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Pharmacology > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

cyclosporine mechanism

A

calcineurin inhibitor
binds cyclophilin
prevents IL-2 transcription –> blocks T cell activation

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2
Q

cyclosporine mechanism

A

calcineurin inhibitor
binds cyclophilin
prevents IL-2 transcription –> blocks T cell activation

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3
Q

side effects cyclosporine (6)

A
  1. nephrotoxicity
  2. HTN
  3. hyperlipidemia
  4. hyperglycemia
  5. hirsuitism
  6. gingival hyperplasia
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4
Q

which immunosuppressants are highly nephrotoxic?

A

calcineurin inhibitors (cyclosporine and tacrolimus)

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5
Q

tacrolimus mechanism

A

calcineurin inhibitor
binds FK506 binding protein (FKBP)
prevents IL-2 transcription –> blocks T cell activation

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6
Q

side effects tacrolimus

A
  1. similar to cyclosporine (nephrotoxocity!)
  2. increased risk diabetes and neurotoxicity
  3. no gingival hyperplasia or hirsuitism
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7
Q

sirolimus (rapamycin) mechanism

A

mTOR inhibitor
binds FKBP
prevents IL-2 signal transduction –> blocks T cell activation

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8
Q

side effects sirolimus (rapamycin)

A
  1. anemia
  2. thrombocytopenia
  3. leukopenia
  4. insulin resistance
  5. hyperlipidemia
  6. NOT NEPHROTOXIC
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9
Q

which IL-2 inhibitor (T cell activation inhibitor) is not nephrotoxic? –> use in pt with decreased renal function

A

sirolimus (rapamycin)

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10
Q

basiliximab mechanism

A

monoclonal antibody against IL-2R

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11
Q

side effects basiliximab

A
  1. edema
  2. hypertension
  3. tremor
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12
Q

azathioprine mechanism

A

antimetabolite precursor of 6-mercaptopurine

inhibits lymphocyte proliferation by blocking nucleotide synthesis

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13
Q

side effects azathioprine

A
  1. leukopenia
  2. anemia
  3. thrombocytopenia
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14
Q

what happens if you give allopurinol to a pt on azathioprine?

A

increases toxicity (6-MP is degraded by xanthine oxidase)

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15
Q

immunosuppressive mechanism of glucocorticoids

A

inhibit NFKB

suppress B and T cell function (decrease cytokine transcription)

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16
Q

side effects glucocorticoids

A
  1. hyperglycemia
  2. osteoporosis
  3. central obesity
  4. muscle breakdown
  5. psychosis
  6. acne
  7. HTN
  8. cataracts
  9. peptic ulcers
  10. Cushing syndrome
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17
Q

what is aldesleukin

A

recombinant IL-2

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18
Q

clinical use aldesleukin

A

renal cell carcinoma

metastatic melanoma

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19
Q

what is sargramostim

A

granulocyte-macrophage colony-stimulating factor

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20
Q

clinical use sargramostim

A

recovery of bone marrow

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21
Q

what is filgrastim

A

granulocyte colony-stimulating factor

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22
Q

clinical use filgrastim

A

recovery of bone marrow

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23
Q

what is oprelvekin

A

recombinant IL-11

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24
Q

clinical use oprelvekin

A

thrombocytopenia

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25
Q

clinical use thrombopoietin

A

thrombocytopenia

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26
Q

clinical use epoetin alpha (erythropoietin)

A

anemia (esp. in renal failure)

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27
Q

what is alemtuzumab

A

anti-CD52

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28
Q

clinical use alemtuzumab (anti-CD52)

A

CLL

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29
Q

what is bevacizumab

A

anti-VEGF

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30
Q

clinical use bevacizumab (anti-VEGF)

A

renal cell carcinoma, colorectal cancer

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31
Q

what is cetuximab

A

anti-EGFR

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32
Q

clinical use cetuximab (anti-EGFR)

A

stage IV colorectal cancer

head and neck cancer

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33
Q

what is rituximab?

A

anti-CD20

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34
Q

clinical use rituximab (anti-CD20)

A

B-cell non-Hodgkin lymphoma
RA (with MTX)
ITP

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35
Q

what is trastuzumab

A

anti-HER2/Neu

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36
Q

clinical use trastuzumab

A

breast cancer, gastric cancer

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37
Q

what is infliximab

A

anti-TNF-alpha

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38
Q

what is adalimumab

A

anti-TNF-alpha

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39
Q

clinical use infliximab/adalimumab

A

IBD
RA
ankylosing spondylitis
psoriasis

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40
Q

what is natalizumab

A

anti-alpha4-integrin

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41
Q

clinical use natalizumab

A

Crohn’s

MS

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42
Q

what is abciximab?

A

anti-glycoprotein IIb/IIIa

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43
Q

clinical use abciximab

A

antiplatelet agent

44
Q

what is denosumab?

A

anti-RANKL

45
Q

clinical use denosumab

A

osteoporosis (inhibits osteoclast maturation, mimics osteoprotegrin - OPG)

46
Q

clinical use digoxin immune Fab

A

antidote for digoxin toxicity

47
Q

what is omalizumab

A

anti-IgE

48
Q

clinical use omalizumab

A

allergic asthma (prevents IgE binding to FcERI)

49
Q

what is palivizumab?

A

anti-RSV F protein

50
Q

clinical use palivizumab

A

RSV prophylaxis for high-risk infants

51
Q

what is calcipotriene?

A

topical vitamin D analog

52
Q

clinical use calcipotriene (and calcitriol, tacalcitol)

A

psoriasis (activate vitamin D receptor, inhibit keratinocyte proliferation)

53
Q

what is etanercept?

