Gastrointestinal Ulceration Despite the COX-1-sparing property of the coxibs, concern remains as to whether they have the same potential to cause gastrointestinal (GI) ulcers as conventional week, randomized, placebo-controlled study, Kivitz et al. compared the risk of GI ulceration with valdecoxib 5, 10, and 20 mg four times a day (QD); naproxen 500 mg BID; [...]

Valdecoxib is metabolized via the cytochrome P(CYP)-450 system, pre dominately 3A4 and 2C9, as well as non-P450 systems, including approximately 20% glucuronidation. Valdecoxib has one metabolite that is excreted in the urine, but it has not been shown to have significant activity or to contribute to the drug’s profile. Because valdecoxib is a substrate for [...]

Valdecoxib is a 4-[5-methyl-3-phenylisox-azol-4-yl]-benzenesulfonamide that works by selectively inhibiting the cyclooxygenase-2 enzyme. The process begins with a stimulus, either inflammatory or physiological, causing the release of arachidondic acid from cell membrane phospholipids. Arachidonic acid is converted to prostaglandins (PG) through the enzyme prostaglandin G/H synthase, also known as cyclooxygenase (COX) or hydroperoxidase (HOX), as seen [...]

Valdecoxib (Bextra, Pharmacia) is the newest addition to the class of cyclooxygenase-2 inhibitors, which also includes celecoxib (Celebrex drug, Pharmacia/Pfizer Inc.) and rofecoxib (Vioxx, Merck). Valdecoxib received FDA approval in November 2001 for treating the signs and symptoms of osteoarthritis (OA) and adult rheumatoid arthritis (RA) and the treatment of pain associated with menstrual cramping [...]