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PFM: Biweekly Exam 3 > Prostanoids and their inhibitors > Flashcards

Prostanoids and their inhibitors Flashcards

1
Q

“prost” mean what kind of drugs

A

prostaglandin-related drugs

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2
Q

Iloprost
Epoprostenol
Treprostinil

are what prostaglandin analogs

A

PGI2

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3
Q

what do PGI2 analogs treat

A

pulmonary arterial hypertension (PAH)

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4
Q

PGE1 analog that maintains temporary patency of Ductus Arteriosus in child being prepared for heart surgery

A

Alprostadil

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5
Q

Alprostadil

A

PGE1 analog

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6
Q

COX 1/2 inhibitor to close DA

A

Indomethacin

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7
Q

child with PDA (patent Ductus Arteriosus) is treated with this drug

A

Indomethacin

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8
Q

methyl PGE1 analog

A

Misoprostol

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9
Q

2 functions of Misoprostil (methyl PGE1 analog):

A
  1. treat aspirin induced ulcers
  2. treats postpartum hemorrhage (contracts uterus)
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10
Q

Dinoprostone

A

PGE2 analog

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11
Q

this PGE2 analog is used to ripen (open) cervix during labor

A

Dinoprostone

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12
Q

Latanoprost

A

PGF2a analog

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13
Q

this PGF2a analog is used to treat glaucoma

A

Latanoprost

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14
Q

Carboprost

A

PGF2a analog used to treat postpartum hemorrhage and abortion

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15
Q

I.V. acetaminophen and ketorolac are used when

A

post-morphine post-op pain

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16
Q

the only COX-2 blocker still used

A

Celecoxib

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17
Q

this COX-2 blocker is used to treat osteoarthritis

A

Celecoxib

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18
Q

COX1/2 blocker used to treat fever

A

Ibuprofen

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19
Q

COX1/2 blocker used to treat migraines

A

Naproxen

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20
Q

COX1/2 blocker (anti-aggregant effect) used for MI

A

Aspirin

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21
Q

COX1/2 blocker that worsens bronchoconstriction(don’t use it for asthma)

A

Aspirin

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22
Q

sits at the sn-2 position (the middle position of the glycerol backbone) of the phospholipid

A

Arachidonic Acid

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23
Q

what phospholipase splits arachidonic acid from the phospholipid it’s attached to

A

PLA2

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24
Q

PGH synthase-1 aka

A

COX1

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25
Q

COX 1 is found where

A

in most cells

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26
Q

PGH synthase-2 aka

A

COX2

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27
Q

COX2 constitutive expression is found where

A

neurons
thick ascending loop (TAL) of kidney

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28
Q

COX2 inducible expression is found in 4 places but what is the main one

A

endothelial cells

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29
Q

PGH synthase-3 aka

A

COX-3

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30
Q

where is COX3 expressed

A

in CNS

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31
Q

steps in synthesis of PGH2

A
  1. Arachidonic acid to PGG2 by the COX’s
  2. PGG2 to PGH2 by HOX
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32
Q

what prostaglandin activates platelets (COX1)

A

TxA2 (thromboxane A2)

33
Q

what prostaglandin activates VSMC, kidney, and brain

A

PGE2

34
Q

what prostaglandin activates endothelial cells (COX2) and platelets

A

PGI2

35
Q

what prostaglandin activates mast cells, and brain

A

PGD2

36
Q

what prostaglandin activates uterus and eye

A

PGF2a

37
Q

arachidonic acid to leukotrienes by what enzyme

A

5-LOX

38
Q

leukotriene that takes part in chemotaxis

A

leukotriene B4

39
Q

leukotriene that takes part in bronchospasm and vasoconstriction

A

leukotriene C4, D4, E4

40
Q

best anti-inflammatory drug b/c it targets the first step in breaking down arachidonic acid

