What is meloxicam (Nonsteroidal Anti-Inflammatory Drug (NSAID))?

What is Meloxicam?

Meloxicam is a COX-2 preferential (selective) nonsteroidal anti-inflammatory drug (NSAID) approved for once-daily treatment of osteoarthritis and rheumatoid arthritis, offering comparable efficacy to traditional NSAIDs but with significantly reduced gastrointestinal toxicity. 1, 2

Drug Classification and Mechanism

• Meloxicam belongs to the enolic acid derivative class of the oxicam group of NSAIDs 3
• It works by selectively inhibiting the COX-2 enzyme (the inducible isoform responsible for inflammation) while relatively sparing COX-1 (the constitutive isoform that protects gastric mucosa and maintains kidney function) 4
• This COX-2 selectivity is most pronounced at the lowest therapeutic doses 1
• The drug inhibits prostaglandin synthesis in inflammatory cells, providing anti-inflammatory, analgesic, and antipyretic effects 5, 1

Clinical Efficacy

• Meloxicam at doses of 7.5 mg and 15 mg daily has been proven as effective as traditional NSAIDs including piroxicam 20 mg, diclofenac 100 mg slow release, and naproxen 750-1000 mg in treating osteoarthritis and rheumatoid arthritis 2, 3
• Clinical trials involving over 5,000 patients demonstrated efficacy significantly superior to placebo 2
• Therapeutic effects become evident after 2 weeks of treatment and are maintained throughout therapy 3
• The 3.75 mg daily dose did not consistently reach statistical significance for all endpoints, making 7.5-15 mg the recommended therapeutic range 3

Superior Safety Profile

The most clinically significant advantage of meloxicam is its markedly reduced gastrointestinal toxicity compared to traditional NSAIDs:

• Perforations, ulcerations, and bleeding occurred in only 0.1% of patients on meloxicam 7.5 mg and 0.2% on 15 mg, compared to 1.2% with piroxicam, 0.6% with diclofenac, and 2.1% with naproxen 2
• Both meloxicam doses produced significantly fewer overall gastrointestinal side effects than comparator NSAIDs (p < 0.05) 2
• Gastrointestinal adverse event rates and dropout rates were comparable to placebo and lower than diclofenac 3
• Severe GI side effects, discontinuations due to GI problems, and less serious events like dyspepsia and abdominal pain were significantly less frequent 2

Pharmacokinetic Properties

• Meloxicam has an elimination half-life of approximately 20 hours, making it ideal for once-daily administration 6, 4
• The drug demonstrates almost complete absorption over a prolonged phase, avoiding high initial peak concentrations 6
• It is more than 99% bound to plasma proteins 6
• Steady-state concentrations are achieved within 3-5 days of daily dosing 6
• The drug is metabolized to four biologically inactive metabolites and excreted in urine and feces 6
• Pharmacokinetic parameters are linear over the entire dose range with no changes during multiple dosing 6

Cardiovascular Considerations

Important caveat: While meloxicam offers gastrointestinal advantages, all COX-2 selective inhibitors carry cardiovascular risks including increased risk of myocardial infarction, stroke, heart failure, and hypertension 5. These risks are greatest in patients with prior cardiovascular disease or at high cardiovascular risk 5. The American Heart Association recommends that COX-2 inhibitors should be used only when there are no appropriate alternatives, at the lowest dose and for the shortest duration necessary 5.

Renal Safety

• No evidence exists that meloxicam causes deterioration in renal function in patients with moderate renal impairment 4
• No drug accumulation occurs with continued use 4
• However, like all NSAIDs, meloxicam can cause kidney disease and heart failure, risks that are well-described in medical literature 5

Drug Interactions

• No clinically significant drug interactions have been detected, making meloxicam suitable for patients with co-existing pathology 4