Meloxicam: a reappraisal of pharmacokinetics, efficacy and safety.

Article Details

Citation

Gates BJ, Nguyen TT, Setter SM, Davies NM

Meloxicam: a reappraisal of pharmacokinetics, efficacy and safety.

Expert Opin Pharmacother. 2005 Oct;6(12):2117-40. doi: 10.1517/14656566.6.12.2117.

PubMed ID
16197363 [ View in PubMed
]
Abstract

The discovery of two distinct isoenzymes of COX has led to the development and clinical introduction of COX-2 inhibitors with increased selectivity onto the market. Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) of the oxicam class, and is a preferential inhibitor of COX-2, demonstrating effectiveness with anti-inflammatory, analgesic and antipyretic activity. Meloxicam is therapeutically utilised in the management of osteoarthritis and rheumatoid arthritis. Trials have examined the risk of gastrointestinal ulceration of meloxicam when compared with traditional non-specific COX-inhibiting NSAIDs with mixed results; meloxicam seems to have a greater gastrointestinal risk than the highly specific COX-2 NSAIDs. Meloxicam has a plasma half-life of approximately 20 h and is convenient for once daily administration. Neither moderate renal nor hepatic insufficiency significantly alters the pharmacokinetics of meloxicam in short-term studies. Furthermore, dose adjustment is not required in the elderly. Recent drug-drug interaction studies have demonstrated that meloxicam interacts with some medications, including cholestyramine, lithium and some inhibitors of cytochrome P450 -2C9 and -3A4. Consequently, increased clinical vigilance should be maintained when coprescribing some medications with meloxicam. Concentration-dependent therapeutic and toxicological effects have yet to be extensively elucidated for meloxicam. Long-term safety in various organ systems, especially in the heart and vascular system and with concomitant drug administration, remains to be proven. The pharmacokinetics of meloxicam enables once daily application, which increases compliance compared with some shorter acting NSAIDs; however, long-term clinical data clearly demonstrating safety and efficacy advantages are lacking.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
MeloxicamProstaglandin G/H synthase 1ProteinHumans
Unknown
Inhibitor
Details
MeloxicamProstaglandin G/H synthase 2ProteinHumans
Yes
Inhibitor
Details
Drug Interactions
DrugsInteraction
Meloxicam
Cholestyramine
The serum concentration of Meloxicam can be decreased when it is combined with Cholestyramine.