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PLAB Pharmacology > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

general mechanism of immunosuppressants

A
  • agents that block lymphocyte activation and proliferation
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2
Q

how would you reduce acute transplant rejection?

A
  • suppress cellular immunity
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3
Q

why would you combine immunosuppressants?

A
  • immunosuppressants are frequently combined to achieve greater efficacy with decrease toxicity
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4
Q

what may occur with chronic immune suppression?

A

increased risk of infection and malignancy

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5
Q

what are the 2 calcineurin inhibitors? what kind of toxicity is likely with both?

A
  • cyclosporine
  • tacrolimus (FK506)
    • highly nephrotoxic
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6
Q

cyclosporine–mechanism

A
  • calcineurin inhibitor
    • binds cyclophilin
    • blocks T cell activaiton by preventing IL-2 transcription
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7
Q

cyclosporine–use

A
  • transplant rejection prophylaxis
  • psoriasis
  • rheumatoid arthritis
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8
Q

cyclosporine–toxicity

A
  • nephrotoxicity
    • hypertention
    • hyperlipidemia
    • neurotoxicity
    • gingival hyperplasia
    • hirsutism
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9
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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10
Q

tacrolimus (FK506)–use

A
  • transplant rejection prophylaxis
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11
Q

tacrolimus (FK506)–toxicity

A
  • similar to cyclosporine
  • inc risk of diabetes and neurotoxicity
  • no gingival hyperplasia or hirsutism
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12
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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13
Q

Sirolimus (Rapamycin)–use

A
  • kidney tranplant rejection prophylaxis
  • drug eluting stents
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14
Q

Sirolimus (Rapamycin)–toxicity

A
  • “PanSirtopenia”–pancytopenia
  • insulin resistance
  • hyperlipidemia
  • not nephrotoxic
    • ​“kidney sir-vives”
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15
Q

what is sirolimus (rapamycin) synergistic with?

A

cyclosporine

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16
Q

Daclizumab, basiliximab–mechanism

A
  • monoclonal antibodies
  • block IL-2R
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17
Q

Daclizumab, basiliximab–use

A
  • kidney transplant rejection prophylaxis
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18
Q

Daclizumab, basiliximab–toxicity

A
  • edema
  • hypertension
  • tremor
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19
Q

azathioprine–mechanism

A
  • antimetabolite precursor of 6-mercaptopurine
    • ​“pronounce ‘azathiopurine’“
  • inhibits lymphocyte proliferation by blocking nucleotide synthesis
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20
Q

azathioprine–use

A
  • transplant rejection prophylaxis
  • rheumatoid arthritis
  • Crohn disease
  • glomerulonephritis
  • other autoimmune conditions
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21
Q

azathioprine–toxicity

A
  • leukopenia
  • anemia
  • thrombocytopenia
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22
Q

what degrades 6-MP?

A

xanthine oxidase

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23
Q

what increases the toxicity of azathioprine?

A

allopurinol

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24
Q

mycophenolate mofetil–mechanism

A
  • reversibly inhibits IMP dehydrogenase
    • prevents purine synthesis of B and T cells
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25
Q

mycophenolate mofetil–use

A
  • transplant rejection prophylaxis
  • lupus nephritis
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26
Q

mycophenolate mofetil–toxicity

A
  • GI upset
  • pancytopenia
  • hypertension
  • hyperglycemia
  • less nephrotoxic and neurotoxic
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27
Q

what is mycophenolate mofetil associated with?

A
  • invasive CMV infection
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28
Q

corticosteroids–mechanism

A
  • inhibit NF-kappaB
  • suppress both B and T cell function by decrease transcriptionof many cytokines
  • induce apoptosis of T lymphocytes
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29
Q

corticosteroids–use

A
  • transplant rejection prophylaxis
  • many autoimmune and inflammatory disorders
30
Q

corticosteroids–toxicity

A
  • hyperglycemia
  • osteoporosis
  • central obesity
  • muscle breakdown
  • psychosis
  • acne
  • hypertension
  • cataracts
  • avascular necrosis (femoral head)
31
Q

what can result due to taking corticosteroids?

A

iatrogenic Cushing syndrome

32
Q

what is the clinical use of Aldesleukin (IL-2)?

