Immunosuppressants Flashcards Preview

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Flashcards in Immunosuppressants Deck (43):
1

Cyclosporine mech

Calcineurin inhibitor; binds cyclophilin. Blocks T cell activation by preventing IL-2 TRANSCRIPTION.

2

Cyclosporine use:

Transplant rejection, prophylaxis, psoriasis, rheumatoid arthritis

3

Cyclosporine Toxicity:

NEPHROTOXICITY, HTN, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia

4

Tacrolimus mech:

Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T cell activation by preventing IL-2 transcription.

5

Tacrolimus use:

Transplant rejection prophylaxis

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Tacrolimus Toxicity:

Similar to cyclosporine, increased risk of diabetes and neurotoxicity; no ginigival hyperplasia or hirsutism.

7

Siroliums (Rapamycin) mech:

mTOR inhibitor; binds FKBP. Blocks T cell activation and B cell differentiation by preventing IL-2 signal transduction.

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Sirolimus (Rapamycin) use:

Kidney transplant rejection prophylaxis

9

Sirolimus (Rapamycin) toxicity:

Anemia, thrombocytopenia, leukopenia, insulin resistance, hyperlipidemia; NON-NEPHROTOXIC.

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Sirolimus notes:

Kidney 'sir-vives'. synergistic with cyclosporine. Also used in drug-eluting stents.

11

Basiliximab mech:

monoclonal antibody; blocks IL-2R

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Basiliximab use:

kidney transplant rejection prophylaxis.

13

Basiliximab toxicity:

Edema, HTN, tremor

14

Azathiprine mech

Antimetabolite precursor of 6-MP. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

15

Azathioprine clinical use:

Transplant rejection prophylaxis, rhematoid arthritis, Crohn disease, glomerolonephritis, other autoimmune conditions

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Azathioprine toxicity:

Leukopenia, anemia, thrombocytopenia

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Azathioprine additional notes:

6-MP degraded by xanthine oxidase; toxicity increased by allopurinol. pronounced 'azathioPURINE'

18

Glucocorticoids mech

inhibit NF-kB. Suppress both B and T cell function by decreasing transcription of many cytokines.

19

Glucocorticoids use:

Transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation

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Glucocorticoids toxicity:

Hyperglycemia, osteoporosis, central obestity, muscle breakdown, psychosis, acne, HTN, cataracts, peptic ulcers

21

Epoetin alfa (erythropoietin) use:

Anemias (especially renal failure

22

Thrombopoietin:

Thrombocytopenia

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Oprelvekin (IL-11) use:

Thrombocytopenia

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Filgrastim (granulocyte colony stimulating factor) use:

Recovery of bone marrow

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Sargramostim (granulocyte-macrophage colony stimulating factor) use:

Recovery of bone marrow

26

Aldesleukin use:

IL-2; RCC, metastatic melanoma

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IFN alpha:

Chronic Hep B and C, Kaposi Sarcoma, Kaposi Sarcoma, Hairy Cell Leukemia, Condyloma Acuminatum, RCC, malignant melanoma

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IFN beta:

MS

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IFN gamma

Chronic granulomatous disease

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Therapeutic antibodies Are next

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Alemtuzumab

TARGET: CD52, Use: CLL, Notes: 'ALYMtuzumab' - chronic LYMphocytic leukemia

32

Bevacizumab

TARGET: VEGF. Use: Colorectal cancer, RCC

33

Cetuximab

Target: EGFR. USE: Stage IV colorectal cancer, head and neck cancer

34

Rituximab

Target CD20. USE: B-cell non-hodgkin lymphoma, rheumatoid arthritis (with MTX), ITP

35

Trastuzumab

Target: HER2/neu. USE: Breast cancer, gastric cancer. Notes: Tras2zumab

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Autoimmune disease therapy:

infliximab, adalimuab, nataliziumab

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INFLIXimab and aDALIMumab

Target: TNF-alpha. USE: IBD, rheumatoid arthritis, ankylosing spondylitis, psoriasis

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Natalizumab

Target: alpha4-integrin (leukocyte adhesion). Use: MS, Crohn disease. RISK OF PML IN PATIENTS WITH JC VIRUS

39

Abciximab

Target: Glycoprotein IIb/IIIa. Clinical Use: anti-platelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention. NOTE: IIb times IIIa = abSIXimab

40

Denosumab

Target: RANKL. osteoporosis; inhibits osteoclast maturation (mimics OPG)

41

Digoxin immune Fab

Target: digoxin. Use: Antidote for digoxin toxicity

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Omalizumab

Use: Allergic asthma; prevents IgE binding to FcERI

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Palivizumab

Target: RSV F protein. USE: RSV prophylaxis for high risk infants. paliVIzumab for VIrus