Immunologic pharmacotherapies

Question 1

why are immunosuppressants frequently combined in therapeutic regimens

Answer 1

to increase efficacy with lower toxicity

Question 2

what kind of immunity do immunosuppressants inhibit

Answer 2

cellular immunity; lymphocyte activation and proliferation is inhibited

Question 3

what are the risks of chronic immunosuppression

Answer 3

infection and malignancy

Question 4

what is the mechanism of action of cyclosporine

Answer 4

inhibits calcineurin by binding cyclophilin; blocks T cell activation by preventing IL-2 transcription

Question 5

what is cyclosporine used to treat

Answer 5

transplant rejection prophylaxis, psoriasis, rheumatoid arthritis

Question 6

what are the toxicities of cyclosporine

Answer 6

nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, hirsutism, gingival hyperplasia

Question 7

how does tacrolimus work

Answer 7

inhibits calcineurin by binding FK506 (FKBP) binding protein; blocks IL-2 transcription to prevent T-cell proliferation

Question 8

what is tacrolimus used for

Answer 8

transplant rejection prophylaxis

Question 9

what are the toxicities of tacrolimus

Answer 9

similar to cyclosporine, but no gingival hyperplasia or hirsutism (just nephrotoxicity, hypertension, hyperlipidemia, and hyperglycemia)

Question 10

how does sirolimus (rapamycin) work

Answer 10

binds FKBP to inhibit mTOR; blocks T cell activation and B cell differentiation by preventing IL-2 signal transduction

Question 11

what is sirolimus (rapamycin) used for

Answer 11

kidney transplant rejection prophylaxis

Question 12

what are the toxicities of rapamycin

Answer 12

edema, hypertension, tremor

Question 13

how does azathioprine work

Answer 13

precursor of 6-mercaptopurine; inhibits lymphocyte proliferation by blocking nucleotide synthesis

Question 14

what is azathioprine used for

Answer 14

transplant rejection prophylaxis, rheumatoid arthritis, Chron’s disease, glomerulonephritis, other autoimmune conditions

Question 15

what are the toxicities of azathioprine

Answer 15

leukopenia, anemia, thrombocytopenia

Question 16

what enzyme is responsible for degrading 6-MP and what drug blocks this enzyme leading to increased azathioprine toxicity

Answer 16

xanthine oxidase;

allopurinol increases toxicity by inhibiting xanthine oxidase

Question 17

how do glucocorticoids acts as immunosuppresants

Answer 17

inhibit NF-kappaB to decrease cytokine transcription and thereby suppress both B and T cell function

Question 18

what are glucocorticoids used for

Answer 18

transplant rejection prophylaxis (immune suppression), many autoimmune disorders, inflammation

Question 19

what are the toxicities of glucocorticoids

Answer 19

hyperglycemia, osteoporosis, central obesity, muscle breakdown, psychosis, acne, hypertension, cataracts and peptic ulcers,
(iatrogenic Cushing’s)

Question 20

what recombinant cytokine is used to treat anemias (especially in renal failure)

Answer 20

erythropoetin alpha

Question 21

what two recombinant cytokines are used to treat thrombocytopenia

Answer 21

thrombopoietin and oprelvekin (interleukin 11)

Question 22

which recombinant cytokines are used to treat bone marrow loss

Answer 22

filgrastim (G-CSF) and sargramostim (GM-CSF)

Question 23

what is aldesleukin and what does it treat

Answer 23

aldesleukin (interleukin-2) is a recombinant cytokine and is used to treat renal cell carcinoma and metastatic melanoma

Question 24

what is IFN-alpha used to treat

Answer 24

HBV, HCV (with ribavirin), Kaposi sarcoma, condyloma acuminatum, hairy cell leukemia, renal cell carcinoma, malignant melanoma

Question 25

what is IFN-beta used for?

IFN- gamma?

Answer 25

IFN-beta is used for MS

IFN-gamma is used for CGD

Question 26

what is the target of alemtuzumab and what does it treat

Answer 26

targets CD52; treats CLL

Question 27

what does bevacizumab target and what does it treat

Answer 27

targets VEGF; treats colorectal cancer and renal cell carcinoma

Question 28

what does cetuximab target and what does it treat

Answer 28

cetuximab targets EGFR (epidermal growth factor receptor)

cetuximab treats stage IV colorectal cancer, and head and neck cancer

Question 29

what does rituximab target and what does it treat

Answer 29

rituximab targets CD20

rituximab treats B-cell non-Hodgkin’s lymphoma, rheumatoid arthritis (with MTX), and ITP

Question 30

what does trastuzumab target and what does it treat

Answer 30

trastuzumab targets HER2/neu

trastuzumab treats breast cancer and gastric cancer

Question 31

what do infliximab and adalimumab target and what do they treat

Answer 31

infliximab and adalimumab target TNF-alpha

infliximab and adalimumab treat IBD, rheumatoid arthritis, ankylosing spondylitis and psoriasis

Question 32

what does natalizumab target and what does it treat

Answer 32

natalizumab targets alpha4-integrin

natalizumab treats MS and Chron disease

Question 33

what contraindication do you have to be wary of when using natalizumab

Answer 33

risk of PML in patients with JC virus because alpha4-integrin plays a role in leukocyte adhesion

Question 34

what does abciximab target and what does it treat

Answer 34

abciximab targets GP2b3a
abciximab is an antiplatelet agent used to prevent ischemic complications in patients undergoing percutaneous coronary intervention

Question 35

what does denosumab target and what does it treat

Answer 35

denosumab targets RANKL

denosumab treats osteoporosis by inhibiting osteoclast maturation (mimics osteoprotegrin)

Question 36

what does digoxin immune Fab target and what does it treat

Answer 36

it targets digoxin as an antidote to digoxin toxicity

Question 37

what does omalizumab target and what does it treat

Answer 37

omalizumab targets IgE and it is used to treat allergic asthma and to prevent IgE from binding to Fc-epsilon-RI (high affinity IgE receptor)

Question 38

what does palivizumab target and what does it treat

Answer 38

palivizumab targets the RSV F protein

palivizumab is used as prophylaxis for high-risk infants