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

Regal- Anti-inflammatory Steroids and Immunosuppressives Flashcards

1
Q

What drugs are anti-inflammatory steroids (glucocorticoids)?

A 
Cortisol
Hydrocortisone
prednisone
methylprednisone
betamethasone
desamethasone
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2
Q

What is the MOA of glucocorticoids?

A

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
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3
Q

How are glucocorticoids eliminated?

A

M: liver

E: renal

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4
Q

What toxicities are associated w/ glucocorticoids?

A

systemic therapy–> increased susceptibility to infections and OSTEOPOROSIS

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5
Q

What glucocorticoid has a short t 1/2?

A

Hydrocortisone

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6
Q

What glucocorticoids have intermediate t 1/2?

A

Prednisone

methylprednisone

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7
Q

What glucocorticoids have long t 1/2?

A

Betamethasone

Dexamethasone

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8
Q

What SE are associated w/ glucocorticoids?

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

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

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9
Q

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

A

Prednisone

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10
Q

What glucocorticoids have the best anti-inflammatory properties?

A

Betamethasone

dexamethasone

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11
Q

What drugs are the three categories of immunosuppressive drugs?

A

calcineurin inhibtors
anti-proliferative
Abs

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12
Q

What drugs are calcineurin inhibitors?

A

cyclosporine

tacrolimus

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13
Q

What is the MOA of cyclosporine?

A

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

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14
Q

How is cyclosporine eliminated?

A

Extensive liver metabolism

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15
Q

What are the SE associated w/ cyclosporine?

A

drug interactions

nephrotoxicity (75% of pts)

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16
Q

What is the MOA of tacrolimus?

A

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

17
Q

What SE are assoicated w/ tacrolimus?

A

nephrotoxicity

18
Q

What drugs are anti-proliferative?

A

sirolimus (rapamycin)

mycophenolate mofetil

19
Q

What is the MOA of siroliums?

A

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

20
Q

What are the SE of sirolimus?

A

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

21
Q

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

A

sirolimus

22
Q

What is the MOA of mycophenolate?

A

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

23
Q

What are the SE of mycophenolate?

A

Hematological : leukopenia

GI: diarrhea, vomiting

24
Q

When is mycophenolate used?

A

organ transplant

25
Q

What drugs are Abs?

A

anti-thymocyte globulin
muromonab-CD3
Daclizumab
Basiliximab

26
Q

What is the MOA of ANti-thymocyte globulin?

A

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

27
Q

What are the SE of anti-thymocyte globulin?

A

Serum sickness
Nephritis
Anaphylaxis rare

28
Q

What is the MOA of muromonab CD-3?

A

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

29
Q

What are the SE of muromonab CD-3?

A

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

*Reduced w/ glucocorticoid admin 1st

30
Q

How is muromonab CD-3 used?

A

to prevent Acute rejection of kidney, liver, heart transplants

31
Q

What is the MOA of daclizumab and basiliximab?

A

Anti- IL-2 receptor (CD25) → block IL-2 mediated T-cell activation events

32
Q

What are the SE of Daclizumab and basiliximab?

A

NO cytokine release syndrome

Anaphylaxis

33
Q

What drugs are commonly used in organ transplantation?

A

Daclizumab

Basiliximab

34
Q

Which drugs have a lower incidence of lymphoproliderative disorders & opportunistic infections than most other immunosuppressant drugs?

A

Daclizumab

Basiliximab

IHO Week 6 (14 decks)

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