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柳氮磺胺吡啶的使用已有45年之久,临床用于治疗溃疡性结肠炎、局部回肠炎有较好的疗效。近年通过对其药动学及毒理学的研究,对本品有了更深入的认识,并在此基础上发展了一些新药。本文对这些进展的概况作了回顾性综述。一、药理学柳氮磺胺吡啶是由一分子5-氨基水杨酸与一分子磺胺吡啶经重氮键相连而成。本品口服吸收约占用药量的1/4～1/3。所吸收的药物一部分以原形由尿排泄,其余的以原形由胆汁排入肠腔,与未被吸收的药物一样在回肠、结肠等部位经肠道细菌的重氮还原酶等酶类作用,使重氮键断裂,分解成5-氨基水杨酸和磺胺吡啶。其中5-氨基水杨酸大
Sulfasalazine has been used for 45 years and is clinically used for the treatment of ulcerative colitis and local ileitis with good efficacy. In recent years through its pharmacokinetics and toxicology research, this product has a more in-depth understanding, and on this basis, the development of a number of new drugs. This article reviews the overview of these advances. First, pharmacology Sulfasalazine is a molecule of 5-amino-salicylic acid and sulfanilamide molecular nitrogen connected by a diazo. Oral absorption of this product takes about 1/4 ~ 1/3 of the dose. The absorbed part of the drug excreted by the prototype of urine, the rest of the prototype by the bile into the intestine, and not absorbed in the same drugs in the ileum, colon and other parts of the intestinal bacteria diazo reductase and other enzymes, so that Diazo bonds break down and decompose into 5-aminosalicylic acid and sulfapyridine. Among them 5-amino salicylic acid large