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Pharmacology 2 > Immunosuppressants Exam 4 > Flashcards

Immunosuppressants Exam 4 Flashcards

1
Q

What are immunesuppresants

A

Suppress the immune system

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2
Q

What can they be used for?

A

Allergy
Autoimmune disease
Minimize risk of transplant rejection

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3
Q

What are the 6 major classes of immunosuppressants?

A
  1. Corticosteroids
  2. Calcineurin Inhibitors
  3. mTOR inhibitors
  4. IMDH (inosine monophosphate dehydrogenase) inhibitors
  5. Biologics
  6. Monoclonal antibodies
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4
Q

What is the ultimate role of corticosteroids?

A

suppress inflammation by blocking Arachidonic Acid

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5
Q

2 Corticosteriods

A

Prednisone

Prednisolone

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6
Q

What is the MOA for Calcineurin inhibitors?

A

suppress IL-2 production in T-lymphocytes

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7
Q

What does calcineurin inhibit?

A

cNF-AT activation

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8
Q

What is the overall goal of calcineurin inhibitor

A

block cell ability to activate transcription factor (cNF-AT)

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9
Q

What is the MOA for mTOR inhibitors?

A

Suppress intracellular signaling pathway (mTOR) important for
cell growth and proliferation of T-lymphocytes

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10
Q

2 Calcineurin inhibitors

A

Cyclosporine

Tacrolimus

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11
Q

2 mTOR inhibitors

A

Sirolimus

Everolimus

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12
Q

What would 2nd generation rapalogs prevent?

A

ATP binding at catalytic site

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13
Q

What is the MOA of IMDH inhibitors

A

Blocks DNA synthesis, expansion of lymphocyte populations

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14
Q

3 IMDH inhibitors

A

Azathioprine
Mycophenolate
Leflunomide

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15
Q

Dx prevent graft versus host disease

A

Cyclosporine

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16
Q

SDE unusual swelling of gums can occur

A

Cyclosporine

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17
Q

Used when NSAIDs are ineffective

A

Biologics

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18
Q

What should you be concern about when taking immunosuppressants?

A

secondary infections

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19
Q

What are DMARDS

A

older, SMALL molecule, drugs

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20
Q

What are 4 DMARDS dx

A

Methotrexate
Hydroxychloroquine
Leflunomide
Gold salts (Auranofin)

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21
Q

What are Biologics

A

LARGER molecules of biologic origin

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22
Q

How can you identify biologics?

A

-mab

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23
Q

Drugs that bind tumor necrosis factor TNF-a

A 
Etanercept (Enbrel)
Indliximab (remicade) 
Adalimumab (humira)
Certolizimab (Cimiza)
Golimumab (Simponi)
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24
Q

Etanercept is a

A

fusion protein

25
Q

What are the 2 MOA for corticosteroids?

A

1) Increase expression of Lipocortin, inhibiting PLA2

2) Block expression of inflammatory (CO2, PLA2, cytokines)

26
Q

What is the ultimate goal of immunosuppressants?

A

to block T-lymphocytes keep them from recruiting other cells (B cells)

27
Q

What is a weird side effect of Cyclosporine?

A

unusual swelling of gums

28
Q

What enzyme metabolizes Cyclosporine?

A

CYP3A4

29
Q

What enzyme metabolizes Tacrolimus?

A

CYP3A4 and CYP3A5

30
Q

What does block cNF-AT do?

A

block IL-2 production in T-lymphocytes

31
Q

What is mTOR inhibitors goals?

A

to prevent proteins from binding to mTOR and producing signaling

32
Q

What drug is used to coat coronary stents?

A

Sirolimus (mTOR inhibitor)

33
Q

Which is drug is used for chemotherapy in HER2 negative breast cancer?

A

Everolimus (mTOR inhibitor) and Leflunomide (IMDH inhibitor)

34
Q

What drug can be used for RA, Crohns, transplant

A

Azathioprine or mycophenolate

35
Q

What is the newest IMDH inhibitor?

A

Mycophenolate

36
Q

What does IMDH inhibit to block DNA synthesis?

A

Inosine monophosphate dehydrogenase

37
Q

WHO drug?

A

Azathioprine

38
Q

What does DMARD stand for?

A

Disease modifying anti-rheumatic drugs

39
Q

What are DMARD drug used for?

A

Rheumatoid arthritis

40
Q

What are some problems w/ Methotrexate?

A
  • Not tolerated well (due to sde)
  • Frequent liver check (fibrosis/ cirrhosis)
  • Immunosuppression, stomatitis, hepatic dysfunction
  • Known TERATOGENIC (X)
  • Interferes w/ folic acid
  • Cause neutropenia
41
Q

What is a alternate to Methotrexate?

A

Leflunomide

42
Q

What drug can cause severe immunosuppression?

A

Gold salts

43
Q

What enzyme does Methotrexate inhibit?

A

Al/CAR transformylase

44
Q

What drugs are used for psoriasis, psoriatic arthritis, ankylosing spondylitis, and Crohns disease?

A

TNFa (monoclonal)

45
Q

What is the side effects of TNF-a monoclonals?

A

all increase risk of infection and reactivation of latent TB

46
Q

MOA of Tocilizumab (Actemara)

A

Blocks the IL-6 receptor

47
Q

T-cell costimulatory blocker

A

Abatacept (Orencia)

48
Q

MOA of Abatacept?

A

prevents t-cell from interfering w/ antigen

49
Q

IL-1 receptor antagonist

A

Anakinra (Kineret)

50
Q

MOA of Anakinra?

A

up regulates endogenous IL-1 antagonist, thus blocking IL-1 (pro-inflammatory cytokine)

51
Q

JAK inhibitor

A

Tofacitinib (Xeljanz)

52
Q

B-cell depleter

A

Rituximab

53
Q

MOA of Tofacitinib

A

interferes with JAK2 cell signaling

54
Q

What drug causes neutropenia and raises cholesterol?

A

Tofacitinib (Xeljanz)

55
Q

MOA of Rituximab?

A

B-cell apoptosis

56
Q

What drug cause increased risk of infection and reactivation of viral infections?

A

Rituximab

57
Q

Used to treat allergic and atopic dermatitis in dogs?

A

Apoquel

58
Q

MOA of Basiliximab

A

Bind CD25 subunit of IL-2 receptor

59
Q

MOA of Moromonab

A

Bind to to CD3 receptor on T-lymphocytes

Pharmacology 2 (9 decks)

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