Sodium meclofenamate

Two compounds of the fenamate class of antiinflammatory drugs are marketed in the United States. Mefenamic acid (Ponstel) is indicated only for analgesia and primary dysmenorrhea when therapy will not exceed 1 week. Meclofenamate sodium (Meclomen) is prescribed for rheumatoid arthritis and osteoarthritis. 

Oral 545, 600 mg tablets 467, 500, 580 mg caplets Meclofenamate sodium (generic)... 

Koup, J. R., Tucker, E., Thomas, D. J., Kinkel, A. W., Sedman, A. J., Dyer, R., Sharoky, M. A single and multiple dose pharmacokinetic and metabolism study of meclofenamate sodium, Biopharm. Drug Dispos. 1990, 11, 1-15. 

Codeine Hydrochloride Dequalinium Acetate Fluorometholone Hexamethonium Bromide Riboflavine Stilbazium Iodide Mianserin Hydrochloride Tacrine Hydrochloride Diclofenac Sodium Vinblastine Sulphate Cyclizine Hydrochloride Amiloride Hydrochloride Protoveratrine B Meclofenamate Sodium 5-Methyltryptamine Hydrochloride Dicoumarol Mebendazole Pipradrol Hydrochloride Carbenoxolone Flucytosine Phanquone Phenytoin... 

Medofenamate Sodium. Meclofenamate sodium,. siv dium iV-(2.6-dichlom-rn-tolyl)anthranilate. Mcclomcn. is... 

Meclofenamate is rapidly absorbed, with peak plasma concentration occurring in 1 honr. It is extensively metabolized to an active metabolite (3-hydroxymethyl metabolite of meclofenamic acid) and at least six other less well-characterized minor metabolites. Only this active metabolite has been shown to inhibit cyclooxygenase activity in vitro with approximately one-fifth the activity of meclofenamate sodium. The 3-hydroxymethyl metabolite of meclofenamic acid with a mean half-life of approximately 15 hours does accumulate following mnltiple dosing. Approximately 70% of the administered dose is excreted... 

Mefenamic acid (Ponstel, Ponstan [United Kingdom], Dysman [United Kingdom]) and meclofenamate sodium [Meclomen] have been used mostly in the short-term treatment of pain in soft-tissue injuries, dysmenorrhea, and in rheumatoid and osteoarthritis. These drugs are not recommended for use in children or pregnant women. 

It may be prepared by the Ulman Condensation of o-iodobenzoic acid with 2, 6-dichloro-w-toluidine in the presence of copper-bronze resulting into the formation of meclofenamie aeid whieh on neutralization with equimolar proportion of sodium hydroxide yields meclofenamate sodium. 

Meclofenamate sodium is rapidly and almost completely absorbed following oral administration, reaching peak plasma levels within 2 hours. It is highly bound to plasma proteins (99%) and has a plasma half-life of 2 to 4 hours. Metabolism involves oxidation of the methyl group, aromatic hydroxylation, monodehalogenation, and conjugation. Urinary excretion accounts for approximately 75% of the administered dose. The major metabolite is the product of 3 -methyl oxidation and has been shown to possess anti-inflammatory activity (Fig. 36.21). 

Meclofenamate sodium is indicated for the relief of mild to moderate pain, the acute and chronic treatment of rheumatoid arthritis and osteoarthritis, the treatment of primary dysmenorrhea, and the treatment of idiopathic, heavy menstrual blood loss. 

Anthranilic acid derivatives Meclofenamate sodium Mefenamate... 

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