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LECOM pharmacology notecards > chapter 45- Immunosuppression > Flashcards

chapter 45- Immunosuppression Flashcards

1
Q

what drugs have the mechanism of action of inhibitor of IMPDH, the rate limiting enzyme in formation of guanosine

A

Mycophenolic acid, mycophenolate, mofetil, mycophenolate sodium

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2
Q

what is the clinical application of mycophenolic acid

A

solid organ transplantation, lupus nephritis, rheumatoid arthritis, pemphigus

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3
Q

what are the adverse effects of mycophenolic acid

A

HTN, peripheral edema, GI hemorrhage, leukopenia, myelosuppression

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4
Q

what cells does mycophenolic acid ac on

A

primarily on lymphocytes

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5
Q

what should you avoid concurrent admin of with use of mycophenolate mofetil

A

iron because it markedly reduces its bioavailability

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6
Q

what is the clinical application of leflunomide

A

rheumatoid arthritis

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7
Q

what are common adverse effects seen with leflunomide

A

interstitial lung disease, alopecia, diarrhea, rash

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8
Q

what is a contraindication for leflunomide use

A

pregnancy

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9
Q

what can be administered if you need rapid removal of leflunomide

A

cholestyramine

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10
Q

what does leflunomide inhibit

A

dihydroorate dehydrogenase (DHOD)

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11
Q

what does the leflunomide lead to the inhibition of

A

pyrimidine synthesis

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12
Q

what is the clinical application of cyclosporine

A

keratoconjunctivitis (topical)

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13
Q

what is the mechanism of action of cyclosporine

A

binds to cyclophilin, the resulting complex inhibits the phosphatase activity of calcineurin (involved in T cell activation)

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14
Q

what interleukin does cyclosporine inhibition the production of

A

IL-2

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15
Q

what drug can increase serum levels of cyclosporine

A

danazol and other androgens

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16
Q

what can reduce serum cyclosporine level

A

Rifampin and St Jonns wort

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17
Q

what are some adverse effects seen with cyclosporine

A

nephrotoxicity, HTN, neurotoxicity, hepatotoxicity, gingival hyperplasia, hirsutism

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18
Q

what is a contraindication of topical cyclosporine use

A

active ocular infection

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19
Q

what is the clinical application of tacrolimus

A

organ transplantation, atopic dermatitis

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20
Q

what are some adverse effects with tacrolimus

A

nephrotoxicity, prolonged QT interval, lymphoma, alopecia, headache

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21
Q

what is a contraindication for tacrolimus use

A

hypersensitivity to hydrogenated castor oil

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22
Q

what is the mechanism of action of tacrolimus

A

binds to FK-binding protein (FKBP), which inhibits calcineurin

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23
Q

what markedly reduces serum levels of tacrolimus

A

St. John’s Wort

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24
Q

what is the clinical application of sirolimus

A

prophylaxis for renal transplant rejection; CAD (cardiac stents)

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25
Q

what is the clinical application of everolimus

A

renal cell carcinoma; CAD (cardiac stents)

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26
Q

what are some adverse effects of sirolimus/everolimus use

A

thrombocytopenia, thrombotic microangiopathy, hyperlipidemia

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27
Q

what is the mechanism of action of sirolimus/everolimus

A

inhibition mTOR

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28
Q

what is the mechanism of action of etanercept

A

soluble TNF receptor dimer

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29
Q

what is the clinical application of etanercept

A

rheumatoid arthritis, juvenile idiopathic arthritis, plaque psoriasis, psoriatic arthritis, ankylosing spondylitis

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30
Q

what must people undergo screening for before using etanercept

A

TB

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31
Q

what are contraindications for etanercept use

A

sepsis, HF

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32
Q

what is the mechanism of action of infliximab

A

monoclonal anti-TNF antibodies

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33
Q

what monoclonal anti-TNF antibody can be used to treat juvenile idiopathic arthritis

A

adalimmumab

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34
Q

what monoclonal anti-TNF antibody can be used to treat ulcerative colitis

A

infliximab

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35
Q

what is the major difference between infliximab, adalimumab/golumumab, and certolizumab

A

inf is a partially humanized mouse antibody against human TNF-alpha; adal/gol are fully human IgG antibodies against TNF-alpha; cert is a pegylated anti-TNF-alpha antibody fragment

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36
Q

what is the mechanism of action of ustekinumab

A

human IgG monoclonal antibody that binds the p40 protein subunit shared by Il-12 and IL-23

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37
Q

what is the clinical application of ustekinumab

A

plaque psoriasis

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38
Q

what are some adverse rxns with ustekinumab

A

increased risk of infection, reversible posterior leukoencephalopathy syndrome

39
Q

how is ustekinumab administered

A

after initial loading dose, ustekinumab is admin subcutaneously every 3 months

40
Q

what is the mechanism of action of anakinra

A

recombinant IL-1 receptor antagonist

41
Q

what is the clinical application of anakinra

A

rheumatoid arthritis

42
Q

what are some adverse effects seen with anakinra

A

neutropenia, increased risk of infection

43
Q

what does anakinra significantly reduce

A

bony erosions, possibly by decreasing metalloproteinase release by synovial cells

44
Q

what is the clinical application of rilonacept and canakinumab

A

cryopyrin-associated periodic fever syndrome (familial cold auto inflammatory syndrome and muckle-wells syndrome

