ジクロフェナクナトリウム 化学特性,用途語,生産方法
外観
白色〜わずかにうすい黄色, 結晶〜粉末
溶解性
メタノール,エタノールに易溶、水,酢酸にやや可溶、アセトンに難溶、エーテル,クロロホルムにほとんど不溶。
用途
フェニル酢酸系化合物です。シクロオキシゲナーゼ(COX)を阻害し、プロスタグランジン生合成抑制作用を示します。
用途
薬理・生理作用研究用。
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
商品名
ジクロード (わかもと製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ナボール (久光製薬); ボルタレン (ノバルティスファーマ); ボルタレン (ノバルティスファーマ); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工); ボルタレン (同仁医薬化工)
説明
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC
50s = 0.9-2.7 and 1.5-20 μM, for human COX-1 and COX-2, respectively). It is also an active metabolite of diclofenac methyl ester and diclofenac amide . Diclofenac inhibits release of arachidonic acid (Item Nos.
90010 |
90010.1 |
10006607) induced by A23187 in isolated rat peritoneal neutrophils and macrophages (IC
50s = 60 and 10 μM, respectively). Transdermal administration of diclofenac inhibits carrageenan-induced paw edema in rats. Formulations containing diclofenac have been used in the treatment of pain associated with osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
化学的特性
Off-White Crystalline Solid
使用
Diclofenac sodium is a nonsteroidal anti-inflammatory compound and cyclooxygenase (COX) inhibitor. Oxidation of diclofenac sodium produces the metabolite 4'-hydroxy diclofenac) which demonstrates specific inhibition of Cox-2. Inhibition of Cox by diclofenac and 4'-hydroxy diclofenac suppresses prostaglandin E2 synthesis, producing anti-inflammatory and analgesic effects. Diclofenac is also shown to stabilize the native tetrameric conformation of transthyretin (TTR) fibrils, preventing the formation of insoluble amyloidogenic TTR deposits. Diclofenac Sodium is a substrate of CYP2C9. It is also used as an inhibitor of Cox-1 and Cox-2.
定義
ChEBI: Diclofenac sodium is the sodium salt of diclofenac. It contains a diclofenac(1-).
世界保健機関（WHO）
The World Health Organization currently has no information to
suggest that diclofenac is less safe than other widely available non-steroidal
antiinflammatory substances of this type, or that children are particularly liable to
react adversely. It is registered in many countries in several dosage forms,
including a 12.5 mg suppository indicated for juvenile arthritis.
一般的な説明
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Diclofenac is a derivative of benzeneacetic acid. It is categorized under the class of non-steroidal anti-inflammatory drugs (NSAIDs). It shows inflammatory, analgesic and antipyretic activities.
臨床応用
Diclofenac sodium is indicated for the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.
合成
Synthesis: Acylation of N-phenyl-2,6- dichloroaniline with chloroacetyl chloride gives the corresponding chloroacetanilide, which is fused with aluminum chloride to give 1-(2,6- dichlorophenyl)-2-indolinone. Hydrolysis of the indolinone with dilute aqueous-alcoholic sodium hydroxide affords the desired sodium salt directly.
ジクロフェナクナトリウム 上流と下流の製品情報
原材料
準備製品