Department of Gastroenterology, Lyon Sud Hospital, Pierre Benite, France.
Aliment Pharmacol Ther. 2013 Apr;37(8):767-75. doi: 10.1111/apt.12266. Epub 2013 Mar 4.
Aminosalicylates are first-choice treatment for mild-to-moderately active ulcerative colitis (UC); however, multi-dosing regimens are inconvenient.
To compare the efficacy and safety of once- (OD) vs. twice- (BD) daily prolonged-release mesalazine (Pentasa, Ferring, Saint-Prex, Switzerland) for active mild-to-moderate UC in a non-inferiority study.
Eligible patients (n = 206) were randomised to 8 weeks of mesalazine (4 g/day), either OD with two sachets of 2 g mesalazine granules in the morning (n = 102) or BD with one 2 g sachet in the morning and one in the evening (n = 104). Patients also received 4 weeks of mesalazine enema 1 g/day. Disease activity was assessed at randomisation, weeks 4, 8 and 12 using the UC Disease Activity Index (UC-DAI). Clinical and endoscopic remission (primary endpoint) was assessed after 8 weeks. Patients recorded stool frequency and rectal bleeding in a daily diary.
The primary endpoint, non-inferiority in clinical and endoscopic remission with OD vs. BD mesalazine at 8 weeks, was met (intent-to-treat population: 52.1% vs. 41.8%, respectively, 95% confidence interval -3.4, 24.1; P = 0.14). Improvement of UC-DAI score (92% vs. 79%; P = 0.01) and mucosal healing (87.5% vs. 71.1%; P = 0.007) were significantly better, time to remission significantly shorter (26 vs. 28 days; P = 0.04) and safety similar with OD vs. BD dosing.
When combined with mesalazine enema, prolonged-release mesalazine once-daily 4 g is as effective and well tolerated as 2 g twice-daily for inducing remission in patients with mild-to-moderately active ulcerative colitis (Clinicaltrials.gov: NCT00737789).
氨基水杨酸制剂是轻度至中度活动溃疡性结肠炎（UC）的首选治疗药物；然而，多次剂量方案不太方便。
在一项非劣效性研究中，比较单次（OD）与每日两次（BD）口服延长释放美沙拉嗪（Pentasa，Ferring，Saint-Prex，瑞士）治疗活动期轻度至中度 UC 的疗效和安全性。
符合条件的患者（n = 206）被随机分为 8 周的美沙拉嗪（4 g/天）治疗，分别给予 OD 方案（2 袋 2 g 美沙拉嗪颗粒，每日早晨服用，n = 102）或 BD 方案（每日早晨和晚上各服用 1 袋 2 g 美沙拉嗪，n = 104）。所有患者还接受 4 周的 1 g/天美沙拉嗪灌肠治疗。在随机分组时、第 4、8 和 12 周使用溃疡性结肠炎疾病活动指数（UC-DAI）评估疾病活动度。第 8 周后评估临床和内镜缓解（主要终点）。患者在每日日记中记录粪便频率和直肠出血情况。
OD 与 BD 美沙拉嗪在第 8 周时临床和内镜缓解的非劣效性主要终点达到（意向治疗人群：分别为 52.1%和 41.8%，95%置信区间 -3.4，24.1；P = 0.14）。UC-DAI 评分的改善（92% vs. 79%；P = 0.01）和黏膜愈合（87.5% vs. 71.1%；P = 0.007）显著更好，缓解时间更短（26 天 vs. 28 天；P = 0.04），OD 与 BD 剂量组安全性相似。
当与美沙拉嗪灌肠联合使用时，每日一次口服延长释放美沙拉嗪 4 g 与每日两次口服 2 g 一样有效且耐受良好，可诱导轻度至中度活动溃疡性结肠炎患者缓解（Clinicaltrials.gov：NCT00737789）。
