Immunosuppressives

Question 1

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

Answer 1

Dr. Joseph Murray

Question 2

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

Answer 2

1. ) Depletion agents

2. ) Immune modulators

Question 3

Include antithymocyte globulin and Muromonab CD3 mAb

Answer 3

Depleting agents

Question 4

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

Answer 4

Immune modulators

Question 5

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

Answer 5

Calcineurin inhibitor, glucocorticoids, and mycophenolate mofetil

Question 6

For maintenance therapy, you want to use protocols without

Answer 6

Steroids

Question 7

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

Answer 7

Sirolimus (Rampmycin)

Question 8

Treatment of established rejection requires the use of agents against activated

Answer 8

T cells

Question 9

What are the two calcineurin inhibitors?

Answer 9

Cyclosporine and Tacrolimus (FK 506)

Question 10

What are two cytotoxic drugs used for transplantation?

Answer 10

Azathioprine and mycophenolate mofetil

Question 11

What are the two mTOR inhibitors used for transplantation?

Answer 11

Sirolimus (rampamycin) and Everolimus

Question 12

The most important drug in the history of organ transplantation

Answer 12

Cyclosporine

Question 13

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

Answer 13

Calcineurin inhibitors

Question 14

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

Answer 14

Calcineurin inhibitors

Question 15

Calcineurin inhibitors are also useful for autoimmune disorders such as

Answer 15

Psoriasis and RA

Question 16

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

Answer 16

Tacrolimus

Question 17

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

Answer 17

Cyclosporine

Question 18

The peak level of cyclosporine in plasma occurs in

Answer 18

1.5-2 hours after oral administration

Question 19

Tacrolimus and cyclosporine interact with other drugs that affect the

Answer 19

P450 system

Question 20

What should be avoided when taking cyclosporine and tarolimus?

Answer 20

Grapefruit and grapefruit juice

Question 21

Enhanced by sirolimus through reduced drug metabolism by P450

Answer 21

Renal toxicity

Question 22

Bacterially produced macrolide and is structurally related to tacrolimus

Answer 22

Sirolimus

Question 23

An ester-derivative of sirolimus

Answer 23

Everolimus

Question 24

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

Answer 24

mTOR inhibitors

Question 25

The mTOR inhibitors reach peak level within

Answer 25

1 Hour of administration

Question 26

Absorption of the mTOR inhibitors can be affected by a

Answer 26

High-fat diet

Question 27

The mTOR inhibitors are mainly metabolized by P450 and transported by

Answer 27

P-glycoprotein

Question 28

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

Answer 28

Everolimus

Question 29

Causes a dose-dependent increase in serum cholesterol and triglycerides

Answer 29

The mTOR inhibitors

Question 30

Close attention should be given to drugs that affect the activity of -such as the mTOR inhibitors

Answer 30

CYP3A4 and P-glycoprotein

Question 31

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

Answer 31

Azathioprine

Question 32

The main side effect of azathioprine is

Answer 32

Bone marrow suppression

Question 33

zathiprine use also possesses risks of

Answer 33

Neoplasia and infections

Question 34

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

Answer 34

Allopurinol

Question 35

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

Answer 35

Mycophenolate Mofetil

Question 36

Unlike other cell types, B and T cells lack

Answer 36

Purine salvage pathways

Question 37

Therefore, mycophenolate selectively suppresses

Answer 37

Lymphocyte proliferation

Question 38

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

Answer 38

Mycophenolate

Question 39

Can cause GI disturbances, myelosuppression, headache and hypertension

Answer 39

Mycophenolate

Question 40

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

Answer 40

Immunosuppression

Question 41

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

Answer 41

Organ transplant rejection

Question 42

Tend to be more specific than other immunosuppressents

Answer 42

Immunosuppressive antibodies

Question 43

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

Answer 43

Anti-lymphocyte/thymocyte antibodies

Question 44

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

Answer 44

Anti-lymphocyte/thymocyte antibodies

Question 45

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

Answer 45

Daclizumab monoclonal antibody

Question 46

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

Answer 46

IL-2 induced T-cell proliferation

Question 47

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

Answer 47

Muromonab-CD3 antibody

Question 48

The muromonab-CD3 antibody causes the destruction of

Answer 48

CD3 bearing T cells

Question 49

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

Answer 49

Muromonab

Question 50

An adverse effect of muromonab-CD3 is

Answer 50

Cytokine release syndrome

Question 51

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

Answer 51

Cytokine Release Syndrome

Question 52

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

Answer 52

Anti-TNF-a function

Question 53

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

Answer 53

Etanercept (Enbrel)

Question 54

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

Answer 54

Immune checkpoint inhibitors

Question 55

A class of natural and synthetic steroid hormones

Answer 55

Glucocorticoids

Question 56

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

Answer 56

Glucocorticoids