Leyka M. Barbosa, MD
COX-2 Inhibitors are a novel class of anti-inflammatory pain relievers, and are a subset of the NSAID’s. The first one available on the market was celecoxib (Celebrex), which was first introduced in November 1998. Rofecoxib (Vioxx) was the next medication in this class, introduced to the market in 1999, then removed in late 2004 by the manufacturer over safety concerns. Valdecoxib (Bextra) was released in 2002, and removed in early 2005, also over safety concerns. Celecoxib has been approved for use in osteoarthritis, rheumatoid arthritis, and acute pain therapies. They all have been proven effective for therapy in different types of arthritis, soft tissue injuries, and other situations in which pain relief and/or decreased inflammation are required.
The acronym COX stands for the cyclooxygenase enzymes, of which two subtypes have been identified. The COX-1 enzyme is associated with certain protective abilities, chiefly gastrointestinal, whereas the COX-2 enzyme is associated with fever, pain and inflammation. The traditional non-steroidal anti-inflammatory drugs (NSAID’s) block both COX-1 and COX-2, thus interfering with the beneficial activity of COX-1. By selectively blocking the activity of COX-2, celecoxib, rofecoxib, and valdecoxib can target the deleterious effects of COX-2 without interfering with the protective activity of the COX-1 enzyme.
The efficacy of these newer NSAID’s was defined by comparing them to pre-established NSAID’s, such as ibuprofen, naproxen and diclofenac. Their safety profile has been extensively studied, with the most recent studies being CLASS, for celecoxib, and VIGOR, for rofecoxib. Newer related COX-2 inhibitors were being developed as well, but at this time (December, 2005) there is a question as to when and whether they will ever be approved and marketed. These derived medications offer parenteral access for pain relief, as well as the potential for being more effective and safer drugs.
Other pharmacological benefits have been associated with the COX-2 inhibitors. Celecoxib also has the indication for use in familial adenomatous polyposis (FAP), a hereditary condition that causes intestinal cancer, even at a young age. Studies are underway to find out if these compounds can be helpful in other conditions, such as Alzheimer's disease.
2020
JointCare.Org