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Pharmacology -- Test #2 > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

Immunopharmacology focuses on…

A

Primary and secondary disorders of the immune system and the production of modulators of the immune system

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2
Q

Two types of immunopharmacological drugs

A

Immunosuppressants

Immunostimulants

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3
Q

The development of the adaptive immune response happens over about….days

A

8-14

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4
Q

Basophils can release

A 
Histamine
Bradykinin
Serotonin
Hepatin
SRSA
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5
Q

Immunosuppressants are used to…

A

Inhibit normal immune responses

Organ transplant, Autoimmune disorders

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6
Q

What immune response are immunosuppressants most effective with

A

Primary

Start before antigen exposure

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7
Q

Acute organ rejection =

A

Rejection that occurs 24 hrs-several weeks after transplant

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8
Q

Acute rejection is mediated primarily by…

A

T cells and cytokines

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9
Q

Six Classess of Immunosuppressants

A
  1. Regulators of Gene Expression
  2. Alkylating Agents
  3. Inhibitors of de novo purine synth.
  4. Inhibitors of de novo pyramidine synth.
  5. Kinases and phosphatase inhibitors
  6. Protein immunosuppressive drugs
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10
Q

End result of immunosuppressant regulators of gene expression?

A
  1. Reduced Circulating Lymphocytes
  2. Blocked lymphocyte activation needed for antigen pres.
  3. Block T-cell proliferation
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11
Q

How do Immunosuppressant regulators of gene expression block T cell proliferation?

A

Inhibition of IL-2 gene transcription

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12
Q

immunosuppressant regulators of gene expression.

Induction, Maintenance, or both?

A

Both

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13
Q

Example of immunosuppressant alkylating agent?

A

Cytotoxic drug cyclophosphamide

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14
Q

First generation immunosuppressant inhibitor of de novo purine synthesis

A

Azathioprine

6-mercaptopurine

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15
Q

Important non-1st gen immunosuppressant inhibitors of de novo purine synthesis?

A

Mycophenylate mofetil
Methotrexate
Polygentamate

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16
Q

immunosuppressant inhibitors of de novo purine synthesis.

Induction, Maintenance, or both?

A

Both

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17
Q

immunosuppressant alkylating agents.

Induction, Maintenance, or both?

A

Both

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18
Q

Difference between effects of de novo purine and pyrimidine inhibiton

A

DN pyramadine inhib. has less CV risk and less nephrotoxicity, but they’re also less effective

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19
Q

How do immunosuppressant inhibitors of de novo pyrimidine synthesis work?

A

Inhibitior of dihydroorotate, a key enzyme in pyramidine synthesis

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20
Q

Three classic examples of immunosuppressant kinases and phosphotase inhibitors

A

Cyclosporine
Tacrolimus
Sirolimus

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21
Q

Effects of dosing with Cyclosporine or tacrolimus?

A

They block T-cell signalling pathways that stimulate IL-2

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22
Q

Cyclosporine or tacrolimus

Induction, Maintenance, or both?

A

Both

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23
Q

Cyclosporine method of administration?

Concentrates in which cells?

A

IV or Per Os

Dist. widely, but conc. in RBC and WBC

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24
Q

Cyclosporine metabolism?

A

Metabolized by liver and mainly excreted in feces

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25
Q

Cyclosporine schedule?

A

Given 4-24 hrs before transplant

Lowered doses at weekly interval afterward

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26
Q

Cyclosporine toxicity?

A

Mainly renal (proximal tubule)
Gingival
Neuronal
Sometimes hepatic

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27
Q

Cyclosporine Mechanism?

A

Assoc. w/ Calcineurin and inhibits its phosphotase activity. This prevents translocation of NFAT TFs to the nucleus of lymphocytes. Blocks lymphokine synthesis.

Also blocks JNK and p38

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28
Q

Tacrolimus is what kind of anti-biotic?

A

Macrolide

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29
Q

Tacrolimus Mechanism?

A

Binds to cytoplasmic FK506 binding protein, making a complex that inhibits phosphatase activity of calcineurin

Also blocks JNK and p38

30
Q

How is Tacrolimus dosed?

A

IV or Per Os

31
Q

Distribution and metabolism of Tacrolimus?

A

Loss widely distrib. than cyclosporine

Metabolized by liver and excreted in the feces

32
Q

Who is more potent, cyclosprorine or Tacrolimus

A

Tacrolimus is about 100x more potent

33
Q

Tacrolimus may be useful to treat what specific disease?

A

Myasthenia gravis

34
Q

Mechanism of Sirolimus action?

A

Inhibition of calcineurin (and blocking of T cell resp. to cytokines) by binding onto FKBP12.

35
Q

Is Sirolimus used alone or in combination treatment?

A

Yes

Both – better w/ cyclo.

36
Q

Look up Everolimus in the ppt.

A

well shit.

page 5 of my notes

37
Q

How do antilymphocyte globulins work?

