Pharmacokinetics and tolerability of meloxicam after i.m. administration

1 The pharmacokinetics and tolerability of a new nonsteroidal anti‐inflammatory drug (NSAID), meloxicam, administered i.m., were investigated in two studies conducted in healthy male volunteers. Study 1 was an open, placebo‐controlled design in which 32 volunteers were randomized to a single ascending i.m. dose of meloxicam (5, 10, 20, and 30 mg) or placebo. Study 2 had an open, randomized two way crossover design in which 12 volunteers received single i.m. and i.v. doses of meloxicam (15 mg).

2 Meloxicam showed an excellent tolerability in both studies. No effect was seen on serum creatinphosphokinase (CK, the isoenzyme of the skeletal muscle enzyme, CK‐MM, was determined).

3 Following i.m. administration meloxicam was rapidly and completely absorbed (mean absolute bioavailability 102%). Dose‐proportionality was demonstrated with respect to C_max (maximum plasma concentration) and AUC (extrapolated area under the plasma concentration‐time curve from zero time to infinity) over a range of 5–30 mg.

4 Intravenous administration of meloxicam (15 mg) resulted in higher initial plasma concentrations (C_3min, i.e. concentration in plasma 3 min after start of injection = 2.99 ± 0.75 μg·ml^‐1) than after i.m. injection (C_max: 1.62 ± 0.20 mg ml^‐1). All other pharmacokinetic parameters were similar for both routes of administration (apparent elimination half‐life = 15–22 h; plasma clearance = 7–9 ml min^‐1).

5 In conclusion, the excellent tolerability of i.m. meloxicam together with its rapid and complete absorption may provide an alternative to oral administration of this drug.

DOI: 10.1111/j.1365-2125.1996.tb00171.x

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