Arakawa T, Kobayashi K, Yoshikawa T, Tarnawski A
Third Department of Internal Medicine, Osaka City University Medical School, Osaka, Japan.
Dig Dis Sci. 1998 Sep;43(9 Suppl):5S-13S.
Rebamipide, a gastroprotective drug, is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers. This drug stimulates prostaglandin generation in gastric mucosa and improves not only the speed but also the quality of ulcer healing. In addition, it protects the gastric mucosa against acute injury caused by various noxious and ulcerogenic factors. Based on these experimental results, rebamipide had been subsequently tested in several clinical trials and approved in Japan for therapeutic use in patients with gastric ulcers and patients with acute gastritis. The main purpose of developing this type of drug was to improve the quality of ulcer healing, especially in that antisecretory drugs lack this advantage. In a preliminary clinical study, rebamipide improved the quality of gastric ulcer healing and reduced future ulcer recurrence. A number of basic research studies have been performed to clarify the mechanisms of rebamipide's action. These studies demonstrated unique properties of rebamipide and convincingly showed that it increases gastric mucus glycoprotein components, stimulates migration and proliferation of wounded epithelial cell monolayers, increases expression of epidermal growth factor and its receptor in normal and ulcerated gastric mucosa, and scavenges active oxygen radicals. The drug also attenuates the activity of neutrophils and the production of inflammatory cytokines stimulated by NSAIDs and/or H. pylori. Therefore, rebamipide can contribute to the management of patients who are taking NSAIDs or are infected with H. pylori. The inhibition of immunoinflammatory responses by rebamipide in H. pylori-infected patients may prevent development of gastritis, peptic ulcer disease, its recurrence, and possibly gastric cancer. Moreover, rebamipide may enhance eradication of H. pylori-infection using standard eradication therapy. Further studies are needed to clarify these possible advantages of rebamipide.
瑞巴派特是一种胃黏膜保护药物，它是从500多种2(1H)-喹啉酮氨基酸类似物中筛选出的化合物，这些类似物均经过胃黏膜保护作用及愈合实验性胃溃疡疗效的测试。该药物可刺激胃黏膜中前列腺素的生成，不仅能提高溃疡愈合的速度，还能改善愈合质量。此外，它能保护胃黏膜免受各种有害及致溃疡因素引起的急性损伤。基于这些实验结果，瑞巴派特随后在多项临床试验中进行了测试，并在日本被批准用于治疗胃溃疡患者和急性胃炎患者。研发这类药物的主要目的是提高溃疡愈合质量，尤其是因为抗分泌药物缺乏这一优势。在一项初步临床研究中，瑞巴派特改善了胃溃疡的愈合质量，并降低了未来溃疡复发的几率。已经开展了多项基础研究以阐明瑞巴派特的作用机制。这些研究揭示了瑞巴派特的独特特性，并令人信服地表明它能增加胃黏液糖蛋白成分，刺激受损上皮细胞单层的迁移和增殖，增加正常及溃疡胃黏膜中表皮生长因子及其受体的表达，以及清除活性氧自由基。该药物还能减弱中性粒细胞的活性以及非甾体抗炎药和/或幽门螺杆菌刺激引起的炎性细胞因子的产生。因此，瑞巴派特有助于治疗正在服用非甾体抗炎药或感染幽门螺杆菌的患者。瑞巴派特对幽门螺杆菌感染患者免疫炎症反应的抑制作用可能会预防胃炎、消化性溃疡疾病的发生、复发以及可能的胃癌。此外，瑞巴派特可能会增强使用标准根除疗法根除幽门螺杆菌感染的效果。需要进一步研究来阐明瑞巴派特这些可能的优势。
