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Active ingredient: Meclofenamate - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors

Dosage Forms

  • Capsules (containing 50 mg or 100 mg meclofenamic acid as the sodium salt)

Brands / Synonyms

Acide meclofenamique [INN-French]; Acido meclofenamico [INN-Spanish]; Acidum meclofenamicum [INN-Latin]; Arquel; Meclofenamate; Meclofenamic acid; Meclofenamic acid [USAN:BAN:INN]; Meclofenamic acid(USAN); Meclomen (free acid); Meclophenamic acid

Indications

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.

Pharmacology

Meclofenamate is a nonsteroidal agent which has demonstrated anti-inflammatory, analgesic, and antipyretic activity in laboratory animals.

Mechanism of Action

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, meclofenamate was found to inhibit prostaglandin synthesis and to compete for binding at the prostaglandin receptor site. In vitro meclofenamate was found to be an inhibitor of human leukocyte 5-lipoxygenase activity. These properties may be responsible for the anti-inflammatory action of meclofenamate. There is no evidence that meclofenamate sodium alters the course of the underlying disease.

Absorption

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 meclofenamate. 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 meclofenamate capsules one-half hour after a meal, the average extent of bioavailability decreased by 26%, the average peak concentration (Cmax) decreased fourfold and the time to Cmax was delayed by 3 hours.

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Hepatic. Meclofenamate is extensively metabolized to an active metabolite (Metabolite I; 3-hydroxymethyl metabolite of meclofenamate) and at least six other less well characterized minor metabolites. Only this Metabolite I has been shown in vitro to inhibit cyclooxygenase activity with approximately one fifth the activity of meclofenamate.

Contraindications

Meclofenamate sodium should not be used in patients who have previously exhibited hypersensitivity to it.

Cross-sensitivity to aspirin or other nonsteroidal anti-inflammatory drugs: meclofenamate sodium should not be given to patients in whom these drugs induce symptoms of bronchospasm, allergic rhinitis, or urticaria.

Drug Interactions

Warfarin

Meclofenamate sodium enhances the effect of warfarin. Therefore, when meclofenamate sodium is given to a patient receiving warfarin, the dosage of warfarin should be reduced to prevent excessive prolongation of the prothrombin time.

Aspirin

Concurrent administration of aspirin may lower meclofenamate sodium plasma levels, possibly by competing for protein-binding sites. The urinary excretion of meclofenamate sodium is unaffected by aspirin, indicating no change in meclofenamate sodium absorption. Meclofenamate sodium does not affect serum salicylate levels. Greater fecal blood loss results from concomitant administration of both drugs than from either drug alone.

Propoxyphene

The concurrent administration of propoxyphene hydrochloride does not affect the bioavailability of meclofenamate sodium.

Antacids

Concomitant administration of aluminum and magnesium hydroxides does not interfere with absorption of meclofenamate sodium.

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