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瑞巴派特

维基百科,自由的百科全书
瑞巴派特
瑞巴派特的化学结构
臨床資料
商品名Mucosta(美国达)、Rebagen(瑞巴根)、Rebagit
AHFS/Drugs.com国际药品名称
给药途径口服
ATC碼
法律規範狀態
法律規範
  • 处方药
藥物動力學數據
血漿蛋白結合率98.4%
药物代谢肝脏细胞色素P450
生物半衰期约2小时
排泄途徑肾脏(尿液)
识别信息
  • 2-[(4-氯苯甲酰)氨基]-3-(2-氧代-1H-喹啉-4-基)丙酸
CAS号90098-04-7  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
化学信息
化学式C19H15ClN2O4
摩尔质量370.79 g/mol
3D模型(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

瑞巴派特(英語:Rebamipide)是2-(1H)-喹啉酮的氨基酸衍生物,用于黏膜保护、[1]治疗消化性溃疡以及胃炎的治疗。[2]它通过增强黏膜防御、清除自由基[3]以及暂时激活编码环氧合酶-2英语Prostaglandin-endoperoxide synthase 2(COX-2)的基因来发挥作用。[4]

研究表明,瑞巴派特可以对抗非甾体抗炎药(NSAIDs)对胃肠道黏膜的损伤作用,[5]最近的研究还发现其对小肠也有保护作用,但对萘普生引起的胃损伤无效。[6]

瑞巴派特在多个亚洲国家使用,包括日本(商品名Mucosta)、韩国中国[7]印度(商品名Rebagen)。该药也在俄罗斯获得批准,商品名为Rebagit。[8]

作用机制

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瑞巴派特可增加胃黏膜前列腺素E2的水平,保护胃黏膜,从而抑制胃黏膜损伤,并增加胃黏液分泌和胃黏膜血流量,改善血流动力学障碍,抑制炎症并修复胃黏膜。

参考文献

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  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" (俄文). Russian State Register of Medicines. Retrieved 10 June 2017.

外部链接

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