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Clinical pharmacokinetics of meloxicam
1Department of Pharmacokinetics and Metabolism, Dr. Karl Thomae GmbH, Biberach an der Riss, Germany.
Abstract:
Meloxicam (CAS 71125-38-7, UH-AC 62 XX) is a new non-steroidal anti-inflammatory drug (NSAID) which was developed for the treatment of osteoarthritis and rheumatoid arthritis. The basic clinical pharmacokinetics of meloxicam (7.5-30 mg) have been investigated in 78 healthy male volunteers after single and multiple dosing via oral, intravenous and rectal routes. Plasma concentrations of meloxicam were determined by validated high performance liquid chromatography (HPLC) methods. The pharmaco-kinetic profile of meloxicam is characterized by almost complete absorption over a prolonged phase-avoiding high initial drug concentrations- and is bound to plasma proteins by more than 99.5%. Meloxicam is metabolized to four biologically inactive metabolites and excreted 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 pharmacokinetic parameters are linear over the entire dose range, there are no changes with multiple dosing and bioequivalence was shown for a number of different formulations. The results indicate that meloxicam is suitable for once-daily administration and that a switch from one formulation to another is easily possible if necessary or convenient for the patient.
Insights
Meloxicam, a novel non-steroidal anti-inflammatory drug (NSAID), demonstrates favorable pharmacokinetics for treating arthritis. Its predictable absorption and long half-life support convenient once-daily dosing.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Drug Development
Background:
- Meloxicam is a new non-steroidal anti-inflammatory drug (NSAID) developed for osteoarthritis and rheumatoid arthritis.
- Understanding its clinical pharmacokinetics is crucial for effective therapeutic use.
Purpose of the Study:
- To investigate the basic clinical pharmacokinetics of meloxicam.
- To assess meloxicam's behavior after single and multiple doses via oral, intravenous, and rectal routes.
- To evaluate pharmacokinetic parameters across a dose range of 7.5-30 mg.
Main Methods:
- Clinical pharmacokinetic study in 78 healthy male volunteers.
- Single and multiple dosing via oral, intravenous, and rectal administration.
- Plasma concentrations determined using validated high-performance liquid chromatography (HPLC).
Main Results:
- Meloxicam exhibits prolonged absorption, minimizing high initial concentrations.
- Plasma protein binding exceeds 99.5%.
- Metabolized into four inactive metabolites; excreted via urine and feces with an elimination half-life of approximately 20 hours.
- Total plasma clearance is 7-8 ml/min; steady state achieved in 3-5 days.
- Linear pharmacokinetic parameters, no changes with multiple dosing, and bioequivalence across formulations were observed.
Conclusions:
- Meloxicam's pharmacokinetic profile supports suitability for once-daily administration.
- Formulation switching is feasible, enhancing patient convenience.
- The drug's predictable pharmacokinetics are advantageous for managing inflammatory conditions.