Test 2 NSAIDs Flashcards
Aspirin
Irreversible inhibitor of COX-1 (primarily)/COX-2, rapidly metabolized to salicylic acid which is a reversible inhibitor.
Treatment of mild to moderate pain, inflammatory diseases, fever reduction, prophylactic prevention of cardiovascular events (unique to low-dose aspirin via inhibition of platelet TXA2 production), cancer chemoprevention (experimental)
Protein-bound
Tox: high doses lead to hyperthermia, hyperventilation, metabolic acidoses, hypoglycemia, cerebral edema, confusion, tremors, seizure, respiratory depression, coma, and death
Treat by alkalinizing urine
Ibuprofen
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
Rapid onset (15-30min), less GI bleeding than aspirin
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
Naproxen
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
Rapid onset (60min) and long serum half-life (14hrs), ideal for antipyretic use. Safest NSAID.
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
Oxaprozin
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
Very long serum half-life (50-60hrs), but slow onset of action. Useful for gout treatment.
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
Indomethacin
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
10-40x more potent than aspirin as anti-inflammatory agent. Not tolerated as well as ibuprofen (~50% of users experience side effects, ~20% discontinue). Used to promote closure of patent ductus arteriosus.
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
Ketorolac
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
IV analgesic for post-surgical pain. Used as a replacement for opioid analgesics like morphine.
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
Diclofenac
Competitive inhibitors of COX activity, non-selective (COX-1/COX-2)
Relatively selective for COX-2, increased heart/stroke risk similar to -coxibs (40% increase)
Anti-inflammatory, antipyretic, and analgesic
Use: Mild to moderate pain, fever, inflammation associated with rheumatoid arthritis, osteoarthritis, and acute gout
NSAID adverse effects
GI toxicity
Kidney impairment
Anti-platelet effect/increased risk of bleeding
Exacerbation of hypertension and heart disease
NSAID hypersensitivity
Pregnancy-related adverse effects (early ductus closure)
Aspirin and salicylic acid adverse effects
Reye’s syndrome (aspirin to young children and adolescents during a febrile viral infection)
Increased risk of gout (at low doses)
GI toxicity
Kidney impairment
Anti-platelet effect/increased risk of bleeding
Exacerbation of hypertension and heart disease
NSAID hypersensitivity
Pregnancy-related adverse effects (early ductus closure)
Celecoxib
COX-2 inhibitor
Anti-inflammatory, antipyretic, analgesic similar to NSAIDs
Treatment of rheumatoid arthritis and osteoarthritis
Good for patients with increased risk of GI complications and patients with increased risk of bleeding
Similar renal toxicities to traditional NSAIDs, potentially associated with increased risk of developing cardiovascular events, esp. at higher doses (not recommended as a first choice NSAID)
Inhibits CYP2C9 (warfarin metabolism)
Acetaminophen
Inhibits COX1/2 in CNS, weak COX-1/2 inhibitor in peripheral tissues (b/c of hydroperoxides)
Antipyretic and analgesic, (NOT an anti-inflammatory or anti-platelet)
Active metabolite (metabolized in brain) is AM404 –> also inhibits COX-2, as well as cannabinoid system (decreases pain and fever)
For pain not associated with inflammation, preferred for children with febrile viral infections, patients with peptic ulcers, hemophilia/increased risk of bleeding, and hypersensitivity to aspirin/NSAIDs.
Fewer adverse effects compared to aspirin/NSAIDs
Tox: Liver digesting to NAPQI when overwhelmed, normally NAPQI is cleared by glutathione, but if not then hepatic cell death. Treat with N-acetyl cysteine to replace glutathione.
