Nonsteroidal anti-inflammatory drugs (
NSAIDs) reduce
pain and
inflammation by inhibiting the synthesis of
prostanoids. However, these drugs inhibit both
cyclooxygenase-1 (COX-1), which is essential for the regulation of homeostasis in many tissues, as well as COX-2, which is an important mediator of
pain and
inflammation. Disruption of COX-1 enzymatic activity by
NSAIDs leads to such side effects as interference with platelet functions and
gastric ulcers. The recent development of COX-2-specific inhibitors, such as
celecoxib, raises the possibility of relieving
pain and
inflammation with reduced risk of gastrointestinal complications. In Phase II and III studies,
celecoxib has demonstrated efficacy in alleviating dental
pain and the signs and symptoms of
osteoarthritis and
rheumatoid arthritis. This COX-2-specific inhibitor was also associated with a markedly lower rate of gastroduodenal injury than is seen typically with
NSAIDs. Incidence of most adverse events (including gastrointestinal) and withdrawal rates resulting from adverse events with
celecoxib were similar to placebo.
Celecoxib appears to be both safe and effective in the treatment of
osteoarthritis and
rheumatoid arthritis. Its COX-2-specific inhibitory properties thus introduce the possibility of effective relief of arthritic and other types of
pain and
inflammation with less risk of the mechanism-based toxicities observed with conventional
NSAIDs.