nsaids Flashcards

1
Q

types of prostanoids

A

prostaglandin PGD2
PGE2
PGF2a
prostacyclin (PGI2)
thromboxane (TXA2)

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2
Q

how are prostanoids synthesized

A

phospholipid -> arachidonic acid (COX1/2) -> prostanoids

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3
Q

PGD2 effect

A

immune response

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4
Q

PGE2 effect

A

pain

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5
Q

PGF2a effect

A

constricts uterus SM

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6
Q

PGI2 effect

A

relaxes smooth vascular muscle

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7
Q

TXA2 produced by

A

platelets

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8
Q

how does aspirin act as an NSAID

A

inhibit COX1/2: binds to allosteric site -> enzymatic site blocked -> prostanoids not produced

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9
Q

effects of aspirin

A

anti inflammation
analgesic
anti pyretic

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10
Q

how aspirin act as anti inflammation

A

lowers:
vasodilation (redness, heating, edema)
vascular permeability (swelling)
pain (by inflamm)

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11
Q

how aspirin act as analgesic

A

blocks PGE which sensitizes pain signal
doesnt block nociceptor (pain receptor) activation
analgesic ceiling

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12
Q

how aspirin act as antipyretic

A

decreases PGE2 which adjusts the body’s thermostat, brings temp down to normal

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13
Q

how does aspirin act as an anti platelet drug and what are some effects

A

blocks cox1
PGI2: inhibits platelet agg (has nucleus)
TXA2: promotes platelet agg (no nucleus)

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14
Q

adverse effects of traditional nsaids

A

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

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15
Q

what are coxibs

A

cox 2 selective inhibitor
better for GI tract
doesnt inhibit cox1
eg celecoxib

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16
Q

limitations of coxibs

A

GI tract not completely spared bc still got some cox1 inhibited

increased txa2 -> increased platelet agg -> higher risk HA n stroke

17
Q

advantages of paracetamol

A

good analgesic
good antipyretic
spares GI tract
relatively safe for pediatric use
few n uncommon side effects

18
Q

disadvantages of paracetamol

A

weak anti inflammatory
toxic dose leads to liver toxicity (hepatoxicity)