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Flashcards in immunology - drugs Deck (68):
1

immunosuppressants - mechanism of action

agents that block lymphocyte activation and proliferation

2

immunosuppressants reduce acute transplant immunity by suppressing

cellular immunity

3

immunosuppressants - frequently combined to ...

achieve greater efficacy with decreased toxicity

4

immunosuppressants - chronic suppression -->

high risk of: 1. infection 2. malignancy

5

immunosuppressants - drugs

1. cyclosporine
2. tacrolimus
3. Sirolimus (Rapamycin)
4. Daclizumab
5. Basiliximab
6. Azathioprine
7. Mycophenolate mofetil
8. Corticosteroids

6

Cyclosporine - mechanism of action

binds cyclophilin --> the complex inhibits Calcineurin (a TCR downstream protein that activates NFAT, a TF, through de-phosphorylation) --> prevent IL-2 transcription
--> blocks T cell activation

7

Cyclosporine - clinical use

1. transplant rejection prophylaxis
2. psoriasis
3. RA

8

Cyclosporine - toxicity

1. Nephrotoxity
2. hypertension
3. hyperlipidemia
4. neurotoxicity
5. gingival hyperplasia
6. hirsutism

9

Tacrolimus - mechanism of action

binds FK506 --> the complex inhibits Calcineurin (a TCR downstream protein that activates NFAT, a TF, through de-phosphorylation) --> prevent IL-2 transcription
--> blocks T cell activation

10

Tacrolimus - clinical use

transplant rejection prophylaxis

11

Tacrolimus - side effects

1. diabetes
2. neuphrotoxic
3. neuroticity
4. hypertension

12

Tacrolimus and cyclosporine are both highly .... (side effect)

nephrotoxic

13

Sirolimus (Rapamycin) - mechanism of action

binds FKB --> the complex inhibits mTOR (IL-2R downstream) --> blocks T-cell activation and B-cell differentiation by preventing RESPONSE TO IL-2

14

Sirolimus (Rapamycin) - clinical use

1. kidney transplant rejection prophylaxis
2. also used in drug-eluting stents

15

A drug-eluting stent (DES) is a

peripheral or coronary stent placed into narrowed peripheral or coronary arteries --> slowly releases a drug to block cell proliferation --> prevents fibrosis + clots --> prevent restenosis

16

Sirolimus (Rapamycin) - side effects

1. pancytopenia
2. insulin resistance
3. Hyperlipidemia
NOT NEPHROTOXIC

17

Sirolimus (Rapamycin) is NOT (toxicity)

nephrotoxic

18

Sirolimus (Rapamycin) act synergic with

cyclosporine

19

Daclizumab - mechanism of action

monoclonal antibody that blocks IL-2R

20

Basiliximab - mechanism of action

monoclonal antibody that blocks IL-2R

21

Daclizumab, Basiliximab - clinical use

kidney transplant rejection prophylaxis

22

Daclizumab, Basiliximab - side effects

1. edema
2. hypertension
3. tremor

23

Azathioprine - mechanism of action

Antmetaboite precursor of 6-MP --> inhibit PRPP amidotransferase --> decrease de novo purine synthesis
--> inhibits lymphocyte proliferation

24

Azathioprine - toxicity

1. Myelosuppresion
2. GI. toxicity
3. Liver toxicity

25

Azathioprine and MP-6 are metabolized by

Xantine oxidase

26

Azathioprine - clinical use

1. Transplant rejection prophylaxis
2. RA
3. IBD
4. Glomerulonephritis
5. other autoimmune conditions

27

Mycophenolate mofetil - mechanism of action

Reversibly inhibits IMP dehydrogenase preventing purine synthesis of B and T cells

28

Mycophenolate mofetil - clinical use

1. Transplant rejection
2. lupus nephritis

29

Mycophenolate mofetil - toxicity

1. GI upset
2. pancytopenia
3. hypertension
4. hyperglycemia
5. Associated with invasive CMV infecion
LESS NEPHROTOXIC AND NEUROTOXIC

30

Corticosteroids as immunosuppressants - mechanism of action

1. Inhibit NF-kB --> suppress both B and T-cell function by decreased transcriptio nof many cytokines
2. induce apotptosis of T-lymphocytes

31

Corticosteroids as immunosuppressants - clinical use

1. Transplant rejection prophylaxis
2. many autoimmune disorders
3. many inflammatory disorders

32

Corticosteroids as immunosuppressants - toxicity

1. iatrogenic cushing
2. cataracts
3. avascular necrosis of femoral head

33

monoclanal antibodies against IL-2R

1. Daclizumab
2. Basiliximab

34

recombinant cytokines - agents

1. Aldesleukin (IL-2)
2. erythropietin (epoetin alfa)
3. Filgrastim (G-CSF)
4. Sargramostim (GM-CSF)
5. IFN-α
6. IFN-β
7. IFN-γ
8. Oprelvekin (IL-11)
9. Romiplostim, eltrombopag (thrombopoietin receptor agonists)

35

erythropoietin (epoetin alfa) - clinical use

anemias (esp in renal failure)

