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Immunosuppressants Flashcards

(52 cards)

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1
Q

What are the three general uses of immunosuppressants?

A

transplantations
Autoimmune diseases
Inflammatory diseases

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2
Q

What are grafts between identical twins called?

A

Isografts

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3
Q

What are allografts?

A

Grafts from other people

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4
Q

True or false: you can never truly induce remission of autoimmune diseases with immunosuppressants?

A

False

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5
Q

What are the four major classes of Immunosuppressants?

A
  • Glucocorticoids
  • Calcineurin inhibitors
  • Anti-proliferative/antimetabolic agents
  • biologicals
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6
Q

Malignancies with immunosuppressants usually have what etiology?

A

Latent viral infections

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7
Q

What are steroids, technically?

A

Compounds with a common ring structure

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8
Q

What are corticosteroids, technically?

A

Adrenal cortex steroids

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9
Q

What are the two major MOAs of glucocorticoids?

A

Genomic

Non-genomic

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10
Q

What are the genomic effects of glucocorticoids?

A

Binds to a cytosolic receptor, and translocates to the DNA (1% of genome) to alter transcription/translation

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11
Q

What are the non-genomic effects of glucocorticoids?

A

Can influence cell signalling pathways and intercalate into the cell membrane to alter ion transport

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12
Q

What are the effects of glucocorticoids?

A
  • Rapid decrease in peripheral blood lymphocyte

- Downregulate IL-1, IL-6, IFN-g, TNF-a

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13
Q

What is the function of IL-2?

A

T cell proliferation

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14
Q

What is the effect of glucocorticoids on PMNs?

A

reduce chemotaxis and lysosomal enzyme release

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15
Q

What is the effect of glucocorticoids on humoral immunity?

A

Little

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16
Q

What is the effect of CD3?

A

***Cytokine storm

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17
Q

What are the adverse effects of glucocorticoids?

A

Growth retardation
Impaired wound healing
HTN
Hyperglycemia

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18
Q

Rapid withdrawal of glucocorticoids may result in what?

A

Glucocorticoid crisis

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19
Q

What is low, medium, high, and very high doses of glucocorticoids?

A

Low = (0, 7.5] mg
Med = (7.5, 30]
High = (30, 100]
Very high = (100, 250]

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20
Q

What is the half-life of prednisone?

A

5 hours (intermediate)

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21
Q

What are the two, short acting glucocorticoids?

Study These Flashcards
A

Cortisone

Hydrocortisone

22
Q

What are the four intermediate acting glucocorticoids?

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A

Prednisone
Prednisolone
Methylprednisolone
Triamcinolone

23
Q

What are the two long acting glucocorticoids?

Study These Flashcards
A

Dexamethasone

Betamethasone

24
Q

What is pulse therapy with glucocorticoid use?

Study These Flashcards
A

Greater than 250 mg of prednisone for 1 day

25
What is the MOA of cyclosporine?
Suppress T cell-mediated immunity by forming a complex with cyclophilin, and prevent dephosphorylation of NFAT
26
What is the transcription factor that cyclosporine suppresses? What does this produce?
NFAT--leads to IL-2 production
27
What is the function of IL-12?
Th1 cell production
28
What is the function of IL-4?
Th2 cell production
29
What are the therapeutic uses for cyclosporine? Side effects?
Prophylaxis for kidney transplant, RA Nephrotoxic, HTN, Hirsutism
30
What is the effect of grapefruit juice on cyclosporine? Tacrolimus?
Inhibits p450 enzyme, causing an increase in cyclosporine and tacrolimus
31
What is the MOA of tacrolimus? What are the therapeutic uses? Side effects?
calcineurin inhibitor, preventing NFAT phosphorylation Prophylaxis of allograft rejection Nephro/neurotoxic, HTN, DM,
32
What is the MOA of Azathioprine?
Purine antimetabolite that is metabolized to 6-mercaptopurine to inhibit lymphocyte proliferation
33
What are the two purines?
A | G
34
Why is it that most cells can overcome Azathioprine actions, but lymphocytes cannot?
Lymphocytes do not have a salvage pathway
35
What are the therapeutic uses of Azathioprine? Adverse effects?
Organ transplant rejection RA Myelosuppression Hepatotoxic
36
Azathioprine increases that susceptibility to what viral infections?
Varicella | HSVs
37
What is the MOA of Mycophenolate Mofetil?
Prodrug that is hydrolyzed to MPA, which inhibits inosine monophosphate dehydrogenase, which is required for the synthesis of guanine. Inhibits T and B cells
38
What are the therapeutic uses, and side effects of mycophenolate?
Transplant rejection SLE CMV infections Teratogenic Leukopenia
39
What is the MOA of sirolimus?
Inhibits T lymph proliferation by binding to FKBP (same as tacrolimus), to inhibit mTOR, and cell cycle progression
40
What are the therapeutic uses, and side effects of sirolimus?
Renal transplant Anemia Hypokalemia
41
What is Antithymocyte globulin?
rabbit serum antibodies against human thymocytes
42
What is the CD protein that all T cells express?
CD3
43
What are the two mechanisms that Antithymocyte globulin uses to destroy thymocytes?
Complement mediated cytotoxicity Inhibition of lymphocyte functions by binding surface molecules
44
What are the therapeutic uses, and side effects of Antithymocyte globulin?
Induction immunosuppression TNF-a release (ILI) Serum sickness Anaphylaxis *Cytokine storm*
45
What is the MOA of Muromonab-CD3?
Mouse antibodies against CD3 cause T lymphocyte depletion
46
What are the therapeutic uses, and side effects of Muromonab-CD3?
Reverse organ transplant rxn Cytokine storm Anaphylaxis Will not work more than once (immune response)
47
What are the three Anti-TNF-alpha reagents?
Infliximab Adalimumab Etanercept
48
What is the MOA of Anti-TNF-alpha reagents?
Prevents TNF-alpha from binding to its receptors by binding directly to the cytokine
49
What is infliximab?
Anti-TNF alpha antibody
50
What is Adalimumab?
Recombinant human IgG1 monoclonal against TNF-a
51
What is Etanercept?
Ligand binding portion of human anti-TNF alpha fused to the Fc portion of human IgG1
52
What are the therapeutic uses, and side effects of Anti-TNF alpha reagents?
Crohn's, UC Increase risk of infx and malignancies

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