NSAIDs Flashcards
What three symptoms do NSAIDs primarily treat? What diseases are they often used with?
Fever, pain, inflammation
Rheumatoid arthritis and osteoarthritis
What is the mechanism of NSAIDs?
Inhibition of prostaglandin synthesis by targeting COX 1 and COX 2
Which prostaglandin modulates gastric mucosal acid secretion, mucus levels, and blood flow?
PGE2
Which prostaglandin has vasodilatory properties?
PGI2
Which prostaglandins cause systemic fever, local heat, and pain?
PGE2 and PGI2
What do all of the prostaglandins cause?
Erythema
Which COX is constitutive and protective?
COX-1
Which COX is inducible and inflammatory?
COX-2
What does PUBS stand for?
Perforations, symptomatic ulcers, GI bleeds
What are the most common and frequently encountered side FX of NSAIDs?
Gastric or intestinal ulceration (inh of PGI2 and PGE2), disturbances in platelet function (inh of TxA2)
What is Stevens-Johnson syndrome?
Diffuse, severe, mucocutaneous eruption involving 2 or more mucosal surfaces w/ or w/o visceral involvement
What is the most popular reason people use aspirin?
Heart disease
What is mechanism of salicylates?
Nonselective inhibition of COX-1 and COX-2
Acetylsalicylic acid (Aspirin)
Covalently, irreversibly inhibits COX-1 and COX-2 and platelet aggregation
Inflammation, pain, fever, prophylaxis for thromboembolic conditions (prevents clot formation)
What toxicities are associated with aspirin?
CNS - highs and lows, respiratory alkalosis, respiratory acidosis, Reye’s syndrome (swelling of liver and brain)
Should children take aspirin?
NO
Acetaminophen (Tylenol)
Weak peripheral COX-1 and COX-2 antagonist
Decreases prostaglandins synthesis
Pain, fever
What are toxicities associated with acetaminophen?
Hepatic damage
Tylenol is toxic at ____ the therapeutic dose and fatal at ____ the therapeutic dose.
10x
20x
What do you administer for tylenol overdose?
N-acetyl-cysteine (Mucomyst) to replace hepatic glutathione and activated charcoal to decrease further absorption
What do you administer for aspirin overdose?
Sodium bicarb
Should alcoholics take acetaminophen?
NO - their liver function is impaired
Ibuprofen (Advil/Motrin) and Naproxen (Aleve)
Proprionic acid derivative that reversibly inhibits COX-1 and COX-2
Decreases prostaglandin synthesis
Pain - acute and chronic RA and osteoarthritis, reduce fever, anti-inflammatory
Indomethacin (Indocin)
Acetic acid derivative; reversibly inhibits COX-1 and COX-2, less prostaglandins made
Acute gouty arthritis, ankylosing spondylitis, promotes closure of patent ductus arteriosus in newborns, reduces fever, anti-inflammatory
Diclofenac (Cambia)
NSAID
Decreases arachidonic acid levels
Ketorolac (Toradol)
NSAID
Potent analgesic useful for post-op pain if trying to avoid narcotics and approved for parenteral administration
***coxib - Celecoxib (Celebrex)
***coxib - COX-2 specific inhibitor (minimizes risk of stomach ulcers)
NSAID - pain/inflammation
Increases risk of heart attack or stroke
What should we only use aspirin for?
Prophylaxis against thromboembolic disorders
