RiteMED Meloxicam Mechanism of Action

Non-Steroidal Anti-inflammatory Drug (NSAID).
Pharmacology: Pharmacodynamics: Meloxicam is an oxicam derivative non-steroidal anti-inflammatory drug (NSAID) which exhibits analgesic, antipyretic and anti-inflammatory activities by inhibiting cyclooxygenase (COX)-1 and COX-2 isoenzymes resulting in inhibition of prostaglandin synthesis.
Meloxicam inhibits the COX-2 isoform of prostaglandin endoperoxide synthase more than it inhibits the COX-1 isoform as shown in in vitro and in vivo studies. However, Meloxicam is classified as a "preferential" rather than a "selective" COX-2 inhibitor since its COX-2 selectively is dose-dependent and is diminished at higher doses.
Pharmacokinetics: Meloxicam is almost completely absorbed after oral administration with an absolute bioavailability of 89% compared with IV bolus injection. Meloxicam's bioavailability is not markedly affected by concomitant food intake. Maximum plasma concentration (C_max) after a 30 mg oral dose is reached in about 9 to 11 hours while C_max for a 15 mg dose is achieved in about 2.5 to 7 hours. Steady state blood concentrations of Meloxicam are achieved only after 3 to 4 days after oral administration because of its long half-life (around 20 to 24 hours).
Meloxicam is about 99% bound to plasma proteins. Its apparent volume of distribution after oral administration is about10 to 15 L. Meloxicam readily penetrates the synovial fluid with concentrations reaching about 45-57% of plasma concentrations.
Meloxicam is extensively metabolized in the liver to four inactive metabolites. In in vitro studies, Meloxicam is mainly metabolized by the CYP450 2C9 with minor involvement of the CYP3A4 isoenzyme.
Meloxicam is excreted equally in both the urine and feces mainly as metabolites. Its apparent oral clearance ranges from 0.42 to 0.7 L/h.
Meloxicam's pharmacokinetic profile is not significantly altered in elderly patients or in those with mild renal impairment. Meloxicam's pharmacokinetic parameters were also found to be similar in patients with hepatic cirrhosis and healthy volunteers.