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柳氮磺吡啶治疗类风湿关节炎

Authors
Michael H Weisman, MD
Renee Z Rinaldi, MD
Section Editor
Ravinder N Maini, BA, MB BChir, FRCP, FMedSci, FRS
Deputy Editor
Paul L Romain, MD
Translators
郁胜强, 副主任医师，副教授

引言

最初提出将柳氮磺吡啶(sulfasalazine, SSZ)作为类风湿关节炎(rheumatoid arthritis, RA)的治疗用药是由于它具有抗炎和抗菌活性[1,2]。尽管早期研究提示该药物具有有益作用，但其疗效因1948年的一份负面报告的相关结果而受到质疑，虽然这份报告存在严重的研究设计缺陷，但其仍具有影响力[3,4]。在这一时期引入了可的松，该事件被誉为现代医学的奇迹，然而进一步减弱了应用SSZ治疗RA的热情。

20世纪70年代晚期进行的一项试验和1983年的首次安慰剂对照试验报道了SSZ的有益作用，这使得它作为RA的治疗药物再度时兴起来，并得到广泛应用[5,6]。

SSZ在RA治疗中的应用将在此讨论，并将在单独的有关RA的治疗专题中讨论。RA的治疗和SSZ在炎症性肠病中的应用参见其他专题。 (参见“成人类风湿关节炎治疗的一般原则”和“用于成人类风湿关节炎初始治疗的甲氨蝶呤替代药物”和“成人中度到重度活动性类风湿关节炎的初始治疗”，关于‘非生物性传统DMARD替代MTX’一节和“对初始非生物性DMARD治疗抵抗的成人类风湿关节炎的治疗”和“柳氮磺吡啶和5-氨基水杨酸类药物治疗炎症性肠病”)

药理学

大约30%的SSZ可在小肠快速吸收，然后通过肠肝循环基本不变地返回胆汁。因此，摄取药物中约90%作为完整的分子到达大肠[3,7]。SSZ在结肠中会被偶氮还原酶(一种细菌酶)分解为磺胺吡啶和5-对氨基水杨酸(5-aminosalicylic acid, 5-ASA)。因此，大肠杆菌在把相对无活性的母体药物分解为活性成分的过程中发挥着必要作用。磺胺吡啶几乎全部被吸收，而5-ASA则大部分经粪便排出，从而解释了它在炎症性肠病中的功效。

磺胺吡啶随后在肝脏中经羟基化和乙酰化作用被代谢。在慢型乙酰化个体中，这些成分的半衰期延长，该特性可能会影响药物毒性，而不是疗效[3,7]。尚未报道重要的药物间相互作用[3]。

                

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Literature review current through: 2017-06 . | This topic last updated: 2016-09-12.
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