Abstract

Gian Maria Pacifici*

ABSTRACT

Indomethacin is a methylated indole derivative indicated for the treatment of moderate-to-severe rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute gouty arthritis, and acute painful shoulder. Indomethacin is a potent nonselective inhibitor of cyclooxygenase, inhibits the motility of polymorphonuclear leukocytes, and depresses the biosynthesis of mucopolysaccharides. Indomethacin, administered intravenously at the dose of 0.1 to 0.25 mg/kg twice-daily for three doses, is used to close the patent ductus arteriosus in preterm neonates and in adults the intravenous dose of indomethacin is 100 mg twice-daily or thrice-daily. Indomethacin has an excellent bioavailability. The efficacy and safely, the prophylaxis, and the treatment with indomethacin, and the trials conducted with indomethacin have been reviewed. Indomethacin is O-demethylated by CYP2C9, CYP1A2, and by CYP2D6 and is conjugated with glucuronic acid by UGT1A1, UGT1A3, UGT1A9, and by UGT2B7. Indomethacin is an active metabolite of acemetacin. The pharmacokinetics of indomethacin have been studied in health volunteers following the administration of a single dose and multiple doses of 90 mg of acemetacin sustained-release tablets and acemetacin sustained-release capsules. The elimination half-life of indomethacin is about 10 hours following the administration of single and multiple doses of both acemetacin formulations. The interaction of indomethacin with drugs and the toxicity induced by indomethacin have been reviewed. The aim of this study is to review the efficacy and safely, the prophylaxis, and the treatment with indomethacin. In addition, the trials conducted with indomethacin, the metabolism, and the pharmacokinetics of indomethacin, the interaction of indomethacin with drugs, and the toxicity induced by indomethacin have been reviewed.