immunosuppressants

Question 1

cyclosporine inhibits

Answer 1

calcineurin

Question 2

tacrolimus inhibits

Answer 2

calcineurin

Question 3

calcineurin activates

Answer 3

NFAT (which is an imp transcription factor for many cytokines)

Question 4

cyclosporine binds to

Answer 4

cyclophilins which inhibits calcineurin

Question 5

tacrolimus binds to

Answer 5

FK-506 binding protein which inhibits calcineurin

Question 6

cyclosporine is metabolized by

Answer 6

P450

Question 7

tacrolimus is metabolized by

Answer 7

P450

Question 8

side effects of cyclosporine

Answer 8

nephrotoxicity (vasoconstriction of afferent/efferent arterioles
HTN

Question 9

tacrolimus side effects

Answer 9

nephrotoxicity (vasoconstriction of afferent/efferent arterioles
HTN

Question 10

cyclosporine can also cause

Answer 10

hyperuricemia
hyperglycermia
neurotoxicity

Question 11

two unique side effects of cyclosporine

Answer 11

1. gingival hyperplasia
2. hirsutism

Question 12

tacrolimus can also cause

Answer 12

hyperuricemia
hyperglycermia
neurotoxicity

Question 13

sirolimus moa

Answer 13

inhibits mTOR by binding FK binding protein

Question 14

sirolimus block response to

Answer 14

IL-2 in B/T cells

Question 15

sirolimus (rapamycin) side effects

Answer 15

anemia
thrombocytopenia
hyperlipidemia
hyperglycemia

Question 16

coronary stents (drug eluting stents) coated with

Answer 16

anti-proliferative drug that blunts scar tissue growth

Question 17

methotrexate moa

Answer 17

mimics folic acid and inhibits dihydrofolate reductase

Question 18

methotrexate side effects

Answer 18

myelosuppression
stomatitis/mucosisits (mouth soreness)

Question 19

myelosuppression with methotrexate is reversible with

Answer 19

leucovorin

Question 20

mycopheolic acid inhibits

Answer 20

IMP dehydrogenase causing decreased DNA synthesis

Question 21

IMP dehydrogenase is rate limiting step in

Answer 21

purine synthesis in lymphocytes

Question 22

side effects of mycopheolic acid

Answer 22

N/V, cramping, abd pain

Question 23

cyclophosphamide powerful immunosuppressant used in

Answer 23

vasculitis, glomerulonephritis

Question 24

cyclophosphamide requires

Answer 24

bio activation by liver

Question 25

cyclphosphamide is a

Answer 25

alkylating agents (adds alkyl group to N7 position of DNA)

Question 26

cyclophosphamide ultimately causes DNA to cross link causing

Answer 26

inhibition of DNA replication

Question 27

side effects of cyclophosphamide

Answer 27

myelosuppression hemorrhagic cystitis

Question 28

cyclophosphamide toxic metabolite

Answer 28

acrolein

Question 29

cyclophosphamide can also cause

Answer 29

SIADH

Question 30

SIADH leads to

Answer 30

hyponatremia and possible seizures

Question 31

azathioprine is a prodrug converted to

Answer 31

6-mercaptopurine

Question 32

6-MP competes for binding to

Answer 32

hypoxanthine guanine phosphoribzosyltransferase (HGPRT)

Question 33

HGPRT is important for

Answer 33

synthesis of new purine nucleotides

Question 34

azathioprine side effects

Answer 34

anorexia, N/V, bone marrow suppression

Question 35

caution using azathioprine with

Answer 35

allopurinol (blunts metabolism of 6-MP)

Question 36

muromonab-CD3 is a

Answer 36

monoclonal antibody used in organ transplant

Question 37

muromonab-CD3 binds to

Answer 37

CD3 (T cells) and block activation

Question 38

muromonab-CD3 leads to

Answer 38

T cell depletion from circulation

Question 39

key side effect of muromonab-CD3

Answer 39

cytokine release syndrome

Question 40

infliximab is an antibody against

Answer 40

TNF alpha

Question 41

infliximab is used in

Answer 41

RA, crohns

Question 42

infliximab is

Answer 42

chimeric (both mouse and human components)

Question 43

risk of infliximab

Answer 43

reactivation of TB

Question 44

etanercept

Answer 44

decoy receptor for TNF alpha

Question 45

malaria drugs

Answer 45

chloroquine & hydroxychloroquine

Question 46

chloroquine & hydroxychloroquine block

Answer 46

TLR in B cells and increase pH (causing decreased activity)