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