1-OTC painkillers Flashcards

(37 cards)

1
Q

What are prostaglandins

A

sensitive nociceptors to the effects of other pain-causing stimuli

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2
Q

which NSAID is not anti-inflammatory

A

acetaminophen

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3
Q

name 5 examples of OTC NSAIDS

A

naproxen (aleve), ibuprofen (advil), acetylsalicytic acid (bayer aspirin), acetominophen (tylenol), diclofenac (voltaren)

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4
Q

what do CGRP and Substance P do

A

cause vasodilation and histamine release

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5
Q

what is the prostaglandin synthesis pathway

A

arachidonic acid released from cell membranes

COX enzymes turn them into PGH2

then they get isomerated into different compounds (TxA2, PGE2…)

A.A –COX12–> Prostaglandins

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6
Q

which COX promotes gastric mucous secretion

A

COX 1

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7
Q

which COX promotes inflammation

A

COX 2

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8
Q

which COX promotes platelet aggregation and vasoconstriction of vessels

A

COX 1

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9
Q

which COX is known for the good side effects of inhibition by NSAIDS

A

COX 2

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10
Q

which COX is known for the bad side effects of inhibition by NSAIDS

A

COX 1

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11
Q

first NSAID sold

A

acetylsalicytic acid (aspirin)

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12
Q

NSAID Structure (3 things)

A

weak acid with carboxy group, hydrophobic, non-specific

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13
Q

why is it good that NSAIDS are hydrophobic

A

allows them to enter active sites

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14
Q

what class is aspirin in

A

salicylate

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15
Q

what class is ibuprofen in

A

propionic

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16
Q

what class acetaminophen

17
Q

what class diclofenac

18
Q

what class naproxen

19
Q

how does aspirin work

A

irreversibly modifies COX enzymes by donating acetyl group to ser529 (cox1) and ser516(cox2)

20
Q

what are other NSAIDS competitive inhibitors of

A

arachidonic acid

21
Q

what do interleukins do

A

released from immune, induces COX2 in CNS and results in PGE2 formation

22
Q

where are PGE2 receptors found

23
Q

what does PGE2 activation in hypothalamus cause

24
Q

how do NSAIDS stop fever

A

dont let COX2 make PGE2 (interleukin pathway)

25
how do NSAIDS stop headache
reduction in prostaglandins that cause vasodilation
26
why can NSAIDS be bad to tummy
because they stop COX1 which make gstric mucose and inhibit acid secretion
27
what so special about celecoxib
COX2 inhibition 30:1 over COX1
28
why they make coxibs
so that you only get COX2 inhibition, but not really as good as you would want because it increases bad heart things
29
who has a bigger active site, COX1 or COX2
COX2
30
which drug is the leading cause of liver failure
acetaminophen tylenol!
31
what does acetaminophen get turned into in the liver
toxic metabolite NAPQI (by CYP enzymes)
32
how is acetaminophen's toxic metabolite usually detoxified
glutathione addition/conjugation
33
how is aspirin primarily used
decreasing thrombotic events by inhibiting thromboxane A2 in platelets
34
what is salicylism
symptoms from aspirin overdose
35
what is acetaminophen primarily used for now
analgesic and antipyretic, weak anti-inflammatory
36
how does acetaminophen work
inhibit COX3
37
which drugs boosts the endocannabinoid system
acetaminophen