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© 1996 British Society for Rheumatology

Pharmacology of Meloxicam, A New Non-Steroidal Anti-Inflammatory Drug with an Improved Safety Profile Through Preferential Inhibition of COX-2

G. Engelhardt

Dr Karl Thomae GmbH, Department of BiologicalResearch.D-88400 Biberach/Riss Germany

Correspondence to: Correspondence to: Professor Sir John Vane, The William Harvey Research Institute, Charter House Square, London EC1M 6BQ.


  Abstract

This review focuses on key pharmacological findings with a new NSAID, meloxicam. Unlike established NSAIDs, it preferentiallyinhibits inducible COX-2 in guinea-pig peritoneal macrophages and human COX-2 in COS cells. Compared with other NSAIDs,meloxicam is the most potent inhibitor of prostaglandin biosynthesis in pleural and peritoneal exudate, but only a weak inhibitor inthe gastric tract and kidney. Ulcerogenicity in the rat stomach is weak in relation to anti-inflammatory potency, resulting in a hightherapeutic index. Meloxicam's high anti-inflammatory potency combined with good tolerability can be explained by itspreferential inhibition of COX-2. In adjuvant arthritis rats, meloxicam inhibits not only paw swelling, but also bone and cartilagedestruction and systemic signs of disease. It inhibits leucocyte migration, but has no effect on leucotriene B4 or C4. Meloxicamshows a long-lasting anti-inflammatory and analgesic effect on inflammatory pain and reduces pyrogen-induced fever, but has nocentral nervous system effects. The pharmacokinetic profile of meloxicam in the rat is similar to that in man. Metabolites areinactive

KEY WORDS: Meloxicam, Anti-inflammatory, Cyclooxygenas, Pharmacology, Prostaglandins


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