A

binds TNFalpha

54
Q

clinical use etanercept

A

psoriasis

55
Q

side effects cyclosporine (6)

A
  1. nephrotoxicity
  2. HTN
  3. hyperlipidemia
  4. hyperglycemia
  5. hirsuitism
  6. gingival hyperplasia
56
Q

which immunosuppressants are highly nephrotoxic?

A

calcineurin inhibitors (cyclosporine and tacrolimus)

57
Q

tacrolimus mechanism

A

calcineurin inhibitor
binds FK506 binding protein (FKBP)
prevents IL-2 transcription –> blocks T cell activation

58
Q

side effects tacrolimus

A
  1. similar to cyclosporine (nephrotoxocity!)
  2. increased risk diabetes and neurotoxicity
  3. no gingival hyperplasia or hirsuitism
59
Q

sirolimus (rapamycin) mechanism

A

mTOR inhibitor
binds FKBP
prevents IL-2 signal transduction –> blocks T cell activation

60
Q

side effects sirolimus (rapamycin)

A
  1. anemia
  2. thrombocytopenia
  3. leukopenia
  4. insulin resistance
  5. hyperlipidemia
  6. NOT NEPHROTOXIC
61
Q

which IL-2 inhibitor (T cell activation inhibitor) is not nephrotoxic? –> use in pt with decreased renal function

A

sirolimus (rapamycin)

62
Q

basiliximab mechanism

A

monoclonal antibody against IL-2R

63
Q

side effects basiliximab

A
  1. edema
  2. hypertension
  3. tremor
64
Q

azathioprine mechanism

A

antimetabolite precursor of 6-mercaptopurine

inhibits lymphocyte proliferation by blocking nucleotide synthesis

65
Q

side effects azathioprine

A
  1. leukopenia
  2. anemia
  3. thrombocytopenia
66
Q

what happens if you give allopurinol to a pt on azathioprine?

A

increases toxicity (6-MP is degraded by xanthine oxidase)

67
Q

immunosuppressive mechanism of glucocorticoids

A

inhibit NFKB

suppress B and T cell function (decrease cytokine transcription)

68
Q

side effects glucocorticoids

A
  1. hyperglycemia
  2. osteoporosis
  3. central obesity
  4. muscle breakdown
  5. psychosis
  6. acne
  7. HTN
  8. cataracts
  9. peptic ulcers
  10. Cushing syndrome
69
Q

what is aldesleukin

A

recombinant IL-2

70
Q

clinical use aldesleukin

A

renal cell carcinoma

metastatic melanoma

71
Q

what is sargramostim

A

granulocyte-macrophage colony-stimulating factor

72
Q

clinical use sargramostim

A

recovery of bone marrow

73
Q

what is filgrastim

A

granulocyte colony-stimulating factor

74
Q

clinical use filgrastim

A

recovery of bone marrow

75
Q

what is oprelvekin

A

recombinant IL-11

76
Q

clinical use oprelvekin

A

thrombocytopenia

77
Q

clinical use thrombopoietin

A

thrombocytopenia

78
Q

clinical use epoetin alpha (erythropoietin)

A

anemia (esp. in renal failure)

79
Q

what is alemtuzumab

A

anti-CD52

80
Q

clinical use alemtuzumab (anti-CD52)

A

CLL

81
Q

what is bevacizumab

A

anti-VEGF

82
Q

clinical use bevacizumab (anti-VEGF)

A

renal cell carcinoma, colorectal cancer

83
Q

what is cetuximab

A

anti-EGFR

84
Q

clinical use cetuximab (anti-EGFR)

A

stage IV colorectal cancer

head and neck cancer

85
Q

what is rituximab?

A

anti-CD20

86
Q

clinical use rituximab (anti-CD20)

A

B-cell non-Hodgkin lymphoma
RA (with MTX)
ITP

87
Q

what is trastuzumab

A

anti-HER2/Neu

88
Q

clinical use trastuzumab

A

breast cancer, gastric cancer

89
Q

what is infliximab

A

anti-TNF-alpha

90
Q

what is adalimumab

A

anti-TNF-alpha

91
Q

clinical use infliximab/adalimumab

A

IBD
RA
ankylosing spondylitis
psoriasis

92
Q

what is natalizumab

A

anti-alpha4-integrin

93
Q

clinical use natalizumab

A

Crohn’s

MS

94
Q

what is abciximab?

A

anti-glycoprotein IIb/IIIa

95
Q

clinical use abciximab

A

antiplatelet agent

96
Q

what is denosumab?

A

anti-RANKL

97
Q

clinical use denosumab

A

osteoporosis (inhibits osteoclast maturation, mimics osteoprotegrin - OPG)

98
Q

clinical use digoxin immune Fab

A

antidote for digoxin toxicity

99
Q

what is omalizumab

A

anti-IgE

100
Q

clinical use omalizumab

A

allergic asthma (prevents IgE binding to FcERI)

101
Q

what is palivizumab?

A

anti-RSV F protein

102
Q

clinical use palivizumab

A

RSV prophylaxis for high-risk infants

103
Q

what is calcipotriene?

A

topical vitamin D analog

104
Q

clinical use calcipotriene (and calcitriol, tacalcitol)

A

psoriasis (activate vitamin D receptor, inhibit keratinocyte proliferation)

105
Q

what is etanercept?

A

binds TNFalpha

106
Q

clinical use etanercept

A

psoriasis

Pharmacology (8 decks)

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