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© 1996 British Society for Rheumatology

A Review of the Clinical Pharmacokinetics of Meloxicam

D. Türck, W. Roth and U. Busch

Department of Pharmacokinetics and Drug Metabolism, Dr Karl Thomae GmbH, Birkendorfer Straβe 65 88397 Biberachl Riss, Germany

Correspondence to: Correspondence to: Dr D. Türck, Department of Pharmacokinetics and Drug Metabolism, Dr Karl Thomae GmbH, Birkendorfer Straβe 65, D-88397 Biberach/Riss, Germany


  Abstract

Meloxicam is a new preferential cyclooxygenase-2 (COX-2) inhibitor currently for the treatment of osteoarthritis and rheumatoid arthritis. Its pharmacokinetic profile is characterized by a prolonged and almost complete absorption and the drug is >99.5% bound to plasma proteins. Meloxicam is metabolized to four biologically inactive main metabolites, which are excreted in both urine and faeces. The elimination half-life (t1/2) of meloxicam is ~20 h. This is reflected in a total plasma clearance (CL) of 0.42 – 0.481/h. Steady-state plasma concentrations are achieved within 3—5 days. The pharmacokinetic parameters of meloxicam are linear over the dose range 7.5–30 mg and bioequivalence has been shown for a number of different formulations. No interactions were observed following the concomitant administration of food, cimetidine, antacid, aspirin, β-acetyldigoxin, methotrexate, warfarin or furosemide. Neither hepatic insufficiency nor moderate renal dysfunction have any relevant effects on the pharmacokinetics of meloxicam and dosage adjustments in the elderly are not required.

KEY WORDS: Meloxicam, Pharmacokinetic properties, Absorption, Distribution, Metabolism, Elimination, Interactions


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