Howden C W, Burget D W, Silletti C, Van Eeden A, Tomkins K B, Hunt R H
Division of Gastroenterology, McMaster University, Hamilton, Ontario, Canada.
Aliment Pharmacol Ther. 1987 Aug;1(4):305-13. doi: 10.1111/j.1365-2036.1987.tb00630.x.
The gastric antisecretory effects of three different doses of enisoprost, a new synthetic PGE1 analogue, were compared with placebo and misoprostol in 20 healthy male volunteers. Enisoprost 100, 200 and 400 micrograms all significantly (P less than 0.0001; ANOVA) suppressed histamine-stimulated acid and pepsin output when compared with placebo or misoprostol 200 micrograms. Misoprostol produced a significant decrease of stimulated acid output when compared with placebo (P = 0.0012). The concentration of pepsin in gastric juice was significantly (P less than 0.0001) decreased by enisoprost at the commencement of histamine stimulation. This effect was short-lived, and was maximal with enisoprost 400 micrograms. There was a significant dose-response relationship for enisoprost for inhibition of stimulated acid output (P = 0.0065). Enisoprost was well tolerated, and no consistent drug-related adverse effects were detected. The profile of antisecretory effect of enisoprost, producing marked suppression of both acid and pepsin secretion independently, is unusual. This combination of activity along with any mucosal protective properties might be particularly effective in the treatment of peptic ulcer disease.
在20名健康男性志愿者中，将三种不同剂量的新型合成PGE1类似物依尼前列素的胃抗分泌作用与安慰剂和米索前列醇进行了比较。与安慰剂或200微克米索前列醇相比，100、200和400微克依尼前列素均能显著（P<0.0001；方差分析）抑制组胺刺激的胃酸和胃蛋白酶分泌。与安慰剂相比，米索前列醇能显著降低刺激后的胃酸分泌（P=0.0012）。在组胺刺激开始时，依尼前列素能显著（P<0.0001）降低胃液中胃蛋白酶的浓度。这种作用是短暂的，400微克依尼前列素的作用最强。依尼前列素对刺激后胃酸分泌的抑制存在显著的剂量反应关系（P=0.0065）。依尼前列素耐受性良好，未检测到与药物相关的一致不良反应。依尼前列素的抗分泌作用特点是能独立显著抑制胃酸和胃蛋白酶分泌，这是不常见的。这种活性组合以及任何黏膜保护特性可能在消化性溃疡疾病的治疗中特别有效。
