ジフルニサル 化学特性,用途語,生産方法
効能
鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ阻害薬
説明
Diflunisal is more
potent than aspirin but produces fewer side effects and has a biological half-life three to four times greater than that
of aspirin. It is rapidly and completely absorbed on oral administration, with peak plasma levels being achieved within
2 to 3 hours of administration. It is highly bound (99%) to plasma proteins after absorption. Its elimination half-life is
8 to 12 hours, and it is excreted into urine primarily as glucuronide conjugates. The most frequently reported side
effects include disturbances of the GI system (e.g., nausea, dyspepsia, and diarrhea), dermatological reactions, and
CNS effects (e.g., dizziness and headache).
化学的特性
White Solid
使用
As a prostaglandin synthetase inhibitor, diflunisal exhibits analgesic, fever-reducing, and
anti-inflammatory action. It is used for long- and short-lasting symptomatic relief of low
to moderate pain in osteoarthritis and rheumatoid arthritis.
一般的な説明
Diflunisal (Dolobid), is a longer acting and more potent drugthan aspirin because of its hydrophobic, 2,4-difluorophenylgroup attached to the 5-position of the salicyclic acid. In alarge-scale comparative study with aspirin, it was also bettertolerated with less GI complications than aspirin. It ismarketed in tablet form for treating mild to moderate postoperativepain as well as RA and OA.
Diflunisal is highly protein bound. Its metabolism is subjectto a dose-dependent, saturable, and capacity-limitedglucuronide formation. This unusual pharmacokineticprofile is a result of an enterohepatic circulation and the reabsorptionof 65% of the drug and its glucuronides, followedby cleavage of its unstable, acyl glucuronide back tothe active drug. Thus, diflunisal usage in patients with renalimpairment should be closely monitored.
薬物動態学
Diflunisal is more
potent than aspirin but produces fewer side effects and has a biological half-life three to four times greater than that
of aspirin. It is rapidly and completely absorbed on oral administration, with peak plasma levels being achieved within
2 to 3 hours of administration. It is highly bound (99%) to plasma proteins after absorption. Its elimination half-life is
8 to 12 hours, and it is excreted into urine primarily as glucuronide conjugates. The most frequently reported side
effects include disturbances of the GI system (e.g., nausea, dyspepsia, and diarrhea), dermatological reactions, and
CNS effects (e.g., dizziness and headache).
臨床応用
Diflunisal (pKa 3.3) was introduced in the United States in 1982 and has gained considerable acceptance as an
analgetic and as a treatment of rheumatoid arthritis and osteoarthritis. Diflunisal is metabolized primarily to ether and
ester glucuronide conjugates.
安全性プロファイル
Poison by ingestion,
subcutaneous, and intraperitoneal routes.
Human systemic effects by ingestion: tolerance, and cholestatic jaundce (due to
the stoppage of the flow of bile),
agranulocytosis, increased body temperature.
An experimental teratogen. Other
experimental reproductive effects. An
analgesic and anti-inflammatory agent.
When heated to decomposition it emits
toxic fumes of F-. See also FLUORIDES.
ジフルニサル 上流と下流の製品情報
原材料
準備製品