IMMUNO - Immunosuppressants Flashcards

1
Q

Immunosuppressant general use

A

Block lymphocyte proliferation and activation

Decrease ACUTE graft rejection by decreasing CELLULAR immunity

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2
Q

Immunosuppressant general toxicity

A

Long-term use increases risk of infections and cancer

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3
Q

Cyclosporin MOA

A
Binds cyclophilin
to inhibit calcineurin
blocking NFAT dephosphorylation
so NFAT can't get into nucleus 
so no IL-2 TC

Blocks IL-2 TC

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4
Q

cyclosporin use

A

Transplant rejection prophylaxis
Psoriasis
RA

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5
Q

Cyclosporin toxicity

A
NEPHROTOXICITY
Gingival hyperplasia
Hirsutism
HTN
hyperlipidemia
neurotoxicity
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6
Q

Tacrolimus (FK508) MOA

A
Binds FKBP
To inhibit calcineurin
blocking NFAT dephosphorylation
so NFAT can't get into nucleus 
so no IL-2 TC

Blocks IL-2 TC

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7
Q

Tacrolimus (FK508) use

A

transplant rejection prophylaxis

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8
Q

Tacrolimus (FK508) toxicity

A

NEPHROTOXICITY
HTN
hyperlipidemia (more risk of DM)
neurotoxicity (more risk)

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9
Q

Sirolimus (rapamycin) MOA

A

binds FKBP
to inhibit mTOR
to block T-cell activation and B-cell differentiation

Inhibits cells RESPONSE to IL-2 (IL-2 activates mTOR)

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10
Q

Sirolimus (rapamycin) use

A

KIDNEY transplant rejection prophylaxis

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11
Q

Sirolimus (rapamycin) toxicity

A
Anemia
Thrombocytopenia
Leukopenia
Insulin resistance and hyperlipidemia
*NOT nephrotoxic*
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12
Q

Daclizumab MOA

A

monoclonal Ab to block IL-2R

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13
Q

Daclizumab use

A

KIDNEY transplant rejection prophylaxis

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14
Q

Daclizumab toxicity

A

Edema
HTN
Tremor

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15
Q

Basiliximab MOA

A

monoclonal Ab to block IL-2R

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16
Q

Basiliximab use

A

KIDNEY transplant rejection prophylaxis

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17
Q

Basiliximab toxicity

A

Edema
HTN
Tremor

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18
Q

Azathioprine MOA

A

Antimetabolite: blocks NT (purine) synthesis inhibiting lymphocyte proliferation
Precursor of 6-MP.

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19
Q

Azathioprine use

A
Transplant rejection prophylaxis
RA
Chrons
Glomerulonephritis
Other autoimmunes
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20
Q

Azathioprine toxicities

A

Leukopenia
Anemia
Thrombocytopenia

*6MP degraded by XO, so increased toxicity by allopurinol

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21
Q

Glucocorticoids MOA

A

Inhibits NF-KB, inhibiting cytokine TC, suppressing B and T cell function

22
Q

Random glucocorticoid toxicity:

A

Cushings
Psyhchosis
Cataracts
Avascular necrosis

23
Q

Alemtuzumab (target)

A

Cancer therapy: CD52

24
Q

Bevacizumab (target)

A

Cancer therapy: VEGF

25
Cetuximab (target)
Cancer therapy: EGFR
26
Rituximab (target)
Cancer therapy: CD20
27
Trastuzumab (target)
Cancer therapy: HER2/neu
28
Alemtuzumab (Clinical use)
Cancer therapy: CLL
29
Bevacizumab (Clinical use)
Cancer therapy: Colorectal cancer, renal cell carcinoma
30
Cetuximab (Clinical use)
Cancer therapy: Stage IV colorectal cancer, head and neck cancer
31
Rituximab (Clinical use)
Cancer therapy: B-cell non-hodgkin lymphoma, CLL, rheumatoid arthritis, ITP
32
Trastuzumab (Clinical use)
Cancer therapy: Breast cancer
33
Adalimumab (Target)
Autoimmune therapy: Soluble TNF-alpha
34
infliximab (Target)
Autoimmune therapy: Soluble TNF-alpha
35
Eculizumab (Target)
Autoimmune therapy: Compliment protein C5
36
Natalizumab (Target)
Autoimmune therapy: alpha4-integrin
37
Etanercept (Target)
Decoy TNF-alhpa receptor (not monoclonal ab)
38
Adalimumab (Clinical use)
IBD, rheumatoid arthriis, ankylosing spondylitis, psoriasis
39
Infliximab (Clinical use)
IBD, rheumatoid arthriis, ankylosing spondylitis, psoriasis
40
Eculizumab (Clinical use)
paroxysmal nocturnal hemoglobinuria
41
Natalizumab (Clinical use) (+AE)
Multiple sclerosis, Crohn disease | *risk of PML
42
ABCiximab (target)
Platelet glycoproteins IIb/IIIa
43
Denosumab (target)
RANKL
44
Digoxin immune fab (target)
digoxin
45
Omalizumab (target)
IgE
46
Palivizumab (target)
RSV F protein
47
Ranibizumab (target)
VEGF
48
ABCixumab (Clinical use)
Prevention of ischemic complications in percutaneous coronary intervention
49
Denosumab (Clinical use)
Osteoporosis; prevents osteoclast maturation
50
Omalizumab (Clinical use)
Allergic asthma; prevents IgE biding FcR1
51
Palivizumab (Clinical use)
RSV prophylaxis for high risk infants
52
Ranibizumab (Clinical use)
Neovascular age-related macular degeneration