Immunosuppressant Drugs I Flashcards Preview

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Flashcards in Immunosuppressant Drugs I Deck (23)
1

What is the mechanism of action of cyclosporine?

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)

2

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

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

3

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

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

4

What is the mechanism of action of Azathioprine?

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

5

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

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)

6

What are the clinical uses of Cyclosporine?

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

7

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

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

8

What are the clinical uses of Sirolimus (rapamycin)?

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

9

What are the clinical uses of Azathioprine?

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

10

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

Immunosuppression after kidney transplantation (p.209)

11

What are the toxicities associated with Cyclosporine?

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

12

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

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

13

What are the toxicities associated with Sirolimus (rapamycin)?

Hyperlipidemia, thrombocytopenia, leukopenia (p.209)

14

What are the toxicities associated with Azathioprine?

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

15

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

Cytokine release syndrome, hypersensitivity reaction (p.209)

16

Name nine recombinant cytokine drugs.

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)

17

What recombinant cytokine agent does Aldesleukin resemble?

IL-2 (p.210)

18

What recombinant cytokine agent does Epoetin alfa resemble?

Erythropoeitin (p.210)

19

What recombinant cytokine agent does Filgrastim resemble?

Granulocyte colony stimulating factor (p.210)

20

What recombinant cytokine agent does Sargramostim resemble?

Granulocyte macrophage colony stimulating factor (p.210)

21

What recombinant cytokine agent does Oprelvekin resemble?

IL-11 (p.210)

22

What conditions is Aldesleukin used to treat?

Renal cell carcinoma, metastatic melanoma (p.210)

23

What conditions is Epoetin alfa used to treat?

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