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AU14 Pharmacology > Exam 4; Immunosuppressants > Flashcards

Exam 4; Immunosuppressants Flashcards

1
Q

All of the immunosuppressants carry an increased risk of this

A

infection

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2
Q

Many immunosuppressants cause an increased risk of this

A

malignancy

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3
Q

What are four immunosuppressants that affect T cell activation

A

atgam
antithymocyte globulin
abatacept
belatacept

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4
Q

This agent that affects T cell activation can be used to treat acute renal transplant (polyclonal antibodies)

A

antithymocyte globulin

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5
Q

This agent that affects T cell activation bind to and inhibits CD80 and CD86; used to treat RA

A

abatacept

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6
Q

This agent that affects T cell activation binds to CD80 and CD86, is used in renal transplant and causes an increase in malignancies

A

belatacept

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7
Q

How can you tell which drug is a monoclonal antibody

A

it ends in -mab

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8
Q

The middle (Li or Tu) of a monoclonal antibody drug signifies what

A

target
Li = immune cell
Tu = tumor cell

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9
Q

How can you tell the source of a monoclonal antibody drug

A 
Xi = chimeric source
Zu = humanized
U = fully human
O = fully mouse
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10
Q

Which source of a monoclonal antibody is the most antigenic

A 
Xi = chimeric (foreign with human)
O = fully mouse
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11
Q

Natalizumab is what kind of monoclonal antibody

A

immune cell = Li

humanized = zu

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12
Q

What is the mechanism behind natalizumab

A

binds to alpha integrins on the CD4 cell and other immune cell

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13
Q

What disease is natalizumab linked with

A

progressive multi-focal leukoenephalopathy (PML)

fatal viral CNS disease

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14
Q

Tocilizumab is what kind a monoclonal antibody

A

immune cell = Li

fully human = U

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15
Q

What is the mechanism behind tocilizumab

A

bind to IL-6 receptors; T, B, and macrophages

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16
Q

Ustekinumab is what kind of monoclonal antibody

A

immune cell = Li

fully human = U

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17
Q

What is the mechanism behind ustekinumab

A

binds to IL-12 and IL-23

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18
Q

Which condition is ustekinumab designed to treat

A

psoriasis

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19
Q

What condition is tocilizumab designed to treat

A

RA

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20
Q

What conditions are natalizumab designed to treat

A

Crohn’s and MS

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21
Q

What is the mechanism behind etanercept

A

binds to TNF itself (binds to an interleukin)

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22
Q

What is the route of administration of etanercept

A

given subQ

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23
Q

What is different about etanercept that the other agents that bind to TNF

A

it is not a monoclonal antibody

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24
Q

What disorder is entanercept used to treat

A

RA

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25
Q

Infliximab is what kind of monoclonal antibody

A

chimeric = Xi

immune cell = Li

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26
Q

What is the mechanism behind infliximab

A

it binds to TNF

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27
Q

What disorder is imfliximab used to treat

A

RA and Crohn’s

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28
Q

What are two side effects of infliximab

A

can induce an immune response

if given IV, the infusion can cause itching, hypotension, and fever

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29
Q

What is the concern with taking infliximab if you have a pre-existing condition

A

a pre-existing infection with a fungus or TB will flare up

30
Q

Adalimumab is what kind of monoclonal antibody

A

immune cell = Li

fully human = U

31
Q

What is the mechanism behind adalimumab

A

binds to TNF

32
Q

What is certolizumab used to treat

A

RA and Crohn’s

33
Q

What is golumumab used to treat

A

RA
ulcerative colitis
psoriatic arthritis

34
Q

What is the mechanism behind anakinra

A

blocks the IL-1 receptor

35
Q

What condition is anakinra used to treat

36
Q

What is the method of administration of anakinra

37
Q

What other medications should anakrina be used with and NOT used with

A

use with other immunosuppressants like methotrexate, but not with TNF inhibitors

38
Q

What is the mechanism behind rilonacept

A

binds to IL-1 molecule

39
Q

This was the first drug that allowed transplantation to work properly

A

cyclosporine

40
Q

What conditions is cyclosporine used for now

A

transplantation
psoriasis
dry eye

41
Q

What is the mechanism behind cyclosporine

A

inhibits calcineurin phosphatase (ENZYME INHIBITOR) preventing the NFAT complex which prevents activation of the gene for IL-2, IL-3, and TNF

