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deck_3459905 Flashcards

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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
Daclizumab, basiliximab mechanism
Monoclonal antibodies; block IL-2R. 
26
Daclizumab, basiliximab uses
Kidney transplant rejection prophylaxis. 
27
Daclizumab, basiliximab toxicities
* Edema * Hypertension * Tremor
28
Azathioprine mechanism
Antimetabolite precursor of 6-mercaptopurine.Inhibits lymphocyte proliferation by blocking nucleotide synthesis. 
29
Axathioprine uses
* Transplant rejection prophylaxis * rheumatoid arthritis * Crohn disease * glomerulonephritis * other autoimmune conditions 
30
Azathioprine toxicity
Leukopenia anemia thrombocytopenia 
31
Azathioprine facts
6-MP degraded by xanthine oxidase; toxicity ↑ by allopurinol.Pronounce “azathio- purine.” 
32
Glucocorticoid mechanism
Inhibit NF-κB. Suppress both B- and T-cell function by
33
Glucocorticoid uses
Transplant rejection prophylaxis (immuno-suppression), many autoimmune disorders, inflammation. 
34
Glucocorticoid toxicity
* Hyperglycemia * osteoporosis * central obesity * muscle breakdown * psychosis * acne * hypertension * cataracts * avascular necrosis
35
Glucocorticoid facts
Can cause iatrogenic Cushing syndrome. 
36
Monoclonal antibodies; block IL-2R. 
Daclizumab, basiliximab mechanism
37
Kidney transplant rejection prophylaxis. 
Daclizumab, basiliximab uses
38
* Edema * Hypertension * Tremor
Daclizumab, basiliximab toxicities
39
Antimetabolite precursor of 6-mercaptopurine.Inhibits lymphocyte proliferation by blocking nucleotide synthesis. 
Azathioprine mechanism
40
* Transplant rejection prophylaxis * rheumatoid arthritis * Crohn disease * glomerulonephritis * other autoimmune conditions 
Axathioprine uses
41
Leukopenia anemia thrombocytopenia 
Azathioprine toxicity
42
6-MP degraded by xanthine oxidase; toxicity ↑ by allopurinol.Pronounce “azathio- purine.” 
Azathioprine facts
43
Inhibit NF-κB. Suppress both B- and T-cell function by
Glucocorticoid mechanism
44
Transplant rejection prophylaxis (immuno-suppression), many autoimmune disorders, inflammation. 
Glucocorticoid uses
45
* Hyperglycemia * osteoporosis * central obesity * muscle breakdown * psychosis * acne * hypertension * cataracts * avascular necrosis
Glucocorticoid toxicity
46
Can cause iatrogenic Cushing syndrome. 
Glucocorticoid facts
47
Draw a diagram and show where the immunosuppressants work
48
What is Aldesleukin (IL-2) used for?
Renal cell carcinoma, metastatic melanoma 
49
What recombinant cytokine can you use for renal cell carcinoma, metastatic melanoma? 
Aldesleukin (IL-2)
50
What is Epoetin alfa (erythropoietin) used for?
Anemias (especially in renal failure) 
51
What recombinant cytokine can you use for anemias (especially in renal failure)? 
Epoetin alfa (erythropoietin) 
52
What is Filgrastim (G-CSF) used for?
Recovery of bone marrow 
53
What is Sargramostim (GM-CSF) used for?
Recovery of bone marrow 
54
What recombinant cytokine can you use for recovery of bone marrow?
* Filgrastim (G-CSF)  | * Sargramostim (GM-CSF) 
55
What is IFN-α  used for?
* Chronic hepatitis B and C * Kaposi sarcoma * malignant melanoma 
56
What recombinant cytokine can you use for chronic hepatitis B and C, Kaposi sarcoma, and malignant melanoma?
IFN-α 
57
What is IFN-β used for?
Multiple sclerosis 
58
What recombinant cytokine can you use for multiple sclerosis?
