, Volume 71, Issue 18, pp 2457-2489


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Celecoxib (Celebrex®) was the first cyclo-oxygenase (COX)-2 selective inhibitor (coxib) to be introduced into clinical practice. Coxibs were developed to provide anti-inflammatory/analgesic activity similar to that of nonselective NSAIDs, but without their upper gastrointestinal (GI) toxicity, which is thought to result largely from COX-1 inhibition. Celecoxib is indicated in the EU for the symptomatic treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis in adults. This article reviews the clinical efficacy and tolerability of celecoxib in these EU-approved indications, as well as overviewing its pharmacological properties.

In randomized controlled trials, celecoxib, at the recommended dosages of 200 or 400 mg/day, was significantly more effective than placebo, at least as effective as or more effective than paracetamol (acetaminophen) and as effective as non-selective NSAIDs and the coxibs etoricoxib and lumiracoxib for the symptomatic treatment of patients with active osteoarthritis, rheumatoid arthritis or ankylosing spondylitis.

Celecoxib was generally well tolerated, with mild to moderate upper GI complaints being the most common body system adverse events. In meta-analyses and large safety studies, the incidence of upper GI ulcer complications with recommended dosages of celecoxib was significantly lower than that with non-selective NSAIDs and similar to that with paracetamol and other coxibs. However, concomitant administration of celecoxib with low-dose cardioprotective aspirin often appeared to negate the GI-sparing advantages of celecoxib over NSAIDs.

Although one polyp prevention trial noted a dose-related increase in cardiovascular risk with celecoxib 400 and 800 mg/day, other trials have not found any significant difference in cardiovascular risk between celecoxib and placebo or non-selective NSAIDs. Meta-analyses and database-derived analyses are inconsistent regarding cardiovascular risk. At recommended dosages, the risks of increased thrombotic cardiovascular events, or renovascular, hepatic or hypersensitivity reactions with celecoxib would appear to be small and similar to those with NSAIDs.

Celecoxib would appear to be a useful option for therapy in patients at high risk for NSAID-induced GI toxicity, or in those responding suboptimally to or intolerant of NSAIDs. To minimize any risk, particularly the cardiovascular risk, celecoxib, like all coxibs and NSAIDs, should be used at the lowest effective dosage for the shortest possible duration after a careful evaluation of the GI, cardiovascular and renal risks of the individual patient.

Various sections of the manuscript reviewed by: A. Lanas, University of Zaragoza. IIS Aragón, Zaragoza, Spain; F. McKenna, Rheumatic Diseases Unit, Trafford General Hospital, Manchester, UK; P. Patrignani, Department of Neuroscience and Imaging, “G. d’Annunzio” University and Center of Excellence on Aging (CeSI), Chieti, Italy; L.S. Simon, SDG LLC, Cambridge, MA, USA.

Data Selection

Sources: Medical literature (including published and unpublished data) on ‘celecoxib’ was identified by searching databases since 1996 (including MEDLINE and EMBASE and in-house AdisBase), bibliographies from published literature, clinical trial registries/databases and websites (including those of regional regulatory agencies and the manufacturer). Additional information (including contributory unpublished data) was also requested from the company developing the drug.
Search strategy: MEDLINE, EMBASE and AdisBase search terms were ‘celecoxib’ and (‘arthritis’ or ‘osteoarthritis’ or ‘rheumatoid arthritis’ or ‘arthritis, rheumatoid’ or ‘ankylosing spondylitis’ or ‘spondylitis, ankylosing’). Searches were last updated 16 November 2011.
Selection: Studies in patients with osteoarthritis, rheumatoid arthritis or ankylosing spondylitis who received celecoxib. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.
Index terms: Celecoxib, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability, pharmacoeconomics.