NSAIDS Flashcards
Aspirin
NSAID
++analgesic +antipyretic + GI bleed
Irreversible inhibitor of COX1 & COX2 by phosphorylating serine @ 502
Prophylactically for MI 75mg/day
SE - Reyes Syndrome (rare acute encephalopathy in kids) so c/i in pts <20yrs, Gout bc conjugation with salicylate makes it compete with uric acid so more uric acid left in body, salicylism (tinnitus, deafness, vertigo) @ high doses. Also be careful using in asthma and diabetics.
NOT to be used with WARFARIN. or METHOTREXATE bc induces its secretion in tubule of kidney
Can be given with misoprostol (PGE1 analog) or PPI to reduce GI disturbance
SE of NSAIDS
PGE for neuron sensitivity (pain), mucosa production in stomach, GFR, antiinflammation, fever
PGI from vECs for GFR, vasodilation (antiinflammation)
PGD from mast cells for vasodilation
TX2 from platelets for platelet aggregation
If we inhibit COX1 we inhibit all including TXA2
Good effects - blood thinning
SE - see below for COX2 PG inhibition effects
If we inhibit COX2 we inhibit the PGs
Good effects - reduce fever & pain relief (sensitivity to neurons)
SE - Hypersensitivity (asthma) bc more leukotrienes, Reduced renal BF, sodium and water retention (bc decrease renin release), GI disturbance/bleed, prolong gestation/inhibit labour
Ibuprofen
NSAID
+analgesic +anti-inflammatory +antipyretic +GI bleed
Competitive inhibitor of COX1 & COX2. Fast onset. Better tolerated than aspirin and indomethacin
NOT to be used with ASPIRIN - will reduce its cardioprotective effects
Naproxen
NSAID
similar to ibuprofen but has WARNING for GI bleed
Sold as “Vimovo” with PPI
Indomethacin
NSAID
+++anti-inflammatory
serious GI disturbance
Sulindac
Prodrug NSAID
better tolerated than indomethacin
Converted to active form Sulindac Sulfide by liver enzymes/colonic bacteria - nonselective for COX1 and COX2
Paracetamol
NSAID
+analgesic +antipyretic only
COX2 selective - only one other than COXIBS
NAPQI toxicity if overdose (bc glutathione depletion) so c/i in liver disease & heavy alcohol consumption (bc alcohol is CYP inducer so more NAPQI buildup) TOXIC DOSE is LOWER in CHRONIC ALCHOHOLICS
DDI - CYP inducers - cigarettes, barbiturates, phenytoin, carbamazepine, rifampicin, alcohol
Treat toxicity: acetylcysteine (breaks down to glutathione) i.v. or oral methionine
Celecoxib & etoricoxib
COXIBS - new NSAIDs
COX2 selective
Used for OA, RA - orally administered
C/i in ulcer patients WARNING for cardiac patients
SE- GIT minor, dizziness, respiratory, psyche, increased BP
The only NSAID that is cardioprotective
Aspirin
The rest have slight increase risk of MI bc reduced PGI2
What to use for mild/moderate pain
paracetamol/ibuprofen
what to use for GI irritation
paracetamol, COXIB
What to use during pregnancy
paracetamol
GI toxicity is increased in patients that…
> 60yrs
multiple NSAIDS concomitantly
concomitant use of steroid (bc increased risk of GI bleed)
use >3mths
Hx PUD
cigarettes
alcohol
