Indomethacin
Indomethacin. Indole-acetic NSAID — potent non-selective COX inhibitor. First-line for acute gout + pericarditis. High CNS penetration →… Oral half-life 4.5 h.
Indole-acetic NSAID — potent non-selective COX inhibitor. First-line for acute gout + pericarditis. High CNS penetration → headache, dizziness, confusion in elderly. CYP2C9 substrate.
PK: the rectal bioavailability of 0.8 is verbatim, "The bioavailability after the two rectal forms was found to be almost the same, about 80%" (PMID:4090993, 8 volunteers) — though it pools a rectal solution with suppositories whose times to peak differ threefold, and another human study reports complete rectal availability instead. THE INTRAVENOUS ROUTE WAS REMOVED: its cited study is oral-only. V 21 L dropped as worse than unsourced — at 0.30 L/kg it sits BELOW the observed human range of 0.34 to 1.57 L/kg (PMID:1100305). The oral F of 0.98 and both absorption rates are dropped as unstated; the cited abstract only numbers are times to peak of 1.11, 1.25 and 1.97 hours, the classic collision.
Pharmacokinetics
- Oral — t½ 4.5 h
- Rectal — t½ 4.5 h · F 80%
Sources: PMID:22913908, PMID:1100305