Immunosuppressants Flashcards

1
Q

Gluocorticoids MOA

A

Genomic: Bind to cytosolic receptor and translocating to nucleus to bind to DNA
Non-genomic: Insert themselves into cell membrane, influence signaling pathways, etc.

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2
Q

Gluocorticoids MOA

A

Genomic: Bind to cytosolic receptor and translocating to nucleus to bind to DNA
Non-genomic: Insert themselves into cell membrane, influence signaling pathways, etc.

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3
Q

Glucocorticoid effects

A

Rapid decrease in peripheral lymphocytes
Decrease pro-inflammatory cytokines=> IL-1, IL-6, TNFa, Infy
Inhibit IL-2 production by T cells
Little effect on humoral immunity

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4
Q

Glucocorticoid therapeutic uses

A

Treat transplant rejection, usually co administered with something else
Treat graft vs host disease
Blocks first dose cytokine storm
Treat autoimmune disorders

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5
Q

Glucocorticoids adverse

A

Increased risk of infection
Poor wound healing
HTN
Adrenal crisis upon discontinuation

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6
Q

Low dose glucocorticoids

A
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7
Q

Medium dose glucocorticoids

A

> 7.5 mg, but

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8
Q

High dose glucocorticoids

A

> 30 mg, but

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9
Q

Glucocorticoids pulse therapy

A

> 250 mg prednisone equivalent per day for 1 day or a few days

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10
Q

Glucocorticoids pulse therapy

A

> 250 mg prednisone equivalent per day for 1 day or a few days

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11
Q

Glucocorticoid effects

A

Rapid decrease in peripheral lymphocytes
Decrease pro-inflammatory cytokines=> IL-1, IL-6, TNFa, Infy
Inhibit IL-2 production by T cells
Little effect on humoral immunity

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12
Q

Glucocorticoid therapeutic uses

A

Treat transplant rejection, usually co administered with something else
Treat graft vs host disease
Blocks first dose cytokine storm
Treat autoimmune disorders

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13
Q

Glucocorticoids adverse

A

Increased risk of infection
Poor wound healing
HTN
Adrenal crisis upon discontinuation

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14
Q

Low dose glucocorticoids

A
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15
Q

Medium dose glucocorticoids

A

> 7.5 mg, but

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16
Q

Azathrioprine class and MOA

A

Purine antimetabolite
Metabolized into 6-mercaptopurine->other metabolites, incorporated into DNA, inhibiting lymphocyte proliferation
Lymphocytes do not have a salvage pathway=>cannot compensate

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17
Q

Very high dose glucocorticoids

A

> 100 mg prednisone equivalent per day

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18
Q

Glucocorticoids pulse therapy

A

> 250 mg prednisone equivalent per day for 1 day or a few days

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19
Q

Cyclosporine class and MOA

A

Calcineurin inhibitor
Suppresses T-cell mediated immunity by forming a complex w/ cyclophilin=>binds to and inhibits calcineurin=>IL-2 (T cell growth factor) is not produced

20
Q

Cyclosporine uses

A

Very effective for prophylaxis for organ transplants, except for renal transplants b/c it is nephrotoxic

21
Q

Cyclosporine adverse

A
Renal dysfunciton
HTN
Hyperlipidemia 
Swollen/painful gums
Hirsutism 
Do not drink grapefruit juice
22
Q

Tacrolimus class and MOA

A

Calcineurin inhibitor

same MOA as cyclosporine

23
Q

Tacrolimus uses

A

Prophylaxis of allograft rejection in solid-organ transplantation

24
Q

Sirolimus adverse

A

Anemia/leukopenia/thrombocytopenia
hypokalemia
GI
Increased risk of infections

25
Q

Azathioprine class adn MOA

A

Purine antimetabolite
Metabolized into 6-mercaptopurine->other metabolites, inserts into DNA, inhibiting lymphocyte proliferation
Lymphocytes do not have a salvage pathway=>cannot compensate

26
Q

Azathriopine uses

A

Prevention of organ transplant rejection
Severe RA
Some autoimmune disorders

27
Q

Azathriopine adverse

A

Bone marrow suppression=> leukopenia
hepatotoxicity
Increased susceptibility to infections

28
Q

Mycophenolate Mofetil MOA

A

MMF is a prodrug, hydrolezed to MPA=>selective inhibitor of an enzyme required for synthesis of guanine =>destroys de novo pathway

29
Q

Mycophenolate Mofetil uses

A

Transplant rejection

Lupus

30
Q

Mycophenolate Mofetil adverse

A

leukopenia
Increased risk for CMV
Congenital abnormalities

31
Q

Sirolimus MOA

A

Inhibits T-lymphocyte proliferation, blocks G1-S phase transition

32
Q

Sirolimus Uses

A

Prophylaxis for organ transplant rejection

In renal transplant for pts who cannot tolerate calcineurin inhibitors

33
Q

Sirolimus adverse

A

Anemia/leukopenia/thrombocytopenia
hypokalemia
GI
Increased risk of infections

34
Q

Antithymocyte Globulin MOA

A

Contains antibodies from a rabbit that binds to things like CD3 (and much more CDs) to deplete human T lymphocytes

35
Q

Antithymocyte Globulin uses

A

Induction immunosuppression

Tx of acute reaction of solid organ transplants

36
Q

Antithymocyte Adverse

A

fevers, chills, malaise, hypotension due to release of cytokines (TNF-a)=> cytokine storm
Serum sickness

37
Q

Murononab-CD3 MOA

A

Mouse antibody directed against CD3=> cause depletion of T lymphocytes

38
Q

Muromonab-CD3 uses

A

Reverse glucocorticoid resistant organ transplant rejection episodes
Can only use this drug once!!

39
Q

Muomonab-CD3 adverse

A

cytokine storm

tremor, nausea, weakness

40
Q

Anti-TNFa reagants

A

Infliximab, adalimumab, and etanercept

41
Q

Anti-TNFa MOA

A

prevents TNFa form binding to its receptors by binding to it directly

42
Q

Infliximab

A

Monoclonal antibody that is part human and part murine (mouse)

43
Q

Adalimumab

A

Recombinant human IgG1 monoclonal antibody

44
Q

Etanercept

A

Part TNF-a receptor and part portion of human IgG1

45
Q

Anti-TNFa uses

A

RA
Crohn’s
UC, spondylitis, etc

46
Q

Anti-TNFa adverse

A

Increased risk for infections, lymphomas, and other malignancies