Immunosuppressants Flashcards
(72 cards)
1
Q
general mechanism of immunosuppressants
A
- agents that block lymphocyte activation and proliferation
2
Q
how would you reduce acute transplant rejection?
A
- suppress cellular immunity
3
Q
why would you combine immunosuppressants?
A
- immunosuppressants are frequently combined to achieve greater efficacy with decrease toxicity
4
Q
what may occur with chronic immune suppression?
A
increased risk of infection and malignancy
5
Q
what are the 2 calcineurin inhibitors? what kind of toxicity is likely with both?
A
- cyclosporine
- tacrolimus (FK506)
- highly nephrotoxic
6
Q
cyclosporine–mechanism
A
- calcineurin inhibitor
- binds cyclophilin
- blocks T cell activaiton by preventing IL-2 transcription
7
Q
cyclosporine–use
A
- transplant rejection prophylaxis
- psoriasis
- rheumatoid arthritis
8
Q
cyclosporine–toxicity
A
-
nephrotoxicity
- hypertention
- hyperlipidemia
- neurotoxicity
- gingival hyperplasia
- hirsutism
9
Q
tacrolimus (FK506)–mechanism
A
- calcineurin inhibitor
- binds FK506 binding protein (FKBP)
- blocks T cell activation by preventing IL-2 transcription
10
Q
tacrolimus (FK506)–use
A
- transplant rejection prophylaxis
11
Q
tacrolimus (FK506)–toxicity
A
- similar to cyclosporine
- inc risk of diabetes and neurotoxicity
- no gingival hyperplasia or hirsutism
12
Q
Sirolimus (Rapamycin)–mechanism
A
- mTOR inhibitor
- binds FKBP
- blocks T cell activation and B cell differentiation by preventing response to IL-2
13
Q
Sirolimus (Rapamycin)–use
A
- kidney tranplant rejection prophylaxis
- drug eluting stents
14
Q
Sirolimus (Rapamycin)–toxicity
A
- “PanSirtopenia”–pancytopenia
- insulin resistance
- hyperlipidemia
-
not nephrotoxic
- “kidney sir-vives”
15
Q
what is sirolimus (rapamycin) synergistic with?
A
cyclosporine
16
Q
Daclizumab, basiliximab–mechanism
A
- monoclonal antibodies
- block IL-2R
17
Q
Daclizumab, basiliximab–use
A
- kidney transplant rejection prophylaxis
18
Q
Daclizumab, basiliximab–toxicity
A
- edema
- hypertension
- tremor
19
Q
azathioprine–mechanism
A
- antimetabolite precursor of 6-mercaptopurine
- “pronounce ‘azathiopurine’“
- inhibits lymphocyte proliferation by blocking nucleotide synthesis
20
Q
azathioprine–use
A
- transplant rejection prophylaxis
- rheumatoid arthritis
- Crohn disease
- glomerulonephritis
- other autoimmune conditions
21
Q
azathioprine–toxicity
A
- leukopenia
- anemia
- thrombocytopenia
22
Q
what degrades 6-MP?
A
xanthine oxidase
23
Q
what increases the toxicity of azathioprine?
A
allopurinol
24
Q
mycophenolate mofetil–mechanism
A
- reversibly inhibits IMP dehydrogenase
- prevents purine synthesis of B and T cells
25
mycophenolate mofetil--use
* transplant rejection prophylaxis
* lupus nephritis
26
mycophenolate mofetil--toxicity
* GI upset
* pancytopenia
* hypertension
* hyperglycemia
* less nephrotoxic and neurotoxic
27
what is mycophenolate mofetil associated with?
* invasive CMV infection
28
corticosteroids--mechanism
* inhibit NF-kappaB
* suppress both B and T cell function by decrease transcriptionof many cytokines
* induce apoptosis of T lymphocytes
29
corticosteroids--use
* transplant rejection prophylaxis
* many autoimmune and inflammatory disorders
30
corticosteroids--toxicity
* hyperglycemia
* osteoporosis
* central obesity
* muscle breakdown
* psychosis
* acne
* hypertension
* cataracts
* avascular necrosis (femoral head)
31
what can result due to taking corticosteroids?
iatrogenic Cushing syndrome
32
what is the clinical use of Aldesleukin (IL-2)?
* renal cell carcinoma
* metastatic melanoma
33
what is the clinical use of epoetin alfa (erythropoietin)?
* anemias (especially in renal failure)
34
what is the clinical use of filgrastim (G-CSF)?
* recovery of bone marrow
35
what is the clinical use of sargramostim (GM-CSF)?
* recovery of bone marrow
36
what is the clinical use of IFN-alpha?
* chronic hepatitis B and C
* Kaposi sarcoma
* malignant melanoma
37
what is the clinical use of IFN beta?
* multiple sclerosis
38
what is the clinical use of IFN gamma?
* chronic granulomatous disease
39
what is the romiplostim, eltrombopag (thrombopoietin receptor agonists)?
* thrombocytopenia
40
what is the oprelvekin (IL-11)?
* thrombocytopenia
41
name the therapeutic antibodies for cancer therapy
* alemtuzumab
* bevacizumab
* cetuximab
* rituximab
* trastuzumab
42
alemtuzumab--target
* CD52
43
alemtuzumab--use
* CLL
* "A**lym**tuzumab"--chronic **lym**phocytic leukemia
* MS
44
bevacizumab--target
* VEGF
45
bevacizumab--use
* colorectal cancer
* renal cell carcinoma
46
cetuximab--target
* EGFR
47
cetuximab--use
* stage IV colorectal cancer
* head and neck cancer
48
rituximab--target
* CD20
49
rituximab--use
* B cell non Hodgkin lymphoma
* CLL
* rheumatoid arthritis
* ITP
50
trastuzumab--target
* HER2/neu
* HER**2**--"tras**2**zumab"
51
trastuzumab--use
* breast cancer
52
name the therapeutic antibodies for autoimmune disease therapy
* adalimumab, certolizumab, infliximab
* eculizumab
* natalizumab
53
adalimumab, certolizumab, infliximab--target
* soluble TNF alpha
54
adalimumab, certolizumab, infliximab--use
* IBD
* rheumatoid arthritis
* ankylosing spondylitis
* psoriasis
55
etanercept--type of drug
* decoy TNF alpha receptor
* not a monoclonal antibody
56
eculizumab--target
* complement protein C5
57
eculizumab--use
* paroxysmal nocturnal hemoglobinuria
58
natalizumab--target
* alpha 4 integrin
* WBC adhesion
59
natalizumab--use
* multiple sclerosis
* Crohn dz
60
what are patients with JC virus at risk of if given natalizumab?
* PML
61
abciximab--target
* platelet glycoprotein **IIb/IIIa**
* ****"**IIb** times **IIIa** equals 'ab**six**imab'"
62
abciximab--use
* antiplatelet agent for prevention of ischemic complication in patients undergoing percutaneous coronary intervention
63
denosumab--target
* RANKL
* den**os**umab affects **os**teoclasts
64
denosumab--use
* osteoporosis
* inhibits osteoclast maturation
* mimics osteoprotegerin
65
digoxin immune Fab--target
* digoxin
66
digoxin immune Fab--use
* antidote for digoxin toxicity
67
omalizumab--target
* IgE
68
omalizumab--use
* allergic asthma
* prevents IgE binding to FcERI
69
palivizumab--target
* RSV F protein
70
palivizumab--use
* RSV prophylaxis for high risk infants
* "pali**vi**zumab--**vi**rus"
71
ranibizumab, bevacizumab--target
* VEGF
72
ranibizumab, bevacizumab--use
* neovascular age related macular degeneration
