InflammoPharmacology

, Volume 3, Issue 3, pp 259–270

Nabumetone, in contrast to etodolac, lacks gastrointestinal irritancy in the rat: Assessment by the inflammatory marker, haptoglobin, and blood loss

Authors

  • R. Melarange
    • SmithKline Beecham PharmaceuticalsResearch and Development Technologies
  • C. Gentry
    • SmithKline Beecham PharmaceuticalsResearch and Development Technologies
  • P. R. Blower
    • SmithKline Beecham PharmaceuticalsResearch and Development Technologies
  • C. D. N. Toseland
    • Research and Development TechnologiesSmithKline Beecham Pharmaceuticals
  • R. Spangler
    • Worldwide Strategic Product Development, Four Falls Corporate CenterSmithKline Beecham Corporation
Article

DOI: 10.1007/BF02659123

Cite this article as:
Melarange, R., Gentry, C., Blower, P.R. et al. Inflammopharmacology (1995) 3: 259. doi:10.1007/BF02659123

Abstract

The aim of the present study was to compare the effects of the non-acidic anti-inflammatory drug, nabumetone, with those of etodolac on gastrointestinal mucosal integrity and blood loss in the rat. Gastrointestinal damage was absent in nabumetone-treated animals even at a high anti-inflammatory dose (79 mg/kg). Plasma haptoglobin, a marker of mucosal integrity, and caecal haemoglobin, a measure of blood loss, were also unchanged compared with controls. In contrast, etodolac induced both gastric (ED50 30 mg/kg) and ileal (ED50 4.5 mg/kg) ulceration in a dose-related manner. Accompany-ing these changes were increases in haptoglobin concentration and blood loss. It is suggested that nabumetone’s lack of gastrointestinal irritancy may relate, in part, to its non-acidic nature and to its active metabolite’s (6MNA) differential effects on prostanoid production and lack of enterohepatic circulation.

Keywords

NSAIDsGI ulcerationPlasma haptoglobinBlood loss

Copyright information

© Kluwer Academic Publishers 1995