Regal- Anti-inflammatory Steroids and Immunosuppressives Flashcards Preview

IHO Week 6 > Regal- Anti-inflammatory Steroids and Immunosuppressives > Flashcards

Flashcards in Regal- Anti-inflammatory Steroids and Immunosuppressives Deck (34)
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1

What drugs are anti-inflammatory steroids (glucocorticoids)?

Cortisol
Hydrocortisone
prednisone
methylprednisone
betamethasone
desamethasone

2

What is the MOA of glucocorticoids?

Block steroid receptors that normally stimulate pathways that increase transcription of pro-inflammatory cytokines

• decrease COX2 expression (preferentially over COX 1)
•Inhibit AA release from phospholipids, affecting PG & LT formation
•Inhibit mast cell & basophil degranulation
•Inhibit synthesis & release of TNF (cachectin), IL-1, IL-2 & IFN → less immune cells circulating/functioning

3

How are glucocorticoids eliminated?

M: liver

E: renal

4

What toxicities are associated w/ glucocorticoids?

systemic therapy--> increased susceptibility to infections and OSTEOPOROSIS

5

What glucocorticoid has a short t 1/2?

Hydrocortisone

6

What glucocorticoids have intermediate t 1/2?

Prednisone
methylprednisone

7

What glucocorticoids have long t 1/2?

Betamethasone
Dexamethasone

8

What SE are associated w/ glucocorticoids?

•Peptic ulceration
•Behavioral disturbances
•Cataracts
•Inhibition of growth

Discontinuation of long term use → adrenal insufficiency (fever, myalgia, arthralgia, malaise, death d/t hypotension & shock)

9

What glucocorticoid is good for tx ITP, AHA, acute glomulonephritis, autoimmune disease ?

Prednisone

10

What glucocorticoids have the best anti-inflammatory properties?

Betamethasone
dexamethasone

11

What drugs are the three categories of immunosuppressive drugs?

calcineurin inhibtors
anti-proliferative
Abs

12

What drugs are calcineurin inhibitors?

cyclosporine
tacrolimus

13

What is the MOA of cyclosporine?

Binds cyclphillin to inhibit calcineuran phosphatase activity>
blocks cytokine gene expression and T cell activation

14

How is cyclosporine eliminated?

Extensive liver metabolism

15

What are the SE associated w/ cyclosporine?

drug interactions
nephrotoxicity (75% of pts)

16

What is the MOA of tacrolimus?

Binds FKBP to inhibit mTOR >
blocks cell cycle progression
(G1/S)

17

What SE are assoicated w/ tacrolimus?

nephrotoxicity

18

What drugs are anti-proliferative?

sirolimus (rapamycin)
mycophenolate mofetil

19

What is the MOA of siroliums?

Binds to FKBP to inhibit mTOR → blocks cell-cycle progression
(G1/S)

20

What are the SE of sirolimus?

Dose dependent increase in cholesterol and triglycerides
Nephrotoxicity w/ cyclosporine
CYP34A drug intrxns

21

What drug is used in combination therapy for organ transplant rejection?

sirolimus

22

What is the MOA of mycophenolate?

Inhibits IMPDH in de novo guanine nucleotide synth pathway → blocks B & T cell proliferation preferentially

23

What are the SE of mycophenolate?

Hematological : leukopenia

GI: diarrhea, vomiting

24

When is mycophenolate used?

organ transplant

25

What drugs are Abs?

anti-thymocyte globulin
muromonab-CD3
Daclizumab
Basiliximab

26

What is the MOA of ANti-thymocyte globulin?

Binds thymocytes in the circulation → lymphopenia & impaired T cell immune responses

27

What are the SE of anti-thymocyte globulin?

Serum sickness
Nephritis
Anaphylaxis rare

28

What is the MOA of muromonab CD-3?

Binds ε chain of CD3 of T-cells → TCR is internalized → prevents Ag recognition

29

What are the SE of muromonab CD-3?

Cytokine release syndrome: mild flu like illness to life-threatening shock

*Reduced w/ glucocorticoid admin 1st

30

How is muromonab CD-3 used?

to prevent Acute rejection of kidney, liver, heart transplants