| Indication |
For symptomatic treatment of arthritis and osteoarthritis. |
| Pharmacodynamics |
Meloxicam is an nonsteroidal anti-inflammatory drug (NSAID) with
analgesic and antipyretic properties. Prostaglandins are substances
that contribute to inflammation of joints. Meloxicam inhibits
prostaglandin synthetase (cylooxygenase 1 and 2) and leads to a decrease
of the synthesis of prostaglandins, therefore, inflammation is reduced. |
| Mechanism of action |
Anti-inflammatory effects of meloxicam are believed to be due to
inhibition of prostaglandin synthetase (cylooxygenase), leading to the
inhibition of prostaglandin synthesis. As prostaglandins sensitize pain
receptors, inhibition of their synthesis may be associated with the
analgesic and antipyretic effects of meloxicam. |
| Absorption |
Absolute bioavailability = 89% |
| Volume of distribution |
|
| Protein binding |
99.4% bound, primarily to albumin |
| Metabolism |
Meloxicam is almost completely metabolized into inactive
metabolites by the cytochrome P450 (CYP450) isozymes. CYP2C9 is
primarily responsible for metabolism of meloxicam while CYP3A4 plays a
minor role. An intermediate metabolite, 5'-hydroxymethyl meloxicam, is
further metabolized to 5'-carboxy meloxicam, the major metabolite.
Peroxidase activity is thought to produce the two other inactive
metabolites of meloxicam. |
| Route of elimination |
Meloxicam is almost completely metabolized to four
pharmacologically inactive metabolites. Meloxicam excretion is
predominantly in the form of metabolites, and occurs to equal extents in
the urine and feces. Only traces of the unchanged parent compound are
excreted in the urine (0.2%) and feces (1.6%). The extent of the urinary
excretion was confirmed for unlabeled multiple 7.5 mg doses: 0.5%, 6%
and 13% of the dose were found in urine in the form of meloxicam, and
the 5'-hydroxymethyl and 5'-carboxy metabolites, respectively. |
| Half life |
15-20 hours |
| Clearance |
- 8.8 mL/min [Healthy Male Adults (Fed) oral 7.5 mg tablets]
- 9.9 mL/min [Eldery Male (Fed) oral 15 mg capsules]
- 5.1 mL/min [Eldery Female (Fed) oral 15 mg capsules]
- 19 mL/min [Renal Failure (Fasted) oral 15 mg capsules]
- 11 mL/min [Hepatic Insufficiency (Fasted) oral 15 mg capsules]
|
| Toxicity |
LD50, Acute: 84 mg/kg (Rat); Oral 470 mg/kg (Mouse); Oral 320 mg/kg (Rabbit) |
