1-OTC painkillers

Question 1

What are prostaglandins

Answer 1

sensitive nociceptors to the effects of other pain-causing stimuli

Question 2

which NSAID is not anti-inflammatory

Answer 2

acetaminophen

Question 3

name 5 examples of OTC NSAIDS

Answer 3

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

Question 4

what do CGRP and Substance P do

Answer 4

cause vasodilation and histamine release

Question 5

what is the prostaglandin synthesis pathway

Answer 5

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

Question 6

which COX promotes gastric mucous secretion

Answer 6

COX 1

Question 7

which COX promotes inflammation

Answer 7

COX 2

Question 8

which COX promotes platelet aggregation and vasoconstriction of vessels

Answer 8

COX 1

Question 9

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

Answer 9

COX 2

Question 10

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

Answer 10

COX 1

Question 11

first NSAID sold

Answer 11

acetylsalicytic acid (aspirin)

Question 12

NSAID Structure (3 things)

Answer 12

weak acid with carboxy group, hydrophobic, non-specific

Question 13

why is it good that NSAIDS are hydrophobic

Answer 13

allows them to enter active sites

Question 14

what class is aspirin in

Answer 14

salicylate

Question 15

what class is ibuprofen in

Answer 15

propionic

Question 16

what class acetaminophen

Answer 16

aminophenol

Question 17

what class diclofenac

Answer 17

acetic acid

Question 18

what class naproxen

Answer 18

propionic

Question 19

how does aspirin work

Answer 19

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

Question 20

what are other NSAIDS competitive inhibitors of

Answer 20

arachidonic acid

Question 21

what do interleukins do

Answer 21

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

Question 22

where are PGE2 receptors found

Answer 22

hypothalamus

Question 23

what does PGE2 activation in hypothalamus cause

Answer 23

fever

Question 24

how do NSAIDS stop fever

Answer 24

dont let COX2 make PGE2 (interleukin pathway)

Question 25

how do NSAIDS stop headache

Answer 25

reduction in prostaglandins that cause vasodilation

Question 26

why can NSAIDS be bad to tummy

Answer 26

because they stop COX1 which make gstric mucose and inhibit acid secretion

Question 27

what so special about celecoxib

Answer 27

COX2 inhibition 30:1 over COX1

Question 28

why they make coxibs

Answer 28

so that you only get COX2 inhibition, but not really as good as you would want because it increases bad heart things

Question 29

who has a bigger active site, COX1 or COX2

Answer 29

COX2

Question 30

which drug is the leading cause of liver failure

Answer 30

acetaminophen tylenol!

Question 31

what does acetaminophen get turned into in the liver

Answer 31

toxic metabolite NAPQI (by CYP enzymes)

Question 32

how is acetaminophen’s toxic metabolite usually detoxified

Answer 32

glutathione addition/conjugation

Question 33

how is aspirin primarily used

Answer 33

decreasing thrombotic events by inhibiting thromboxane A2 in platelets

Question 34

what is salicylism

Answer 34

symptoms from aspirin overdose

Question 35

what is acetaminophen primarily used for now

Answer 35

analgesic and antipyretic, weak anti-inflammatory

Question 36

how does acetaminophen work

Answer 36

inhibit COX3

Question 37

which drugs boosts the endocannabinoid system

Answer 37

acetaminophen