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Immunity > Immunosuppressives > Flashcards

Immunosuppressives Flashcards

1
Q

Performed the first successful solid organ (kidney) transplant in 1954

A

Dr. Joseph Murray

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2
Q

There are two groups of biologics (antibodies) used for induction therapy. What are they?

A
  1. ) Depletion agents

2. ) Immune modulators

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3
Q

Include antithymocyte globulin and Muromonab CD3 mAb

A

Depleting agents

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4
Q

Include Daclizumab (anti-IL-2R) and Muromonab (anti-CD3) mAbs

A

Immune modulators

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5
Q

A typical combination of drugs for maintenance therapy for a patient with a transplant is use of a

A

Calcineurin inhibitor, glucocorticoids, and mycophenolate mofetil

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6
Q

For maintenance therapy, you want to use protocols without

A

Steroids

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7
Q

For maintenance therapy, you want to use protocols with the reduction of calcineurin inhibitor or switching to

A

Sirolimus (Rampmycin)

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8
Q

Treatment of established rejection requires the use of agents against activated

A

T cells

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9
Q

What are the two calcineurin inhibitors?

A

Cyclosporine and Tacrolimus (FK 506)

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10
Q

What are two cytotoxic drugs used for transplantation?

A

Azathioprine and mycophenolate mofetil

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11
Q

What are the two mTOR inhibitors used for transplantation?

A

Sirolimus (rampamycin) and Everolimus

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12
Q

The most important drug in the history of organ transplantation

A

Cyclosporine

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13
Q

Used for prevention and treatment of transplant rejection for kidney, liver, heart and other organs

A

Calcineurin inhibitors

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14
Q

Typically used at the maintenance doses with other immunosuppressants because of the nephrotoxicity

A

Calcineurin inhibitors

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15
Q

Calcineurin inhibitors are also useful for autoimmune disorders such as

A

Psoriasis and RA

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16
Q

A newer drug that shares the same mechanism of action as cyclosporine, but is up to 100 times more potent

A

Tacrolimus

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17
Q

Can be administered in two different ways:

  1. ) IV in an ethanol-polyoxyethylated castor oil mixture
  2. ) Orally in gelatin capsule or a microemulsion formulation
A

Cyclosporine

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18
Q

The peak level of cyclosporine in plasma occurs in

A

1.5-2 hours after oral administration

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19
Q

Tacrolimus and cyclosporine interact with other drugs that affect the

A

P450 system

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20
Q

What should be avoided when taking cyclosporine and tarolimus?

A

Grapefruit and grapefruit juice

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21
Q

Enhanced by sirolimus through reduced drug metabolism by P450

A

Renal toxicity

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22
Q

Bacterially produced macrolide and is structurally related to tacrolimus

A

Sirolimus

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23
Q

An ester-derivative of sirolimus

A

Everolimus

24
Q

Used in transplants, certain autoimmune conditions, drug-eluting stents, and as an anticancer drug

A

mTOR inhibitors

25
Q

The mTOR inhibitors reach peak level within

A

1 Hour of administration

26
Q

Absorption of the mTOR inhibitors can be affected by a

A

High-fat diet

27
Q

The mTOR inhibitors are mainly metabolized by P450 and transported by

A

P-glycoprotein

28
Q

What has a shorter half-life, sirolimus or everolimus?

A

Everolimus

29
Q

Causes a dose-dependent increase in serum cholesterol and triglycerides

A

The mTOR inhibitors

30
Q

Close attention should be given to drugs that affect the activity of

-such as the mTOR inhibitors

A

CYP3A4 and P-glycoprotein

31
Q

Used as an adjunct for preventing kidney rejection and for treatment of severe rheumatoid arthritis and other autoimmune diseases

A

Azathioprine

32
Q

The main side effect of azathioprine is

A

Bone marrow suppression

33
Q

zathiprine use also possesses risks of

A

Neoplasia and infections

34
Q

Azathioprine is mainly metabolied by xanthine oxidase. Meaning it has interactions with

A

Allopurinol

35
Q

A potent inhibitor of inosine monophosphate dehydrogenase, an enzyme critical for de novo purine synthesis

A

Mycophenolate Mofetil

36
Q

Unlike other cell types, B and T cells lack

A

Purine salvage pathways

37
Q

Therefore, mycophenolate selectively suppresses

A

Lymphocyte proliferation

38
Q

Approved by FDA for oral or iv use with calcineurin inhibitors and corticosteroid in patients with renal, liver or heart transplants

A

Mycophenolate

39
Q

Can cause GI disturbances, myelosuppression, headache and hypertension

A

Mycophenolate

40
Q

Antibodies against lymphocyte cell-surface receptors can prevent lymphocyte activation, thereby achieving

A

Immunosuppression

41
Q

Both polyclonal and monoclonal antibodies against lymphocyte cell-surface receptors are widely used for prevention and treatment of

A

Organ transplant rejection

42
Q

Tend to be more specific than other immunosuppressents

A

Immunosuppressive antibodies

43
Q

Obtained by injection of human thymic lymphocytes into a horse or sheep

A

Anti-lymphocyte/thymocyte antibodies

44
Q

Primarily act on circulating lymphocytes. They will also deplete thymus dependent lymphocytes when administered continuously

A

Anti-lymphocyte/thymocyte antibodies

45
Q

Humanized monoclonal antibody specific for the alpha subunit (CD25) of the IL-2 receptor on activated T cells

A

Daclizumab monoclonal antibody

46
Q

Daclizumab monoclonal antibody is used against acute rejection in renal transplant recipients by competitive antagonism of

A

IL-2 induced T-cell proliferation

47
Q

A mouse monoclonal antibody raised against the CD3 subunit of the T cell receptor (TCR) complex

A

Muromonab-CD3 antibody

48
Q

The muromonab-CD3 antibody causes the destruction of

A

CD3 bearing T cells

49
Q

Useful to prevent acute rejection of heart, kidney and liver transplants. It is also used to deplete T-cells from donor bone marrow prior to bone marrow transplantation

A

Muromonab

50
Q

An adverse effect of muromonab-CD3 is

A

Cytokine release syndrome

51
Q

Engagement of TCR causes lease of cytokines such as TNF-alpha. Glucocorticoids should be administered before injection of Muromonab-CD3

A

Cytokine Release Syndrome

52
Q

Infliximab (Remicade), adalimumab (Humira), certolizumab (Cimzia), and golimumab (Simponi) re all examples of antibodies with

A

Anti-TNF-a function

53
Q

Another anti-TNF-a is a soluble receptor fusion protein called

A

Etanercept (Enbrel)

54
Q

Anti-PD1 antibodies such as pembrolizumab (Keytruda), nivolumab (Opdivo), atezolizumab (Tecentriq), avelumab (Bavencio), and durvalumab (Imfinzi) function as

A

Immune checkpoint inhibitors

55
Q

A class of natural and synthetic steroid hormones

A

Glucocorticoids

56
Q

Inhibit expression of cytokine genes (IL-1, IL-2, IL-6, interferon and TNF-α), and T-cell proliferation and T-cell dependent immunity

A

Glucocorticoids

Immunity (33 decks)

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