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Flashcards in Immunpharmacology Deck (51)
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1

Time for development of primary immune response...

 

Activation of T cells and AB production takes...

8-14d

 

1-3d

2

Basophils release...

  1. histamine
  2. bradykinin
  3. serotonin
  4. heparin
  5. SRSA

3

Immunosuppressants generally work better for______

primary immune response

4

Acute rejection is mainly mediated by ____ and ___

T cells and cytokines

5

Three routes of immunosuppression

  1. Decrease amount of lymphocyte
  2. Divert lymphocyte traffic
  3. Block pathways involved in lymphocytic response

6

6 catergories of immunosuppressants

  1. regulators of gene expression
  2. alkylating agents
  3. inhibitors of de novo pyrimidine synth
  4. inhibitors of de novo purine synth
  5. Kinase phosphatase inhibitors
  6. Protein immunosuppressive drugs

7

Adrenocortical steroid MOA (3)

  • reduce levels of lymphocytes
  • Block  antigen presentation pathway
  • Inhibit IL-2 gene transcription whih is needed for B and T cell clonal expansion

8

Example of alkylating agent

cyclophosphamide (cytotoxic)

9

Examples of first and second generation inhibitors of de novo purine synthesis

1st gen = AZT + 6-Mercaptopurine

2nd Gen = mizoribine + mycophenolate mofetil

10

What is MMF

inosine 5-MP dehydrogenase inhibitor

11

Methotrexate and polygentamate derivatives also belong to which class of drugs?

Purine synthesis inhibitors

12

Alkylating agents and Purine synthesis inhibitors -- how to they induce/maintain immunosuppression

Block DNA/RNA synth

Prevent clonal expansion of B/T cells

13

Examples of Pyrimidine inhibitors

 

What is the MOA?

  • Brequinar
  • Leflunomide
  • malononitrilomides

 

inhibit dihydroorotate dehydrogenase

14

Kinase and phosphatase inhibitor drugs

Cyclosporine and tacrolimus

15

Cyclosporine concentrates in _____

It is given ___ prior to ____

 

**MOA?**

Red/white cells

give 4-24h before transplant

 

Inhibits the phosphatase activity of calcineurin

= prevents NFAT translocation

**also blocks JNK and p38 signaling

16

Tacrolimus category and MOA

macrolide

binds to FK506-BP 12

= inhibits the phosphatase activity of calcineurin

17

Sirolimus MOA

 

What is unique?

Binds FKBP12

(same as tacrolimus)

Complex formation with FKBP12 does not inhibit IL-2 production

18

Antilymphocyte globulins (protein immunosuppressives)

muromonab-CD3

Daclizumab

Basiliximab

19

AntiCD25 mAb's

Daclizumab and Basiliximab

20

Anti CD3 mAb that binds to TCR-associated CD3 complex and alters T cells

Muromonab

21

RA and Hemolyitc Anemia are diseases that involves overexpression of _____

They would benefit from _____

CD20

 

Anti CD20 mAb's (which are difficult to make beacuse of CD20's short extramembrane domain)

22

Belatacept is a _________

Its MOA?

"co-stimulatory blocker"

 

Inhibits CD28-mediated costimulation by binding to CD80 and CD86 --> blocking engagement of CD28 on T cells

23

Use of beletacept is associated with

serious side effects in children

24

Selective targeting of ___ rather than ___ may be more effetive to control post-transplant immune responses

CD28 rather than CD80/86

25

Rapamycin is a _____ that targets _____

macrocyclic lactone

mTOR (regulator of proliferation)

26

Rapamycin is generally replaced by ____

everolimus

27

Everolimus is being tried in patients with ______

renal insufficiency or neoplasia

28

Fingolimod is structurally related to ____

Function?

Myricin (sphingosine analog)

Drives lymphocytes into lymphoid tissue (reducing the number of circulating T cells)

29

TNFa inhibitor

 

Used for?

certolizumab pegol

 

RA

30

Three antibody mediated diseases

AI-mediated Hemolytic Anemia

M.Gravis

Hypoadrenocorticism