214
Views
82
CrossRef citations to date
0
Altmetric
Drug Profile

Rebamipide: a gastrointestinal protective drug with pleiotropic activities

&
Pages 261-270 | Published online: 10 Jan 2014

References

  • Uchida M, Tabusa F, Komatsu M et al. Studies on 2(1H)-quinolinone derivatives as gastric antiulcer active agents. 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl] propionic acid related compounds. Chem. Pharm. Bull.33(9), 3775–3786 (1985).
  • Uchida M, Tabusa F, Komatsu M et al. Studies on 2(1H)-quinolinone derivatives as gastric antiulcer active agents. synthesis and antiulcer activity of the metabolites of 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic acid. Chem. Pharm. Bull.34(9), 4821–4824 (1986).
  • Uchida M, Tabusa F, Komatsu M et al. Studies on 2(1H)-quinolinone derivatives as gastric antiulcer active agents. synthesis and antiulcer activity of optically active a-amino acid derivatives of 2(1H)-quinolinone and oxindole. Chem. Pharm. Bull.35(2), 853–856 (1987).
  • Yamasaki K, Ishiyama H, Imaizumi T et al. Effect of OPC-12759, a novel antiulcer agent, on chronic and acute experimental gastric ulcer, and gastric secretion in rats. Jpn. J. Pharmacol.49(4), 441–448 (1989).
  • Iijima K, Ichikawa T, Okada S et al. Rebamipide, a cytoprotective drug, increases gastric mucus secretion in human: evaluations with endoscopic gastrin test. Dig. Dis. Sci.54(7), 1500–1507 (2009).
  • Yamasaki K, Kanbe T, Chijiwa T, Ishiyama H, Morita S. Gastric mucosal protection by OPC-12759, a novel antiulcer compound, in the rat. Eur. J. Pharmacol.142(1), 23–29 (1987).
  • Kleine A, Kluge S, Peskar BM. Stimulation of prostaglandin biosynthesis mediates gastroprotective effect of rebamipide in rats. Dig. Dis. Sci.38(8), 1441–1449 (1993).
  • Suetsugu H, Ishihara S, Moriyama N et al. Effect of rebamipide on prostaglandin EP4 receptor gene expression in rat gastric mucosa. J. Lab. Clin. Med.136(1), 50–57 (2000).
  • Sun WH, Tsuji S, Tsujii M et al. Induction of cyclooxygenase-2 in rat gastric mucosa by rebamipide, a mucoprotective agent. J. Pharmacol. Exp. Ther.295(2), 447–452 (2000).
  • Ishihara K, Komuro Y, Nishiyama N, Yamasaki K, Hotta K. Effect of rebamipide on mucus secretion by endogenous prostaglandin-independent mechanism in rat gastric mucosa. Arzneimittelforschung42(12), 1462–1466 (1992).
  • Yoshikawa T, Naito Y, Tanigawa T, Kondo M. Free radical scavenging activity of the novel anti-ulcer agent rebamipide studied by electron spin resonance. Arzneimittelforschung43(3), 363–366 (1993).
  • Naito Y, Yoshikawa T, Tanigawa T et al. Hydroxyl radical scavenging by rebamipide and related compounds: electron paramagnetic resonance study. Free Radic. Biol. Med.18(1), 117–123 (1995).
  • Sakurai K, Sasabe H, Koga T, Konishi T. Mechanism of hydroxyl radical scavenging by rebamipide: identification of mono-hydroxylated rebamipide as a major reaction product. Free Radic. Res.38(5), 487–494 (2004).
  • Ogino K, Hobara T, Ishiyama H et al. Antiulcer mechanism of action of rebamipide, a novel antiulcer compound, on diethyldithiocarbamate-induced antral gastric ulcers in rats. Eur. J. Pharmacol.212(1), 9–13 (1992).
  • Suzuki M, Miura S, Mori M et al. Rebamipide, a novel antiulcer agent, attenuates Helicobacter pylori induced gastric mucosal cell injury associated with neutrophil derived oxidants. Gut35(10), 1375–1378 (1994).
