Katz L B, Capetola R J, Argentieri D C, Moore L E, Genna T, Porter M C, Jasty V, Hartnagel R E, Abrutyn D, Shriver D A
J Rheumatol. 1986 Oct;13(5):887-94.
Gastrointestinal irritation is the most significant side effect in patients chronically taking nonsteroidal antiinflammatory drugs (NSAID) for treatment of arthritic conditions. Rioprostil, a primary alcohol prostaglandin E1 analog, prevents gastric bleeding induced by several NSAID in a rat model of arthritis that is similar in many aspects to human rheumatoid arthritis. Daily oral dosing of rioprostil (50 micrograms/kg BID for 15 days) did not influence the course of the adjuvant disease in rats or alter the antiinflammatory or analgesic effect of the NSAID. In a 13 week efficacy study in dogs, rioprostil (40-60 micrograms/kg, PO) completely prevented gastric hemorrhagic lesions induced by daily administration of aspirin.
胃肠道刺激是长期服用非甾体抗炎药(NSAID)治疗关节炎的患者最显著的副作用。利奥前列素是一种伯醇前列腺素E1类似物,在一种关节炎大鼠模型中,它能预防多种NSAID引起的胃出血,该模型在许多方面与人类类风湿关节炎相似。每日口服利奥前列素(50微克/千克,一日两次,共15天)对大鼠佐剂性疾病的病程没有影响,也不会改变NSAID的抗炎或镇痛作用。在一项对犬进行的为期13周的疗效研究中,利奥前列素(40 - 60微克/千克,口服)完全预防了每日服用阿司匹林引起的胃出血性病变。