CLINICAL PHARMACOKINETICS OF MELOXICAM

Meloxicam (GAS 71125-38-7, UH-AC 62 XX) is a new non-steroidal anti-in flammatory drug (NSAID) which was developed for the treatment of osteo arthritis and rheumatoid arthritis. The basic clinical pharmacokinetic s of meloxicam (7.5-30 mg) have been investigated in 78 healthy male v olunteers after single and multiple dosing via oral, intravenous and r ectal routes. Plasma concentrations of meloxicam were determined by va lidated high performance liquid chromatography (HPLC) methods. The pha rmacokinetic profile of meloxicam is characterized by almost complete absorption over a prolonged phase - avoiding high initial drug concent rations - and is bound to plasma proteins by more than 99.5 %. Meloxic am is metabolized to four biologically inactive metabolites and excret ed in urine and faeces with an elimination half-life (t1/2) of around 20 h. This is reflected in a total plasma clearance of 7 to 8 ml/min. Steady state is achieved within 3 to 5 days. In addition, the pharmaco kinetic parameters are linear over the entire dose range, there are no changes with multiple dosing and bioequivalence was shown for a numbe r of different formulations. The results indicate that meloxicam is su itable for once-daily administration and that a switch from one formul ation to another is easily possible if necessary or convenient for the patient.