ロルノキシカム 化学特性,用途語,生産方法
外観
うすい黄赤色～黄色～緑色粉末～結晶
用途
鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ2阻害薬
効能
鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ2阻害薬
商品名
ロルカム (大正製薬)
説明
Lornoxicam is a nonselective NSAID for oral and intravenous administration. It has been available for human use since two decades and there is a growing body of evidence supporting its efficacy and tolerability for management of acute pain.
Xefo, a member of the oxicam family of nonsteroidal antiinflammatory agents, was launched in Denmark for mild to moderate pain and inflammation. A seven step synthesis, beginning with 2,5-dichlorothiophene, provides access to this compound. It inhibits prostaglandin synthesis at the level of cyclooxygenase (Cox1 :Cox2 = 0.6) but does not inhibit 5-lipoxygenase. Xefo did not increase serum levels of pepsinogen I (an indicator of gastric mucosal status) and readily penetrates perivascular interstitial spaces including synovial fluid. It is as effective as morphine, meperidine and tramadol in relieving post operative pain and as efficient as other NSAlDs in relieving the symptoms of osteoarthritis and rheumatoid arthritis. It is 100 times more potent than Tenoxicam in inhibiting PGD2 and more active than indomethacin (6x) or piroxicam (10x) in preventing arachadonic acid influenced lethality in mice. Xefo has inhibitor effects on spinal nocicceptive processing presumably via release of endogenous opiods and evidence suggests it is good for migraine.
化学的特性
Crystalline Solid
使用
Lornoxicam belongs to the oxicam class. It has anti-inflammatory and antipyretic properties. Lornoxicam prevents the synthesis of prostaglandin (PG) by inhibiting cyclo-oxygenase. It is used to relieve various types of symptoms associated with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain.Lornoxicam is approved for use in Japan.
Lornoxicam has been used as a drug in melanin binding study with cassette dosing and rapid equilibrium dialysis inserts. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug.
定義
ChEBI: A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for th
treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.
適応症
Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID) that is used as a painkiller (analgesic). A high level of pain relief is experienced by about 45% of those with moderate to severe postoperative dental pain after a single dose of lornoxicam 8 mg, compared to about 10% with placebo. This is comparable to the proportion experiencing the same level of pain relief with ibuprofen 200 to 400 mg. Adverse events were generally mild and did not differ from placebo in these singe dose studies. There were insufficient data to assess duration of action, but it is likely to be similar to ibuprofen 200 mg.
ロルノキシカム 上流と下流の製品情報
原材料
準備製品