The Third Department of Internal Medicine, Division of Gastroenterology and Hepatology, Kansai Medical University, 2-5-1, Shinmachi, Hirakata, Osaka, 573-1010, Japan.
J Gastroenterol. 2020 Nov;55(11):1013-1022. doi: 10.1007/s00535-020-01713-8. Epub 2020 Aug 10.
5-aminosalicylate is a fundamental treatment for patients with ulcerative colitis with mild-to-moderate disease; however, evidence for 5-aminosalicylate treatment is unclear in some situations. This review discusses the clinical guidelines and previous studies, and highlights the following points: (1) Although rectal 5-aminosalicylate is effective for proctitis, physicians should endeavor to reduce patient's distress when administering suppositories or enema as the first-line therapy. It should be clarified whether oral 5-aminosalicylate alone with a drug delivery system that allows higher 5-aminosalicylate concentrations to reach the distal colon would be as effective as rectal 5-aminosalicylate therapy. (2) There has been no direct evidence demonstrating the clinical efficacy of switching the 5-aminosalicylate treatment to other 5-aminosalicylate formulations. However, switching to a different 5-aminosalicylate formulation may be indicated if clinical symptoms are not progressive. (3) Several studies have shown that colonic mucosal 5-aminosalicylate concentration correlates with clinical and endoscopic severity; however, it is unclear whether a high 5-aminosalicylate concentration has therapeutic efficacy. (4) The maximum dose of 5-aminosalicylate is necessary for patients with risk factors for recurrence or hospitalization. (5) Optimization of 5-aminosalicylate dosage may be indicated even for quiescent patients with ulcerative colitis if mucosal healing is not obtained, and if patients have multiple risk factors for recurrence. (6) Furthermore, the discontinuation of 5-aminosalicylate is acceptable when biologics are used. Because there are many "old studies" providing evidence for 5-aminosalicylate formulations, more clinical studies are needed to establish new evidence.
5-氨基水杨酸是治疗轻中度溃疡性结肠炎患者的基本药物；然而，在某些情况下，5-氨基水杨酸治疗的证据并不明确。本文综述了临床指南和以往的研究，并强调了以下几点：（1）尽管直肠用 5-氨基水杨酸对直肠炎有效，但医生在为患者提供栓剂或灌肠作为一线治疗时，应尽量减少患者的不适。应该明确的是，是否单独使用 5-氨基水杨酸，且药物输送系统能够使更高浓度的 5-氨基水杨酸到达远端结肠，其效果是否与直肠用 5-氨基水杨酸治疗相同。（2）目前尚无直接证据表明将 5-氨基水杨酸治疗转换为其他 5-氨基水杨酸制剂具有临床疗效。但是，如果临床症状没有进展，转换为不同的 5-氨基水杨酸制剂可能是有必要的。（3）多项研究表明，结肠黏膜 5-氨基水杨酸浓度与临床和内镜严重程度相关；然而，高浓度的 5-氨基水杨酸是否具有治疗效果尚不清楚。（4）对于有复发或住院风险的患者，需要使用 5-氨基水杨酸的最大剂量。（5）即使对于处于缓解期的溃疡性结肠炎患者，如果没有达到黏膜愈合，且患者有多个复发的危险因素，也可能需要优化 5-氨基水杨酸的剂量。（6）此外，当使用生物制剂时，可以停止使用 5-氨基水杨酸。由于有许多“旧研究”为 5-氨基水杨酸制剂提供了证据，因此需要更多的临床研究来建立新的证据。
