Division of Gastroenterology and Hepatology, Department of Medicine, Crohn's and Colitis Center of New Jersey, UMDNJ-Robert Wood Johnson Medical School, New Brunswick, NJ, USA.
J Clin Gastroenterol. 2010 Sep;44(8):531-5. doi: 10.1097/MCG.0b013e3181db1a61.
In mild-to-moderate inflammatory bowel disease, particularly ulcerative colitis, 5-aminosalicylic acid (5-ASA) remains a cornerstone of therapy. Sulfasalazine, originally synthesized in 1940 as an arthritis treatment for Sweden's King Gustaf V, is an azo-linked compound between 5-ASA and sulfapyridine. This medication was soon discovered to be effective in treating ulcerative colitis. However, dose-related side effects of the sulfapyridine moiety led to considerable effort in developing medications to deliver 5-ASA to the desired parts of the intestine. The newest generation of 5-ASA medications allows high-dose medication delivery with decreased pill burden, thereby improving patient compliance. This review will describe the pharmacokinetics of various 5-ASA preparations, particularly focusing on high-dose formulations and their role in therapy; will examine current scientific literature; and will review clinical outcomes and safety profiles.
在轻中度炎症性肠病中，特别是溃疡性结肠炎，5-氨基水杨酸（5-ASA）仍然是治疗的基石。柳氮磺胺吡啶于 1940 年最初合成，作为瑞典古斯塔夫五世国王关节炎的治疗药物，是 5-ASA 和磺胺吡啶之间的偶氮连接化合物。这种药物很快被发现对溃疡性结肠炎有效。然而，磺胺吡啶部分的剂量相关副作用导致了相当大的努力来开发将 5-ASA 递送到肠道所需部位的药物。新一代的 5-ASA 药物允许高剂量药物输送，同时减少药丸负担，从而提高了患者的依从性。这篇综述将描述各种 5-ASA 制剂的药代动力学，特别是重点关注高剂量制剂及其在治疗中的作用；将检查当前的科学文献；并回顾临床结果和安全性概况。
Zotero 插件