Immunosuppressant Drugs I

Question 1

What is the mechanism of action of cyclosporine?

Answer 1

Binds to cyclophilins. Complex blocks the differentiation and activation of T cells by inhibiting calcineurin. This prevents production of IL-2 and its receptor (p.209)

Question 2

What is the mechanism of action of Tacrolimus (FK-506)?

Answer 2

Similar to cyclosporine; binds to FK binding protein inhibiting calcineurin and secretion of IL-2 and other cytokines (p.209)

Question 3

What is the mechanism of action of Sirolimus (rapamycin)?

Answer 3

Inhibits mTOR and T cell proliferation in response to IL-2 (p.209)

Question 4

What is the mechanism of action of Azathioprine?

Answer 4

Antimetabolite precursor of 6-mercaptopurine that interferes with the metabolism and synthesis of nucleic acids. It is toxic to proliferating lymphocytes (p.209)

Question 5

What is the mechanism of action of Muromonab- CD3 (OKT3)?

Answer 5

Monoclonal antibody that binds CD3 (epsilon chain) on the surface of T cells. Blocks cellular interaction with CD3 proteins responsible for T cell signal transduction (p.209)

Question 6

What are the clinical uses of Cyclosporine?

Answer 6

Suppression of organ rejection after transplantation; selected autoimmune disorders (p.209)

Question 7

What are the clinical uses of Tacrolimus (FK-506)?

Answer 7

Potent immunosuppressive used in organ transplant recipients (p.209)

Question 8

What are the clinical uses of Sirolimus (rapamycin)?

Answer 8

Immunosuppression after kidney transplant in combination with cyclosporine and corticosteroids. Also used with drug eluting stents (p.209)

Question 9

What are the clinical uses of Azathioprine?

Answer 9

Kidney transplantation, autoimmune disorders (including glomeurlonephritis and hemolytic anemia) (p.209)

Question 10

What are the clinical uses of Muromonab-CD3 (OKT3)?

Answer 10

Immunosuppression after kidney transplantation (p.209)

Question 11

What are the toxicities associated with Cyclosporine?

Answer 11

Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism (p.209)

Question 12

What are the toxicities associated with Tacrolimus (FK-506)?

Answer 12

Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor (p.209)

Question 13

What are the toxicities associated with Sirolimus (rapamycin)?

Answer 13

Hyperlipidemia, thrombocytopenia, leukopenia (p.209)

Question 14

What are the toxicities associated with Azathioprine?

Answer 14

Bone marrow suppression. Active metabolite mercaptopurine is metabolized by xanthine oxidase thus toxic effects may be increased by allopurinol (p.209)

Question 15

What are the toxicities associated with Muromonab- CD3 (OKT3)?

Answer 15

Cytokine release syndrome, hypersensitivity reaction (p.209)

Question 16

Name nine recombinant cytokine drugs.

Answer 16

1.) Aldesleukin (IL-2); 2.) Epoetin alfa (erythropoeitin); 3.) Filgrastim (GCSF); 4.) Sargramostim (granulocyte macrophage colony stimulating factor); 5.) a interferon; 6.) b interferon; 7.) y interferon; 8.) Oprelvekin (IL-11); 9.) Thrombopoietin (p.210)

Question 17

What recombinant cytokine agent does Aldesleukin resemble?

Answer 17

IL-2 (p.210)

Question 18

What recombinant cytokine agent does Epoetin alfa resemble?

Answer 18

Erythropoeitin (p.210)

Question 19

What recombinant cytokine agent does Filgrastim resemble?

Answer 19

Granulocyte colony stimulating factor (p.210)

Question 20

What recombinant cytokine agent does Sargramostim resemble?

Answer 20

Granulocyte macrophage colony stimulating factor (p.210)

Question 21

What recombinant cytokine agent does Oprelvekin resemble?

Answer 21

IL-11 (p.210)

Question 22

What conditions is Aldesleukin used to treat?

Answer 22

Renal cell carcinoma, metastatic melanoma (p.210)

Question 23

What conditions is Epoetin alfa used to treat?

Answer 23

Anemias (especially in renal failure) (p.210)