Immunosuppressant Drugs EC

Question 1

Cyclosporine (MOA, Use, Tox)

Answer 1

Binds to CYCLOPHILINS,complex blocks differentiation and activation of T-cells by inhibiting CALCINEURIN, thus INHIBITING THE PRODUCTION OF IL-2 & IL-2 RECEPTOR

Used to suppress organ rejection after transplantation
Used in some autoimmune disorders

Nephrotoxicity, Hypertension, Hyperlipidemia, Hyperglycemia, Tremor, Gingival hyperplasia, Hirsutism

Question 2

Tacrolimus (FK-506) (MOA, Use, Tox)

Answer 2

Binds FK-BINDING PROTEIN, inhibiting CALCINEURIN and secretion of IL-2

Used in organ transplant

Nephrotoxicity, Hypertension, Hyperlipidemia, Hyperglycemia, Tremor

Question 3

Sirolimus (MOA, Use, Tox)

Answer 3

Inhibits mTOR - inhibits T-cell proliferation in response to IL-2

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

Causes Hyperlipidemia, Thrombocytopenia, Leukopenia

Question 4

Azathioprine (MOA, Use, Tox)

Answer 4

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

Used in kidney transplantation, autoimmune disorders (glomerulonephritis and hemolytic anemia)

Bone marrow suppression
Toxic effects increased by allopurinol (metabolized by xanthine oxidase -which allopurinol inhibits)

Question 5

Muromonab (MOA, Use, Tox)

Answer 5

Monoclonal antibody against CD3 on T-cells
Blocks cellular interaction responsible for T-cell transduction

Immunosuppression after kidney transplantation

Cytokine release syndrome, Hypersensitivity reaction

Question 6

Aldesleukin (MOA, Use)

Answer 6

Recombinant cytokine

Used in renal cell carcinoma and metastatic melanoma

Question 7

Epoetin alfa (MOA, Use)

Answer 7

Recombinant cytokine

Used in anemias

Question 8

Filgrastim (MOA, Use)

Answer 8

Recombinant cytokine - Granulocyte colony stimulating factor

Recovery of bone marrow

Question 9

Sargramostim (MOA, Use)

Answer 9

Recombinant cytokine - Granulocyte-Macrophage colony stimulating factor

Recovery of bone marrow

Question 10

Alpha-Interferon (MOA, Use)

Answer 10

Recombinant cytokine

Hep. B&C, Kaposi’s sarcoma, Leukemias, Malignant melanoma

Question 11

Beta-Interferon (MOA, Use)

Answer 11

Recombinant cytokine

Multiple sclerosis

Question 12

Gamma-Interferon (MOA, Use)

Answer 12

Recombinant cytokine

Chronic granulomatous disease

Question 13

Oprelvekin (MOA, Use)

Answer 13

Recombinant cytokine (IL-11)

Thrombocytopenia

Question 14

Thrombopoietin (MOA, Use)

Answer 14

Recombinant cytokine

Thrombocytopenia

Question 15

Digoxin Immune Fab (MOA, Use)

Answer 15

Therapeutic antibody against Digoxin

Antidote for digoxin intoxication

Question 16

Infliximab, Adalimumab (MOA, Use)

Answer 16

Therapeutic antibody against TNF-alpha

Crohn’s disease, RA, Psoriatic arthritis, (Ankylosing spondylitis - Infliximab only)

Question 17

Abciximab (MOA, Use)

Answer 17

Therapeutic antibody against Glycoprotein IIb/IIIa

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

Question 18

Trastuzumab (MOA, Use)

Answer 18

Therapeutic antibody against HER2

HER2-overexpressing breast cancer

Question 19

Rituximab (MOA, Use)

Answer 19

Therapeutic antibody against CD20

B-Cell non-Hodgkin’s lymphoma