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Immunosuppressants Flashcards

1
Q

Cyclosporine mech

A

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

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2
Q

Cyclosporine use:

A

Transplant rejection, prophylaxis, psoriasis, rheumatoid arthritis

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3
Q

Cyclosporine Toxicity:

A

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

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4
Q

Tacrolimus mech:

A

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

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5
Q

Tacrolimus use:

A

Transplant rejection prophylaxis

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6
Q

Tacrolimus Toxicity:

A

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

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7
Q

Siroliums (Rapamycin) mech:

A

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

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8
Q

Sirolimus (Rapamycin) use:

A

Kidney transplant rejection prophylaxis

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9
Q

Sirolimus (Rapamycin) toxicity:

A

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

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10
Q

Sirolimus notes:

A

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

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11
Q

Basiliximab mech:

A

monoclonal antibody; blocks IL-2R

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12
Q

Basiliximab use:

A

kidney transplant rejection prophylaxis.

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13
Q

Basiliximab toxicity:

A

Edema, HTN, tremor

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14
Q

Azathiprine mech

A

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

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15
Q

Azathioprine clinical use:

A

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

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16
Q

Azathioprine toxicity:

A

Leukopenia, anemia, thrombocytopenia

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17
Q

Azathioprine additional notes:

A

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

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18
Q

Glucocorticoids mech

A

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

19
Q

Glucocorticoids use:

A

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

20
Q

Glucocorticoids toxicity:

A

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

21
Q

Epoetin alfa (erythropoietin) use:

A

Anemias (especially renal failure

22
Q

Thrombopoietin:

A

Thrombocytopenia

23
Q

Oprelvekin (IL-11) use:

A

Thrombocytopenia

24
Q

Filgrastim (granulocyte colony stimulating factor) use:

A

Recovery of bone marrow

25
Q

Sargramostim (granulocyte-macrophage colony stimulating factor) use:

A

Recovery of bone marrow

26
Q

Aldesleukin use:

A

IL-2; RCC, metastatic melanoma

27
Q

IFN alpha:

A

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

28
Q

IFN beta:

29
Q

IFN gamma

A

Chronic granulomatous disease

30
Q

Therapeutic antibodies Are next

31
Q

Alemtuzumab

A

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

32
Q

Bevacizumab

A

TARGET: VEGF. Use: Colorectal cancer, RCC

33
Q

Cetuximab

A

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

34
Q

Rituximab

A

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

35
Q

Trastuzumab

A

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

36
Q

Autoimmune disease therapy:

A

infliximab, adalimuab, nataliziumab

37
Q

INFLIXimab and aDALIMumab

A

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

38
Q

Natalizumab

A

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

39
Q

Abciximab

A

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
Q

Denosumab

A

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

41
Q

Digoxin immune Fab

A

Target: digoxin. Use: Antidote for digoxin toxicity

42
Q

Omalizumab

A

Use: Allergic asthma; prevents IgE binding to FcERI

43
Q

Palivizumab

A

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

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