36

Granulocyte-colony stimuating factor (G-CSF) - drug and clinical use

Filgrastim
Recovery of bone marrow

37

IL-2 - drug and clinical use

Aldesleukin --> 1. Renal cell carcinoma
2. metastatic melanoma

38

Granulocyte/macrophage-colony stimuating factor(GM-CSF) - drug and clinical use

Sargramostin --> Recovery of bone marrow

39

interferons as drugs - clinical use

Interferons - α: 1. chronic hepatitis B, C 2. Kaposi sarcoma 3. hairy cell leukemia 4. condyloma acuminatum 5. renal cell carcinoma 6. malignant melanoma
Interferons - β: multiple sclerosis
Interferons - γ: chronic granulomatous disease

40

IL-11 - drug and clinical use

Oprelvekin --> thrombocytopenia

41

thrombopoietin receptor agonists - drugs and clinical use

Romiplostim, eltrombopag --> thrombocytopenia

42

immunosuppressants - drugs

1. cyclosporine
2. tacrolimus
3. Sirolimus (Rapamycin)
4. Daclizumab
5. Basiliximab
6. Azathioprine
7. Mycophenolate mofetil
8. Corticosteroids

43

Therapeutic antibodies for cancer (drug and target)

1. alemtuzumab --> CD52
2. bevacizumab --> VEGF
3. Cetuximab --> EGFR
4. Rituximab --> CD20
5. Trastuzumab (Herceptic) --> HER2/neu

44

Trastuzumab (Herceptic) - target and clinical use / toxicity

target: HER2/neu
1. HER-2 (+) breast cancer 2. Gastric cancer
SE: cardiotoxicity

45

Bevacizumab - target and clinical use

target: VEGF (inhibits angiogenesis)
1. Colorectal cancer
2. renal cell carcinoma
3. Neovascular age-related macular degeneration (Ranibizumab, Bevacizumab)

46

Bevacizumab - side effects

1. hemorrhage
2. blood clots
3. impaired wound healing

47

Cetuximab - target and clinical use

target: EGFR
1. Stage IV colorectal camcer (Wild type KRAS)
2. head and neck cancer

48

Cetuximab - side effects

1. Rash
2. elevated LFTs
3. diarrhea

49

Rituximab - target / clinical use

target: CD20
1. B cel non-Hodgkin 2. CLL 3. RA
4. Idiopathic thrombocytopenic purpura (ITP)
SE: increased risk for progressive multifocal leukoencephalopathy

50

alemtuzumab - target and clinical use

CD52
1. CLL 2. MC

51

Therapeutic antibodies for cancer (drug and target)

1. alemtuzumab --> CD52
2. bevacizumab --> VEGF
3. Cetuximab --> EGFR
4. Rituximab --> CD20
5. Trastuzumab (Herceptic) --> HER2/neu

52

Therapeutic antibodies for autoimmune disease therapy (drug and target)

1. Adalimumab --> Soluble TNF-α
2. Certolizumab --> Soluble TNF-α
3. Infliximab --> Soluble TNF-α
4. Eculizumab --> Complement protein C5
5. Natalizumab --> a4 integrin

53

monoclonal antibodies against TNF-α

1. Adalimumab
2. Certolizumab
3. Infliximab

54

monoclonal antibodies against TNF-α clinical use / SE

1. IBD
2. RA
3. Psoriasis
4. Ankylosing spondylitis
SE: predispose to: infection, including reactivation of latent TB

55

Etanercept - mechanism of action

fusion protein (receptor for TNF-A+IgG1 FC) produced by recombinant DNA (A DECOY) --> not antibody

56

eculizumab - target and clinical use

target: C5 protein
paroxysmal noctural hemogloinuria

57

Natalizumab - mechanism of action

target α4-integrin -WBC adhesion

58

Natalizumab - clinical use

1. MS
2. Crohn disease

59

Natalizumab - side effect

risk for PML in patients with JC virus

60

Abciximab - mechanism of action

monoclonal antibody against platelet glycoproteins IIb/IIIa

61

Abciximab - clinical use

antiplatelet agent for preventon of ischemic complications in patients undergoing percutaneous coronary intervention

62

Denosumab - mechanism of action / clinical use

monoclonal antibody against RANKL --> inhibits osteoclast maturation (mimics osteoprotegerin)
clinical use: osteoporosis

63

Digoxin immun Fab - mechanism of action and clinical use

monoclonal antibody against Digoxin
Antidote for digoxin toxicity

64

Omalizumab - mechanism of action and clinical use

monoclonal antibody against IgE --> prevent IgE bidning to FCεRI
allergic asthma

65

Palivizumab - mechanism of action / clinical use

monoclona antibody against RSV F protein
clinical use: RSV prophylaxis for high risk infants

66

monoclonal antibodies against VEGF

1. Ranibizumab
2. Bevacizumab

67

monoclonal antibodies against VEGF - clinical use

1. Neovascular age-related macular degeneration (Ranibizumab, Bevacizumab)
2. Colorectal cancer (Bevacizumab)
3. renal cell carcinoma (Bevacizumab)

68

monoclona antibody against CD52 - drugs and clinical use

Alemtuzumab
1. CLL 2. MS