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Pharmacological action of Acemetacin

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 Acemetacin has significant anti-inflammatory and analgesic effects. Pharmacological studies have shown that the experimental adjuvant or carrageenan experimental foot swelling test shows that it has a pharmacological effect that significantly inhibits inflammation; and it has been shown by mouse writhing method. Strong analgesic effect; and have a good dose-effect relationship. Acemexin had no effect on heart rate, blood flow, oxygen saturation, and blood pressure, and had no sedative or antispasmodic effects. No damage to liver and kidney function. The carboxymethyl ester of indomethacin acts in the body to metabolize into indomethacin. In addition to inhibiting the synthesis of prostaglandins, the mechanism of action stabilizes the lysosomal membrane and inhibits the release of inflammatory mediators such as protease, hyaluronidase and histamine; it also has activity against bradykinin and inhibits the action of complement, and this effect Significantly stronger than indomethacin. Therefore, Acemetacin inhibits the inflammatory response from multiple links, thereby exerting its anti-inflammatory and analgesic effects, and the drug has a high concentration in the inflammation site, so the curative effect is good. It inhibits platelet aggregation like other non-steroidal anti-inflammatory drugs. Compared with indomethacin, Acemetacin has a weak ability to inhibit the synthesis of physiological prostaglandins, so it is lightly irritating to the digestive tract and well tolerated.

  Acemetacin absorbs quickly and completely after oral administration. The bioavailability after repeated administration is up to 100%. After 6 hours of oral administration, the steady state was reached, and the levels of active ingredients in synovial fluid, synovial membrane and muscle were significantly higher than the blood levels and reached an effective therapeutic concentration. Acemetacin is metabolized by the liver after oral absorption, and its main active metabolite is indomethacin. After long-term use, the concentration ratio of Acemetacin to indomethacin in the blood is about 1:1. The peak plasma concentrations of Acemetacin and its main metabolite, indomethacin, were 2.4 h and 4 h, respectively. The half-lives were 1.1 h and 7.1 h, respectively. The plasma protein binding rate was between 87.6% and 93.7%. About 40% of Acemetacin is excreted by the kidneys as a prodrug, and the remaining active metabolites (indomexin) and inactive metabolites are excreted by bile through the feces.