42
Q

What is cyclosporine metabolized by

43
Q

What are the side effects of cyclosporine

A 
nephrotoxicity
hepatotoxicity
hypertrichosis (hair growth)
gingival hyperplasia
increase in cholesterol
hypertension
44
Q

What is the mechanism behind tacrolimus

A

binds the FK binding protein (FKBP) which inhibits calcineuron phosphatase

45
Q

Which is more efficacious, cyclosprine or tacrolimus

A

tacrolimus

46
Q

What are the side effects of tacrolimus

A

nephrotoxicity
neurotoxicity
alopecia
diabetes

47
Q

What is tacrolimus metabolized by

48
Q

What is the mechanism of glucocorticoids

A

through the cell membrane → bind to receptor → receptor dimerizes → complex then binds with GC receptor element on DNA

49
Q

What is the mechanism behind sirolimus and everolimus

A

bind to FKBP
inhibit a kinase required for binding of IL-2
decrease in cytokine production

50
Q

What are the side effects of sirolimus and everolimus

A

renal toxicity

lung toxicity

51
Q

What is the mechanism behind basilixumab

A

blocks the IL-2 receptor

52
Q

What other drug is basilixumab used with

A

cyclosporine

53
Q

What are some conditions to watch for with someone taking basilixumab

A

hypersensitivity reaction; hypotension
bronchospasm
pulmonary edema

54
Q

What is the mechanism behind tofacitinib

A

janus kinase inhibitor; inhibits the signal pathway of cytokines and ILs
presents the activation of Signal Transducers and Activators of Transcription (JAK STAT)

55
Q

What are the side effects of tofacinitinib

A

increase infection and malignancy

56
Q

What kind of drug is azathioprine

57
Q

What disorders is azathioprine used to treat

A

transplantation
RA
Crohn’s

58
Q

What is the mechanism behind azathioprine

A

since it is a prodrug, it is converted to 6-mercaptopurine which inhibits the synthesis of purines; inhibit T cell replication

59
Q

What are the side effects of azathioprine

A

bone marrow depression leading to;
megalobalstic anemia
throbocytopenia
leukopenia

60
Q

What conditions are mycophenolate mofetil used to treat

A

transplantation and lupus

61
Q

What is the mechanism behind mycophenolate mofetil

A

inhibits the enzyme inosine monophosphate dehydrogenase; inhibiting the synthesis of guanosine

62
Q

What are the side effect of mycophenolate mofetil

A 
bone marrow depression leading to;
megalobalstic anemia
throbocytopenia
leukopenia
as well as GI destruction
63
Q

This is the drug of choice for early treatment of RA, is disease modifying so it will stop the progression of RA

A

methotrexate

64
Q

What is the mechanism of methotrexate

A

inhibits dihydrofolate reductase
inhibiting mammalian cell division
inhibits a lot of folic acid dependent processes

65
Q

What is dihydrofolate reductase necessary for?

A

the synthesis of dihydro-folic acid and tetrahydrofolic acid

66
Q

What type of drug is leflunomide

A

prodrug that is converted to teriflunomide

67
Q

What is the mechanism behind teriflunomide and leflunomide

A

inhibitors of pyrimidine synthesis

inhibiting the enzyme dihydro-orotate dehydrogenase

68
Q

What are the side effects of leflunomide and teriflunomide

A

diarrhea

teratogen

69
Q

How does leflunomide and teriflunomide affect P450

A

inhibits P450

70
Q

This drug was first developed as a treatment for malaria

A

hydroxychloroquine

71
Q

What is the mechanism of hydrochloroquine

A

taken up my macrophages and concentrated in macrophage lysosome which interferes with macrophage processing of antigens

72
Q

What are the side effects of hydrooxychloroquine

A

GI dysfunction
severe dermatitis
irreversible retinal damage

AU14 Pharmacology (29 decks)

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