45
Q

what is the clinical application of tocilizumab

A

rheumatoid arthritis

46
Q

what is the clinical application of antithymocyte globulin

A

renal transplantation, aplastic anemia

47
Q

what is the clinical application of OKT3

A

organ transplantation

48
Q

what is the mechanism of action of rilonacept

A

recombinant soluble IL-1 receptor Fc fusion protein

49
Q

what is the mechanism of action of canakinumab

A

human IgG1 monoclonal antibody to IL-1beta

50
Q

what is the mechanism of action of tocilizumab

A

recombinant humanized monoclonal antibody to IL-6 receptor

51
Q

what is the mechanism of action of antithymocyte globulin

A

polyclonal rabbit or horse antibodies against human T-cell epitopes

52
Q

what is the mechanism of action of OKT3

A

mouse monoclonal antibody against human CD3

53
Q

what are some adverse rxns seen with rilonacept and canakinumab use

A

serious infection; infection site reaction and URIs

54
Q

what administrations should be avoided with rilonacept and canakinumab use

A

patients with active, recurring or chronic infections; admin of live vaccines

55
Q

what are some adverse rxns seen with tocilzumab

A

serious infections, GI perforation

56
Q

how is tocilizumab administered

A

every 4 weeks as IV infusion

57
Q

what are some adverse rxns seen with antithymocyte globulin

A

cytokine release syndrome, HTN, increased risk of infection

58
Q

what is the cytokine release syndrome

A

fever, shaking chills, myalgia, headache

59
Q

what are some adverse rxns seen with OKT3

A

can result in profound immunosuppression

60
Q

what are some contraindications for antithymocyte globulin use

A

acute viral illness, history of allergy or anaphylaxis to rabbit or horse proteins

61
Q

what are some contraindications for OKT3

A

heart failure, seizures, pregnancy/breastfeeding, uncontrolled HTN

62
Q

what is the mechanism of action of rituximab

A

partially humanized anti-CD20 antibody

63
Q

what is the mechanism of action of ofatumumab

A

fully human anti-CD20 antibody

64
Q

what is the mechanism of action of daclizumab, basiliximab

A

antibodies to CD25, the high affinity IL-2 receptor

65
Q

what is the mechanism of action of alemtuzumab

A

antibody to campath-1 (CD52), an antigen expressed on most mature lymphocytes and some lymphocyte precursors

66
Q

what is the mechanism of action of alefacept

A

LFA-3/Fc fusion protein that interrupts CD2/LFA-3 signaling by binding to T-cell CD-2, leaving to inhibitor of T-cell activation

67
Q

what is the mechanism of action of abatacept and belatecept

A

CTLA-4 analogues fused to an IgG1 constant region

68
Q

what is the mechanism of action of natalizumab

A

monoclonal antibody against alpha-4 intern that inhibits immune cell interaction with cells expressing VCAM-1 and MadCAM-1

69
Q

what is the mechanism of action of eculizumab

A

humanized antibody against C5, a complement protein that mediates late steps in complement activation and assembly of the MAC

70
Q

what is the clinical application of rituximab

A

B-cell non-hodgkin lymphoma, RA, chronic lymphocytic leukemia

71
Q

what is the clinical application of daclizumab, basiliximab

A

organ transplantation; prophylactic in renal transplant

72
Q

what is the clinical application of alemtuzumab

A

B cell chronic lymphocytic leukemia

73
Q

what are contraindications for alemtuzumab use

A

active systemic infection; underlying immunodeficiency

74
Q

what is the clinical application of alefacept

75
Q

what are some contraindications for alefacept use

A

HIV infection; low CD4-T cell count

76
Q

what is the clinical application of abatacept

A

rheumatoid arthritis refractory to methotrexate or TNF-alpha inhibitors

77
Q

what are some adverse effects seen with abatacept use

A

exacerbation of COPD, increased susceptibility to infection, nausea

78
Q

what drugs should abatacept not be administered concurrently with

A

TNF-alpha inhibitors or anakinra

79
Q

what is the clinical application of natalizumab

A

relapsing MS, crohn’s disease

80
Q

what is the clinical application of eculizumab

A

paroxysmal nocturnal hemoglobulinuria

81
Q

what are some adverse reactions seen with natalizumab use

A

progressive multifocal leukoencephalopathy, depression, pneumonia

82
Q

what are some contraindications for natalizumab use

A

history of PML

83
Q

what are some adverse reactions seen witheculizumab usei

A

infections; headache, nasopharyngitis, back pain, nausea

84
Q

what are some contraindications for eculizumab use

A

neisseria meningitides infection

85
Q

what do all patients who discontinue eculizumab need to be monitored for

A

signs and symptoms of intravascular hemolysis, including eval for serum lactate dehydrogenase levels

86
Q

What is the autoantigen seen in acute rheumatic fever

A

Streptococcal cell wall antigens that cross reaction with cardiac muscle

87
Q

What is the autoantigen seen in autoimmune hemolytic anemia

A

Rh blood group antigens

88
Q

What is the autoantigen seen in goodpasture’s syndrome

A

Renal glomerular basement membrane collagen type 4

89
Q

What is the autoantigen seen in immune thrombocytopenic purpura

A

Platelet GPIIB-IIIa

90
Q

What is the autoantigen seen in mixed essential cryoglobulinemia

A

Rheumatoid factor IgG complexes

91
Q

What is the autoantigen seen in SLE

A

DNA, histones, ribosomes, snRNP, scRNP

92
Q

What is the autoantigen seen in experimental autoimmune encephalitis, MS

A

Myelin basic protein, proteolipid protein, myelin oligodendrocyte glycoprotein

93
Q

What is the autoantigen seen in type 1 DM

A

Pancreatic beta cell antigens

LECOM pharmacology notecards (22 decks)

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