Rebamipide

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Rebamipide
Rebamipide.svg
Clinical data
Trade namesMucosta (JP), Rebagen (KR, CN, IN), Rebagit (RU)
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral (tablets)
ATC code
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H15ClN2O4
Molar mass370.786 g/mol g·mol−1
3D model (JSmol)
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Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection,[1] healing of gastroduodenal ulcers, and treatment of gastritis.[2] It works by enhancing mucosal defense, scavenging free radicals,[3] and temporarily activating genes encoding cyclooxygenase-2.[4]

Rebamipide is used in a number of Asian countries including Japan (marketed as Mucosta), South Korea, China[5] and India (where it is marketed under the trade name Rebagen). It is also approved in Russia under the brand name Rebagit.[6] It is not approved by the Food and Drug Administration for use in the United States.

Studies have shown that rebamipide can fight the damaging effects of NSAIDs on the GIT mucosa,[7] and more recently, the small intestine, but not for naproxen-induced gastric damage.[8] It has also been studied for the treatment of Behçet's disease.[9] It was shown to successfully treat pouchitis in a single-N study after first-line therapies for the condition were unsuccessful.[10] Some studies have shown effectiveness in presbyacusis (age-related hearing loss).[11]

It has also been shown to alleviate signs and symptoms of dry eyes in a randomized controlled trial although this is not yet widely available clinically.[12]

References[edit]

  1. ^ Arakawa T, Kobayashi K, Yoshikawa T, Tarnawski A (September 1998). "Rebamipide: overview of its mechanisms of action and efficacy in mucosal protection and ulcer healing". Digestive Diseases and Sciences. 43 (9 Suppl): 5S–13S. PMID 9753220.
  2. ^ Arakawa T, Watanabe T, Fukuda T, Yamasaki K, Kobayashi K (November 1995). "Rebamipide, novel prostaglandin-inducer accelerates healing and reduces relapse of acetic acid-induced rat gastric ulcer. Comparison with cimetidine". Digestive Diseases and Sciences. 40 (11): 2469–72. PMID 7587834.
  3. ^ Takumida M, Anniko M (January 2009). "Radical scavengers for elderly patients with age-related hearing loss". Acta Oto-Laryngologica. 129 (1): 36–44. doi:10.1080/00016480802008215. PMID 18607930.
  4. ^ Tarnawski AS, Chai J, Pai R, Chiou SK (February 2004). "Rebamipide activates genes encoding angiogenic growth factors and Cox2 and stimulates angiogenesis: a key to its ulcer healing action?". Digestive Diseases and Sciences. 49 (2): 202–9. PMID 15104358.
  5. ^ "Rebamipide". Drugs.com.
  6. ^ "Registration Sertificate: Rebagit (rebamipide) Film-Coated Tablets" (in Russian). Russian State Register of Medicines. Retrieved 10 June 2017.
  7. ^ Zhang S, Qing Q, Bai Y, Mao H, Zhu W, Chen Q, Zhang Y, Chen Y (July 2013). "Rebamipide helps defend against nonsteroidal anti-inflammatory drugs induced gastroenteropathy: a systematic review and meta-analysis". Digestive Diseases and Sciences. 58 (7): 1991–2000. doi:10.1007/s10620-013-2606-0. PMID 23456504.
  8. ^ Gagliano-Jucá T, Moreno RA, Zaminelli T, Napolitano M, Magalhães AF, Carvalhaes A, Trevisan MS, Wallace JL, De Nucci G (June 2016). "Rebamipide does not protect against naproxen-induced gastric damage: a randomized double-blind controlled trial". BMC Gastroenterology. 16 (1): 58. doi:10.1186/s12876-016-0472-x. PMC 4893238. PMID 27259970.
  9. ^ Matsuda T, Ohno S, Hirohata S, Miyanaga Y, Ujihara H, Inaba G, Nakamura S, Tanaka S, Kogure M, Mizushima Y (2003). "Efficacy of rebamipide as adjunctive therapy in the treatment of recurrent oral aphthous ulcers in patients with Behçet's disease: a randomised, double-blind, placebo-controlled study". Drugs in R&D. 4 (1): 19–28. doi:10.2165/00126839-200304010-00002. PMID 12568631.
  10. ^ Miyata M, Konagaya T, Kakumu S, Mori T (January 2006). "Successful treatment of severe pouchitis with rebamipide refractory to antibiotics and corticosteroids: a case report". World Journal of Gastroenterology. 12 (4): 656–8. doi:10.3748/wjg.v12.i4.656. PMC 4066106. PMID 16489687.
  11. ^ Takumida M, Anniko M (December 2005). "Radical scavengers: a remedy for presbyacusis. A pilot study". Acta Oto-Laryngologica. 125 (12): 1290–5. doi:10.1080/00016480510037032. PMID 16303676.
  12. ^ Kinoshita S, Oshiden K, Awamura S, Suzuki H, Nakamichi N, Yokoi N (June 2013). "A randomized, multicenter phase 3 study comparing 2% rebamipide (OPC-12759) with 0.1% sodium hyaluronate in the treatment of dry eye". Ophthalmology. 120 (6): 1158–65. doi:10.1016/j.ophtha.2012.12.022. PMID 23490326.