A
  • renal cell carcinoma
  • metastatic melanoma
33
Q

what is the clinical use of epoetin alfa (erythropoietin)?

A
  • anemias (especially in renal failure)
34
Q

what is the clinical use of filgrastim (G-CSF)?

A
  • recovery of bone marrow
35
Q

what is the clinical use of sargramostim (GM-CSF)?

A
  • recovery of bone marrow
36
Q

what is the clinical use of IFN-alpha?

A
  • chronic hepatitis B and C
  • Kaposi sarcoma
  • malignant melanoma
37
Q

what is the clinical use of IFN beta?

A
  • multiple sclerosis
38
Q

what is the clinical use of IFN gamma?

A
  • chronic granulomatous disease
39
Q

what is the romiplostim, eltrombopag (thrombopoietin receptor agonists)?

A
  • thrombocytopenia
40
Q

what is the oprelvekin (IL-11)?

A
  • thrombocytopenia
41
Q

name the therapeutic antibodies for cancer therapy

A
  • alemtuzumab
  • bevacizumab
  • cetuximab
  • rituximab
  • trastuzumab
42
Q

alemtuzumab–target

A
  • CD52
43
Q

alemtuzumab–use

A
  • CLL
    • “Alymtuzumab”–chronic lymphocytic leukemia
  • MS
44
Q

bevacizumab–target

A
  • VEGF
45
Q

bevacizumab–use

A
  • colorectal cancer
  • renal cell carcinoma
46
Q

cetuximab–target

A
  • EGFR
47
Q

cetuximab–use

A
  • stage IV colorectal cancer
  • head and neck cancer
48
Q

rituximab–target

A
  • CD20
49
Q

rituximab–use

A
  • B cell non Hodgkin lymphoma
  • CLL
  • rheumatoid arthritis
  • ITP
50
Q

trastuzumab–target

A
  • HER2/neu
    • HER2–“tras2zumab”
51
Q

trastuzumab–use

A
  • breast cancer
52
Q

name the therapeutic antibodies for autoimmune disease therapy

A
  • adalimumab, certolizumab, infliximab
  • eculizumab
  • natalizumab
53
Q

adalimumab, certolizumab, infliximab–target

A
  • soluble TNF alpha
54
Q

adalimumab, certolizumab, infliximab–use

A
  • IBD
  • rheumatoid arthritis
  • ankylosing spondylitis
  • psoriasis
55
Q

etanercept–type of drug

A
  • decoy TNF alpha receptor
  • not a monoclonal antibody
56
Q

eculizumab–target

A
  • complement protein C5
57
Q

eculizumab–use

A
  • paroxysmal nocturnal hemoglobinuria
58
Q

natalizumab–target

A
  • alpha 4 integrin
    • WBC adhesion
59
Q

natalizumab–use

A
  • multiple sclerosis
  • Crohn dz
60
Q

what are patients with JC virus at risk of if given natalizumab?

A
  • PML
61
Q

abciximab–target

A
  • platelet glycoprotein IIb/IIIa
    • ​“IIb times IIIa equals ‘absiximab’”
62
Q

abciximab–use

A
  • antiplatelet agent for prevention of ischemic complication in patients undergoing percutaneous coronary intervention
63
Q

denosumab–target

A
  • RANKL
    • denosumab affects osteoclasts
64
Q

denosumab–use

A
  • osteoporosis
  • inhibits osteoclast maturation
    • mimics osteoprotegerin
65
Q

digoxin immune Fab–target

A
  • digoxin
66
Q

digoxin immune Fab–use

A
  • antidote for digoxin toxicity
67
Q

omalizumab–target

A
  • IgE
68
Q

omalizumab–use

A
  • allergic asthma
  • prevents IgE binding to FcERI
69
Q

palivizumab–target

A
  • RSV F protein
70
Q

palivizumab–use

A
  • RSV prophylaxis for high risk infants
    • “palivizumab–virus”
71
Q

ranibizumab, bevacizumab–target

A
  • VEGF
72
Q

ranibizumab, bevacizumab–use

A
  • neovascular age related macular degeneration

PLAB Pharmacology (17 decks)

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