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

Comparative studies with indomethacin

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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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  1. Mangan FR: Nabumetone.In Nonsteroidal Anti-inflammatory Drugs. AJ Lewis, DE Furst (eds). New York, Marcel Dekker, 1987, pp 439–472

    Google Scholar 

  2. Greb WH, von Schrader HW, Cerlek S, Domins M, Hauptmann E, Zennic N: Endoscopic studies of nabumetone in patients with reheumatoid arthritis. Am J Med 83(suppl 4b):19–24, 1987

    Google Scholar 

  3. Lemmel EM, Stroehmann I: Experice with nabumetone in the treatment of rehaumatic conditons—results of an application study in 18,047 patients. Fortschr Med 106:63–68, 1988

    Google Scholar 

  4. Lussier A, Davis A, Lussier Y, Le Bel E: Comparative gastrointestinal blood loss associated with placebo, aspirin and nabumetone as assessed by radiochromium (51Cr). J Clin Pharmacol 29:225–229, 1989

    Google Scholar 

  5. Roth SH: New understandings of NSAID gastropathy. Scand J Rheumatol Suppl 78:24–29, 1989

    Google Scholar 

  6. Robert A: Cytopreotection by prostaglandins. Gastroenterology 77:761–767, 1979

    Google Scholar 

  7. Dearden JC, Nicholson RM: Correlation between gastric irritancy and anti-inflammatory activity of non-steroidal antiinlflammatory drugs. J Pharm Pharmacol 36:713–715, 1984

    Google Scholar 

  8. Melarange R, Rashbrook LC: Comparison of the effects of nabumetone with indomethacin on rat gastric mucosal 6-keto-PGF1 α production and on bile salt-induced changes in gastric mucosal function. J Pharm Pharmacol, 39:717–720, 1987

    Google Scholar 

  9. Melarange R, Blower PR, Gentry C, O'Connell C: Nabumetone, an effective anti-inflammatory agent lacks the gastric irritancy potential of piroxicam or ibuprofen. Br J Pharmacol 99:172P, 1990

    Google Scholar 

  10. Boyle E, Freeman PC, Goudie AC, Mangan FR, Thomson M: The role of copper in pregenting gastrointestinal damage by acidic anti-inflammatory drugs. J Pharm Pharmacol 28:865–868, 1976

    Google Scholar 

  11. Melarange R, Rashbrook LC: A rat gastric mucosal preparation for studying agents which affect thein vitro production of prostanoids. Prostaglandins Leuktrienes Med 22:89–100, 1986

    Google Scholar 

  12. Brett MA, Greb WH, Kurth HJ, Rulandr G, Haddock RE, Thawley AR: Absence of enterolhepatic circulation of the active metabolite of nabumetone. Fortschr Med 106:736–737, 1988

    Google Scholar 

  13. Hemmati M, Abtahi F, Farrokhsiar M, Djahanguiri B: Prevention of restraint and indomethacin-induced gastric ulcertion by bile duct or pylorus ligation in rats. Digestion 10:108–112, 1974

    Google Scholar 

  14. Abtahi FS, Djahanguiri B: Decreased incidence of indomethacin-induced gastric ulceration in rats by bile duct diversion. Br J Surg 62:113–114, 1975

    Google Scholar 

  15. Duggan DE, Hooke KF, Noll RM, Kwan KC: Enterohepatic circulation of indomethacin and its role in intestinal irritation. Biochem Pharmacol 25:1749–1754, 1975

    Google Scholar 

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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).

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