Meloxicam
Meloxicam is an oral non-steroidal anti-inflammatory drug with preferential COX-2 inhibition, used in adults for osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. The long half-life supports once-daily dosing.
- Chemical formula
- C14H13N3O4S2
- CAS number
- 71125-38-7
- ATC code
- M01AC06
- Molecular weight
- 351.40 g/mol
- Drug class
- NSAID (preferential COX-2 inhibitor)
- Also known as
- UH-AC 62, Meloxicam
What is it?
Meloxicam is an enolic acid derivative NSAID introduced in the 1990s. It is supplied as oral tablets, oral suspension, orally disintegrating tablets and parenteral solution. Meloxicam is dispensed only on prescription. The molecule has preferential, although not strictly selective, inhibition of COX-2 over COX-1, with a tolerability profile intermediate between traditional NSAIDs and selective COX-2 inhibitors.
Mechanism of action
Meloxicam inhibits cyclooxygenase enzymes with a preference for COX-2 at low therapeutic doses. By reducing prostaglandin synthesis, it decreases pain, fever and inflammation. The COX-2 preference partially preserves prostaglandins involved in gastric mucosal protection, which contributes to a lower upper gastrointestinal toxicity than non-selective NSAIDs at equivalent doses. Selectivity is concentration-dependent and decreases at higher doses.
Pharmacokinetics
Meloxicam is well absorbed orally, with peak plasma concentrations reached after five to six hours and a delayed second peak. Bioavailability is approximately 89%. Plasma protein binding exceeds 99%. The drug is metabolised by CYP2C9 and to a lesser extent CYP3A4 to inactive metabolites and excreted in urine and faeces. The terminal half-life is approximately 20 hours, supporting once-daily dosing.
Indications
Meloxicam is approved in adults for the symptomatic treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. In some markets it is also approved in juvenile idiopathic arthritis from age 2 with weight-based dosing. According to clinical guidelines, the lowest effective dose for the shortest necessary duration should be used, with regular reassessment of cardiovascular, gastrointestinal and renal risk factors.
Safety profile
Common adverse effects include gastrointestinal symptoms, peripheral oedema, hypertension and headache. Like other NSAIDs, meloxicam carries class warnings on cardiovascular thrombotic events including myocardial infarction and stroke, and on serious gastrointestinal events. Renal impairment, hyperkalaemia and hepatotoxicity have been reported. According to the prescribing information, contraindications include severe heart failure, recent CABG surgery, active peptic ulcer and severe hepatic or renal impairment.
Products containing this ingredient
Frequently asked questions
How is meloxicam different from celecoxib? ▾
Both have preferential or selective COX-2 inhibition, but celecoxib is more strictly selective at therapeutic doses while meloxicam preference fades at higher doses. Both have a lower rate of upper gastrointestinal adverse events than non-selective NSAIDs. According to clinical guidelines, the choice between them depends on the indication, dose, comorbidity and individual response, and is made by the prescriber.
Why is meloxicam taken once daily? ▾
Meloxicam has a long terminal half-life of approximately 20 hours, which supports once-daily dosing. According to the prescribing information, the usual adult dose for chronic inflammatory conditions is 7.5mg or 15mg once daily, with the lowest effective dose for the shortest period recommended. Steady state is reached after several days of regular dosing.
Does meloxicam cause stomach problems? ▾
Meloxicam can cause gastrointestinal symptoms including dyspepsia, nausea and abdominal pain, and rarely upper gastrointestinal ulcers and bleeding. The risk is lower than with non-selective NSAIDs at equivalent doses but higher than with strictly selective COX-2 inhibitors at higher meloxicam doses. According to the prescribing information, gastric protection should be considered in high-risk patients, with the regimen tailored by the prescriber.
Can meloxicam be used long-term? ▾
Meloxicam is approved for the symptomatic treatment of chronic inflammatory conditions and can be used long-term when needed. According to clinical guidelines, however, the lowest effective dose for the shortest necessary duration should be used, with periodic reassessment of cardiovascular, gastrointestinal and renal risk factors. Long-term use should be supervised by the prescriber, who may add gastric or renal protection.
What are the main contraindications for meloxicam? ▾
Meloxicam is contraindicated in known hypersensitivity to meloxicam or other NSAIDs, in active peptic ulcer or gastrointestinal bleeding, in severe heart failure, in the perioperative period of coronary artery bypass graft surgery, in severe hepatic or renal impairment and during the third trimester of pregnancy. Caution is required in cardiovascular risk factors and elderly patients. According to the prescribing information, the medical history must be reviewed by a clinician before any prescription.
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