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 α production with an absence of gastric damage, in contrast with indomethacin. In repeat dose studies. 6MNA failed to indece gastrointestinal damage even at doses where general toxicity was evident. These results show that in the rat, 6MNA is an effective antiinnflammatory drug but even in very high intravneous doses does not have the propensity to induce gastrointestinal damage.
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Melarange, R., Gentry, C., O'conell, C. et al. Antiinflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6-methoxy-2-naphthylacetic acid (6MNA). Digest Dis Sci 37, 1847–1852 (1992). https://doi.org/10.1007/BF01308078
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DOI: https://doi.org/10.1007/BF01308078