Baak L C, Biemond I, Jansen J B, Lamers C B
Dept. of Gastroenterology and Hepatology, University Hospital, Leiden, The Netherlands.
Scand J Gastroenterol. 1991 Jul;26(7):737-46. doi: 10.3109/00365529108998593.
We determined the effect of four times daily dosing with intravenous omeprazole on 24-h intragastric acidity, serum gastrin, and serum pepsinogen A and C in 10 fasting subjects (median age, 23.5 years). Two dose regimens (80-20-20-20 mg and 80-40-40-40 mg) were compared in a randomized placebo-controlled crossover study. Intragastric pH was continuously monitored during 24 h, using combined glass electrodes, and blood samples were taken every 6 h. Repeated boluses of omeprazole every 6 h significantly increased (p less than 0.01) the median 24-h intragastric pH compared with placebo (median pH, 3.7 (140 mg/day), 4.3 (200 mg/day), and 1.4 (placebo)) but failed to continuously raise pH levels above 4.0 in 8 (140 mg/day) or 9 (200 mg/day) of 10 subjects. No advantage of the 200-mg dose over the 140-mg dose was demonstrated. A cumulative effect of intravenous omeprazole was shown after repeated boluses but also a marked interindividual variation in response, which was correlated with the omeprazole area under the plasma concentration time curve. A significant elevation of serum gastrin coincided with the increased pH levels, which was followed after 12-18 h by a significant increase of both serum pepsinogens.
我们在10名禁食受试者(中位年龄23.5岁)中确定了每日静脉注射4次奥美拉唑对24小时胃内酸度、血清胃泌素以及血清胃蛋白酶原A和C的影响。在一项随机、安慰剂对照的交叉研究中比较了两种给药方案(80 - 20 - 20 - 20毫克和80 - 40 - 40 - 40毫克)。使用组合玻璃电极在24小时内连续监测胃内pH值,每6小时采集一次血样。与安慰剂相比(中位pH值,安慰剂组为1.4,140毫克/天组为3.7,200毫克/天组为4.3),每6小时重复推注奥美拉唑显著提高了(p < 0.01)24小时胃内pH值中位数,但10名受试者中有8名(140毫克/天组)或9名(200毫克/天组)未能使pH值持续升至4.0以上。未显示200毫克剂量优于140毫克剂量。重复推注静脉注射奥美拉唑后显示出累积效应,但个体反应也存在明显差异,这与血浆浓度 - 时间曲线下的奥美拉唑面积相关。血清胃泌素显著升高与pH值升高同时出现,12 - 18小时后血清胃蛋白酶原均显著增加。