Antiinflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Comparative studies with indomethacin.

Abstract	6MNA, the active metabolite of the nonacidic antiinflammatory drug nabumetone, was investigated using intravenous administration for effects on (1) carrageenan paw edema and gastric irritancy compared with either oral nabumetone or both oral and intravenous indomethacin when given acutely and (2) gastrointestinal irritancy when given in repeat dosing studies. Oral doses of nabumetone or intravenous 6MNA produced effective antiinflammatory activity together with significant inhibition of paw exudate PGE2. Antiinflammatory oral doses of nabumetone or intravenous 6MNA produced minimal effects on gastric 6-keto PGF1 alpha production with an absence of gastric damage, in contrast with indomethacin. In repeat dose studies, 6MNA failed to induce gastrointestinal damage even at doses where general toxicity was evident. These results show that in the rat, 6MNA is an effective antiinflammatory drug but even in very high intravenous doses does not have the propensity to induce gastrointestinal damage.
Authors	R Melarange, C Gentry, C O'Connell, P R Blower, C Neil, A S Kelvin, C D Toseland
Journal	Digestive diseases and sciences (Dig Dis Sci) Vol. 37 Issue 12 Pg. 1847-52 (Dec 1992) ISSN: 0163-2116 [Print] United States
PMID	1473433 (Publication Type: Comparative Study, Journal Article)
Chemical References	Anti-Inflammatory Agents, Non-Steroidal Butanones Naphthaleneacetic Acids Prostaglandins Carrageenan 6-methoxy-2-naphthylacetic acid Nabumetone Indomethacin
Topics	Administration, Oral Animals Anti-Inflammatory Agents, Non-Steroidal (pharmacology) Butanones (administration & dosage, pharmacology) Carrageenan Digestive System (drug effects, pathology) Edema (metabolism, prevention & control) Female Foot Gastric Mucosa (drug effects, metabolism) Indomethacin (administration & dosage, pharmacology) Inflammation (chemically induced, drug therapy, prevention & control) Injections, Intravenous Male Nabumetone Naphthaleneacetic Acids (administration & dosage, pharmacology) Prostaglandins (biosynthesis) Rats Rats, Sprague-Dawley Rats, Wistar

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