immunosuppressants Flashcards Preview

Year 2 Pharmacology > immunosuppressants > Flashcards

Flashcards in immunosuppressants Deck (43):
1

what are the indications for immunosuppressants?

transplantation - prophylaxis and acute rejection
autoimmune
inflammatory diseases

2

what are the major classes of immunosuppressive agents?

glucocorticoids
calcineurin inhibitors
antiproliferative / antimetabolic agents
biologicals

3

what are the adverse effects of immunosuppressive agents?

infectious disease
malignancy

4

what are the calcineurin inhibitors?

cyclosporine
tacrolimus

5

what are the antiproliferative / antimetabolic agents?

azathioprine
mycophenolate mofenil
sirolimus

6

what are the biological immunosuppressants?

antithymocyte globulin
muromonab-CD3
anti-TNFa

7

what are the general effects of glucocorticoids?

genomic - up to 1% of DNA influence via cytosolic receptors, inhibition of transcription factors

non-genomic - cell signaling pathways, cell membrane

8

what are the key specific effects of glucocorticoids?

1. downregulation of proinflammatory cytokines (IL-1, IL-6)
2. inhibit IL-2 (anti-T cell proliferation)
3. decrease in peripheral WBCs
4. reduce neutrophil chemotaxis

9

what are the adverse effects of glucocorticoids?

growth retardation
increased risk of infection
poor wound healing
hypertension
avascular necrosis of bone
cataracts
hyperglycemia
adrenal crisis upon rapid discontinuation

10

what is considered a low dose of glucocorticoid?

below 7.5 mg prednisone equivalent per day

11

what is considered a medium dose of glucocorticoid?

7.5 - 30 mg prednisone equivalent per day

12

what is considered a high dose of glucocorticoid?

30 - 100 mg prednisone equivalent per day

13

what is considered a very high dose of glucocorticoid?

over 100 mg prednisone equivalent per day

14

what is considered pulse therapy for glucocorticoid?

over 250 mg per day for 1 day or a few days

15

what drug is the standard for glucocorticoid dosing regimens?

prednisone

16

what is the MOA of cyclosporine?

1. suppresses T cell immunity
2. forms complex with cyclophilin, which then binds to calcineurin and eventually leads to prevention of transcription and translation of certain cytokines

17

what is the main adverse toxicity associated with cyclosporine?

nephrotoxicity

18

what is the preferred calcineurin inhibitor for transplantation due to ease of blood level monitoring?

tacrolimus

19

what is the main therapeutic use for tacrolimus?

prophylaxis of allograft rejection in solid organ transplantation

20

what are the main adverse effects of tacrolimus?

nephrotoxicity
HTN
diabetes
grapefruit

21

what is the MOA of azathioprine?

1. metabolized to 6-mercaptopurine
2. metabolites incorporated into DNA
3. inhibition of lymphocyte proliferation (lymphocytes do not have a salvage pathway)

22

what are the adverse reactions of azathioprine?

bone marrow suppression
hepatotoxicity
VZV, HSV

23

what is the MOA of mycophenolate mofetil?

1. knock out de novo synthesis of guanine nts
2. inhibits lymphocyte proliferation

24

what are the therapeutic uses for mycophenolate mofetil?

propylaxis for graft rejection
SLE

25

what are the adverse reactions of mycophenolate mofetil?

hematologic
GI
contraindicated for pregnancy

26

what is the MOA of sirolimus?

inhibits T cell proliferation via prevation of mTOR activation

27

what drug has allowed combination use with cyclosporine and tacrolimus?

sirolimus

28

what is the main therapeutic use of sirolimus?

renal transplant patients that cant tolerate calcineurin inhibitors due to high-risk nephrotoxicity

29

what is the MOA of antithymocyte globulin?

1. antibodies that bind to CDs (especially CD3) and HLAs on T cells
2. depletion of circulating T cells via a) complement cytotoxicity and b) prevention of T cell activation

30

what is the MOA of muromonab CD3?

anti-CD3 antibodies cause depletion of T cells

31

what is the main therapeutic use of muromoab CD3?

reversal of glucocorticoid resistant organ transplant rejection episodes

32

what is the main adverse reaction of muromonab CD3?

cytokine storm

33

what is the MOA of the anti-TNFa reagents?

binds directly and prevents TNFa from binding to its receptors

34

what are the anti-TNFa agents?

infliximab
adalimumab
etanercept

35

what are the therapeutic uses of the anti-TNFa agents?

RA
IBD

36

what class of drug is cyclosporine?

calcineurin inhibitor

37

what class of drug is tacrolimus?

calcineurin inhibitor

38

what class of drug is azathioprine?

antiproliferative / antimetabolite

39

what class of drug is mycophenolate mofenil?

antiproliferative / antimetabolite

40

what class of drug is sirolimus?

antiproliferative / antimetabolite

41

what class of drug is antithymocyte globulin?

biologic

42

what class of drug is muromonab-CD3?

biologic

43

what class of drug is anti-TNFa?

biologic

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