Allgayer H, Klotz U, Böhne P, Schmidt M, Kruis W
Medizinische Klinik I und Krankenhausapotheke des Klinikums Karlsruhe.
Z Gastroenterol. 1994 Nov;32(11):647-50.
In search of new therapies in IBD, the introduction of 4-aminosalicylic acid (4-ASA) has been proposed based on the longstanding, positive clinical experience in tuberculosis, the expected similar modes of action due to the close structural analogy to 5-aminosalicylic acid (5-ASA), an established therapy in IBD, and its inexpensiveness. To better understand the mechanisms of action of aminosalicylates, the intestinal inflammatory response and to develop new, more effective and cost saving drugs it is important to compare 4-ASA with 5-ASA with respect to their pharmacology, mechanisms of action and clinical efficacy. The inhibition of the upregulation of the initial local immune response, the inhibition of the production of inflammatory mediators, e.g. leukotrienes and the direct scavenging of toxic oxygen metabolites are important common antiinflammatory mechanisms. As the clinical experience with 4-ASA is promising, but still limited, 4-ASA currently cannot yet be recommended outside clinical trials. As the costs of 4-ASA are significantly lower compared to 5-ASA, 4-ASA may replace 5-ASA in the near future provided further trials will confirm the therapeutic and pharmacologic equivalency.
为了寻找治疗炎症性肠病（IBD）的新疗法，基于在结核病治疗中长期积累的、积极的临床经验，鉴于4-氨基水杨酸（4-ASA）与已确立的IBD治疗药物5-氨基水杨酸（5-ASA）结构相似，预期作用模式相似，且价格低廉，有人提出引入4-ASA。为了更好地理解氨基水杨酸盐的作用机制、肠道炎症反应，并开发新的、更有效且成本更低的药物，将4-ASA与5-ASA在药理学、作用机制和临床疗效方面进行比较很重要。抑制初始局部免疫反应的上调、抑制炎症介质（如白三烯）的产生以及直接清除有毒氧代谢产物是重要的共同抗炎机制。由于4-ASA的临床经验虽有前景但仍有限，目前在临床试验之外还不能推荐使用4-ASA。由于4-ASA的成本明显低于5-ASA，如果进一步试验能证实其治疗和药理学等效性，4-ASA可能在不久的将来取代5-ASA。
