Indometacin Other names: Indomethacin

Chemical formula: C₁₉H₁₆ClNO₄  Molecular mass: 357.788 g/mol  PubChem compound: 3715

Pharmacodynamic properties

Indometacin has anti-inflammatory, antipyretic, and analgesic effects, it is an inhibitor of prostaglandin synthetase.

Pharmacokinetic properties

Indometacin is rapidly and almost completely absorbed on oral administration, and peak plasma levels are reached in ½ to 2 hours. Absorption is slowed but remains virtually complete when taken with food. About 90% is bound to plasma proteins. It appears to undergo enterohepatic cycling. It is metabolised partly by O-demthylation, partly by N-deacylation, and unchanged drug and metabolites are partly conjugated with glucoronic acid, in man, it is excreted unchanged and as it metabolites in both urine and faeces.

Preclinical safety data

Administration of indomethacin to experimental animals at doses of 0.1-1.94 times the maximum recommended human clinical dose (MRHD) resulted in: i) maternal toxicity and death, ii) increased pre- and post-implantation loss, iii) increased embryotoxicity, foetal resorptions and foetal death, and iv) increased spontaneous abortion.

In pregnant mice and rats, indometacin treatment (during organogenesis) induced developmental defects including retarded foetal ossification and skeletal malformations at doses of 0.02-0.95 times the MRHD.

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