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Immunosuppressants Flashcards

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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
clinical use thrombopoietin
thrombocytopenia
26
clinical use epoetin alpha (erythropoietin)
anemia (esp. in renal failure)
27
what is alemtuzumab
anti-CD52
28
clinical use alemtuzumab (anti-CD52)
CLL
29
what is bevacizumab
anti-VEGF
30
clinical use bevacizumab (anti-VEGF)
renal cell carcinoma, colorectal cancer
31
what is cetuximab
anti-EGFR
32
clinical use cetuximab (anti-EGFR)
stage IV colorectal cancer | head and neck cancer
33
what is rituximab?
anti-CD20
34
clinical use rituximab (anti-CD20)
B-cell non-Hodgkin lymphoma RA (with MTX) ITP
35
what is trastuzumab
anti-HER2/Neu
36
clinical use trastuzumab
breast cancer, gastric cancer
37
what is infliximab
anti-TNF-alpha
38
what is adalimumab
anti-TNF-alpha
39
clinical use infliximab/adalimumab
IBD RA ankylosing spondylitis psoriasis
40
what is natalizumab
anti-alpha4-integrin
41
clinical use natalizumab
Crohn's | MS
42
what is abciximab?
anti-glycoprotein IIb/IIIa
43
clinical use abciximab
antiplatelet agent
44
what is denosumab?
anti-RANKL
45
clinical use denosumab
osteoporosis (inhibits osteoclast maturation, mimics osteoprotegrin - OPG)
46
clinical use digoxin immune Fab
antidote for digoxin toxicity
47
what is omalizumab
anti-IgE
48
clinical use omalizumab
allergic asthma (prevents IgE binding to FcERI)
49
what is palivizumab?
anti-RSV F protein
50
clinical use palivizumab
RSV prophylaxis for high-risk infants
51
what is calcipotriene?
topical vitamin D analog
52
clinical use calcipotriene (and calcitriol, tacalcitol)
psoriasis (activate vitamin D receptor, inhibit keratinocyte proliferation)
53
what is etanercept?
binds TNFalpha
54
clinical use etanercept
psoriasis
55
side effects cyclosporine (6)
1. nephrotoxicity 2. HTN 3. hyperlipidemia 4. hyperglycemia 5. hirsuitism 6. gingival hyperplasia
56
which immunosuppressants are highly nephrotoxic?
calcineurin inhibitors (cyclosporine and tacrolimus)
57
tacrolimus mechanism
calcineurin inhibitor binds FK506 binding protein (FKBP) prevents IL-2 transcription --> blocks T cell activation
58
side effects tacrolimus
1. similar to cyclosporine (nephrotoxocity!) 2. increased risk diabetes and neurotoxicity 3. no gingival hyperplasia or hirsuitism
59
sirolimus (rapamycin) mechanism
mTOR inhibitor binds FKBP prevents IL-2 signal transduction --> blocks T cell activation
60
side effects sirolimus (rapamycin)
1. anemia 2. thrombocytopenia 3. leukopenia 4. insulin resistance 5. hyperlipidemia 6. NOT NEPHROTOXIC
61
which IL-2 inhibitor (T cell activation inhibitor) is not nephrotoxic? --> use in pt with decreased renal function
sirolimus (rapamycin)
62
basiliximab mechanism
monoclonal antibody against IL-2R
63
side effects basiliximab
1. edema 2. hypertension 3. tremor
64
azathioprine mechanism
antimetabolite precursor of 6-mercaptopurine | inhibits lymphocyte proliferation by blocking nucleotide synthesis
65
side effects azathioprine
1. leukopenia 2. anemia 3. thrombocytopenia
66
what happens if you give allopurinol to a pt on azathioprine?
increases toxicity (6-MP is degraded by xanthine oxidase)
67
immunosuppressive mechanism of glucocorticoids
inhibit NFKB | suppress B and T cell function (decrease cytokine transcription)
68
side effects glucocorticoids
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
what is aldesleukin
recombinant IL-2
70
clinical use aldesleukin
renal cell carcinoma | metastatic melanoma
71
what is sargramostim
granulocyte-macrophage colony-stimulating factor
72
clinical use sargramostim
recovery of bone marrow
73
what is filgrastim
granulocyte colony-stimulating factor
74
clinical use filgrastim
recovery of bone marrow
75
what is oprelvekin
recombinant IL-11
76
clinical use oprelvekin
thrombocytopenia
77
clinical use thrombopoietin
thrombocytopenia
78
clinical use epoetin alpha (erythropoietin)
anemia (esp. in renal failure)
79
what is alemtuzumab
anti-CD52
80
clinical use alemtuzumab (anti-CD52)
CLL
81
what is bevacizumab
anti-VEGF
82
clinical use bevacizumab (anti-VEGF)
renal cell carcinoma, colorectal cancer
83
what is cetuximab
anti-EGFR
84
clinical use cetuximab (anti-EGFR)
stage IV colorectal cancer | head and neck cancer
85
what is rituximab?
anti-CD20
86
clinical use rituximab (anti-CD20)
B-cell non-Hodgkin lymphoma RA (with MTX) ITP
87
what is trastuzumab
anti-HER2/Neu
88
clinical use trastuzumab
breast cancer, gastric cancer
89
what is infliximab
anti-TNF-alpha
90
what is adalimumab
anti-TNF-alpha
91
clinical use infliximab/adalimumab
IBD RA ankylosing spondylitis psoriasis
92
what is natalizumab
anti-alpha4-integrin
93
clinical use natalizumab
Crohn's | MS
94
what is abciximab?
anti-glycoprotein IIb/IIIa
95
clinical use abciximab
antiplatelet agent
96
what is denosumab?
anti-RANKL
97
clinical use denosumab
osteoporosis (inhibits osteoclast maturation, mimics osteoprotegrin - OPG)
98
clinical use digoxin immune Fab
antidote for digoxin toxicity
99
what is omalizumab
anti-IgE
100
clinical use omalizumab
allergic asthma (prevents IgE binding to FcERI)
101
what is palivizumab?
anti-RSV F protein
102
clinical use palivizumab
RSV prophylaxis for high-risk infants
103
what is calcipotriene?
topical vitamin D analog
104
clinical use calcipotriene (and calcitriol, tacalcitol)
psoriasis (activate vitamin D receptor, inhibit keratinocyte proliferation)
105
what is etanercept?
binds TNFalpha
106
clinical use etanercept
psoriasis

Pharmacology (8 decks)

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