Dipartimento Biomedico di Medicina Interna e Specialistica, AO Ospedali Riuniti Villa Sofia-Cervello, Palermo, Italy.
Curr Drug Targets. 2011 Sep;12(10):1396-405. doi: 10.2174/138945011796818126.
5-Amino-salacylic acid (5-ASA) is up to now the treatment of choice in the induction and maintenance of remission of mild-to-moderate ulcerative colitis (UC). Sulfasalazine, despite similar efficacy, is hampered by more side effects, but in presence of peripheral arthopaties it remains the treatment of choice. The new delayed release MMX formulation seems to be promising in reducing compliance problems, but further studies are warranted to show the superiority of new MMX formulation compared with the older formulations of 5-ASA. Some trials evaluated also the efficacy and safety of once-daily dosing of older 5-ASA formulations in maintenance of remission, finding a greater adherence to therapy in the group given the once daily regimen, compared with the classic twice daily groups. Regarding the efficacy of alternative treatment such us probiotics and antibiotics, the current data are not sufficient to promote their use in clinical practice. Clinical evidence supports the use of topical 5-ASA in active mild to moderate distal UC showing superior efficacy to placebo, topical corticosteroids, and oral 5-ASA. A combination of oral and rectal 5-ASA produces additional efficacy in both limited and extensive UC. Topical 5-ASA formulations are effective also for the maintenance of remission, however long term treatment may not be acceptable to many patients. Other topical drugs (E. Coli Nissle, propionyl-L-carnitine, butyrate, tacrolimus, rosiglitazone) have been investigated with conflicting results. The possible chemopreventive role of long term treatment with 5-ASA strengthens the indication to the long term use of 5-ASA.
5-氨基水杨酸（5-ASA）至今仍是轻度至中度溃疡性结肠炎（UC）诱导缓解和维持缓解的首选治疗方法。柳氮磺胺吡啶尽管疗效相似，但副作用更多，但在存在外周关节病的情况下，它仍然是首选治疗方法。新的迟释 MMX 制剂似乎有望减少依从性问题，但需要进一步的研究来证明新的 MMX 制剂与旧的 5-ASA 制剂相比具有优越性。一些试验还评估了在维持缓解中使用旧的 5-ASA 制剂的每日一次剂量的疗效和安全性，发现与经典的每日两次组相比，每日一次组的治疗依从性更高。关于替代治疗如益生菌和抗生素的疗效，目前的数据不足以促进它们在临床实践中的应用。临床证据支持在活动期轻度至中度远端 UC 中使用局部 5-ASA，其疗效优于安慰剂、局部皮质类固醇和口服 5-ASA。口服和直肠 5-ASA 的联合应用在有限和广泛的 UC 中均具有额外的疗效。局部 5-ASA 制剂也可有效维持缓解，但长期治疗可能不被许多患者接受。其他局部药物（E. Coli Nissle、丙酰肉碱、丁酸盐、他克莫司、罗格列酮）的研究结果存在冲突。长期使用 5-ASA 可能具有化学预防作用，这进一步加强了长期使用 5-ASA 的适应证。
