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immunosuppressants Flashcards

1
Q

cyclosporine inhibits

A

calcineurin

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2
Q

tacrolimus inhibits

A

calcineurin

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3
Q

calcineurin activates

A

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

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4
Q

cyclosporine binds to

A

cyclophilins which inhibits calcineurin

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5
Q

tacrolimus binds to

A

FK-506 binding protein which inhibits calcineurin

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6
Q

cyclosporine is metabolized by

A

P450

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7
Q

tacrolimus is metabolized by

A

P450

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8
Q

side effects of cyclosporine

A

nephrotoxicity (vasoconstriction of afferent/efferent arterioles
HTN

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9
Q

tacrolimus side effects

A

nephrotoxicity (vasoconstriction of afferent/efferent arterioles
HTN

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10
Q

cyclosporine can also cause

A

hyperuricemia
hyperglycermia
neurotoxicity

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11
Q

two unique side effects of cyclosporine

A
  1. gingival hyperplasia
  2. hirsutism
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12
Q

tacrolimus can also cause

A

hyperuricemia
hyperglycermia
neurotoxicity

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13
Q

sirolimus moa

A

inhibits mTOR by binding FK binding protein

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14
Q

sirolimus block response to

A

IL-2 in B/T cells

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15
Q

sirolimus (rapamycin) side effects

A

anemia
thrombocytopenia
hyperlipidemia
hyperglycemia

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16
Q

coronary stents (drug eluting stents) coated with

A

anti-proliferative drug that blunts scar tissue growth

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17
Q

methotrexate moa

A

mimics folic acid and inhibits dihydrofolate reductase

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18
Q

methotrexate side effects

A

myelosuppression
stomatitis/mucosisits (mouth soreness)

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19
Q

myelosuppression with methotrexate is reversible with

A

leucovorin

20
Q

mycopheolic acid inhibits

A

IMP dehydrogenase causing decreased DNA synthesis

21
Q

IMP dehydrogenase is rate limiting step in

A

purine synthesis in lymphocytes

22
Q

side effects of mycopheolic acid

A

N/V, cramping, abd pain

23
Q

cyclophosphamide powerful immunosuppressant used in

A

vasculitis, glomerulonephritis

24
Q

cyclophosphamide requires

A

bio activation by liver

25
Q

cyclphosphamide is a

A

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

26
Q

cyclophosphamide ultimately causes DNA to cross link causing

A

inhibition of DNA replication

27
Q

side effects of cyclophosphamide

A

myelosuppression
hemorrhagic cystitis

28
Q

cyclophosphamide toxic metabolite

A

acrolein

29
Q

cyclophosphamide can also cause

A

SIADH

30
Q

SIADH leads to

A

hyponatremia and possible seizures

31
Q

azathioprine is a prodrug converted to

A

6-mercaptopurine

32
Q

6-MP competes for binding to

A

hypoxanthine guanine phosphoribzosyltransferase (HGPRT)

33
Q

HGPRT is important for

A

synthesis of new purine nucleotides

34
Q

azathioprine side effects

A

anorexia, N/V, bone marrow suppression

35
Q

caution using azathioprine with

A

allopurinol (blunts metabolism of 6-MP)

36
Q

muromonab-CD3 is a

A

monoclonal antibody used in organ transplant

37
Q

muromonab-CD3 binds to

A

CD3 (T cells) and block activation

38
Q

muromonab-CD3 leads to

A

T cell depletion from circulation

39
Q

key side effect of muromonab-CD3

A

cytokine release syndrome

40
Q

infliximab is an antibody against

A

TNF alpha

41
Q

infliximab is used in

A

RA, crohns

42
Q

infliximab is

A

chimeric (both mouse and human components)

43
Q

risk of infliximab

A

reactivation of TB

44
Q

etanercept

A

decoy receptor for TNF alpha

45
Q

malaria drugs

A

chloroquine & hydroxychloroquine

46
Q

chloroquine & hydroxychloroquine block

A

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

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