NSAIDs Flashcards
acetylsalicycliac acid
ASA
-aspirin
propionic acid
iboprofen
naproxen
indoleacetic acid
indomethacin
etodolac
hereroaryl acetic acid
ketoralac
COX 2 selective NSAID
celecoxib
non-narcotic analgesic
acetaminophen
weak anti-inflammatory
acetaminophen
anti-inflammatory, analgesic, anti-pyretic
NSAIDs
analgesis, antipyretic
acetaminophen
NSAIDs MOA
inhibit COX - no PG synthesis
precursor to PG
arachidonic acid
free AA enters 1 of 2 pathways
- COX - PG synthesis
- lipoxygenase - leukotriene synthesis
COX1
most tissues present
housekeeping
COX2
undetectable in most tissue
increased during inflammation
irreversible inhibition of COX in platelets
aspirin
-used as anti-coag
analgesic effect
PGE2 sensitizes pain nerve endings
pyresis
cytokines, leukocytes, PGs in brain areas
vasodilation
PGE2 and PGI2
blocked by NSAIDs
apoptosis
PG inhibit apoptosis
NSAID - more apoptosis
used of NSAIDs and reduced risk of cancer
dose of aspirin for anticoag
low dose needed - 85-160mg/day
high dose aspirin
inhibit PGI2 - which is vasodilator and inhibitor of platelet
counterproductive for anticoag effect of aspirin
renal function and NSAIDs
decreased renal blood flow
decrease rate of glomerular filtration
can result - renal failure
reyes syndrome
CI for salicylates in children
with chicken pox of flu
chicken pox or flu
no aspirin or other salicylates in children
use ibuprofen or naproxen instead
NSAIDs other than aspirin
less side effect - particularly GI effects
dysmennorhea
PG - cause cramping
NSAID tx
closure of patent ductus arteriousus
indomethacin
preeclampsia and HTN in pregnancy
low dose aspirin
colorectal cancer
reduced risk with chronic aspirin use
burn off warts
topical salicyclic acid
NSAID pharmacokinetic
liver metabolism
kidney excretion
50-99% protein bound
aspirin admin
should be take with food
-toxic to stomach lining
analog of PGE1
misoprostol
-for chronic NSAID users
CNS action of aspirin
due to salicylic acid
aspirin does not cross BBB
low dose aspirin
retain uric acid
high dose aspirin
excrete uric acid
gout patient
should not use aspirin for analgesia - causes retaining of uric acid
anti-platelet dose of aspirin
160mg/day
analgesia/antipyretic aspirin
2600mg/day
anti-inflammatory aspirin
4000mg/day
toxic dose of salicylates
respiratory depression
ringing in ears
sign of salicylism - mild salicylate intoxication
also - nausea, vomiting, hyperventilation, HA, mental confusion, dizzymnes
third trimester of pregnancy
avoid aspirin and other NSAIDs
reduced birth weights
naproxen
best tolerated
longer half life - less dosing through day
tx rheumatoid arthritis, OA, ankylosing spondylitis, acute gout
indomethacin
suppress contraction in preterm labor
indomethacin
postop analgesia lasting 6-8 hours
etodolac
relatively COX2 selective
NSAID IM or IV
ketorolac
limit to 5 days - because of GI toxicity
selective COX2 inhibitor
celecoxib
COX2
expressed constitituvely in brain and kidney
target for anti-inflammation
COX1
in platelets
weak anti-inflammatory
acetaminophen
only weak COX inhibitor
acute overdose of acetaminophen
hepatotoxicity
tx of acetaminophen toxicity
N-acetylcysteine - restore liver glutathione levels
anti-leukotriene drugs
zafarlukast
montelukast