Immunosuppressants

Question 1

Mech: Binds to cycophilins –> complex blocks differentiation and activation of T cells by inhibiting calcineurin, thus preventing the production of IL-2 and its’ receptor

Answer 1

Cyclosporine

Question 2

Mech: Binds to FK-binding protein, inhibits calcineurin and secretion of IL-2 and other cytokines

Answer 2

Tacrolimus (FK-506)

Question 3

Mech: Inhibits mTOR which will inhibit T-cell proliferation in response to IL-2.

Answer 3

Sirolimus (rapamycin)

Question 4

Mech: Antimetabolite precursor 6-mercaptopurine interferes with metabolism and synthesis of nucleic acids. Is toxic to proliferating lymphocytes.

Answer 4

Azathioprine

Question 5

Mech: Monoclonal antibody that binds CD3 (epsilon chain) on the surface of T cells to block cellular interaction with CD3 protein responsible for T-cell signal transduction

Answer 5

Muromonab-CD3 (OKT3)

Question 6

Suppresses organ rejection after transplantation and used for selected autoimmune disorders

Answer 6

Cyclosporine

Question 7

Potent immunosuppressive used in organ transplant recipients

Answer 7

Tacrolimus (FK-506)

Question 8

Immunosuppression after kidney transplantation in combination with cyclosporine and corticosteroids. Also used in drug-eluting stents.

Answer 8

Sirolimus (rapamycin)

Question 9

Kidney transplantation, AI disorders (including glomerulonephritis and hemolytic anemia)

Answer 9

Azathioprine

Question 10

Immunosuppression after kidney transplantation

Answer 10

Muromonab-CD3 (OKT3)

Question 11

Adverse Rxns Include Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism

Answer 11

Cyclosporine

Question 12

Adverse Rxns Include Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, and tremor but no gingival hyperplasia or hirsutism

Answer 12

Tacrolimus (FK-506)

Question 13

Adverse Rxns Include Hyperlipidemia, thrombocytopenia, and leukopenia

Answer 13

Sirolimus (rapamycin)

Question 14

Adverse Rxns Include Bone Marrow Suppression. Active metabolite mercaptopurine is metabolized by xanthine oxidase so toxicity may be increased by allopurinol.

Answer 14

Azathioprine

Question 15

Adverse Rxns Include Cytokine release syndrome, HSR

Answer 15

Muromonab-CD3 (OKT3)

Question 16

Used for Renal Cell Carcinoma and Metastatic Melanoma

Answer 16

Aldesleukin (IL-2)

Question 17

Used for Anemias (especially in renal failure)

Answer 17

Epoetin alfa (erythropoietin)

Question 18

Used for Recovery of Bone Marrow

Answer 18

Filgrastim (G-CSF) and Sargramostim (GM-CSF)

Question 19

Used for Hep B/C, Kaposi’s Sarcoma, Leukemias, and Malignant Melanoma

Answer 19

Alpha Interferon

Question 20

Used for Multiple Sclerosis

Answer 20

Beta Interferon

Question 21

Used for Chronic Granulomatous Disease

Answer 21

Gamma Interferon

Question 22

Used for Thrombocytopenia

Answer 22

Oprelvekin (IL-11) and Thrombopoietin

Question 23

Prevents acute transplant rejection and targets CD3

Answer 23

Muromonab-CD3 (OKT3)

Question 24

Antidote for Digoxin INtoxication and targets Digoxin

Answer 24

Digoxin Immune Fab

Question 25

Used for Crohn’s Disease, RA, Psoriatic Arthritis and targets TNF-alpha

Answer 25

Infliximab and Adalimumab

Question 26

Prevents cardiac ischemia in unstable angina and in pts treated with percutaneous coronary intervention; targets Glycoprotein IIb/IIIa

Answer 26

Abciximab

Question 27

Used for HER2-overexpressing breast cancer; targets HER2

Answer 27

Trastuzumab (Herceptin)

Question 28

Used for B-cell non-Hodgkin’s Lymphoma; targets CD20

Answer 28

Rituximab

Question 29

Additional Line of treatment for severe asthma; targets IgE

Answer 29

Omalizumab