IFN-β
59
What is IFN-γ used for?
Chronic granulomatous disease 
60
What recombinant cytokine can you use for chronic granulomatous disease? 
IFN-γ
61
What is romiplostim, eltrombopag used for?
Thrombocytopenia
62
What is Oprelvekin (IL-11) used for?
Thrombocytopenia
63
What recombinant cytokine can you use for thrombocytopenia?
* Romiplostim, eltrombopag  | * Oprelvekin (IL-11) 
64
Cancer therapeutic antibodies
* Alemtuzumab  * Bevacizumab  * Cetuximab  * Rituximab  * Trastuzumab 
65
Alemtuzumab 
Cancer therapeutic antibody
66
Bevacizumab 
Cancer therapeutic antibody
67
Cetuximab 
Cancer therapeutic antibody
68
Rituximab 
Cancer therapeutic antibody
69
Trastuzumab 
Cancer therapeutic antibody
70
Cyclosporine 
Immunosuppressant
71
Tacrolimus (FK506) 
Immunosuppressant
72
Sirolimus (Rapamycin) 
Immunosuppressant
73
Daclizumab, basiliximab 
Immunosuppressant
74
Azathioprine 
Immunosuppressant
75
Glucocorticoids 
Immunosuppressant 
76
Alemtuzumab target
CD52 
77
Alemtuzumab clinical use
CLL- chronic lymphocytic leukemia
78
Bevacizumab target
VEGF 
79
Bevacizumab clinical use
Colorectal cancer, renal cell carcinoma 
80
Cetuximab target
EGFR 
81
Cetuximab clinical use
Stage IV colorectal cancer, head and neck cancer 
82
Rituximab target
CD20 
83
Rituximab clinical use
* B-cell non-Hodgkin lymphoma * CLL  * rheumatoid arthritis  * ITP (Idiopathic thrombocytopenic purpura)
84
Trastuzumab target
HER2/neu 
85
Trastuzumab clinical use
Breast cancer 
86
Autoimmune disease thereapeutic antibodies
* Adalimumab, infliximab  * Eculizumab  * Natalizumab 
87
Natalizumab 
Autoimmune therapeutic antibody
88
Eculizumab 
Autoimmune therapeutic antibody
89
Adalimumab, infliximab 
Autoimmune thereapeutic antibody
90
Adalimumab, infliximab target
Soluble TNF-α 
91
Soluble TNF-α clinical use
* IBD  * rheumatoid arthritis  * ankylosing spondylitis * psoriasis 
92
Adalimumab, infliximab fact
Etanercept is a decoy TNF-α receptor and not a monoclonal antibody 
93
Eculizumab target
Complement protein C5 
94
Eculizumab clinical use
Paroxysmal nocturnal hemoglobinuria 
95
Natalizumab target
α4-integrin 
96
Natalizumab clinical use
Multiple sclerosis, Crohn disease 
97
Natalizumab fact
α4-integrin: WBC adhesionRisk of PML in patients withJC virus 
98
Abciximab target
Platelet glycoproteins IIb/IIIa 
99
Abciximab clinical use
Antiplatelet agent for prevention of ischemic complications in patients undergoing percutaneous coronary intervention 
100
Denosumab target
RANKL 
101
Denosumab clinical use
Osteoporosis; inhibits osteoclast maturation (mimicsosteoprotegerin) 
102
Digoxin immune Fab target
Digoxin 
103
Digoxin immune Fab clinical use
Antidote for digoxin toxicity 
104
Omalizumab target
IgE 
105
Omalizumab clinical use
Allergic asthma; prevents IgE binding to FcεRI 
106
Palivizumab target
RSV F protein 
107
Palivizumab clinical use
RSV prophylaxis for high-risk infants 
108
Ranibizumab, bevacizumab target
VEGF 
109
Ranibizumab, bevacizumab clinical use
Neovascular age-related macular degeneration 
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