Exam 2- Lecture 20 & 21 NSAIDS Flashcards
what is the most abundant and important precursor of eicosanoids?
arachidonic acid
arachidonic acid is released from membrane phospholipids by what molecule?
phospholipase A2 (PLA2)
arachidonic acid is an omega ___ ?
6
are eicosanoids long-lived or short-lived mediators?
short-lived (seconds to minutes)
PGE2 function on blood vessels, bronchi, uterus?
dilation; dilation; oxytocic dilation
PGF2α function on blood vessels, bronchi, uterus?
constriction; constriction; oxytocic constriction
PGI2 function on blood vessels and platelets?
dilation; inhibits aggregation
TXA2 function on blood vessels and platelets
constriction; aggregation
eicosanoids bind to what receptors?
GPCRs
PGH synthase has what two enzyme activities?
cyclooxygenase (COX) and hydroperoxidase activities
of the 2 isoforms of PGH synthase, which is constitutively expressed in various tissues?
PGH synthase-1
of the 2 isoforms of PGH synthase, which is expressed upon stimulus in inflammatory and immune cells?
PGH synthase-2
which isoform of PGH-synthase has “housekeeping” functions?
PGH synthase-I
PGH synthase is inhibited by what class of drugs?
NSAIDs
alprostadil use
erectile dysfunction by injection or as suppository (it relaxes smooth muscles and expands blood vessels)
misoprostol use (3 of them)
cytoprotective, prevents peptic ulcer, terminates early pregnancy in combination with mifepristone (RU-486)
latanoprost is a derivative of
a. PGE2
b. PGF2α
c. PGI2
d. TXA2
b. PGF2α
prostacyclin (eproprostenol) use
treat pulmonary arterial hypertension by IV injection or inhalation
prostacyclin is similar to what molecule:
a. PGE2
b. PGF2α
c. PGI2
d. TXA2
c. PGI2
NSAIDs mechanism of action (2 of them, slide 16)
-inhibition of prostaglandin endoperoxide H synthase (PGHS or COX), which catalyzes the formation of prostaglandins
-many NSAIDs inhibit both COX-1 and COX-2 receptors
5 classes of NSAIDs to know
-salicylates
-arylacetic acids
-arylpropionic acids
-non-carboxylate NSAIDs
-COX-2 selective NSAIDs
aspirin is in which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
a. salicylates
ibuprophen is in which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
b. aryl propionic acids
meloxicam is in which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
d. non-carboxylate NSAIDs
celecoxib is in which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
e. COX-2 selective NSAIDs
indomethacin is in which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
c. aryl acetic acids
rank these NSAIDs from most to least GI side effects:
naproxen, indomethacin, sulindac, aspirin
aspirin ~ indomethacin > naproxen > sulindac
why does sulindac have few adverse GI side effects?
it is a prodrug
Reye’s syndrome is specific to which class of NSAIDs?
a. salicylates
b. aryl propionic acids
c. aryl acetic acids
d. non-carboxylate NSAIDs
e. COX-2 selective NSAIDs
a. salicylates
what is Reye’s syndrome?
rare, acute, life-threatening condition characterized by vomiting, delirium, and coma (20-30% mortality)
to reduce chance of Reye’s syndrome, what medicine should not be given to anyone under the age of 12 who has a fever?
aspirin
prevention of GI side effects (slide 21, 3 of them)
-misoprostol
-proton pump inhibitors
-combination products (ex. naproxen/esomeprazole)