Fedorak Richard N, Bistritz Lana
Division of Gastroenterology, University of Alberta, Suite 205 College Plaza, 8215-112 Street, Edmonton, Alberta, Canada T6G 2C8.
Adv Drug Deliv Rev. 2005 Jan 6;57(2):303-16. doi: 10.1016/j.addr.2004.08.009.
Budesonide is a potent corticosteroid with a high first-pass metabolism rate. Two commercially available enteric-coated pH-dependent release formulations (Entocort EC and Budenofalk) deliver budesonide to the ileum and proximal colon, regions most commonly affected in Crohn's disease. The drug's effectiveness in this disease has been proven in multiple, placebo-controlled trials, where it has been shown to be superior to mesalamine and placebo, and equivalent to prednisolone for the control of mild to moderately active right-sided Crohn's disease. This beneficial therapeutic effect comes with less adrenal suppression and a small improvement in the clinical adverse effect profile, as compared to prednisolone. However, budesonide provides no benefit over conventional therapy for left-sided colonic disease, and it is less effective for treatment of more severe disease activity and more distal colonic disease. Continuous budesonide does not prolong remission and is, therefore, best used in an intermittent fashion to treat acute exacerbations.
布地奈德是一种具有高首过代谢率的强效皮质类固醇。两种市售的肠溶包衣pH依赖性释放制剂(Entocort EC和Budenofalk)将布地奈德输送到回肠和近端结肠,这些区域是克罗恩病最常受累的部位。该药物在这种疾病中的有效性已在多项安慰剂对照试验中得到证实,试验表明它优于美沙拉嗪和安慰剂,并且在控制轻度至中度活动性右侧克罗恩病方面与泼尼松龙等效。与泼尼松龙相比,这种有益的治疗效果伴随着较少的肾上腺抑制和临床不良反应情况的小幅改善。然而,布地奈德对左侧结肠疾病的传统治疗没有益处,并且对更严重的疾病活动和更远端的结肠疾病治疗效果较差。持续使用布地奈德不会延长缓解期,因此,最好以间歇方式用于治疗急性加重期。