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deck_3459905 Flashcards

1
Q

Immunosuppressant actions

A

Agents that block lymphocyte activation and proliferation.Reduce acute transplant rejection by suppressing cellular immunity.Frequently combined to achieve greater efficacy with

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2
Q

Immunosuppressants

A
  • Cyclosporine
  • Tacrolimus (FK506)
  • Sirolimus (Rapamycin)
  • Daclizumab, basiliximab
  • Azathioprine
  • Glucocorticoids
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3
Q

Cyclosporine mechanism

A

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

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4
Q

Cyclosporine use

A
  • Transplant rejection
  • prophylaxis
  • psoriasis
  • rheumatoid arthritis
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5
Q

Cyclosporine toxicity

A

Nephrotoxicity

  • hypertension
  • hyperlipidemia
  • neurotoxicity
  • gingival hyperplasia
  • hirsutism.
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6
Q

Calcineurin inhibitors

A
  • Cyclosporine

* Tacrolimus (FK506)Both calcineurin inhibitors are highly nephrotoxic.

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7
Q

Tacrolimus (FK506) Mechanism

A

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

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8
Q

Tacrolimus use

A

Transplant rejection prophylaxis.

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9
Q

Tacrolimus toxicity

A
  • Nephrotoxicity
  • hypertension
  • hyperlipidemia
  • neurotoxicity
  • ↑ risk of diabetes
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10
Q

Sirolimus (Rapamycin) mechanism

A

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

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11
Q

Sirolimus (Rapamycin) use

A

Kidney transplant rejection prophylaxis.

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12
Q

Sirolimus (Rapamycin) toxicity

A
  • Anemia
  • thrombocytopenia
  • leukopenia
  • insulin resistance
  • hyperlipidemia
  • not nephrotoxic.
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13
Q

Sirolimus random facts

A

Synergistic withcyclosporine. Also used in drug-eluting stents.

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14
Q

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

A

Cyclosporine mechanism

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15
Q
  • Transplant rejection
  • prophylaxis
  • psoriasis
  • rheumatoid arthritis
A

Cyclosporine use

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16
Q

Nephrotoxicity

  • hypertension
  • hyperlipidemia
  • neurotoxicity
  • gingival hyperplasia
  • hirsutism.
A

Cyclosporine toxicity

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17
Q
  • Cyclosporine

* Tacrolimus (FK506)Both calcineurin inhibitors are highly nephrotoxic.

A

Calcineurin inhibitors

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18
Q

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

A

Tacrolimus (FK506) Mechanism

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19
Q

Transplant rejection prophylaxis.

A

Tacrolimus use

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20
Q
  • Nephrotoxicity
  • hypertension
  • hyperlipidemia
  • neurotoxicity
  • ↑ risk of diabetes
A

Tacrolimus toxicity

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21
Q

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

A

Sirolimus (Rapamycin) mechanism

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22
Q

Kidney transplant rejection prophylaxis.

A

Sirolimus (Rapamycin) use

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23
Q
  • Anemia
  • thrombocytopenia
  • leukopenia
  • insulin resistance
  • hyperlipidemia
  • not nephrotoxic.
A

Sirolimus (Rapamycin) toxicity

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24
Q

Synergistic withcyclosporine. Also used in drug-eluting stents.

A

Sirolimus random facts

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25
Q

Daclizumab, basiliximab mechanism

A

Monoclonal antibodies; block IL-2R.

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26
Q

Daclizumab, basiliximab uses

A

Kidney transplant rejection prophylaxis.

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27
Q

Daclizumab, basiliximab toxicities

A
  • Edema
  • Hypertension
  • Tremor
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28
Q

Azathioprine mechanism

A

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

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29
Q

Axathioprine uses

A
  • Transplant rejection prophylaxis
  • rheumatoid arthritis
  • Crohn disease
  • glomerulonephritis
  • other autoimmune conditions
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30
Q

Azathioprine toxicity

A

Leukopenia anemia thrombocytopenia

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31
Q

Azathioprine facts

A

6-MP degraded by xanthine oxidase; toxicity ↑by allopurinol.Pronounce “azathio- purine.”

