Celecoxib properties

Rao, C.V., Cooma, I., Simi, B., Maiming, P.T., Connor, J.R. and Reddy, B.S., Chemopreventive properties of a selective inducible nitric oxide synthase inhibitor in colon carcinogenesis, administered alone or in combination with celecoxib, a selective cyclooxygenase-2 inhibitor. Cancer Res., 62, 165, 2002. 

In a similar study, Mamdani et al. conducted a retrospective cohort study from 1998- 2001 with NSAID naive elderly patients who had either celecoxib, ro-fecoxib, naproxen, or other non-naproxen NSAIDs. [155] Prior to adjusting compared to the community group there was a significant increased risk of AMIs for all NSAIDs except naproxen which only trended towards an increase. But once the values were adjusted for comparison to their controls none of the groups had an increased risk that was significantly different than the controls. This study was designed to determine if naproxen had would decrease the risk of AMIs and they concluded that naproxen has no cardioprotective properties. This study also showed an increased risk of AMI for high dose ibuprofen. 

The sulfonamide can have superior bioavailability and physicochemical properties that are manifested in greater in vivo efficacy in the anti-inflammatory models. Celecoxib has incorporated the sulfonamideas a balance of selectivity and in vivo efficacy. The JTE-522 compound (73)introduced a flu-... 

Initially this increased risk of myocardial infarction was attributed to the myocardial protective properties of the nonselective COX inhibitors. COX-2 selective inhibitors may lack this protective capability. Later meta analysis suggested that the degree of myoprotection associated with naproxen could not account for the difference in the incidence of myocardial infarction. Merck, the maker of rofecoxib, withdrew the drug from the market because of this association. The other two coxibs, celecoxib and lumiracoxib, remain on the market as no similar increase in myocardial infarction has been associated with these drugs. It must be stated here that there is controversy regarding this issue and only time will provide the ultimate answer regarding the car-diotoxic potential of these two coxibs. 

Koki, A.T., and Masferrer, J.L. (2002) Celecoxib A Specific COX-2 Inhibitor with Anticancer Properties, Cancer Control 9, 28-35. 

Andrews GP, Abu-Diak O, Kusmanto F, Hornsby P, Hui Z, Jones DS (2010) Physicochemical characterization and drug-release properties of celecoxib hot-melt extruded glass solutions. J Pharm Pharmacol 62 1580-1590... 

NSAIDs can be classified on the basis of their COX inhibitory and selective properties. Most NSAIDs inhibit both COX-1 and COX-2 to some extent. Most are mainly COX-1 inhibitory, e.g., aspirin, ibuprofen, diclofenac, naproxen, while some are COX-2 inhibitory, e.g., celecoxib, rofecoxib, and lumiracoxib. Vane et al. established the relative inhibitory potencies of NSAID COX-1 and COX-2 inhibitors. NSAIDs with the highest gastrointestinal toxicity have the highest COX-1 selectivity. 

B. Cappello, C. di Maio, M. lervolino, and A. Miro, Combined effect of hydroxypropyl methylcellulose and hydroxypropyi p-cyclodextrin on physicochemical and dissolution properties of celecoxib, /. Incl. Phenom. Macrocycl. Chem., 59,237-244,2007. 

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