Anti-inflammatory cyclooxygenase-2 inhibitors

Anti-inflammatory Cyclooxygenase inhibitor, inhibits prostaglandin, prostacyclin, thromboxane biosynthesis Anti-inflammatory Cyclooxygenase inhibitor, inhibits prostaglandin, prostacyclin, thromboxane biosynthesis... 

Chapter 2. Anti-inflammatory Cyclooxygenase-2 Selective Inhibitors Celecoxib (Celebrex ) and Rofecoxib (Vioxx )... 

Anti-inflammatory cyclooxygenase-2 (COX-2) selective inhibitor celecoxib (Celebrex) has the tri-substituted pyrazole as its core structure. 

Not many pyrazoles and indazoles exist in nature. However, many synthetic medicines do contain pyrazoles, pyrazolones, and indazoles. For instance, an anti-inflammatory cyclooxygenase-2 (COX-2) selective inhibitor celecoxib (Celebrex) has the tri-substituted pyrazole as its core structure. A fully substituted pyrazole, rimonabant (Acomplia), is a selective inverse agonist for the cannabinoid receptor type 1 (CBi). Acomplia was marketed in 56 countries for the treatment of obesity by Sanofi-Aventis starting in... 

Unlike aspirin and other cyclooxygenase inhibitors that work on the COX-1 and COX-2 enzymes, acetaminophen works on the COX-3 enzyme, which is present in the spinal column and brain. This helps it to avoid shutting down prostaglandin function elsewhere in the body, which is why it has no anti-inflammatory effects and does not affect blood platelets or the stomach lining. 

Like aspirin, ibuprofen is a nonsteroidal anti-inflammatory drug. It is a cyclooxygenase inhibitor that interferes with COX-1 and COX-2 forms of that enzyme. Its effects on COX-2 give it fever-reducing (antipyretic), analgesic (pain relief), and anti-inflammatory functions. 

Zembowicz A, Mastalerz L, Setkowicz M, Radzis-zewski W, Szczeklik A Safety of cyclooxygenase-2 inhibitors and increased leukotriene synthesis in chronic idiopathic urticaria with sensitivity to nonsteroidal anti-inflammatory drugs. Arch Dermatol 2003 139 1577-1582. 

Non-steroidal anti-inflammatory drugs cyclooxygenase 2 inhibitors... 

Cyclooxygenase-2 (COX-2) Inhibitors and Non-steroidal Anti-Inflammatory Drugs (NSAIDs)... 

FIGURE 55-2. Treatment of osteoarthritis. OA, osteoarthritis COX-2, cyclooxygenase-2 CV, cardiovascular Gl, gastrointestinal, IA, intraarticular NSAID, nonsteroidal anti-inflammatory drug PPI, proton pump inhibitor. 

Aspirin, acetaminophen, and many other nonsteroidal anti-inflammatory drugs (e.g., Advil) are inhibitors of cyclooxygenase, COX. 

Tenidap (Figure 8.26) is a dual cyclooxygenase (COX) and 5-lipoxygenase (5-LPO) inhibitor developed as an anti-inflammatory agent. Severe abnormalities in hepatic function were reported in Japanese clinical trials [28]. Although the thiophene is not directly implicated in these findings, the ready activation of this system to potential reactive metabolites may be suggestive of the involvement of this function. 

Masferrer JL, Isakson PC, Seibert K. Cyclooxygenase-2 inhibitors. A new class of anti-inflammatory agents that spare the gastrointestinal tract. Gastroenterol Clin North Am 1996 25 363-372. 

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