Pharmacology: Meloxicam is a non-steroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mode of action of Meloxicam may be related to prostaglandin synthetase (cyclooxygenase) inhibition.
Pharmacokinetics: Absorption: Absolute bioavailability of a single oral dose is 89%. Neither the rate nor the extent of absorption is affected by multiple dose administration. Administration with food does not affect the extent of absorption.
Distribution: VolD-10 L. Penetration into red blood cells is less than 10%. Concentrations in synovial fluid after a single oral dose range from 40% to 50% of those in plasma. The free fraction in synovial fluid is 2.5 times higher than in plasma, due to the lower albumin content in synovial fluid.
Protein binding: Very high (99.4%).
Biotransformation: Almost completely metabolized to 4 pharmacologically inactive metabolites. Metabolized largely by cytochrome P450 2C9.
Half-life: Elimination 15 to 20 hours.
Time to peak concentration: 5 to 6 hours.
Peak serum concentration: 1.05 micrograms/mL in healthy male adults at steady state, with a 7.5 mg dose.
Elimination: Only traces of unchanged parent compound are excreted in the urine (0.2%) and feces (1.6%). Excretion is predominantly in the form of metabolites and occurs to an equal extent in the urine and feces.