Selective COX-2 Inhibitor -⁠ Meloxicam: Survey of Pharmacological Properties andClinical Experiences

Overview

Meloxicam belongs to the group of selective inhibitors of COX-2. Like piroxicam, meloxicam isa member of oxicams. Meloxicam differs from piroxicam mostly by its better tolerance and verylow incidence of adverse effects, which depends on its selective inhibition of COX-2 isoenzymeand thus on the inhibition of formation of inflammatory prostanoids. Simultaneously its minorinfluence on COX-1 results in a minor influence on PGE2 synthesis in the gastric mucosa.Similarly as other „classic“ NSAIDs, meloxicam exerts excellent anti-inflammatory, analgesic,and antipyretic effects which are mostly even more pronounced than those exerted by classicNSAIDs (such as diclofenac, ibuprofen and naproxen). Alike the above mentioned NSAIDs,meloxicam is also an effective inhibitor of the generation of oxyradicals released from humanpolymorphonuclear leukocytes during inflammation. Besides, meloxicam does not inhibitthromboxan A2 synthesis and therefore it is free of the effects on platelet aggregation. Inaddition, meloxicam exerts a suitable chemoprotective effect which may be used even in thetreatment of colorectal cancer.Meloxicam is well absorbed with high bioavailability from the GI tract. It is bound to plasmaproteins from 99% and its volume of distribution is limited to extracellular water only. However,significant concentrations are found also in the inflamed tissues.Meloxicam is an effective drug in the treatment of rheumatoid arthritis and osteoarthritis witha long-lasting disappearance of pain and with the improved quality of life.Meloxicam is very well tolerated. Incidence of adverse GI effects such as a perforation of thewall, ulceration and bleeding from the GI tract similarly as dyspepsia and abdominal pain,together with impairment of renal functions, is very rare when compared with the classicNSAIDs.

Key words:
selective COX-2 inhibitor -⁠ meloxicam -⁠ rheumatoid arthritis -⁠ osteoarthritis treatment.