Thomson A B
Department of Medicine, University of Alberta, Edmonton, Canada.
Aliment Pharmacol Ther. 1991 Oct;5(5):449-70. doi: 10.1111/j.1365-2036.1991.tb00515.x.
Sulphasalazine is composed of sulphapyridine and mesalazine (5-aminosalicylic acid, 5-ASA or mesalazine) joined by an azo bond. Sulphasalazine has been used clinically for 40 years but less than 10 years ago it was recognized that the active moiety is 5-ASA. Sulphapyridine appears to act only as a carrier molecule to deliver mesalazine to the bowel, yet it is the sulphapyridine which appears to be responsible for many of the adverse effects observed with sulphasalazine. Normally, mesalazine is rapidly absorbed from the upper gastrointestinal tract. Since the action of mesalazine is thought to be locally at the site of disease in the intestine, the 5-ASA must be 'protected' to ensure its release in the terminal ileum and colon, the site of bowel inflammation in patients with Crohn's disease or ulcerative colitis. Recent clinical studies have confirmed the efficacy of topical (suppositories and enemas) therapy for ulcerative proctitis and left-sided colitis; oral mesalazine has been proven to be useful for the treatment of acute ulcerative colitis and for the maintenance of remission. There is preliminary evidence for the clinical usefulness of mesalazine in acute Crohn's disease as well as for the maintenance of remission.
柳氮磺胺吡啶由磺胺吡啶和通过偶氮键连接的美沙拉嗪(5-氨基水杨酸,5-ASA或美沙拉嗪)组成。柳氮磺胺吡啶已临床使用40年,但不到10年前人们才认识到其活性部分是5-ASA。磺胺吡啶似乎仅作为一种载体分子将美沙拉嗪输送至肠道,但正是磺胺吡啶似乎导致了柳氮磺胺吡啶观察到的许多不良反应。通常,美沙拉嗪会从上消化道迅速吸收。由于美沙拉嗪的作用被认为是在肠道疾病部位局部发挥,因此5-ASA必须得到“保护”,以确保其在回肠末端和结肠释放,这是克罗恩病或溃疡性结肠炎患者肠道炎症的部位。最近的临床研究证实了局部(栓剂和灌肠剂)疗法对溃疡性直肠炎和左侧结肠炎的疗效;口服美沙拉嗪已被证明对治疗急性溃疡性结肠炎和维持缓解有用。有初步证据表明美沙拉嗪在急性克罗恩病以及维持缓解方面具有临床实用性。