Ashworth M, Arthur M, Turmer A D, Smith P R
Pharmatherapeutica. 1984;3(8):551-5.
A study was carried out in 14 patients with quiescent ulcerative colitis to compare serum levels of sulphasalazine and some of its metabolites after 7-days' treatment orally with 1 g sulphasalazine 3-times daily followed by 7-days' treatment with a 3 g sulphasalazine enema daily. The results showed that, although there were wide individual variations in levels after oral and rectal administration, with the same dosage the levels were far higher when the drug was given orally. Dose-related side-effects such as nausea and headache have been shown previously to occur more commonly with high serum levels of sulphapyridine to which sulphasalazine is metabolized. Levels after rectal administration were below those normally associated with side-effects. In view of the finding that at least 70% of patients with mild to moderate ulcerative colitis respond to rectal treatment it is suggested that this route of administration should be considered for patients experiencing side-effects after oral sulphasalazine.
对14例静止期溃疡性结肠炎患者进行了一项研究，以比较口服1克柳氮磺胺吡啶，每日3次，共7天，随后每日使用3克柳氮磺胺吡啶灌肠治疗7天后，血清中柳氮磺胺吡啶及其一些代谢产物的水平。结果显示，尽管口服和直肠给药后水平存在广泛的个体差异，但相同剂量下，口服给药时的水平要高得多。先前已表明，与柳氮磺胺吡啶代谢产生的高血清水平的磺胺吡啶相关的剂量相关副作用，如恶心和头痛，更常发生。直肠给药后的水平低于通常与副作用相关的水平。鉴于至少70%的轻度至中度溃疡性结肠炎患者对直肠治疗有反应这一发现，建议对口服柳氮磺胺吡啶后出现副作用的患者考虑这种给药途径。
