Angelucci Erika, Malesci Alberto, Danese Silvio
Division of Gastroenterology, Policlinico Umberto I, Universita' Sapienza, Rome, Italy.
Curr Med Chem. 2008;15(24):2527-35. doi: 10.2174/092986708785909049.
Crohn's disease and ulcerative colitis are chronic relapsing inflammatory bowel diseases with extremely great variability in presentation and clinical course. For many decades, corticosteroids and aminosalicylates have been the mainstay of the treatment for both Crohn's disease and ulcerative colitis, for the induction and maintenance of remission, respectively. The main limiting factors for the repeated use of corticosteroids or the use as a maintenance treatment are the very high prevalence of systemic side effects, together with the possibility of developing dependency on and/or resistance to the drug, which are reported in more than one third of patients with inflammatory bowel disease. In the last decade, a number of corticosteroids with enhanced topical activity and low systemic activity have been developed. Among them, budesonide and beclomethasone dipropionate are the most used for the treatment of the inflammatory bowel diseases. Indeed, budesonide is the drug of choice for the treatment of ileo(-cecal) active Crohn's disease with mild-to-moderate activity, due to controlled ileal release. Budesonide foam and/or enemas are also efficacious in the treatment of left-sided/distal ulcerative colitis. Gastro-resistant, extended release tablets characterized by a multimatrix structure (i.e. MMX-budesonide), have also been developed to allow uniform release along the length of the colon. This paper reviews the mechanism-of-action, safety and efficacy of budesonide in the treatment of inflammatory bowel disease.
克罗恩病和溃疡性结肠炎是慢性复发性炎症性肠病,其临床表现和临床病程具有极大的变异性。几十年来,皮质类固醇和氨基水杨酸类药物一直分别是治疗克罗恩病和溃疡性结肠炎诱导缓解及维持缓解的主要药物。反复使用皮质类固醇或用作维持治疗的主要限制因素是全身副作用的发生率非常高,以及出现药物依赖性和/或耐药性的可能性,在超过三分之一的炎症性肠病患者中都有相关报道。在过去十年中,已开发出多种具有增强局部活性和低全身活性的皮质类固醇。其中,布地奈德和二丙酸倍氯米松是治疗炎症性肠病最常用的药物。事实上,由于回肠控释作用,布地奈德是治疗轻度至中度活动性回肠(-盲肠)活动性克罗恩病的首选药物。布地奈德泡沫剂和/或灌肠剂在治疗左侧/远端溃疡性结肠炎方面也有效。还开发了具有多基质结构(即MMX-布地奈德)的胃内滞留型缓释片剂,以实现沿结肠全长的均匀释放。本文综述了布地奈德治疗炎症性肠病的作用机制、安全性和有效性。