Meloxicam: a selective COX-2 inhibitor non-steroidal anti-inflammatory drug

Expert Opin Investig Drugs. 1997 Mar;6(3):321-34. doi: 10.1517/13543784.6.3.321.


Meloxicam is a new non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits the inducible isoform of the cyclo-oxygenase (COX)-2 enzyme. This enzyme has a major role in mediating the inflammatory response, while synthesis of prostaglandins required for normal physiological functioning of the stomach and kidneys is under the control of the constitutive isoform, COX-1. Other NSAIDs in clinical use show varying degrees of selectivity towards COX-1. Only meloxicam and (albeit to a lesser extent) nimesulide could be described as selective for COX-2. In comparative trials of patients with osteo- and rheumatoid arthritis, meloxicam has been found to be at least as effective as other NSAIDs, but with a greatly reduced incidence of gastrointestinal side-effects. There is no evidence that meloxicam causes any deterioration in renal function in patients with moderate degrees of renal failure, and no evidence of drug accumulation with continued use. Meloxicam's half-life of 20 h makes it ideal for once daily administration, and it is 99% converted to inactive metabolites prior to excretion. No clinically significant drug interactions have been detected, making it suitable for use in patients with co-existing pathology. Meloxicam's safety and tolerability make it a significant advance in the treatment of rheumatic disease.