  • Kim JS, Kim JM, Jung HC, Song IS. Expression of cyclooxygenase-2 in human neutrophils activated by Helicobacter pylori water-soluble proteins: possible involvement of NF-κB and MAPK signaling pathway. Dig. Dis. Sci.46(10), 2277–2284 (2001).
  • Yoshida N, Yoshikawa T, Iinuma S et al. Rebamipide protects against activation of neutrophils by Helicobacter pylori. Dig. Dis. Sci.41(6), 1139–1144 (1996).
  • Murakami K, Okajima K, Uchiba M et al. Rebamipide attenuates indomethacin-induced gastric mucosal lesion formation by inhibiting activation of leukocytes in rats. Dig. Dis. Sci.42(2), 319–325 (1997).
  • Naito Y, Kuroda M, Mizushima K et al. Transcriptome analysis for cytoprotective actions of rebamipide against indomethacin-induced gastric mucosal injury in rats. J. Clin. Biochem. Nutr.41(3), 202–210 (2007).
  • Kinjo N, Kawanaka H, Akahoshi T et al. Significance of ERK nitration in portal hypertensive gastropathy and its therapeutic implications. Am. J. Physiol. Gastrointest. Liver Physiol.295(5), G1016–1024 (2008).
  • Nishizawa T, Suzuki H, Nakagawa I et al. Rebamipide-promoted restoration of gastric mucosal sonic hedgehog expression after early Helicobacter pylori eradication. Digestion79(4), 259–262 (2009).
  • Hasegawa S, Sekino H, Matsuoka O et al. Bioequivalence of rebamipide granules and tablets in healthy adult male volunteers. Clin. Drug Investig.23(12), 771–779 (2003).
  • Shioya Y, Shimizu T. High-performance liquid chromatographic procedure for the determination of a new anti-gastric ulcer agent, 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic acid, in human plasma and urine. J. Chromatogr.434(1), 283–287 (1988).
  • Koyama N, Sasabe H, Miyamoto G. Involvement of cytochrome P450 in the metabolism of rebamipide by the human liver. Xenobiotica32(7), 573–586 (2002).
  • Blume H, Donath F, Warnke A, Schug BS. Pharmacokinetic drug interaction profiles of proton pump inhibitors. Drug Saf.29(9), 769–784 (2006).
  • Hansten PD. Aliment drug interactions with antisecretory agents. Pharmacol. Ther.5(Suppl. 1), 121–128 (1991).
  • Arakawa T, Kobayashi K, Yoshikawa T, Tarnawski A. Rebamipide: overview of its mechanisms of action and efficacy in mucosal protection and ulcer healing. Dig. Dis. Sci.43(9 Suppl.), 5S–13S (1998).
  • Arakawa T, Higuchi K, Fujiwara Y et al. 15th anniversary of rebamipide: looking ahead to the new mechanisms and new applications. Dig. Dis. Sci.50(Suppl. 1), S3–S11 (2005).
  • Turner J. Intestinal mucosal barrier function in health and disease. Nat. Rev. Immunol.9(11), 799–809 (2009).
  • Suzuki T, Yoshida N, Nakabe N et al. Prophylactic effect of rebamipide on aspirin-induced gastric lesions and disruption of tight junctional protein zonula occludens-1 distribution. J. Pharmacol. Sci.106(3), 469–477 (2008).
  • Hashimoto K, Oshima T, Tomita T et al. Oxidative stress induces gastric epithelial permeability through claudin-3. Biochem. Biophys. Res. Commun.376(1), 154–157 (2008).
  • Laharie D, Menard S, Asencio C et al. Effect of rebamipide on the colonic barrier in interleukin-10-deficient mice. Dig. Dis. Sci.52(1), 84–92 (2007)
  • Terano A, Arakawa T, Sugiyama T et al. Rebamipide, a gastro-protective and anti-inflammatory drug, promotes gastric ulcer healing following eradication therapy for Helicobacter pylori in a Japanese population: a randomized, double-blind, placebo-controlled trial. J. Gastroenterol.42(8), 690–693 (2007).
  • Ohashi Y, Aihara E, Takasuka H, Takahashi K, Takeuchi K. Antral ulcers induced by alendronate, a nitrogen-containing biphophonate, in rat stomachs – prophylactic effect of rebamipide. J. Physiol. Pharmacol.60(3), 85–93 (2009).
