メクロフェナミン酸ナトリウム一水和物 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
抗炎症薬, シクロオキシゲナーゼ阻害薬
説明
Meclofenamate is a time-
dependent, non-
specific competitive inhibitor of COX-
1 and -
2. The IC
50 values for inhibition of human recombinant COX-
1 and -
2 are 1.5 and 9.7 μM, respectively for instantaneous inhibition. However, the IC
50 is much lower if pre-
incubated with the enzyme.
使用
Meclofenamate Sodium is an NSAID used in the treatment of chronic pain.
定義
ChEBI: An organic sodium salt derived from meclofenamic acid. Its monohydrate is used for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.
適応症
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.
一般的な説明
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.
薬物動態学
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.
臨床応用
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.
メクロフェナミン酸ナトリウム一水和物 上流と下流の製品情報
原材料
準備製品