nsaids Flashcards
types of prostanoids
prostaglandin PGD2
PGE2
PGF2a
prostacyclin (PGI2)
thromboxane (TXA2)
how are prostanoids synthesized
phospholipid -> arachidonic acid (COX1/2) -> prostanoids
PGD2 effect
immune response
PGE2 effect
pain
PGF2a effect
constricts uterus SM
PGI2 effect
relaxes smooth vascular muscle
TXA2 produced by
platelets
how does aspirin act as an NSAID
inhibit COX1/2: binds to allosteric site -> enzymatic site blocked -> prostanoids not produced
effects of aspirin
anti inflammation
analgesic
anti pyretic
how aspirin act as anti inflammation
lowers:
vasodilation (redness, heating, edema)
vascular permeability (swelling)
pain (by inflamm)
how aspirin act as analgesic
blocks PGE which sensitizes pain signal
doesnt block nociceptor (pain receptor) activation
analgesic ceiling
how aspirin act as antipyretic
decreases PGE2 which adjusts the body’s thermostat, brings temp down to normal
how does aspirin act as an anti platelet drug and what are some effects
blocks cox1
PGI2: inhibits platelet agg (has nucleus)
TXA2: promotes platelet agg (no nucleus)
adverse effects of traditional nsaids
upset gastric, ulcer (cox1 inhibition)
non aspirin nsaids: incr risk stroke n heart attack
bleeding bc blood thinning
aspirin induced asthma: leukotriene induces bronchoconstriction
kidney failure
what are coxibs
cox 2 selective inhibitor
better for GI tract
doesnt inhibit cox1
eg celecoxib