Lanza F L, Robinson M G, Isenberg J I, Basuk P M, Karlin D A
Houston Institute for Clinical Research, TX 77074.
Aliment Pharmacol Ther. 1990 Dec;4(6):601-13. doi: 10.1111/j.1365-2036.1990.tb00508.x.
Enprostil is a synthetic dehydro-prostaglandin E2 with gastroduodenal ulcer-healing and mucosal-protective properties. One hundred and three healthy volunteers were randomized to receive capsules of enprostil 35 micrograms b.d. (the clinically recommended dose), enprostil 70 micrograms b.d., or placebo b.d. All underwent endoscopic assessment of the gastroduodenal mucosa, scored using a 0-4 scale, at baseline and on Days 3, 7, 14, 21 and 28 of dosing. Mean and median maximum scores demonstrated a dose response, and the mean maximum scores were statistically significantly higher for both enprostil groups on each endoscopy day when compared with placebo. The majority of enprostil-treated subjects had petechial haemorrhages. The proportion of volunteers with small white-based mucosal breaks (erosions) was significantly higher for the fundus in the enprostil 70-microgram group on Days 21 and 28 when compared with placebo, but there were no significant differences between treatment groups for any area on the other study days. The 70-microgram dose was associated with significantly more gastrointestinal adverse events than the 35-microgram dose, which was similar to placebo. There were no significant differences between groups for large white-based mucosal breaks (ulcers). We conclude that oral enprostil produced gastric mucosal petechial haemorrhages, primarily in the fundus of the stomach. Gastric mucosal petechial haemorrhages are probably without clinical significance because they are very common in the general population (10-15%) and do not progress to erosions and ulcers.
恩前列素是一种具有治疗胃十二指肠溃疡和黏膜保护特性的合成脱氢前列腺素E2。103名健康志愿者被随机分为三组，分别每日两次服用35微克（临床推荐剂量）、70微克恩前列素胶囊或每日两次服用安慰剂。所有受试者在基线期以及给药的第3、7、14、21和28天接受胃十二指肠黏膜的内镜评估，评估采用0 - 4分制进行评分。平均和中位数最高评分显示出剂量反应，与安慰剂相比，恩前列素治疗的两组在每次内镜检查日的平均最高评分在统计学上均显著更高。大多数接受恩前列素治疗的受试者出现瘀点性出血。与安慰剂相比，在第21天和28天，70微克恩前列素组胃底出现以白色为基底的小黏膜破损（糜烂）的志愿者比例显著更高，但在其他研究日，各治疗组在任何区域均无显著差异。70微克剂量组的胃肠道不良事件明显多于35微克剂量组，35微克剂量组与安慰剂组相似。对于以白色为基底的大黏膜破损（溃疡），各组之间无显著差异。我们得出结论，口服恩前列素会导致胃黏膜瘀点性出血，主要发生在胃底。胃黏膜瘀点性出血可能无临床意义，因为它们在普通人群中非常常见（10 - 15%），且不会进展为糜烂和溃疡。
