PMID: 8592871Nov 1, 1995Paper

Meloxicam: metabolic profile and biotransformation products in the rat

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
J SchmidH Wachsmuth

Abstract

1. The metabolic fate of 14C-labelled meloxicam was investigated in the urine and bile of rat following oral and intraduodenal administration. Structural elucidation of metabolites was performed by nuclear magnetic resonance, mass spectrometry (electron impact and fast atom bombardment). 2. A mean total of 76.3% 14C-radioactivity was recovered in urine over 96 h, with the remainder in the faeces. The metabolic pattern in the excreta was independent of dose (1 versus 10 mg/kg) and collection period (0-8 versus 24-48 h). In bile one of the main metabolites was absent. 3. Meloxicam underwent extensive metabolism with only small amounts of unchanged drug recovered in the urine (< 0.5%) or bile (4.5%). Principal routes of biotransformation were: oxidation of the 5-methyl group of the N-heteroaryl-carbamoyl side chain to yield the 5'-hydroxymethyl derivative (33% of metabolites in urine, 22% in bile) and the 5'-carboxy derivative (16% in urine, 49% in bile). Oxidative cleavage of the benzothiazine-ring yielded an oxamic acid metabolite in urine (23.5%), which was not present in bile. 4. The introduction of a methyl-group into the N-heteroaryl-carbamoyl side chain increased lipophilicity and facilitated metabolic excretion compared wi...Continue Reading

References

Jan 1, 1992·European Journal of Drug Metabolism and Pharmacokinetics·T F WoolfT Chang
Jan 1, 1989·Drug Metabolism Reviews·T F Woolf, L L Radulovic
Apr 15, 1985·Biochemical Pharmacology·S IchiharaM Tateishi
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Nov 30, 1984·Journal of Chromatography·H M RuijtenH de Bree
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Citations

Dec 1, 1995·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·G EngelhardtC Schnitzler
Jan 8, 2011·Annual Review of Pharmacology and Toxicology·John S Walsh, Gerald T Miwa
Aug 6, 2008·Expert Opinion on Drug Metabolism & Toxicology·Graham Lappin, Lloyd Stevens
Mar 1, 1997·Expert Opinion on Investigational Drugs·M Schattenkirchner
Feb 11, 2010·Bioorganic & Medicinal Chemistry Letters·Stephanos IoannidisMichael Zinda
Sep 25, 2007·Chemistry & Biodiversity·Bernard Testa, Stefanie D Krämer
Jun 4, 2011·Journal of Veterinary Pharmacology and Therapeutics·I A WasfiK M Al Neaimi
Jun 1, 1997·Seminars in Arthritis and Rheumatism·D E Furst
Sep 10, 2010·Chemical Research in Toxicology·Yohannes TefferaZhiyang Zhao

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