A

steroids

41
Q

Dexamethasone
Budesonide

A

steroids that block PLA2

42
Q

COX2 selective inhibitor that has no GI bleeding

A

Celecoxib

43
Q

non-selective COX 1 and 2 inhibitor that is irreversible and causes GI bleeding

A

Aspirin

44
Q

non-selective CNS COX 3 inhibitor

A

acetaminophen

45
Q

drug that blocks 5-LOX to treat asthma (if 5-LOX is not inhibited, leads to bronchoconstriction and vasodilation)

A

Zileuton

46
Q

Montelukast
Zafirlukast
Pranlukast

A

leukotriene receptor blockers to tx asthma

47
Q

prostaglandin that causes
redness (rubor)
heat (calor)
pain (dolor)
swelling (tumor)

A

PGE2

48
Q

PGI2 aka

A

prostacyclin (think I like cyclops)

49
Q

misoprostol and mifepristone used in combination for what purpose

A

to induce abortion

50
Q

what drug induces COX2 in TAL to help with diuresis (increased production of urine w/ decreased water absorption in blood)

A

Furosemide

51
Q

patient on furosemide and doctor prescribes NSAIDs without knowing they are on furosemide: what happens

A

NSAIDs negate furosemide function

52
Q

“tan prostitutes get falsies to attract”

A

PGF2a agonist LATANOPROST

53
Q

PGF2a agonist that aids in ciliary m. relaxation and increased aqueous humor outflow

A

Latanoprost

54
Q

mechanism of action for NSAIDs

A

inhibit PGH synthase (COX)

55
Q

phase of drug development that deals with discovery

A

phase I

56
Q

phase of drug development that deals with preclinical studies

A

phase II

56
Q

phase of drug development that deals with clinical development

A

phase III

56
Q

phase of drug development that deals with market approval

A

phase IV

57
Q

COX2 inhibitor (celecoxib), blocks what synthesis in endothelial cells

A

PGI2

58
Q

what happens when PGI2 is inhibited in endothelial cells

A

vessel cannot dilate

59
Q

what can PGI2 inhibition by celecoxib eventually cause (from constant constriction by platelet TxA2 production)

A

heart attack

60
Q

keratolyte used for tx of warts and eczema

A

salicylic acid

61
Q

acetylsalicylic acid

A

aspirin

62
Q

acetylates serine on COX1 and 2 enzymes which prevents binding of arachidonic acid (no PGH’s made)

A

aspirin

63
Q

when aspirin is given at 1000mg q6-8 hrs, what effect is it producing

A

anti-inflammatory

64
Q

when aspirin is used as anti-inflammatory, what is NOT blocked

A

leukocyte infiltration

65
Q

when aspirin is given at 81mg/day, what effect is it producing

A

anti-aggregant

66
Q

what is aspirin’s role as an anti-aggregant

A

inhibits platelet aggregation/prevents synthesis of new PGH; lasts 8-10 days

67
Q

2 main GI side effects of aspirin

A

ulcer, bleeding

68
Q

sx’s of chronic salicylism

A

tinnitus, decrease in hearing, vertigo

69
Q

triad:
fatty liver degeneration
increased ALT, AST
encephalopathy (due to increased NH3)

A

REYE Triad (REYE syndrome)

70
Q

this syndrome is due to aspirin use and peaks at age 6-8

A

REYE syndrome

71
Q

hepatocyte mitochondrial dysfunction to increased NH3 and then encephalopathy

A

REYE syndrome pathogenesis

72
Q

to dx REYE syndrome:

A

3 fold increase in ALT/AST and serum NH3

73
Q

inhibits COX 3 in the brain and is tolerable for patients w/ peptic ulcers or asthma

A

acetaminophen

74
Q

N-arachidonoylphenolamine

A

agonist for TRPV1 and CB1 that minimizes pain

75
Q

acetaminophen toxicity treated with _____ that restores GSH (glutathione in hepatocytes)

A

N-acetylcysteine

76
Q

glutathione peroxidase cofactor

A

selenium (Se)

PFM: Biweekly Exam 3 (20 decks)

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