メフェナム酸 化学特性,用途語,生産方法
外観
白色～うすい黄色粉末～結晶
解説
メフェナム酸，白色の結晶．融点230～231 ℃．pKa 4.2．λmax 285，340 nm(0.1 mol L－1 水酸化ナトリウム)．水に不溶，エタノールに難溶，アルカリに可溶．鎮痛，消炎，解熱剤として使用される．
森北出版「化学辞典（第2版）
用途
消炎?鎮痛剤 抗リウマチ薬 非ステロイド系消炎薬
効能
鎮痛薬, 抗炎症薬, 解熱薬, シクロオキシゲナーゼ阻害薬
製造
メフェナム酸，o-クロロ安息香酸と2,3-ジメチルアニリンとを縮合させると得られる．
商品名
ポンタール (第一三共); ポンタール (第一三共); ポンタール (第一三共); ルメンタール (福地製薬)
化学的特性
white or light yellow crystalline powder, odorless, insoluble in water, slightly soluble in ethanol, chloroform, slightly soluble in ether. Melting point 230-231°C, mefenamic acid is an anti-inflammatory analgesic with antipyretic, analgesic and anti-inflammatory effects.
使用
Mefenamic acid is used for the same indications as flufenamic acid. Synonyms for this drug are
parkemed, ponstan, ponstel, and others.
定義
ChEBI: An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to b
minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.
適応症
Mefenamic acid (Ponstel) is indicated only for analgesia
and primary dysmenorrhea when therapy will not exceed
1 week.
一般的な説明
Mefenamic acid (Ponstel, Ponstan) is one of the oldestNSAIDs, introduced into the market in 1967 for mild tomoderate pain and for primary dysmenorrhea. It is rapidly absorbed with peak plasma levels occurring 2 to 4 hoursafter oral administration. It undergoes hepatic benzylic hydroxylationof its 3'methyl group regioselectively into twoinactive metabolites, 3'-hydroxymethylmefenamic acid andthe 3'carboxylate metabolite (via further oxidation of thebenzylic alcohol group). The parent drugs and these metabolitesare conjugated with glucuronic acid and excreted primarilyin the urine. Thus, although patients with knownliver deficiency may be given lower doses, it is contraindicatedin patients with preexisting renal dysfunction.
Common side effects associated with its use include diarrhea,drowsiness, and headache. The possibility of blood disordershas also prompted limitation of its administration to 7days. It is not recommended for children or during pregnancy.
臨床応用
Mefenamic acid is synthesized from o-chlorobenzoic acid and 2,3-dimethylaniline under catalytic conditions.
Mefenamic acid is the only fenamic acid derivative that produces analgesia centrally and peripherally. Mefenamic
acid is indicated for the short-term relief of moderate pain and for primary dysmenorrhea.
代謝
Mefenamic acid is absorbed rapidly following oral administration, with peak plasma levels being attained within 2 to 4
hours. It is highly bound to plasma proteins (78.5%) and has a plasma half-life of 2 to 4 hours. Metabolism occurs
through regioselective oxidation of the 3′-methyl group and glucuronidation of mefenamic acid and its metabolites.
Urinary excretion accounts for approximately 50 to 55% of an administered dose, with unchanged drug accounting for
6%, the 3′-hydroxymethyl metabolite (primarily as the glucuronide) accounting for 25%, and the remaining 20% as the
dicarboxylic acid (of which 30% is the glucuronide conjugate). These metabolites are essentially
inactive.
メフェナム酸 上流と下流の製品情報
原材料
準備製品