Ruderman W B
Department of Gastroenterology, Cleveland Clinic, Florida, Fort Lauderdale.
Med Clin North Am. 1990 Jan;74(1):133-53. doi: 10.1016/s0025-7125(16)30591-0.
Topical 5-ASA Agents. Observations that 5-ASA may be the clinically active component of sulfasalazine have stimulated extensive pharmaceutical efforts to develop a new class of agents for the treatment of the inflammatory bowel diseases. Both oral and rectal forms of 5-ASA have been designed, tested, and released for use in Europe and Canada. Only one rectal 5-ASA formulation is now commercially available in the United States. Studies with topical 5-ASA have demonstrated that this formulation is safe and effective for distal colitis, even in patients with disease refractory to standard therapy. Adverse effects of topical 5-ASA are minimal. However, optimal treatment doses have not been defined, relapse is common after withdrawal of therapy, and issues regarding maintenance regimens are not yet resolved. Other disadvantages include the expense and inconvenience of enema therapy. However, rectally administered 5-ASA is an appropriate initial therapy for the treatment of distal ulcerative colitis, or as a therapeutic option for refractory distal colitis. Data are insufficient to make recommendations regarding the use of topical 5-ASA in Crohn's disease. Whether this class of agents will be of benefit for Crohn's proctitis or for perineal disease must await further clinical trials. Oral 5-ASA Agents. There appears to be a well-substantiated benefit equivalent to that of sulfasalazine achieved by the new oral formulations of 5-ASA when used for the treatment of acute mild to moderate ulcerative colitis, and as maintenance treatment of ulcerative colitis in remission. Adverse reactions to these agents are uncommon, usually mild, and infrequently require withdrawal of therapy. The major problem reported with these agents is watery diarrhea, most commonly associated with olsalazine, but the practical importance of this adverse effect is disputed. Rare occurrences of reversible pericarditis and acute pancreatitis have been encountered during clinical application of these agents. As more experience is obtained, these agents may become the initial therapy of choice for the treatment of mild to moderate ulcerative colitis and for maintenance in inactive disease. Currently available data have defined a role for these agents as an important alternative for the treatment of patients intolerant or allergic to sulfasalazine. As with sulfasalazine, these agents should not be used as the sole treatment for severely active ulcerative colitis. Many unanswered questions remain regarding therapy with these agents for ulcerative colitis. Still undefined are optimal drug dosages, appropriate dosing intervals, and the necessary duration of therapy.(ABSTRACT TRUNCATED AT 400 WORDS)
局部用5-氨基水杨酸制剂。5-氨基水杨酸可能是柳氮磺胺吡啶的临床活性成分这一发现,激发了制药行业为开发用于治疗炎症性肠病的新型药物付出巨大努力。口服和直肠用的5-氨基水杨酸制剂均已设计、测试并在欧洲和加拿大上市。目前在美国只有一种直肠用5-氨基水杨酸制剂可在市场上买到。局部用5-氨基水杨酸的研究表明,即使对于标准治疗无效的患者,该制剂对远端结肠炎也是安全有效的。局部用5-氨基水杨酸的不良反应极小。然而,最佳治疗剂量尚未确定,停药后复发很常见,而且维持治疗方案的问题尚未解决。其他缺点包括灌肠疗法的费用和不便。然而,直肠给药的5-氨基水杨酸是治疗远端溃疡性结肠炎的合适初始疗法,或作为难治性远端结肠炎的一种治疗选择。关于局部用5-氨基水杨酸在克罗恩病中的应用,现有数据不足以给出推荐。这类药物对克罗恩直肠炎或会阴疾病是否有益,必须等待进一步的临床试验。口服5-氨基水杨酸制剂。新的口服5-氨基水杨酸制剂用于治疗急性轻至中度溃疡性结肠炎以及作为缓解期溃疡性结肠炎的维持治疗时,似乎有充分证据表明其疗效等同于柳氮磺胺吡啶。这些药物的不良反应不常见,通常较轻微,很少需要停药。这些药物报告的主要问题是水样腹泻,最常与奥沙拉嗪相关,但这种不良反应的实际重要性存在争议。在这些药物的临床应用中,曾罕见地出现可逆性心包炎和急性胰腺炎。随着经验的积累,这些药物可能会成为治疗轻至中度溃疡性结肠炎及维持非活动期疾病的首选初始疗法。目前可得的数据已确定这些药物可作为治疗对柳氮磺胺吡啶不耐受或过敏患者的重要替代药物。与柳氮磺胺吡啶一样,这些药物不应作为重度活动性溃疡性结肠炎的唯一治疗药物。关于这些药物治疗溃疡性结肠炎,仍有许多未解决的问题。最佳药物剂量、合适的给药间隔以及必要的治疗持续时间仍未明确。(摘要截选至400词)