Pharmacology: Pharmacodynamics: Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID), an oxicam derivative. It inhibits the biosynthesis of prostaglandins as inflammatory mediators. It has inhibitory effect to 2 isoenzymes of cyclooxygenases (COXs or prostaglandin endoperoxide syntases): COX-1 and COX-2. The normal dose of Meloxicam is preferential inhibitor of COX-2, associated with anti-inflammatory effect, than COX-1, associated with adverse gastrointestinal effect.
Pharmacokinetics: Meloxicam is well absorbed after oral doses. Timing of meals or concomitant use of antacids does not affect the drug pharmacokinetics. Maximum plasma concentration (Cmax) is reached within 5-10 hours of administration. It is about 99% bound to plasma proteins. The volume of distribution is increased in renal failure.
Meloxicam is extensively metabolized in the liver principally via cytochrome P450 (CYP) 2C9 isoenzyme, with minor contribution by CYP3A4, to inactive metabolites including 5'-carboxymeloxicam as the major metabolite. Both drug and its metabolites are excreted in the similar amounts in the urine and in the feces; small amount is excreted unchanged (< 5%). Second maximum plasma concentration occurs prolongedly around 12-14 hours of administration, as some amount of the biliary excretion has enterohepatic recirculation. It has an elimination half-life of about 15-20 hours.
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