Return To The Previous Page
Buy a Package
Number Of Visible Items Remaining : -28 Item

Selected nonsteroidal anti-inflammatory drugs (NSAIDs) and other analgesics: Selectivity for cyclooxygenase 2 and potency in inhibiting gastric COX activity

Selected nonsteroidal anti-inflammatory drugs (NSAIDs) and other analgesics: Selectivity for cyclooxygenase 2 and potency in inhibiting gastric COX activity
  COX-2 selectivity* Gastric IC50 (micromolar)
NSAIDs
Ketoprofen 0.1 0.08
Ibuprofen 0.6 0.70
Indomethacin 0.7 0.85
Naproxen 1.0 0.52
Piroxicam 1.3 0.87
Ketorolac 1.5 0.33
Nabumetone 1.6 0.48
Etodolac 7.9 3.20
Celecoxib 9.2 11.14
Mefenamic acid 12.1 0.70
Nimesulide (not available in United States) 58.3 1.49
Other analgesics
Aspirin (acetylsalicylic acid) 0.3 0.03
Salsalate (salicylsalicylic acid) ≥2.8 >100
Acetaminophen 4.0 >100

6MNA: 6-methoxy-2-naphthylacetic acid; COX: cyclooxygenase; IC50: half-maximal inhibitory concentration; PG: prostaglandin.

* In whole blood assays in man. A number ≅1 indicates COX nonselectivity, while numbers much >1 indicate COX-2 selectivity. Values for nabumetone are for its active metabolite, 6MNA.

¶ Concentration of drug that inhibits human gastric mucosal COX activity by 50% and thus gastric mucosal PG production by 50%. The lower the IC50, the more potent the inhibition of gastric COX activity for a given drug.
Adapted from: Cryer B, Feldman M. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med 1998; 104:413.
Graphic 54253 Version 7.0