A

Inhibition of acutre graft rejection by binding onto lymphocyte surface proteins
Ex. muromonab for induction and treatment of rejection

38
Q

Antilymphocyte globulins are used against what targets?

A

CD 25 (Basiliximab)
CD3 (Muromonab)
CD52, CD20 – Antithymocyte

39
Q

Diseases with CD20 overexpression?

A

RA, Hemolytic anemia

40
Q

Significance of Beltacept?

A

Equivalent alternative to calcineurin inhibitors for kidney transplant recipients. It is an inhibitor of CD28 mediated T cell costimulation.

41
Q

Mechanism for Beltacept

A

Binds to CD80 and 86, blocking CD28 engagement on T cells.

Prevents T cell activation.

42
Q

Beltacept is associated with…

A

more frequent post-transplant lymphoproliferative disorders than other suppressants.
Serious side effects in children.

43
Q

Non-medical downside of Baltacept?

A

It’s fuckin expensive.

44
Q

Studies on rejection in kidney transplant with beltacept use suggest that targeting ______ might be more valueable than targeting CD80/86

A

CD28

45
Q

Important details for Rapamycine

A

Macrocyclic Lactone
Targets mTOR (regulator of cell proliferation)
May help by preventing the proliferation of smooth muscle cells and fibroblasts
Everolimus is a related compound

46
Q

Why can’t Everolimus replace calcineurin inhibitors?

A

When used alone, it triggers de novo donor-specific alloantibodies associated with antibody mediated rejection

47
Q

What is FTY720?

A 
First in class synthetic small molecule
Reduces circulating Ts by driving them into lymphoid tissues
Treats MS
48
Q

TNF-alpha inhibitors are used primarily to treat…

A

RA

49
Q

Which cell usually mediates auto-immunity?

A

T cell

50
Q

Examples of Ab mediated auto-immunity

A

Autoimmune mediated hemolytic anemia
Myasthenia gravis
Hypoadrenocorticism

51
Q

Disease in which exposure to an antigen will program for search and destruction of the antigen in the future

A

Thyroiditis

Autoimmune hypothyroidism

52
Q

Six major drugs for treatment of autoimmune disorders

A 
Corticosteroids
Cyclophosphamide
Asathioprine
Mercaptopurine
Leflunomide
Cyclosporine
53
Q

Primary drugs used in any autoimune disease?

A

Corticosteroids

54
Q

Why not use Corticosteroids long term?

A

Infections, Ulcers, Hyperglycemia, Osteoporosis

55
Q

How does cyclophosphamide work?

A

Inhibits DNA synthesis and function by alkylation

Affects B Cells more than T cells

56
Q

How does Azathioprine work?

A

Purine anti-metabolite that interferes w/ DNA synthesis
Affects all rapidly growing cells
Takes weeks to see results

57
Q

Effects of Azathioprine cytotoxicity?

A

Leukopenia
Thrombocytopenia
GI Dysfunction
Possible infections and hepatic lesions

58
Q

Azathioprine is metabolized into…

A

Mercaptopurine

59
Q

Mercaptopurine effects?

A

Interferes with RNA and DNA synthesis after conversion to a purine antagonist.
Mostly hits humoral immunity
Side effects - BM+GI depletion

60
Q

Effects of Leflunomide?

A

Inhibitor of pyrimidine synthesis
Active metabolite has a long half life of several weeks
used for RA

61
Q

Why are frequent blood measures of Cyclosporine levels necessary?

A

Variability of Cyclosporine absorption
Cyclosporine saturates tissues, so dosage may need adjusting
Drug interactions

62
Q

To get the full benefit of Cyclosporine, the patient must…

A

be on a very strict feeding and dosing schedule.
Diet consistent
Made difficult by loss of appetite

63
Q

Three drug classes important to the treatment of allergies

A

Fatty Acids
Antihistamines
Biotin

64
Q

What is atopy?

A

Inhalant allergy

65
Q

Fatty acids used in allergy treatment may include…

A

linoleic and gamma-linoleic acids

66
Q

Why give an allergy sufferer fatty acids?

A

They work in the skin to help reduce the amount/effects of histamine.
Very safe, few side effects

67
Q

Typical mechanism for anti-histamines?

A

H1 blockers.

prevent attachment of histamine to its target

68
Q

Example of a common antihistamine?

A

Diphenhydramine

69
Q

If all else fails in allergy treatment and patients are symptomatic more than 4 months per year, what should you consider?

A

Immunotherapy

Weekly/Monthly injections with allergens to induce desensitization in most treated patients

70
Q

For patients with severe symptoms of allergies after other options are exhausted, use…

A

Corticosteroids (ex. dexamethasone, methylprednisone)

71
Q

Some major risks of imunosuppressants

A 
GVH
Infections
Reappearance of latent disease (ex. Hep)
CV events
Neoplasia

Pharmacology -- Test #2 (13 decks)

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