Меклофенамовая натриевая сол

Описание

Meclofenamate is a time-dependent, non-specific competitive inhibitor of COX-1 and -2. The IC₅₀ values for inhibition of human recombinant COX-1 and -2 are 1.5 and 9.7 μM, respectively for instantaneous inhibition. However, the IC₅₀ is much lower if pre-incubated with the enzyme.

Использование

Meclofenamate Sodium is an NSAID used in the treatment of chronic pain.

Определение

ChEBI: An organic sodium salt derived from meclofenamic acid. Its monohydrate is used for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.

Показания

Meclofenamate sodium (Meclomen) is prescribed for rheumatoid arthritis and osteoarthritis. The fenamates show no clear superiority in antiinflammatory activity and may produce more adverse effects than other NSAIDs.

Общее описание

Meclofenamate sodium (Meclomen) is available for use inthe treatment of acute and chronic RA, OA, and primarydysmenorrhea. It is metabolized in a similar manner tomefenamic acid discussed above, thus a similar restriction isalso applied to meclofenamate. The most significant side effectsare GI, including diarrhea.

Фармакокине?тика

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.

Клиническое использование

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.