University of Rome "La Sapienza", Rome, Italy.
J Crohns Colitis. 2009 Sep;3(3):149-56. doi: 10.1016/j.crohns.2009.05.001. Epub 2009 May 29.
The advent of salicylates in the treatment of ulcerative colitis started in 1938 with the discovery of Salazopyrin by Nanna Svartz. This drug offered for the first time a therapeutic chance to patients with ulcerative colitis. In this paper we describe the fascinating history of Salazopyrin and salicylates from the first serendipitous observations to the last randomized clinical trials. Attention was paid to the pharmacokinetics and the mechanism of action of 5-aminosalicylates and, in particular, to the issue of the mucosal concentrations of 5-aminosalicylates and its therapeutic efficacy. Moreover a look at the new oral mesalazine formulations that allow the homogenous distribution of 5-aminosalicylate through all the large bowel was taken. Lastly, the possible use of mesalazine in the prevention of colorectal cancer was reviewed.
柳氮磺胺吡啶在溃疡性结肠炎治疗中的应用始于 1938 年,Nanna Svartz 发现了柳氮磺胺吡啶。这种药物为溃疡性结肠炎患者提供了首次治疗机会。本文描述了柳氮磺胺吡啶和水杨酸类药物从最初的偶然观察到最后的随机临床试验的迷人历史。本文关注了 5-氨基水杨酸的药代动力学和作用机制,特别是 5-氨基水杨酸的粘膜浓度及其治疗效果问题。此外,还观察了新的口服美沙拉嗪制剂,这些制剂可使 5-氨基水杨酸在整个大肠内均匀分布。最后,还回顾了美沙拉嗪在预防结直肠癌方面的可能应用。