Source: Health Products Regulatory Authority (ZA) Revision Year: 2012 Publisher: Aurogen South Africa (Pty) Ltd, Woodhill Office Park, Building 1, 53 Phillip Engelbrecht Avenue, Meyersdal, Ext. 12, 1448, Johannesburg, South Africa
A 3.1 Antirheumatics (anti-inflammatory agents)
Meloxicam, an oxicam (enolic acid) derivative, is a non-steroidal anti-inflammatory compound (NSAID) with analgesic, antipyretic and anti-inflammatory activities. The action of meloxicam is related to inhibition of the enzyme cyclo-oxygenase (COX), resulting in the decreased formation of prostaglandins (mediators of inflammation) and thromboxanes. A selective COX-2 inhibitory (antiinflammatory effect) in vitro in relation to COX-1 has been demonstrated. Inhibition of COX-1 (gastrointestinal, renal and platelet effects) in vivo occurs. It is suggested that the extent of inhibition of COX-1 in vivo is a function of dose and inter-individual variability of meloxicam concentrations.
The extent of absorption after oral administration is 89% and concomitant administration with food does not affect absorption. Meloxicam is 99% protein bound and has an elimination half-life of 15-20 hours. Meloxicam is extensively metabolized in the liver (mainly by oxidation) and less than 5% of the daily dose is excreted unchanged in the faeces and urine.
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