Prostanoids and their inhibitors

Question 1

“prost” mean what kind of drugs

Answer 1

prostaglandin-related drugs

Question 2

Iloprost
Epoprostenol
Treprostinil

are what prostaglandin analogs

Answer 2

PGI2

Question 3

what do PGI2 analogs treat

Answer 3

pulmonary arterial hypertension (PAH)

Question 4

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

Answer 4

Alprostadil

Question 5

Alprostadil

Answer 5

PGE1 analog

Question 6

COX 1/2 inhibitor to close DA

Answer 6

Indomethacin

Question 7

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

Answer 7

Indomethacin

Question 8

methyl PGE1 analog

Answer 8

Misoprostol

Question 9

2 functions of Misoprostil (methyl PGE1 analog):

Answer 9

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

Question 10

Dinoprostone

Answer 10

PGE2 analog

Question 11

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

Answer 11

Dinoprostone

Question 12

Latanoprost

Answer 12

PGF2a analog

Question 13

this PGF2a analog is used to treat glaucoma

Answer 13

Latanoprost

Question 14

Carboprost

Answer 14

PGF2a analog used to treat postpartum hemorrhage and abortion

Question 15

I.V. acetaminophen and ketorolac are used when

Answer 15

post-morphine post-op pain

Question 16

the only COX-2 blocker still used

Answer 16

Celecoxib

Question 17

this COX-2 blocker is used to treat osteoarthritis

Answer 17

Celecoxib

Question 18

COX1/2 blocker used to treat fever

Answer 18

Ibuprofen

Question 19

COX1/2 blocker used to treat migraines

Answer 19

Naproxen

Question 20

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

Answer 20

Aspirin

Question 21

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

Answer 21

Aspirin

Question 22

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

Answer 22

Arachidonic Acid

Question 23

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

Answer 23

PLA2

Question 24

PGH synthase-1 aka

Answer 24

COX1

Question 25

COX 1 is found where

Answer 25

in most cells

Question 26

PGH synthase-2 aka

Answer 26

COX2

Question 27

COX2 constitutive expression is found where

Answer 27

neurons thick ascending loop (TAL) of kidney

Question 28

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

Answer 28

endothelial cells

Question 29

PGH synthase-3 aka

Answer 29

COX-3

Question 30

where is COX3 expressed

Answer 30

in CNS

Question 31

steps in synthesis of PGH2

Answer 31

1. Arachidonic acid to PGG2 by the COX's 2. PGG2 to PGH2 by HOX

Question 32

what prostaglandin activates platelets (COX1)

Answer 32

TxA2 (thromboxane A2)

Question 33

what prostaglandin activates VSMC, kidney, and brain

Answer 33

PGE2

Question 34

what prostaglandin activates endothelial cells (COX2) and platelets

Answer 34

PGI2

Question 35

what prostaglandin activates mast cells, and brain

Answer 35

PGD2

Question 36

what prostaglandin activates uterus and eye

Answer 36

PGF2a

Question 37

arachidonic acid to leukotrienes by what enzyme

Answer 37

5-LOX

Question 38

leukotriene that takes part in chemotaxis

Answer 38

leukotriene B4

Question 39

leukotriene that takes part in bronchospasm and vasoconstriction

Answer 39

leukotriene C4, D4, E4

Question 40

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

Answer 40

steroids

Question 41

Dexamethasone Budesonide

Answer 41

steroids that block PLA2

Question 42

COX2 selective inhibitor that has no GI bleeding

Answer 42

Celecoxib

Question 43

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

Answer 43

Aspirin

Question 44

non-selective CNS COX 3 inhibitor

Answer 44

acetaminophen

Question 45

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

Answer 45

Zileuton

Question 46

Montelukast Zafirlukast Pranlukast

Answer 46

leukotriene receptor blockers to tx asthma

Question 47

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

Answer 47

PGE2

Question 48

PGI2 aka

Answer 48

prostacyclin (think I like cyclops)

Question 49

misoprostol and mifepristone used in combination for what purpose

Answer 49

to induce abortion

Question 50

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

Answer 50

Furosemide

Question 51

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

Answer 51

NSAIDs negate furosemide function

Question 52

"tan prostitutes get falsies to attract"

Answer 52

PGF2a agonist LATANOPROST

Question 53

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

Answer 53

Latanoprost

Question 54

mechanism of action for NSAIDs

Answer 54

inhibit PGH synthase (COX)

Question 55

phase of drug development that deals with discovery

Answer 55

phase I

Question 56

phase of drug development that deals with preclinical studies

Answer 56

phase II

Question 56

phase of drug development that deals with clinical development

Answer 56

phase III

Question 56

phase of drug development that deals with market approval

Answer 56

phase IV

Question 57

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

Answer 57

PGI2

Question 58

what happens when PGI2 is inhibited in endothelial cells

Answer 58

vessel cannot dilate

Question 59

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

Answer 59

heart attack

Question 60

keratolyte used for tx of warts and eczema

Answer 60

salicylic acid

Question 61

acetylsalicylic acid

Answer 61

aspirin

Question 62

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

Answer 62

aspirin

Question 63

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

Answer 63

anti-inflammatory

Question 64

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

Answer 64

leukocyte infiltration

Question 65

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

Answer 65

anti-aggregant

Question 66

what is aspirin's role as an anti-aggregant

Answer 66

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

Question 67

2 main GI side effects of aspirin

Answer 67

ulcer, bleeding

Question 68

sx's of chronic salicylism

Answer 68

tinnitus, decrease in hearing, vertigo

Question 69

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

Answer 69

REYE Triad (REYE syndrome)

Question 70

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

Answer 70

REYE syndrome

Question 71

hepatocyte mitochondrial dysfunction to increased NH3 and then encephalopathy

Answer 71

REYE syndrome pathogenesis

Question 72

to dx REYE syndrome:

Answer 72

3 fold increase in ALT/AST and serum NH3

Question 73

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

Answer 73

acetaminophen

Question 74

N-arachidonoylphenolamine

Answer 74

agonist for TRPV1 and CB1 that minimizes pain

Question 75

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

Answer 75

N-acetylcysteine

Question 76

glutathione peroxidase cofactor

Answer 76

selenium (Se)