Source: Health Products Regulatory Authority (ZA) Revision Year: 2023 Publisher: PHARMACARE LIMITED, Healthcare Park, Woodlands Drive, Woodmead 2191
Category and class: A 3.1 Antirheumatics (anti-inflammatory agents)
Pharmacotherapeutic group: Anti-inflammatory and antirheumatic products, non-steroids, Oxicams
ATC code: M01AC06
Meloxicam is a non-steroidal anti-inflammatory medicine (NSAID) of the enolic acid class which has shown anti-inflammatory, analgesic and antipyretic properties. A common mechanism for the above effects may exist in the ability of meloxicam to inhibit the biosynthesis of prostaglandins, known mediators of inflammation.
The discovery of an inducible form of cyclooxygenase 2 (COX-2) whose expression is enhanced by inflammatory mediators has suggested that the COX-2 isoform might be responsible for production of prostaglandins at inflammatory sites.
Selective inhibition of COX-2 is anticipated to be related to the anti-inflammatory effect. A selective inhibition of cyclo-oxygenase-2 (COX-2) relative to cyclo-oxygenase-1 (COX-1) by meloxicam has been demonstrated.
COX-2 inhibition relates to the anti-inflammatory effects of NSAIDs whereas inhibition of constitutive COX-1 is thought to be responsible for gastric and renal side-effects.
Meloxicam is well absorbed from the gastrointestinal tract, which is reflected by a high absolute bioavailability of about 90% following oral administration.
Following single dose administration of meloxicam, median maximum plasma concentrations are achieved within 5 to 6 hours.
Extent of absorption for meloxicam following oral administration is not altered by concomitant food intake or the use of inorganic antacids.
Dose linearity was demonstrated after oral administration in the therapeutic dose range of 7,5 to 15 mg. With multiple dosing, steady state conditions were reached within 3 to 5 days. Once daily dosing leads to mean meloxicam plasma concentrations with a relatively small peak-trough fluctuation in the range of 0,4 to 1,0 μg/mL for 7,5 mg doses and 0,8 to 2,0 μg/mL for 15 mg doses, respectively (Cmin and Cmax at steady state, correspondingly). Mean maximum plasma concentrations of meloxicam at steady state, are achieved within five to six hours
Steady state conditions are achieved in three to five days. 99 % is bound to plasma proteins. Meloxicam penetrates into synovial fluid to give concentrations approximately half those in plasma.
Volume of distribution is low, i.e. approximately 11 L after i.m. or i.v. administration, and shows interindividual variation in the order of 7 to 20%.
The volume of distribution following administration of multiple oral doses of meloxicam (7,5 to 15 mg) is about 16 L with coefficients of variation ranging from 11 to 32%.
Meloxicam is extensively metabolised. The major metabolic pathway is the oxidation of the methyl group of the thiazoolyl-moeity. Neither hepatic, nor mild or moderate renal insufficiency does substantially affect meloxicam’s pharmacokinetics.
Meloxicam undergoes extensive hepatic biotransformation. Four different metabolites of meloxicam were identified in urine, which are all pharmacodynamically inactive.
Less than 5% of the daily dose is excreted unchanged in the faeces, while only traces of the unchanged compound are excreted in the urine. Meloxicam is eliminated from the body with a mean half-life of 20 hours. Plasma clearance is on average 8 ml/min. Clearance is halved in the elderly.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.