Meclomen

Uses

Meclomen is an NSAID used to treat mild to moderate pain, primary dysmenorrhea, heavy menstrual blood loss, rheumatoid arthritis, and osteoarthritis.

For the relief of mild to moderate pain, for the treatment of primary dysmenorrhea and for the treatment of idiopathic heavy menstrual blood loss. Also for relief of the signs and symptoms of acute and chronic rheumatoid arthritis and osteoarthritis.

Meclomen is also used to associated treatment for these conditions: Acute Gouty Arthritis, Ankylosing Spondylitis (AS), Fever, Hypermenorrhea, Juvenile Idiopathic Arthritis (JIA), Mild pain, Osteoarthritis (OA), Primary Dysmenorrhoea, Rheumatoid Arthritis, Acute Subacromial bursitis, Moderate Pain, Supraspinatus tendinitis

How Meclomen works

The mode of action, like that of other nonsteroidal anti-inflammatory agents, is not known. Therapeutic action does not result from pituitary-adrenal stimulation. In animal studies, meclofenamic acid was found to inhibit prostaglandin synthesis and to compete for binding at the prostaglandin receptor site. In vitro meclofenamic acid was found to be an inhibitor of human leukocyte 5-lipoxygenase activity. These properties may be responsible for the anti-inflammatory action of meclofenamic acid. There is no evidence that meclofenamic acid alters the course of the underlying disease.

Toxicity

After a massive overdose, CNS stimulation may be manifested by irrational behavior, marked agitation and generalized seizures. Following this phase, renal toxicity (falling urine output, rising creatinine, abnormal urinary cellular elements) may be noted with possible oliguria or anuria and azotemia. A 24 year-old male was anuric for approximately one week after ingesting an overdose of 6 to 7 grams of meclofenamate sodium. Spontaneous diuresis and recovery subsequently occurred.

Food Interaction

• Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of developing a gastrointestinal bleed.
• Take with or without food. Taking meclofenamic acid with food reduces the rate and extent of its absorption; however it also reduces gastrointestinal upset caused by meclofenamic acid.

Volume of Distribution

• 9.1 to 43.2 L

Elimination Route

Rapidly absorbed in man following single and multiple oral doses with peak plasma concentrations occurring in 0.5 to 2 hours. The concomitant administration of antacids (aluminum and magnesium hydroxides) does not interfere with absorption of meclofenamic acid. Unlike most NSAIDs, which when administered with food have a decrease in rate but not in extent of absorption, meclofenamic acid is decreased in both. It has been reported that following the administration of meclofenamic acid capsules one-half hour after a meal, the average extent of bioavailability decreased by 26%, the average peak concentration (C_max) decreased fourfold and the time to C_max was delayed by 3 hours.

Half Life

In a study in 10 healthy subjects following a single oral dose the apparent elimination half-life ranged from 0.8 to 5.3 hours. Metabolite I (3-hydroxymethyl metabolite of meclofenamic acid) has a mean half-life of approximately 15 hours.

Clearance

• Oral cl=206 mL/min

Elimination Route

Other metabolites, whose excretion rates are unknown, account for the remaining 35% to 62% of the dose excreted in the urine. The remainder of the administered dose (approximately 30%) is eliminated in the feces (apparently through biliary excretion). Trace amounts of meclofenamate sodium are excreted in human breast milk.

Innovators Monograph

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