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Owenpharm Block 2 > Immunopharmacology > Flashcards

Immunopharmacology Flashcards

1
Q

What is the general/overall mechanism of immunosuppressant drugs?

A

They block the proliferation or interaction of immune cells or block actions or release of cytokines

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2
Q

What are the two major uses of immunosuppressant drugs?

A

Treat autoimmune diseases and prevent allograft rejection

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3
Q

What prototype corticosteroid is used for immunosuppression?

A

Prednisolone

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4
Q

What 4 cytotoxic agents are prototype immunosuppressants?

A
  1. Azathiaprine
  2. Methotrexate
  3. Cyclophosphamide
  4. Mycophenolate Mofetil
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5
Q

What 3 cyclosporine like drugs are prototype immunosuppressants?

A
  1. Cyclosporine
  2. Tacrolimus
  3. Sirolimus
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6
Q

What type of cell growth do immune cells have? (3 points)

A

Synchronized bursts of cell growth that is stimulated by antigens/cytokines

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7
Q

What type of cell growth do cancer cells have? (3 points)

A

Random, unsynchronized, and unstimulated

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8
Q

How is cytotoxic drug therapy used against immune cells? (3 points)

A
  1. Used at initial exposure
  2. Kills selected rapidly proliferating clones
  3. Low daily dose for prolonged periods
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9
Q

How is cytotoxic drug therapy used against cancer cells?

A
  1. Kills rapidly growing cancer cells
  2. Intermittent therapy to allow immune system to recover
  3. High doses for short periods
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10
Q

Azathioprine is metabolized into what substance?

A

6-mercaptopurine

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11
Q

6-mercaptopurine has what effect on rapidly proliferating cells?

A

Inhibits the denovo synthesis of purines by preventing the production of AMP and GMP

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12
Q

What metabolite of 6-mercaptopurine inhibits the salvage pathway of purine synthesis?

A

ThioGMP

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13
Q

What part of DNA and subsequently protein synthesis is inhibited by Methotrexate?

A

Purine synthesis (same step as Azathioprine/6-mercaptopurine)

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14
Q

What is the major side effect of Azathioprine?

A

Bone marrow suppression

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15
Q

What is the primary therapeutic use of Azathioprine?

A

Inhibit rejection of transplanted organs and in some autoimmune diseases like rheumatoid arthritis.

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16
Q

What effect does prednisolone have on cell traffic or accumulation?

A

It reduces access of cells to target tissue

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17
Q

Why does prednisolone produce lymphocytopenia and monocytopenia?

A

It redistribute cells to outside of the vascular space.

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18
Q

What effect does prednisolone have on neutrophils?

A

It prevents adherence to endothelium and inhibits the actions of chemotactic factors

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19
Q

What effects does prednisolone have on cell function? (3 items)

A
  1. Interferes with macrophage antigen processing
  2. Blocks the actions of lymphokines
  3. Inhibits binding to Fc receptors
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20
Q

What are the two primary uses of prednisolone?

A
  1. Management of autoimmune diseases

2. Prevent graft rejection

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21
Q

What are the major side effects/toxicity of prednisolone?

A
  1. Suppression of adrenal-pituitary axis
  2. Acute adrenal insufficiency on abrupt withdrawal
  3. Cushing’s syndrome
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22
Q

What is the major contraindication for prednisolone?

A

Existing infection

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23
Q

Name the alkylating agent that results in cross-linking of DNA to kill replicating and non-replicating cells.

A

Cyclophosphamide

24
Q

What type of cell activity is Cyclophosphamide most effective in suppressing? Why?

A

Humoral immunity. Its toxic effect is more pronounce on B-cells

25
Q

What is Cyclophosphamide used for? What is it not effective for?

A

It is used to treat autoimmune diseases in combination with other drugs. It is not effect in preventing graft rejection.

26
Q

What is the major side effect of cyclophosphamide?

A

bone marrow suppression

27
Q

What medication is an inhibitor of dihydrofolate reductase that inhibits folate dependent steps in purine synthesis and in turn inhibits DNA synthesis?

A

Methotrexate

28
Q

What is the mechanism of action of methotrexate?

