Ulcerogenicity and effect on inhibition of prostaglandin generation of indometacin farnesil, a prodrug of indomethacin, in rat gastric mucosa: comparison with indomethacin or loxoprofen.
Indometacin farnesil was compared with indomethacin and loxoprofen in rats to ascertain whether it caused less gastric mucosal damage than the two older drugs. Damage was evaluated in terms of the size of ulcers that formed after oral administration and the changes in concentrations of prostaglandins E2 and I2 in the mucosa. Indometacin farnesil caused less damage than indomethacin and tended to cause less damage than loxoprofen. Indometacin farnesil was less potent than indomethacin in inhibiting prostaglandin generation by gastric mucosa. This property of indometacin farnesil may contribute to the low ulcerogenicity of this compound.
Arakawa
T
T
Third Department of Internal Medicine, Osaka City University Medical School, Japan.
Fukuda
T
T
Nakagawa
K
K
Higuchi
K
K
Watanabe
T
T
Tominaga
K
K
Kobayashi
K
K
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology* / Q000633:toxicity*; D015232:Dinoprostone / Q000096:biosynthesis; D011464:Epoprostenol / Q000096:biosynthesis; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D007213:Indomethacin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D010666:Phenylpropionates / Q000494:pharmacology* / Q000633:toxicity*; D011355:Prodrugs / Q000494:pharmacology* / Q000633:toxicity*; D011448:Prostaglandin Antagonists / Q000494:pharmacology* / Q000633:toxicity*; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced* / Q000473:pathology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D010666:Phenylpropionates; D011355:Prodrugs; D011448:Prostaglandin Antagonists; C040656:loxoprofen; D011464:Epoprostenol; D015232:Dinoprostone; C060022:indomethacin farnesil; D007213:Indomethacin