Immunosuppresive drugs

Question 1

6 general classes

Answer 1

1. corticosteroids
2. antiproliferative agents
3. agents that block T-cell activation
4. antibodies
5. fusion proteins
6. other

Question 2

2 uses for IS drugs

Answer 2

self - autoimmune

non-self - transplant

Question 3

4 ways to classify IS

Answer 3

1. action on one or multiple systems?
2. target in or outside of cell
3. action inside or outside of cell
4. large protein or small molecule

Question 4

what is effect of IS on cancer

Answer 4

some meds for cancer (hematologic) can be IS, but in other cases IS can cause malignancies

Question 5

2 risks with IS

Answer 5

1. infection - varies based on degree, type of infeciton

2. malignancy

Question 6

mech of action of glucocorticoids

Answer 6

bind to gluco-R and unreg or downreg gene transcription

Question 7

most common glucocort

Answer 7

PO - prednisone, many other routes of administration

Question 8

possible cort. dosing

Answer 8

1. pulse
2. high dose and taper
3. short course
4. chronic low dose
5. topical

Question 9

SE of corts.

Answer 9

HT, infection, hyperlipidemia, weight gain, skin chnages, osteopenia/porosis, muscle atrphy ……..

Question 10

what are antiproliferative agents

Answer 10

1. prevent proliferation of lymphocytes causing attack or rejection
2. bone marrow supression

Question 11

what is cyclophosphamide

Answer 11

alkylating agent used in oncology

• crosslinks with DNA - cell death
• SE = hematuria, neutropenia, ovarian failure

Question 12

main MOA in antiproliferatives

Answer 12

prevent DNA synthesis - cell can’t reporduce

Question 13

what is sirolimus

Answer 13

block mTOR - cell can;t progress from G1- s phase of mitosis

Question 14

what are calcineurin inhibitors

Answer 14

block T cell response by not allowing transcription of IL-2, so don’t get Tcell activaiton

Question 15

indications for calcineurin inhib.

Answer 15

1. transplant
2. glomerulonephritis
3. psoriasis
4. RA
5. opthalmic disease

Question 16

what is rationale behind AB use

Answer 16

find specific target to block in given disease (cell surface recptors, serum molecules)

Question 17

what are most antibody types in use

Answer 17

monoclonal - to specific antigen

Question 18

probs. with monocloncal antibodies (2)

Answer 18

1. anti AB AB can dev.

2. increases risk of infection and malignanacy

Question 19

what is a chimeric AB

Answer 19

part human and part mouse or other animal

Question 20

2 examples of mABs

Answer 20

Basiliximab - binds to IL-2 receptor on T-cell

Infliximab - and TNF AB, also leads to apop of TNF producing cells

Question 21

what is thymoglobin

Answer 21

• polyclonal AB
• against 40+ antigens
• mainly active against T-cell - prevent avtivation and binds and clears from that system
  SE = prolonged and profound lymphopenia

Question 22

what is IVIg

Answer 22

pooled immunoglobin from many donors

- multiple mech of action

Question 23

IVIg mechs

Answer 23

1. inhib ABs
2. inhibs complement
3. inhibs B-cells
4. inhibs adehesion molecules

Question 24

adv and dis of IVIg

Answer 24

well tolerated

• lo risk of infection or malig
• limited supply
• expensive

Question 25

what is fusion protien

Answer 25

join together - receptor to target antigen with Fc of an antibody

• cept

Question 26

MOA of fusion protein

Answer 26

prevents molecule from binding and activation

Question 27

what is etanercept

Answer 27

TNF blocker

- fusion of TNF -R and Fc IgG

Question 28

2 other types. of IS drugs

Answer 28

1. sulfa drugs - MOA unknown

2. hydrochloroquinine - for malaria