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32
Q

Glucocorticoid mechanism

A

Inhibit NF-κB. Suppress both B- andT-cell function by

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33
Q

Glucocorticoid uses

A

Transplant rejection prophylaxis (immuno-suppression), many autoimmune disorders, inflammation.

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34
Q

Glucocorticoid toxicity

A
  • Hyperglycemia
  • osteoporosis
  • central obesity
  • muscle breakdown
  • psychosis
  • acne
  • hypertension
  • cataracts
  • avascular necrosis
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35
Q

Glucocorticoid facts

A

Can cause iatrogenic Cushing syndrome.

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36
Q

Monoclonal antibodies; block IL-2R.

A

Daclizumab, basiliximab mechanism

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37
Q

Kidney transplant rejection prophylaxis.

A

Daclizumab, basiliximab uses

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38
Q
  • Edema
  • Hypertension
  • Tremor
A

Daclizumab, basiliximab toxicities

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39
Q

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

A

Azathioprine mechanism

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40
Q
  • Transplant rejection prophylaxis
  • rheumatoid arthritis
  • Crohn disease
  • glomerulonephritis
  • other autoimmune conditions
A

Axathioprine uses

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41
Q

Leukopenia anemia thrombocytopenia

A

Azathioprine toxicity

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42
Q

6-MP degraded by xanthine oxidase; toxicity ↑by allopurinol.Pronounce “azathio- purine.”

A

Azathioprine facts

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43
Q

Inhibit NF-κB. Suppress both B- andT-cell function by

A

Glucocorticoid mechanism

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44
Q

Transplant rejection prophylaxis (immuno-suppression), many autoimmune disorders, inflammation.

A

Glucocorticoid uses

45
Q
  • Hyperglycemia
  • osteoporosis
  • central obesity
  • muscle breakdown
  • psychosis
  • acne
  • hypertension
  • cataracts
  • avascular necrosis
A

Glucocorticoid toxicity

46
Q

Can cause iatrogenic Cushing syndrome.

A

Glucocorticoid facts

47
Q

Draw a diagram and show where the immunosuppressants work

A
48
Q

What isAldesleukin (IL-2) used for?

A

Renal cell carcinoma, metastatic melanoma

49
Q

What recombinant cytokine can you use for renal cell carcinoma, metastatic melanoma?

A

Aldesleukin (IL-2)

50
Q

What isEpoetin alfa (erythropoietin) used for?

A

Anemias (especially in renal failure)

51
Q

What recombinant cytokine can you use for anemias (especially in renal failure)?

A

Epoetin alfa (erythropoietin)

52
Q

What isFilgrastim (G-CSF) used for?

A

Recovery of bone marrow

53
Q

What isSargramostim (GM-CSF) used for?

A

Recovery of bone marrow

54
Q

What recombinant cytokine can you use for recovery of bone marrow?

A
  • Filgrastim (G-CSF)

* Sargramostim (GM-CSF)

55
Q

What isIFN-α used for?

A
  • Chronic hepatitis B and C
  • Kaposi sarcoma
  • malignant melanoma
56
Q

What recombinant cytokine can you use for chronic hepatitis B and C, Kaposi sarcoma, and malignant melanoma?

A

IFN-α

57
Q

What isIFN-β used for?

A

Multiple sclerosis

58
Q

What recombinant cytokine can you use for multiple sclerosis?

A

IFN-β

59
Q

What isIFN-γ used for?

A

Chronic granulomatous disease

60
Q

What recombinant cytokine can you use for chronic granulomatous disease?

A

IFN-γ

61
Q

What is romiplostim, eltrombopag used for?

A

Thrombocytopenia

62
Q

What isOprelvekin (IL-11) used for?

A

Thrombocytopenia

63
Q

What recombinant cytokine can you use for thrombocytopenia?