A

Inhibition of dihydrofolate reductase which inhibits folate dependent purine synthesis which inhibits DNA synthesis.

29
Q

What is the major use for methotrexate?

A

treatment of autoimmune disease like psoriasis

30
Q

What is methotrexate not used for?

A

Transplants

31
Q

What is the major toxic side effect of methotrexate?

A

hepatic toxicity

32
Q

Is mycophenolate mofetil active in its given form? If not, what is the active metabolite?

A

No. Mycophenolic acid is the active metabolite.

33
Q

What type of immunosuppression does mycophenolate mofetil produce?

A

Lymphocyte selective immunosuppression

34
Q

What is the mechanism of action of mycophenolate mofetil?

A
  1. It inhibits IMP dehydrogenase preventing IMP conversion to GMP.
  2. Prevents denovo synthesis of purines.
  3. No effect on salvage pathway.
35
Q

Why does inhibition of de novo pathway and not salvage pathway create selectivity for lymphocytes?

A

Lymphocytes are the only cells not able to make GMP via the salvage pathway

36
Q

What are the two major effects of mycophenolate mofetil?

A
  1. Inhibition of lymphocyte proliferation

2. Inhibition of expression of cell surface adhesion molecules

37
Q

How does mycophenolate mofetil compare with azathioprine and methotrexate in its selectivity and effectiveness?

A

It is more selective

It is equally effective

38
Q

What is mycophenolate mofetil used for and in combination with what other drugs?

A

It is used for allograft rejection in combination with cyclosporine and corticosteroids

39
Q

How does mycophenolate mofetil allow for decreased toxicity?

A

It allows for lower doses of cyclosporine

40
Q

What can mycophenolate mofetil be used for other than allograft rejection?

A

Autoimmune disease like rheumatoid arthritis and refractory psoriasis

41
Q

What type of patients should mycophenolate mofetil be used with caution? (3 items)

A
  1. Active GI disease
  2. Reduced renal function
  3. Active infection
42
Q

What are the side effects associated with mycophenolate mofetil? (3 items)

A
  1. Increased risk of infection
  2. Leukopenia
  3. Anemia
43
Q

Why should pregnant women not be given mycophenolate mofetil?

A
  1. loss of pregnancy

2. Congenital malformation

44
Q

What lipophilic peptide antibiotic can be used for immunosuppression?

A

Cyclosporin

45
Q

What is the mechanism of action of Cyclosporin in immunosuppression?

A

It binds to the cellular receptor Cyclophilin and inhibits calcium-dependent phosphatase (Calcineurin). This blocks activation of transcription factor (NFAT) necessary for IL-2 production

46
Q

What secondary action of Cyclosporin also inhibits IL-2?

A

Inhibition of mRNA synthesis that codes for IL-2 and other lymphokines.

47
Q

What effect does Cyclosporin blockage of IL-2 synthesis create?

A

It blocks T-cell helper function and therefore inhibits T-cell proliferation and cytotoxicity

48
Q

How does cyclosporine alter T-cell response to IL-2?

A

It doesn’t!

49
Q

Why is cyclosporine more specific in its action?

A

It is not lymphotoxic

50
Q

What are the uses for cyclosporine?

A

Anti-rejection and some autoimmune diseases

51
Q

What is the major side effect of cyclosporine?

Is this reversible?

A

Nephrotoxicity in 25-40%

Yes, with reduction in dosage or discontinuation

52
Q

What is the mechanism of action for Tacrolimus?

A

It binds FK binding protein (FK BP-12), a cyclophilin related protein which inhibits calcineurin and subsequently IL-2

53
Q

What is the relative potency of Tacrolimus to Cyclosporine?

A

Tacrolimus is 50-100 times more potent

54
Q

How is the mechanism of action of Sirolimus and Tacrolimus similar and different?

A

They both bind FK-BP12 and inhibit T-cell activation & IL-2

The sirolimus FKBP12 complex does not affect calcineurin activity. Instead it inhibits mTOR.

55
Q

What is a unique use of Sirolimus?

A

Coating of cardiac stents

Owenpharm Block 2 (11 decks)

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