  • Aihara E, Hayashi S, Amagase K, Kato S, Takeuchi K. Prophylactic effect of rebamipide against the irritative and healing impairment actions of alendronate in rat stomachs. Inflammopharmacology15(5), 196–202 (2007).
  • Yoshikawa T, Naito Y, Nakamura S et al. Effect of rebamipide on lipid peroxidation and gastric mucosal injury induced by indometacin in rats. Arzneimittelforschung43(12), 1327–1330 (1993).
  • Naito Y, Kuroda M, Mizushima K et al. Transcriptome analysis for cytoprotective actions of rebamipide against indomethacin-induced gastric mucosal injury in rats. J. Clin. Biochem. Nutr.41(3), 202–210 (2007).
  • Iwai A, Iwashita E. Changes in colonic inflammation induced by dextran sulfate sodium (DSS) during short- and long-term administration of rebamipide. Dig. Dis. Sci.43(9 Suppl.), 143S–147S (1998).
  • Kishimoto S, Haruma K, Tari A et al. Rebamipide, an antiulcer drug, prevents DSS-induced colitis formation in rats. Dig. Dis. Sci.45(8), 1608–1616 (2000).
  • Okayama M, Tsubouchi R, Nishio H, Kato S, Takeuchi K. Protective effect of intra-rectal administration of rebamipide on dextran sulfate sodium-induced rat colitis. Digestion70(4), 240–249 (2004).
  • Nakashima T, Maeda T, Nagamoto H et al. Rebamipide enema is effective for treatment of experimental dextran sulfate sodium induced colitis in rats. Dig. Dis. Sci.50(Suppl. 1), S124–S131 (2005).
  • Murai R, Kanbe T, Mukoyama T et al. Effect of rectal administration of rebamipide on dextran sulfate sodium-induced colitis: role of hepatocyte growth factor. Inflamm. Res.56(6), 240–245 (2007).
  • Tarnawski A, Pai R, Chiou SK, Chai J, Chu EC. Rebamipide inhibits gastric cancer growth by targeting survivin and Aurora-B. Biochem. Biophys. Res. Commun.334(1), 207–212 (2005).
  • Tanigawa T, Pai R, Arakawa T, Tarnawski AS. Rebamipide inhibits gastric cancer cell growth. Dig. Dis. Sci.52(1), 240–247 (2007).
  • Higuchi K, Fujiwara Y, Tominaga K et al. Is eradication sufficient to heal gastric ulcers in patients infected with Helicobacter pylori? A randomized, controlled, prospective study. Aliment. Pharmacol. Ther.17(1), 111–117 (2003).
  • Terano A, Arakawa T, Sugiyama T et al. A pilot study to evaluate a new combination therapy for gastric ulcer: Helicobacter pylori eradication therapy followed by gastroprotective treatment with rebamipide. J. Gastroenterol. Hepatol.21(1 Pt 1), 103–109 (2006).
  • Kato T, Araki H, Onogi F et al. Clinical trial: rebamipide promotes gastric ulcer healing by proton pump inhibitor after endoscopic submucosal dissection – a randomized controlled study. J. Gastroenterol.45(3), 285–290 (2009).
  • Talley NJ, Zinsmeister AR, Schleck CD et al. Dyspepsia and dyspepsia subgroups: a population-based study. Gastroenterology102(4 Pt 1), 1259–1268 (1992).
  • Talley NJ, Riff DS, Schwartz H, Marcuard SP. Double-blind placebo-controlled multicentre studies of rebamipide, a gastroprotective drug, in the treatment of functional dyspepsia with or without Helicobacter pylori infection. Aliment. Pharmacol. Ther.15(10), 1603–1611 (2001).
  • Miwa H, Osada T, Nagahara A et al. Effect of a gastro-protective agent, rebamipide, on symptom improvement in patients with functional dyspepsia: a double-blind placebo-controlled study in Japan. J. Gastroenterol. Hepatol.21(12), 1826–1831 (2006).
