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美沙拉嗪治疗炎症性肠病的化学、药理学、药代动力学及临床应用

Chemistry, pharmacology, pharmacokinetics, and clinical applications of mesalamine for the treatment of inflammatory bowel disease.

作者信息

Small R E, Schraa C C

机构信息

Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0533.

出版信息

Pharmacotherapy. 1994 Jul-Aug;14(4):385-98.

PMID:7937276
Abstract

Mesalamine is the therapeutically active moiety of sulfasalazine used to treat inflammatory bowel disease. A controlled-release mesalamine capsule (Pentasa) is designed to release the agent continuously, and largely unaffected by intestinal pH, throughout the small and large bowel due to a diffusion-dependent, semipermeable ethylcellulose coating. It is a safe and efficacious single agent for inducing remission and producing therapeutic benefit in patients with mild to moderately active ulcerative colitis (UC) (2 or 4 g/day) or Crohn's disease (4 g/day), as well as for significantly enhancing quality of life for patients with mild to moderately active UC (2 or 4 g/day). It is also effective for maintaining remission in patients with quiescent UC and Crohn's disease (4 g/day). Disease location (left-sided UC or pancolitis) did not affect the agent's effect in active disease or maintaining remission. Fewer treatment-related adverse events were reported with mesalamine than with placebo in treating UC. In the treatment of active Crohn's disease, data showed no statistically significant differences in response for patients with ileitis, ileocolitis, or Crohn's colitis. This formulation of mesalamine may also be a possible steroid-sparing agent for patients with either active or quiescent Crohn's disease.

摘要

美沙拉嗪是用于治疗炎症性肠病的柳氮磺胺吡啶的治疗活性部分。一种控释美沙拉嗪胶囊(颇得斯安)旨在持续释放药物,由于其依赖扩散的半透性乙基纤维素包衣,在整个小肠和大肠中基本不受肠道pH值影响。对于轻度至中度活动性溃疡性结肠炎(UC)(2或4克/天)或克罗恩病(4克/天)患者,它是一种安全有效的单一药物,可诱导缓解并产生治疗益处,对于轻度至中度活动性UC(2或4克/天)患者,还能显著提高生活质量。它对静止期UC和克罗恩病(4克/天)患者维持缓解也有效。疾病部位(左侧UC或全结肠炎)不影响该药物在活动性疾病或维持缓解中的效果。在治疗UC时,与安慰剂相比,美沙拉嗪报告的治疗相关不良事件较少。在治疗活动性克罗恩病时,数据显示回肠炎、回结肠型或克罗恩结肠炎患者的反应在统计学上无显著差异。这种美沙拉嗪制剂也可能是活动性或静止期克罗恩病患者的一种可能的类固醇节约剂。

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Chemistry, pharmacology, pharmacokinetics, and clinical applications of mesalamine for the treatment of inflammatory bowel disease.美沙拉嗪治疗炎症性肠病的化学、药理学、药代动力学及临床应用
Pharmacotherapy. 1994 Jul-Aug;14(4):385-98.
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