Immunopharmacology Flashcards

1
Q

What are the 2 Calcineurin inhibitors?

A

Cyclosporine, Tacrolimus/FK506

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2
Q

What do the calcineurin inhibitors (cyclosporine and tacrolimus/FK506) block?

A

block IL2 production

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3
Q

What is the mTOR inhibitor?

A

Sirolimus

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4
Q

What does Sirolimus block?

A

it blocks T cell proliferation

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5
Q

What is the synthetic steroid?

A

Prednisone

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6
Q

What does Prednisone suppress?

A

it suppresses cytokine production

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7
Q

What is the alkylating agent?

A

Cyclophosphamide

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8
Q

What does cyclophosphamide do?

A

it kills dividing cells

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9
Q

What is the antimetabolite (folate mimic)?

A

Methotrexate

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10
Q

What does Methotrexate do?

A

it kills dividing cells

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11
Q

What is the other antimetabolite?

A

Mycophenolate Mofetil

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12
Q

What does mycophenolate mofetil do?

A

it kills dividing cells

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13
Q

What are the antibodies that can be used as immunosuppressants (6)?

A

Rituximab, Inflixumab, Tocilizumab, Daclizumab, RHOGAM, Muromonab-CD3 (OKT-3)

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14
Q

What are the 2 purposes of immunosuppressive drugs?

A

Prevention of organ transplant rejection, treatment of autoimmune diseases

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15
Q

What are some autoimmune disease examples?

A

multiple sclerosis, lupus, rheumatoid arthritis, Crohn’s disease, Type I diabetes

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16
Q

What is the cellular basis for rejection (4 steps)?

A
  1. Antigen presenting cell (APC) activates T cells
  2. T cells produce Interleukin 2 (IL2)
  3. IL2 stimulates the proliferation of T cells and the production of additional cytokines that stimulate the proliferation of multiple types of immune cells: T cells, B cells, macrophages, etc.
  4. activated immune cells attack transplanted organ (allograft)
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17
Q

What is IL2?

A

T cell growth factor

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18
Q

What is the molecular basis for rejection (6)?

A

1) APC activates T-cells
2) Calcium mediates something that makes Calcineurin
3) Calicineurin somehow makes NFAT-PO3 become NFAT nuclear factor of activated T cells in the nucleus
4) NFAT basically makes IL-2 protein
5) IL-2 stimulates the proliferation of T cells by binding to IL2 receptor on T cell and then via mTOR
6) the new T cells produce cytokines that further stimulate proliferation of T cells (and others)

This card sucks.

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19
Q

Which drug works on the cytokines?

A

prednisone

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20
Q

Which drugs work on calcineurin?

A

Tacrolimus (FK506)/FKBP, Cyclosporine/Cyclophilin. These are primary drugs used for preventing organ transplant rejection

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21
Q

Which drugs work on mTOR?

A

Sirolimus (Rapamycin)/FKBP

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22
Q

Which drugs work on cell proliferation?

A

cyclophosphamide, methotrexate, mycophenolate mofetil

23
Q

What are the other two sites that drugs can work?

A

IL-2, IL-2 receptor

24
Q

Which drugs are signaling inhibitors?

A

cyclosporine, tacrolimus, sirolimus

25
Q

Which drugs inhibit calcineurin?

A

cyclosporine, tacrolimus

26
Q

What are the adverse effects of cyclosporine and tacrolimus?

A

nephrotoxicity, hepatotoxicity, neurotoxicity

27
Q

Which drug inhibits mTOR?

A

sirolimus

28
Q

What are the adverse effects of sirolimus?

A

hyperlipidemia

29
Q

Which drug is the corticosteroid and what does it do?

A

prednisone-inhibits cytokine production

30
Q

What are the adverse effects of prednisone?

A

insomnia, hypomania, ulcers

31
Q

Which drugs are the proliferation inhibitors?

A

cyclophosphamide, methotrexate, mycophenolate mofetil

32
Q

What are the adverse effects of the proliferation inhibitors?

A

myelosuppression (proliferation-associated toxicities)

33
Q

What are antibodies?

A

proteins produced by B cells (plasma cells)

34
Q

How do antibodies function?

A

they function by binding to antigens and neutralizing them through several mechanisms

35
Q

What is RHOGAM?

A

Rh(D) immune globulin

36
Q

What will happen if an Rh(D) negative mom has an Rh(D) positive newborn?

A

Mom will generate antibodies to the Rh(D) on the erythrocytes of the Rh(D) positive newborn. the mom will be exposed to the newborn erythrocytes shortly after giving birth.

37
Q

What happens if the mom is given Rh(D) immune globulin shortly after giving birth (within 72 hours)?

A

it will lyse the erythrocytes from the baby before the mother generates an immune response

38
Q

What will this do to a subsequent Rh(D) positive baby?

A

a subsequent Rh(D) positive baby will be protected from hemolytic disease

39
Q

When will RHOGAM not work?

A

once the mother has developed Rh(D) antibodies

40
Q

What was the first therapeutic monoclonal antibody, used as a transplant rejection drug?

A

OKT3 aka muromonab 3

41
Q

What is the suffix for murine monoclonal antibodies?

A

-omab

42
Q

What is the suffix for chimeric monoclonal antibodies?

A

-ximab

43
Q

What is the suffix for humanized monoclonal antibodies?

A

-zumab

44
Q

What is the suffix for human monoclonal antibodies?

A

-umab

45
Q

What is Muromonab-CD3 (OKT-3)?

A

binds CD3 on the surface of T cells and inhibits T cell function; used to treat acute transplant rejection

46
Q

What is this Anti-IL-2 receptor antibody?

A

Daclizumab

47
Q

What does Daclizumab do?

A

blocks IL-2 receptor activation, thus blocking T cell activation; used to treat acute transplant rejection

48
Q

What is Rituximab?

A

a chimeric monoclonal antibody against the CD20 B-cell antigen

49
Q

What is Rituximab used for (3)?

A
  1. used to treat relapsed indolent lymphomas
  2. approved for the treatment of rheumatoid arthritis when combined with methotrexate
  3. may be useful in the treatment of multiple sclerosis
50
Q

What is Infliximab?

A

chimeric anti-TNF-a neutralizing antibody

51
Q

What is Infliximab used for (2)?

A
  1. useful in the treatment of rheumatoid arthritis (used in combo with methotrexate in patients refractory to methotrexate alone)
  2. useful in patients with moderate to severe Crohn’s disease who have failed conventional therapy
52
Q

What is Tocilizumab?

A

chimeric anti-IL-6 receptor neutralizing antibody

53
Q

What is Tocilizumab used for?

A

may be useful in the treatment of rheumatoid arthritis