Treatment of ulcerative colitis with oral mesalamine: advances in drug formulation, efficacy expectations and dose response, compliance, and chemoprevention.

William J Sandborn
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Abstract

Sulfasalazine, olsalazine, balsalazide, delayed-release mesalamine, controlled-release mesalamine, mesalamine pellets, and Multi-Matrix System mesalamine are effective first-line therapies for the treatment of mildly to moderately active ulcerative colitis and for subsequent maintenance of remission. For induction therapy it is unclear if there is a dose response above 1.5 g, and for maintenance therapy existing data do not support a dose response above 1.5 g. Sulfasalazine has more frequent side effects than olsalazine, balsalazide, and mesalamine formulations. Once-daily dosing with multi-matrix system mesalamine 1.2 g tablets may lead to optimal compliance. Mesalamine >/= 1.2 g and sulfasalazine >/= 2 g reduce the risk of colorectal cancer in patients with ulcerative colitis. Drug formulations, efficacy expectations and dose response, toxicity expectations, compliance considerations, and chemoprevention considerations are reviewed.

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口服美沙拉胺治疗溃疡性结肠炎:药物配方、疗效预期和剂量反应、依从性和化学预防方面的进展。
柳氮磺胺嘧啶、奥萨拉嗪、balsalazide、缓释美沙拉胺、控释美沙拉胺、美沙拉胺颗粒和多基质系统美沙拉胺是治疗轻度至中度活动性溃疡性结肠炎和随后维持缓解的有效一线疗法。对于诱导治疗,尚不清楚是否有超过1.5 g的剂量反应,对于维持治疗,现有数据不支持超过1.5 g的剂量反应。柳氮磺胺吡啶比奥萨拉嗪、balsalazide和美沙拉胺制剂有更频繁的副作用。每日一次多基质系统美沙拉胺1.2 g片剂可达到最佳依从性。美沙拉明>/= 1.2 g和磺胺氮嗪>/= 2 g可降低溃疡性结肠炎患者结直肠癌的发生风险。回顾了药物配方、疗效预期和剂量反应、毒性预期、依从性考虑和化学预防考虑。
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