  • Chitapanarux T, Praisontarangkul OA, Lertprasertsuke N. An open-labeled study of rebamipide treatment in chronic gastritis patients with dyspeptic symptoms refractory to proton pump inhibitors. Dig. Dis. Sci.53(11), 2896–2903 (2008).
  • Du Y, Li Z, Zhan X et al. Anti-inflammatory effects of rebamipide according to Helicobacter pylori status in patients with chronic erosive gastritis: a randomized sucralfate-controlled multicenter trial in China-STARS study. Dig. Dis. Sci.53(11), 2886–2895 (2008).
  • Naito Y, Yoshikawa T, Yoshida N, Kondo M. Role of oxygen radical and lipid peroxidation in indomethacin-induced gastric mucosal injury. Dig. Dis. Sci.43(9 Suppl.), 30S–34S (1998).
  • Naito Y, Iinuma S, Yagi N et al. Prevention of Indomethacin-induced gastric mucosal injury in Helicobacter pylori-negative healthy volunteers: a comparison study rebamipide vs famotidine. J. Clin. Biochem. Nutr.43(1), 34–40 (2008).
  • Kim HK, Kim JI, Kim JK et al. Preventive effects of rebamipide on NSAID-induced gastric mucosal injury and reduction of gastric mucosal blood flow in healthy volunteers. Dig. Dis. Sci.52(8), 1776–1782 (2007).
  • Yamao J, Kikuchi E, Matsumoto M et al. Assessing the efficacy of famotidine and rebamipide in the treatment of gastric mucosal lesions in patients receiving long-term NSAID therapy (FORCE – famotidine or rebamipide in comparison by endoscopy). J. Gastroenterol.41(12), 1178–1185 (2006).
  • Park SH, Cho CS, Lee OY et al. Comparison of prevention of NSAID-Induced gastrointestinal complications by rebamipide and misoprostol: a randomized, multicenter, controlled trial – STORM STUDY. J. Clin. Biochem. Nutr.40(2), 148–155 (2007).
  • Ono S, Kato M, Imai A et al. Preliminary trial of rebamipide for prevention of low-dose aspirin-induced gastric injury in healthy subjects: a randomized, double-blind, placebo-controlled, cross-over study. J. Clin. Biochem. Nutr.45(2), 248–253 (2009).
  • Niwa Y, Nakamura M, Ohmiya N et al. Efficacy of rebamipide for diclofenac-induced small-intestinal mucosal injuries in healthy subjects: a prospective, randomized, double-blinded, placebo-controlled, cross-over study. J. Gastroenterol.43(4), 270–276 (2008).
  • Mizoguchi H, Ogawa Y, Kanatsu K et al. Protective effect of rebamipide on indomethacin-induced intestinal damage in rats. J. Gastroenterol. Hepatol.16(10), 1112–1119 (2001).
  • Watanabe T, Sugimori S, Kameda N et al. Small bowel injury by low-dose enteric-coated aspirin and treatment with misoprostol: a pilot study. Clin. Gastroenterol. Hepatol.6(11), 1279–1282 (2008).
  • Makiyama K, Takeshima F, Kawasaki H, Zea-Iriarte WL. Anti-inflammatory effect of rebamipide enema on proctitis type ulcerative colitis: a novel therapeutic alternative. Am. J. Gastroenterol.95(7), 1838–1839 (2000).
  • Makiyama K, Takeshima F, Hamamoto T. Efficacy of rebamipide enemas in active distal ulcerative colitis and proctitis: a prospective study report. Dig. Dis. Sci.50(12), 2323–2329 (2005).
  • Miyata M, Kasugai K, Ishikawa T et al. Rebamipide enemas-new effective treatment for patients with corticosteroid dependent or resistant ulcerative colitis. Dig. Dis. Sci.50(Suppl. 1), S119–S123 (2005).
  • Furuta R, Kusugami K, Goto H. [Enema therapy for ulcerative colitis patients]. Nippon Rinsho63(5), 845–849 (2005).
  • Arakawa T, Kobayashi K. Quality of ulcer healing – a new concept to rank healed peptic ulcers. Gastroenterol. Jpn.28(Suppl. 5), 158–162 (1993).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.