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Indomethacin, also known as anti-inflammatory pain, is a strong non-corticosteroidal anti-inflammatory, antipyretic and analgesic drug, which inhibits the formation of nociceptive nerve impulses in inflamed tissues by inhibiting cyclooxygenase to reduce the synthesis of prostaglandins (PG), and inhibits the inflammatory response, including the inhibition of the chemotaxis of leukocytes and release of lysosomal enzymes, which in turn generates the effects of antipyretics, analgesia and inflammation.
The anti-inflammatory effect of indomethacin is stronger than that of pau taisone and hydrocortisone, and the combined application can reduce the dosage and side effects of the latter.
The antipyretic effect is 10 times that of aminopyrine. But the analgesic effect is weak, only for inflammatory pain has obvious analgesic effect.
Gastrointestinal absorption is rapid and complete after internal administration in monogastric animals. The peak time of blood drug is 1.5~2h, and the plasma protein binding rate reaches 90%. In the liver and glucuronic acid binding, excreted by the kidneys.
Some of it is also reabsorbed into the intestine with bile, and the rest is excreted by faeces. Used for postoperative trauma, arthritis, tendinitis, muscle injury and other inflammatory pain.
Uses and functions of Indometacin.
Cyclooxygenase (COX) inhibitor, selectively inhibits COX-1; blocks prostasol biosynthesis.
It has obvious anti-inflammatory and antipyretic effects in medicine, and is mainly used in rheumatic arthritis, ankylosing spondylitis, osteoarthritis, etc., which are not easy to tolerate salicylic acid drugs or the therapeutic effect is not significant.
The anti-inflammatory effect of indomethacin is stronger than that of pau taisone and hydrocortisone, and the combined application can reduce the dosage and side effects of the latter.
The antipyretic effect is 10 times that of aminopyrine. But the analgesic effect is weak, only for inflammatory pain has obvious analgesic effect.
Gastrointestinal absorption is rapid and complete after internal administration in monogastric animals. The peak time of blood drug is 1.5~2h, and the plasma protein binding rate reaches 90%. In the liver and glucuronic acid binding, excreted by the kidneys.
Some of it is also reabsorbed into the intestine with bile, and the rest is excreted by faeces. Used for postoperative trauma, arthritis, tendinitis, muscle injury and other inflammatory pain.
Adverse Reaction of Indometacin.
① Nausea, vomiting, abdominal pain, diarrhoea, poor appetite, and in severe cases, ulcers may develop and cause bleeding and perforation. Can be taken immediately after meals to reduce the incidence.
② Common headache, dizziness, fatigue, occasional convulsions, confusion, fainting and so on. Attention should be paid to stop the drug at the right time.
③ Itchy skin, erythema, urticaria and rarely asthma attack, dyspnoea and even inhibition of respiration and circulation.
④ Inhibition of the haematopoietic system such as granulocytopenia, aplastic anaemia and thrombocytopenia. Although rare, the consequences are more serious. There are other reactions that are similar to aspirin and the precautions are the same.
Production Method of Bulk Indometacin Powder.
P-aminoanisole is diazotised, reduced, acidified, hydrolysed and cyclised to give anti-inflammatory pain.
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