Immunosuppressants Exam 4

Question 1

What are immunesuppresants

Answer 1

Suppress the immune system

Question 2

What can they be used for?

Answer 2

Allergy
Autoimmune disease
Minimize risk of transplant rejection

Question 3

What are the 6 major classes of immunosuppressants?

Answer 3

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

Question 4

What is the ultimate role of corticosteroids?

Answer 4

suppress inflammation by blocking Arachidonic Acid

Question 5

2 Corticosteriods

Answer 5

Prednisone

Prednisolone

Question 6

What is the MOA for Calcineurin inhibitors?

Answer 6

suppress IL-2 production in T-lymphocytes

Question 7

What does calcineurin inhibit?

Answer 7

cNF-AT activation

Question 8

What is the overall goal of calcineurin inhibitor

Answer 8

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

Question 9

What is the MOA for mTOR inhibitors?

Answer 9

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

Question 10

2 Calcineurin inhibitors

Answer 10

Cyclosporine

Tacrolimus

Question 11

2 mTOR inhibitors

Answer 11

Sirolimus

Everolimus

Question 12

What would 2nd generation rapalogs prevent?

Answer 12

ATP binding at catalytic site

Question 13

What is the MOA of IMDH inhibitors

Answer 13

Blocks DNA synthesis, expansion of lymphocyte populations

Question 14

3 IMDH inhibitors

Answer 14

Azathioprine
Mycophenolate
Leflunomide

Question 15

Dx prevent graft versus host disease

Answer 15

Cyclosporine

Question 16

SDE unusual swelling of gums can occur

Answer 16

Cyclosporine

Question 17

Used when NSAIDs are ineffective

Answer 17

Biologics

Question 18

What should you be concern about when taking immunosuppressants?

Answer 18

secondary infections

Question 19

What are DMARDS

Answer 19

older, SMALL molecule, drugs

Question 20

What are 4 DMARDS dx

Answer 20

Methotrexate
Hydroxychloroquine
Leflunomide
Gold salts (Auranofin)

Question 21

What are Biologics

Answer 21

LARGER molecules of biologic origin

Question 22

How can you identify biologics?

Answer 22

-mab

Question 23

Drugs that bind tumor necrosis factor TNF-a

Answer 23

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

Question 24

Etanercept is a

Answer 24

fusion protein

Question 25

What are the 2 MOA for corticosteroids?

Answer 25

1) Increase expression of Lipocortin, inhibiting PLA2 | 2) Block expression of inflammatory (CO2, PLA2, cytokines)

Question 26

What is the ultimate goal of immunosuppressants?

Answer 26

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

Question 27

What is a weird side effect of Cyclosporine?

Answer 27

unusual swelling of gums

Question 28

What enzyme metabolizes Cyclosporine?

Answer 28

CYP3A4

Question 29

What enzyme metabolizes Tacrolimus?

Answer 29

CYP3A4 and CYP3A5

Question 30

What does block cNF-AT do?

Answer 30

block IL-2 production in T-lymphocytes

Question 31

What is mTOR inhibitors goals?

Answer 31

to prevent proteins from binding to mTOR and producing signaling

Question 32

What drug is used to coat coronary stents?

Answer 32

Sirolimus (mTOR inhibitor)

Question 33

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

Answer 33

Everolimus (mTOR inhibitor) and Leflunomide (IMDH inhibitor)

Question 34

What drug can be used for RA, Crohns, transplant

Answer 34

Azathioprine or mycophenolate

Question 35

What is the newest IMDH inhibitor?

Answer 35

Mycophenolate

Question 36

What does IMDH inhibit to block DNA synthesis?

Answer 36

Inosine monophosphate dehydrogenase

Question 37

WHO drug?

Answer 37

Azathioprine

Question 38

What does DMARD stand for?

Answer 38

Disease modifying anti-rheumatic drugs

Question 39

What are DMARD drug used for?

Answer 39

Rheumatoid arthritis

Question 40

What are some problems w/ Methotrexate?

Answer 40

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

Question 41

What is a alternate to Methotrexate?

Answer 41

Leflunomide

Question 42

What drug can cause severe immunosuppression?

Answer 42

Gold salts

Question 43

What enzyme does Methotrexate inhibit?

Answer 43

Al/CAR transformylase

Question 44

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

Answer 44

TNFa (monoclonal)

Question 45

What is the side effects of TNF-a monoclonals?

Answer 45

all increase risk of infection and reactivation of latent TB

Question 46

MOA of Tocilizumab (Actemara)

Answer 46

Blocks the IL-6 receptor

Question 47

T-cell costimulatory blocker

Answer 47

Abatacept (Orencia)

Question 48

MOA of Abatacept?

Answer 48

prevents t-cell from interfering w/ antigen

Question 49

IL-1 receptor antagonist

Answer 49

Anakinra (Kineret)

Question 50

MOA of Anakinra?

Answer 50

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

Question 51

JAK inhibitor

Answer 51

Tofacitinib (Xeljanz)

Question 52

B-cell depleter

Answer 52

Rituximab

Question 53

MOA of Tofacitinib

Answer 53

interferes with JAK2 cell signaling

Question 54

What drug causes neutropenia and raises cholesterol?

Answer 54

Tofacitinib (Xeljanz)

Question 55

MOA of Rituximab?

Answer 55

B-cell apoptosis

Question 56

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

Answer 56

Rituximab

Question 57

Used to treat allergic and atopic dermatitis in dogs?

Answer 57

Apoquel

Question 58

MOA of Basiliximab

Answer 58

Bind CD25 subunit of IL-2 receptor

Question 59

MOA of Moromonab

Answer 59

Bind to to CD3 receptor on T-lymphocytes