Exam 4; Immunosuppressants Flashcards Preview

AU14 Pharmacology > Exam 4; Immunosuppressants > Flashcards

Flashcards in Exam 4; Immunosuppressants Deck (72):
1

All of the immunosuppressants carry an increased risk of this

infection

2

Many immunosuppressants cause an increased risk of this

malignancy

3

What are four immunosuppressants that affect T cell activation

atgam
antithymocyte globulin
abatacept
belatacept

4

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

antithymocyte globulin

5

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

abatacept

6

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

belatacept

7

How can you tell which drug is a monoclonal antibody

it ends in -mab

8

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

target
Li = immune cell
Tu = tumor cell

9

How can you tell the source of a monoclonal antibody drug

Xi = chimeric source
Zu = humanized
U = fully human
O = fully mouse

10

Which source of a monoclonal antibody is the most antigenic

Xi = chimeric (foreign with human)
O = fully mouse

11

Natalizumab is what kind of monoclonal antibody

immune cell = Li
humanized = zu

12

What is the mechanism behind natalizumab

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

13

What disease is natalizumab linked with

progressive multi-focal leukoenephalopathy (PML)
fatal viral CNS disease

14

Tocilizumab is what kind a monoclonal antibody

immune cell = Li
fully human = U

15

What is the mechanism behind tocilizumab

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

16

Ustekinumab is what kind of monoclonal antibody

immune cell = Li
fully human = U

17

What is the mechanism behind ustekinumab

binds to IL-12 and IL-23

18

Which condition is ustekinumab designed to treat

psoriasis

19

What condition is tocilizumab designed to treat

RA

20

What conditions are natalizumab designed to treat

Crohn's and MS

21

What is the mechanism behind etanercept

binds to TNF itself (binds to an interleukin)

22

What is the route of administration of etanercept

given subQ

23

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

it is not a monoclonal antibody

24

What disorder is entanercept used to treat

RA

25

Infliximab is what kind of monoclonal antibody

chimeric = Xi
immune cell = Li

26

What is the mechanism behind infliximab

it binds to TNF

27

What disorder is imfliximab used to treat

RA and Crohn's

28

What are two side effects of infliximab

can induce an immune response
if given IV, the infusion can cause itching, hypotension, and fever

29

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

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

30

Adalimumab is what kind of monoclonal antibody

immune cell = Li
fully human = U

31

What is the mechanism behind adalimumab

binds to TNF

32

What is certolizumab used to treat

RA and Crohn's

33

What is golumumab used to treat

RA
ulcerative colitis
psoriatic arthritis

34

What is the mechanism behind anakinra

blocks the IL-1 receptor

35

What condition is anakinra used to treat

RA

36

What is the method of administration of anakinra

subQ

37

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

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

38

What is the mechanism behind rilonacept

binds to IL-1 molecule

39

This was the first drug that allowed transplantation to work properly

cyclosporine

40

What conditions is cyclosporine used for now

transplantation
psoriasis
dry eye

41

What is the mechanism behind cyclosporine

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

42

What is cyclosporine metabolized by

P450

43

What are the side effects of cyclosporine

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

44

What is the mechanism behind tacrolimus

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

45

Which is more efficacious, cyclosprine or tacrolimus

tacrolimus

46

What are the side effects of tacrolimus

nephrotoxicity
neurotoxicity
alopecia
diabetes

47

What is tacrolimus metabolized by

P450

48

What is the mechanism of glucocorticoids

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

49

What is the mechanism behind sirolimus and everolimus

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

50

What are the side effects of sirolimus and everolimus

renal toxicity
lung toxicity

51

What is the mechanism behind basilixumab

blocks the IL-2 receptor

52

What other drug is basilixumab used with

cyclosporine

53

What are some conditions to watch for with someone taking basilixumab

hypersensitivity reaction; hypotension
bronchospasm
pulmonary edema

54

What is the mechanism behind tofacitinib

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

55

What are the side effects of tofacinitinib

increase infection and malignancy

56

What kind of drug is azathioprine

pro-drug

57

What disorders is azathioprine used to treat

transplantation
RA
Crohn's

58

What is the mechanism behind azathioprine

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

59

What are the side effects of azathioprine

bone marrow depression leading to;
megalobalstic anemia
throbocytopenia
leukopenia

60

What conditions are mycophenolate mofetil used to treat

transplantation and lupus

61

What is the mechanism behind mycophenolate mofetil

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

62

What are the side effect of mycophenolate mofetil

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

63

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

methotrexate

64

What is the mechanism of methotrexate

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

65

What is dihydrofolate reductase necessary for?

the synthesis of dihydro-folic acid and tetrahydrofolic acid

66

What type of drug is leflunomide

prodrug that is converted to teriflunomide

67

What is the mechanism behind teriflunomide and leflunomide

inhibitors of pyrimidine synthesis
inhibiting the enzyme dihydro-orotate dehydrogenase

68

What are the side effects of leflunomide and teriflunomide

diarrhea
teratogen

69

How does leflunomide and teriflunomide affect P450

inhibits P450

70

This drug was first developed as a treatment for malaria

hydroxychloroquine

71

What is the mechanism of hydrochloroquine

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

72

What are the side effects of hydrooxychloroquine

GI dysfunction
severe dermatitis
irreversible retinal damage