A
  • Romiplostim, eltrombopag

* Oprelvekin (IL-11)

64
Q

Cancer therapeutic antibodies

A
  • Alemtuzumab
  • Bevacizumab
  • Cetuximab
  • Rituximab
  • Trastuzumab
65
Q

Alemtuzumab

A

Cancer therapeutic antibody

66
Q

Bevacizumab

A

Cancer therapeutic antibody

67
Q

Cetuximab

A

Cancer therapeutic antibody

68
Q

Rituximab

A

Cancer therapeutic antibody

69
Q

Trastuzumab

A

Cancer therapeutic antibody

70
Q

Cyclosporine

A

Immunosuppressant

71
Q

Tacrolimus (FK506)

A

Immunosuppressant

72
Q

Sirolimus (Rapamycin)

A

Immunosuppressant

73
Q

Daclizumab, basiliximab

A

Immunosuppressant

74
Q

Azathioprine

A

Immunosuppressant

75
Q

Glucocorticoids

A

Immunosuppressant

76
Q

Alemtuzumabtarget

A

CD52

77
Q

Alemtuzumabclinical use

A

CLL- chronic lymphocytic leukemia

78
Q

Bevacizumabtarget

A

VEGF

79
Q

Bevacizumabclinical use

A

Colorectal cancer, renal cell carcinoma

80
Q

Cetuximabtarget

A

EGFR

81
Q

Cetuximabclinical use

A

Stage IV colorectal cancer, head and neck cancer

82
Q

Rituximabtarget

A

CD20

83
Q

Rituximabclinical use

A
  • B-cell non-Hodgkin lymphoma
  • CLL
  • rheumatoid arthritis
  • ITP (Idiopathic thrombocytopenic purpura)
84
Q

Trastuzumabtarget

A

HER2/neu

85
Q

Trastuzumabclinical use

A

Breast cancer

86
Q

Autoimmune disease thereapeutic antibodies

A
  • Adalimumab, infliximab
  • Eculizumab
  • Natalizumab
87
Q

Natalizumab

A

Autoimmune therapeutic antibody

88
Q

Eculizumab

A

Autoimmune therapeutic antibody

89
Q

Adalimumab, infliximab

A

Autoimmune thereapeutic antibody

90
Q

Adalimumab, infliximabtarget

A

Soluble TNF-α

91
Q

Soluble TNF-αclinical use

A
  • IBD
  • rheumatoid arthritis
  • ankylosing spondylitis
  • psoriasis
92
Q

Adalimumab, infliximabfact

A

Etanercept is a decoy TNF-α receptor and not a monoclonal antibody

93
Q

Eculizumabtarget

A

Complement protein C5

94
Q

Eculizumabclinical use

A

Paroxysmal nocturnal hemoglobinuria

95
Q

Natalizumabtarget

A

α4-integrin

96
Q

Natalizumabclinical use

A

Multiple sclerosis, Crohn disease

97
Q

Natalizumabfact

A

α4-integrin: WBC adhesionRisk of PML in patients withJC virus

98
Q

Abciximabtarget

A

Platelet glycoproteins IIb/IIIa

99
Q

Abciximabclinical use

A

Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention

100
Q

Denosumab target

A

RANKL

101
Q

Denosumabclinical use

A

Osteoporosis; inhibits osteoclast maturation (mimicsosteoprotegerin)

102
Q

Digoxin immune Fabtarget

A

Digoxin

103
Q

Digoxin immune Fabclinical use

A

Antidote for digoxin toxicity

104
Q

Omalizumabtarget

A

IgE

105
Q

Omalizumabclinical use

A

Allergic asthma; prevents IgE binding to FcεRI

106
Q

Palivizumabtarget

A

RSV F protein

107
Q

Palivizumabclinical use

A

RSV prophylaxis for high-risk infants

108
Q

Ranibizumab, bevacizumabtarget

A

VEGF

109
Q

Ranibizumab, bevacizumabclinical use

A

Neovascular age-related macular degeneration

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