Celecoxib Research Paper

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID). All COX-2 inhibitors are diaryl-5-membered heterocycles. Celecoxib has a central pyrazole ring and two adjacent phenyl substituents, one containing a methyl group and the other a polar sulfonamide moiety; the sulfonamide binds to a distinct hydrophilic region that is present on COX-2 but not COX-1.

The COX-2 inhibitors have analgesic, antipyretic and inflammatory activity comparable to NSAIDs and are used therapeutically in OA, RA, acute pain andprimary dysmenorrhea. These compounds produce less GI ulceration and hemorrhage than NSAIDs due to their COX-2 selectivity. Also they do not inhibit platelet aggregation and have minimal renal and CV side effects. These drugs should not be used in 3rd trimester of pregnancy since they promote closure of ductus arteriosus.
Celecoxib is more acidic (sulfonamide versus sulfone). Besides, it is highly bound by plasma proteins. Celecoxib contains only one functional group that is efficiently metabolized, the benzylic methyl. Drug inactivation and clearance are caused by complete oxidation and conjugation at this position.

Both COX-2 inhibitors have a relatively long duration of action (>10 hours) because of relatively slow clearance. Both compounds display somewhat balanced excretion and celecoxib is eliminated primarily in the feces. Some of these drugs (valdecoxib) are also weak inhibitors of cytochromic