High Quality Raw Material Powder Meloxicam CAS 71125-38-7 with good price and fast delivery

Meloxicam More Info

Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) primarily used to treat pain and inflammation associated with osteoarthritis, rheumatoid arthritis, and juvenile rheumatoid arthritis.

Mechanism of Action

Meloxicam works by selectively inhibiting cyclooxygenase enzymes (COX), particularly COX-2 over COX-1 at low therapeutic doses. COX enzymes convert arachidonic acid into prostaglandin H2, the precursor of prostaglandins that mediate inflammation, pain, and fever. By blocking COX-2, meloxicam reduces the synthesis of pro-inflammatory prostaglandins, thereby alleviating inflammation and pain while sparing COX-1 to some extent, which may reduce gastrointestinal side effects compared to non-selective NSAIDs.
Meloxicam achieves significant penetration into synovial fluid, with concentrations about 40–50% of plasma levels and a higher free drug fraction due to lower albumin content in synovial fluid. This may contribute to its efficacy in treating arthritis.

Applications

Osteoarthritis
Rheumatoid arthritis
Juvenile rheumatoid arthritis
Other inflammatory conditions as determined by a healthcare provider

Pharmacokinetics

Absorption: Oral bioavailability is somewhat reduced compared to intravenous administration. Peak plasma concentrations occur approximately 5 to 6 hours after oral dosing. A high-fat meal can increase peak levels by about 22%, but no specific meal restrictions are generally recommended.
Distribution: Volume of distribution is about 10 liters. Meloxicam is highly protein-bound (>99%), mainly to albumin.
Metabolism: Extensively metabolized in the liver by CYP2C9 and to a lesser extent CYP3A4 into four inactive metabolites.
Excretion: Eliminated equally via urine and feces, primarily as metabolites. The elimination half-life ranges from 15 to 20 hours, supporting once-daily dosing.
Steady state: Achieved within 3 to 5 days of repeated dosing.

Safety and Side Effects

Common side effects: Diarrhea, constipation, gas, dizziness, headache, and upper respiratory symptoms.
Serious risks:
Cardiovascular: Increased risk of fatal heart attack or stroke, especially with long-term use, high doses, or pre-existing heart disease.
Gastrointestinal: Risk of stomach or intestinal bleeding, ulceration, and perforation, which can be fatal and may occur without warning.
Liver: Possible liver problems including elevated liver enzymes, jaundice, and hepatitis.
Kidney: Potential for renal impairment and fluid retention.
Hypersensitivity: Allergic reactions, severe skin reactions (e.g., Stevens-Johnson syndrome), and anaphylaxis.
Warnings: Avoid use just before or after coronary artery bypass graft (CABG) surgery. Use the lowest effective dose for the shortest duration possible to minimize risks.
Monitoring: Regular medical tests may be required during long-term therapy.

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