Watkinson G
Drugs. 1986;32 Suppl 1:1-11. doi: 10.2165/00003495-198600321-00003.
Sulphasalazine, devised by Dr Nana Svartz for the treatment of 'infective polyarthritis', has been used in the treatment of inflammatory bowel disease for more than 40 years. Many controlled trials have shown that sulphasalazine 4g daily will induce remissions in between one-half and three-quarters of patients with acute attacks of ulcerative colitis. When given in a dosage of 2g daily it will prevent relapses in quiescent colitis. Relapses are 5 times more likely in untreated patients. It is less effective in Crohn's disease, where it exerts only a transient benefit in patients with active colonic disease and fails to prevent relapse or recurrence. Sulphasalazine is absorbed from the small intestine, re-excreted in bile and carried to the colon, where its azo bond is split by bacteria to release sulphapyridine, which is absorbed and is responsible for most of the drug's side effects, and 5-aminosalicylic acid, which is the active therapeutic moiety of the drug and exerts a beneficial topical action on the colonic mucosa. Side effects are common but are mainly reversible and not serious. Those related to high concentrations of sulphapyridine and to poor acetylation of the drug include gastrointestinal intolerance, malaise, headache, arthralgia, drug fever, effects on red blood cells and reversible male infertility. More serious, idiosyncratic side effects are skin rashes, leucopenia and agranulocytosis. Rarely, neurotoxicity, hepatotoxicity, polyarteritis, pulmonary fibrosis, a lupus-like syndrome and haemorrhagic colitis are produced. It is possible to desensitise most patients with drug-induced skin rashes. A number of less toxic alternatives to sulphasalazine have been devised and are undergoing trial. They either convey 5-aminosalicylic acid in a coated tablet to the colon or, when conjugated to a non-toxic carrier, release 5-aminosalicylic acid by bacterial cleavage there. Sulphasalazine remains a most useful drug in the treatment of inflammatory bowel disease after 40 years of use.
柳氮磺胺吡啶由纳纳·斯瓦尔茨博士发明，用于治疗“感染性多关节炎”，在治疗炎症性肠病方面已使用了40多年。许多对照试验表明，每日服用4克柳氮磺胺吡啶可使一半至四分之三的溃疡性结肠炎急性发作患者病情缓解。每日剂量为2克时，可预防静止期结肠炎复发。未经治疗的患者复发可能性高5倍。在克罗恩病中效果较差，仅对活动性结肠疾病患者有短暂益处，无法预防复发或再发。柳氮磺胺吡啶从小肠吸收，经胆汁再排泄至结肠，在结肠中其偶氮键被细菌裂解，释放出被吸收且是药物大部分副作用来源的磺胺吡啶，以及作为药物活性治疗部分并对结肠黏膜发挥有益局部作用的5-氨基水杨酸。副作用常见，但大多可逆且不严重。与高浓度磺胺吡啶及药物乙酰化不良相关的副作用包括胃肠道不耐受、不适、头痛、关节痛、药物热、对红细胞的影响及可逆性男性不育。更严重的特异质性副作用有皮疹、白细胞减少和粒细胞缺乏症。极少情况下会产生神经毒性、肝毒性、多动脉炎、肺纤维化、狼疮样综合征和出血性结肠炎。多数药物性皮疹患者可进行脱敏治疗。已设计出多种毒性较低的柳氮磺胺吡啶替代药物并正在进行试验。它们要么通过包衣片将5-氨基水杨酸输送至结肠，要么与无毒载体结合后在结肠经细菌裂解释放5-氨基水杨酸。经过40年的使用，柳氮磺胺吡啶仍是治疗炎症性肠病极为有用的药物。
