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Flashcards in Immunopharmacology Deck (65):
0

Mention the prototype immunophilin ligand?

Cyclosporine

1

What is the mechanism of action of cyclosporine?

The complex of cyclosporin-cyclophilin inhibits calcineurin.

2

What is the clinical use of cyclosporine?

1. Organ transplantation
2. GVH disease
3. Some autoimmunes

3

How is cyclosporine metabolized?

Via CYP450 (drug-drug interactions).

4

What are the 3 main side effects of cyclosporine?

1. Renal dysfuction
2. HTN
3. Neurotoxicity

5

What is tacrolimus?

Like cyclosporine but inhibits calcineurin by binding to FK506 immunophilin.

6

What is sirolimus and what is its mechanism of action?

A immunophilin ligand - binds to cyclophilin and inhibits the IL-2 pathway.

7

What are the main side effects of sirolimus?

1. Hypertriglyceridemia
2. Hepatotoxicity
3. Diarrhea
4. Myelosuppression

8

Mention 2 drugs similar to sirolimus?

1. Everolimus
2. Temsirolimus

9

Mention the prototype purine antagonist.

Mycophenolate mofetil

10

What is the mechanism of action of mycophenolate mofetil?

Blocks de novo GTP synthesis by inhibiting inosine monophosphate dehydrogenase.

11

What is the clinical use of mycophenolate mofetil?

1. Organ transplantation
2. GVH disease
3. Some autoimmunes

12

How is mycophenolate mofetil administered?

Orally or parenterally

13

What are the 2 main side effects of mycophenolate mofetil?

1. GI disturbances
2. Myelosuppression

14

What is the mechanism of action of thalidomide?

Complex immune effects including reduction in TNF-a production.

15

What is the clinical use of thalidomide?

1. Erythema nodosum leprosum
2. Multiple myeloma

16

How is thalidomide administered?

Orally

17

What are the side effects of thalidomide?

1. Teratogen
2. Somnolence
3. Peripheral neuropathy
4. Neutropenia

18

What is lenalidomide?

Thalidomide analog approved for multiple myeloma.

19

Mention the prototype CD-2 receptor blocker.

Alefacept

20

What is the mechanism of action of alefacept?

Binds to T-cell CD2 receptor and blocks its association with LFA-3.

21

What is the clinical use of alefacept?

Psoriasis

22

How is alefacept administered?

Parenterally (it is a recombinant protein)

23

What are the main side effects of alefacept?

1. Reduced T-cell count
2. Hepatotoxicity
3. Hypersensitivity reaction
4. Infection
5. Malignancy

24

Mention three types of immunosuppressive sera?

1. Antithymocyte globulin
2. Antilymphocyte globulin
3. Immune globulin IV

25

What is the mechanism of action of antithymocyte globulin?

Binds to T-cell and triggers complement-based cytotoxicity.

26

What is the clinical use of antithymocyte globulin?

Transplantation

27

How is antithymocyte globulin administered?

Parenterally

28

What are the side effects of antithymocyte globulin?

1. HSR
2. Injection site reaction
3. Malignancy

29

What is the antilymphocyte globulin?

Like antithymocyte globulin.

30

What is the immune globulin IV?

Immunoglobulin preparation of pooled IgG from healthy donors.

31

What is the clinical use of IGIV?

Wide range - immunodeficiencies and autoimmunes.

32

What is the mechanism of action of anti-Rho(D) antibody?

Prevents Rh sensitization by binding to Rh0(D) antigens.

33

What is the clinical use of Anti-Rho antibody?

Administered to Rho(D) negative mothers who carry a Rho(D) positive fetus.

34

How is the anti-Rho(D) antibody administered?

Parenterally

35

What are the main side effects of anti-Rho(D) antibody?

1. Injection-site reactions
2. Hemolysis if given to Rh-positive person

36

What is the prototype CD3 blocker?

Muromonab-CD3

37

What is the mechanism of action of muromonab-CD3?

MAb that inhibits cytotoxic T cells by binding to CD3.

38

What is the clinical use of muromonab-CD?

Allograft rejection

39

How is muromonab-CD3 administered?

Parenterally

40

What are the side effects of muromonab-CD3?

1. Anaphylactic reactions
2. Neuropsychiatric effects
3. HSR

41

What is the prototype IL-2 blocker?

Daclizumab

42

What is the mechanism of action of daclizumab?

MAb that blocks T-cell IL-2 receptor.

43

What is the clinical use of daclizumab?

Renal transplantation

44

How is daclizumab administered?

Parenterally

45

What are the side effects of daclizumab?

1. HSR
2. Infections
3. Malignancy

46

Mention a chimeric MAb similar to daclizumab.

Basiliximab

47

Mention 3 major anti-TNF-a agents.

1. Infliximab
2. Adalimumab
3. Etanercept

48

What is the mechanism of action of infliximab?

MAb binds to TNF-a and prevents it from activating TNF-a receptor.

49

What is the clinical use of infliximab?

1. Inflammatory bowel disease
2. RA
3. Ankylosing spondylitis
4. Psoriatic arthritis

50

How is infliximab administered?

Parenterally

51

What are the toxicities of infliximab?

1. HSR
2. Infection
3. Malignancy

52

Mention a human MAb similar to daclizumab.

Adalimumab

53

What is the etanercept?

Dimer of human TNF receptor fused to IgG constant region.

54

Mention the prototype recombinant IL-2.

Aldesleukin

55

What is the mechanism of action of aldesleukin?

Activates IL-2 receptors on T,B, and NK cells.

56

What is the clinical use of aldesleukin?

RCC and melanoma

57

How is aldesleukin administered?

Parenterally

58

What are the main side effects of aldesleukin?

1. Capillary leak syndrome
2. Exacerbation of preexisting inflammatory/autoimmune disease
3. HSR

59

Mention the 3 main interferons that are used.

Interferon-α-2a
Interferon-α-1b
Interferon-γ-1b

60

What is the mechanism of action of IFN-α-2a?

Enhances immune responses by activating IFN-α receptors.

61

What is the clinical use of IFN-α-2a?

1. Leukemia
2. Melanoma
3. HepB and C

62

How is IFN-α-2a administered?

Parenterally

63

What is the clinical use of IFN-α-1b?

MS

64

What is the clinical use of IFN-γ-1b?

Chronic granulomatous disease

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