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Rebamipide

From Wikipedia, the free encyclopedia
Amino acid derivative
Pharmaceutical compound
Rebamipide
Clinical data
Trade namesMucosta(JP), Rebagen(KR,CN,IN), Rebagit(RU), Ramiper, Rebamax(ID)
AHFS/Drugs.comInternational Drug Names
Routes of
administration
By mouth (tablets)
ATC code
Identifiers
  • 2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1H-quinolin-4-yl)propanoic acid
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC19H15ClN2O4
Molar mass370.79 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1)C(=O)NC(C(=O)O)CC2=CC(=O)Nc3ccccc32
  • InChI=1S/C19H15ClN2O4/c20-13-7-5-11(6-8-13)18(24)22-16(19(25)26)9-12-10-17(23)21-15-4-2-1-3-14(12)15/h1-8,10,16H,9H2,(H,21,23)(H,22,24)(H,25,26) checkY
  • Key:ALLWOAVDORUJLA-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Rebamipide, anamino acid derivative of 2-(1H)-quinolinone, is used formucosal protection,[1] healing ofgastroduodenal ulcers, and treatment ofgastritis.[2] It works by enhancing mucosal defense, scavenging freeradicals,[3] and temporarily activating genes encodingcyclooxygenase-2.[4]

Studies have shown that rebamipide can fight the damaging effects ofNSAIDs on theGIT mucosa,[5] and more recently, the small intestine, but not for naproxen-induced gastric damage.[6]

Availability

[edit]

Rebamipide is used in a number of Asian countries includingJapan (marketed as Mucosta),South Korea,China[7] andIndia (where it is marketed under the trade name Rebagen). It is also approved inRussia under the brand name Rebagit.[8]

Effects

[edit]

Rebamipide increases gastric mucosalprostaglandin E2, protects gastric mucosa, thereby suppresses gastric mucosal damage and increases gastric mucus secretion and gastric mucosal blood flow, to improve hemodynamic impairment, suppress inflammation and repair the gastric mucosa. It is usually used to treat gastric ulcer and improve gastric mucosal lesion (erosion, bleeding, redness and edema) in acute gastritis and acute exacerbation period of chronic gastritis.

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.doi:10.1007/bf02063257.PMID 7587834.S2CID 22807270.
  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.S2CID 16906464.
  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.doi:10.1023/b:ddas.0000017439.60943.5c.PMID 15104358.S2CID 31756608.
  5. ^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.S2CID 4887031.
  6. ^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.
  7. ^"Rebamipide".Drugs.com.
  8. ^"Registration Sertificate: Rebagit (rebamipide) Film-Coated Tablets" (in Russian). Russian State Register of Medicines. Retrieved10 June 2017.
H2 antagonists ("-tidine")
Prostaglandins (E)/
analogues ("-prost-")
Proton-pump inhibitors
("-prazole")
Potassium-competitive
acid blockers
("-prazan")
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