotoxicity
HTN
Hyperlipidemia
Hyperglycemia
Tremor

Question 7

Sirolimus MOA

Answer 7

Inhibits mTOR

Inhibits T cell proliferation in response to IL2

Question 8

Sirolimus Clinical Use

Answer 8

Immunosupression after kidney transplantation in combo with cyclosporine and corticosteroids
Drug-eluting stents

Question 9

Sirolimus Toxicity

Answer 9

Hyperlipidemia
Thrombocytopenia
Leukopenia

Question 10

Azathioprine MOA

Answer 10

Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids
Toxic to proliferating lymphocytes

Question 11

Azathioprine Clinical Use

Answer 11

Kidney transplantation
Autoimmune disorders (glomerulonephritis and hemolytic anemia)

Question 12

Azathioprine Toxicity

Answer 12

Bone marrow suppression

Active metabolite mercaptopurine is metabolized by xanthine oxidase so toxic effects can be increased by allopurinol

Question 13

Muromonab-CD3 (OKT3) MOA

Answer 13

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

Question 14

Muromonab-CD3 (OKT3) Clinical Use

Answer 14

Immunosuppression after kidney transplantation

Question 15

Muromonab-CD3 (OKT3) Toxicity

Answer 15

Cytokine release syndrome

Hypersensitivity reaction

Question 16

Aldesleukin

Answer 16

IL-2 (anti-tumor)

Renal Cell Carcinoma
Metastatic Melanoma

Question 17

Epoetin Alfa

Answer 17

Erythropoietin

Anemias (esp in renal failure)

Question 18

Filgrastim

Answer 18

Granulocyte colony-stimulating factor

Recovery of bone marrow

*-GRA (granulocyte), -STIM (stimulating)

Question 19

Sargramostim

Answer 19

Granulocyte-macrophage colony stimulating factor

Recovery of bone marrow

*-GRA (granulocyte), -MO (macrophage), -STIM (stimulating)

Question 20

alpha-interferon

Answer 20

Hepatitis B and C
Kaposi’s sarcoma
Leukemias
Malignant melanoma

Question 21

beta-interferon

Answer 21

Multiple sclerosis

Question 22

gamma-interferon

Answer 22

Chronic granulomatous disease

Question 23

Oprelvekin

Answer 23

IL-11

Thrombocytopenia

Question 24

Thrombopoietin

Answer 24

Thrombocytopenia

Question 25

Muromonab-CD3 (OKT3)

Answer 25

Targets CD3

Prevent acute transplant rejection

Question 26

Digoxin Immune Fab

Answer 26

Targets Digoxin

Antidote for digoxin intoxication

Question 27

Infliximab

Answer 27

Targets TNF-alpha

Crohn’s dz, RA, psoriatic arthritis, ankylosing spondylitis

Question 28

Adalimumab

Answer 28

Targets TNF-alpha

Crohn’s dz, RA, psoriatic arthritis

Question 29

Abciximab

Answer 29

Targets glycoprotein IIb/IIIa

Prevents cardiac ischemia in unstable angina and in patients treated with percutaneous coronary intervention

Question 30

Trastuzumab (Herceptin)

Answer 30

Targets HER2

HER2 overexpressing breast cancer

Question 31

Rituximab

Answer 31

Targets CD20

B-cell non-Hodgkin’s lymphoma

Question 32

Omalizumab

Answer 32

Targets IgE

Additional line of treatment for severe asthma