Olbe L, Cederberg C, Lind T, Olausson M
Dept. of Surgery, Sahlgrenska Hospital, Gothenburg, Sweden.
Scand J Gastroenterol Suppl. 1989;166:27-32; discussion 41-2. doi: 10.3109/00365528909091240.
Single doses of omeprazole inhibit pentagastrin-stimulated gastric acid secretion and almost complete inhibition can be achieved for 4-6 hours with a single dose of 80 mg. Acid secretion then slowly returns and reaches normal levels after 3-4 days. Omeprazole also dose-dependently inhibits basal acid secretion as well as acid secretion stimulated with histamine, peptone and modified sham feeding, with similar efficiency. During repeated once-daily dosing with an enteric-coated granule capsule formulation, inhibition of acid secretion increased initially, and stabilized within about 4 days. Dose-response studies in patients with duodenal ulcers and healthy subjects have shown that 20-40 mg/day results in a peak reduction (80-100%) of pentagastrin-stimulated acid secretion 6 hours after dose. Studies of 24-hour intragastric acidity in duodenal ulcer patients have shown that 4 weeks of treatment with omeprazole, 20 mg once daily, resulted in a reduction of median intragastric acidity by 97%, which was superior to the 57% median reduction achieved with ranitidine, 150 mg b.d., for 4 weeks in the same patients. During omeprazole treatment, fasting plasma gastrin increased in relation to the degree of inhibition of acid secretion. After discontinuation of treatment, plasma gastrin normalized. Treatment with omeprazole, 20 mg, increased 24-hour plasma gastrin to the same extent as after highly selective vagotomy. Long-term treatment with omeprazole, 20-40 mg, for up to 2 years has not been associated with any progressive rise in fasting plasma gastrin.
单次服用奥美拉唑可抑制五肽胃泌素刺激的胃酸分泌，单次服用80mg时，4-6小时内几乎可实现完全抑制。随后胃酸分泌缓慢恢复，3-4天后达到正常水平。奥美拉唑还可剂量依赖性地抑制基础胃酸分泌以及组胺、蛋白胨和改良假饲刺激的胃酸分泌，且效率相似。在每日一次重复服用肠溶颗粒胶囊制剂期间，胃酸分泌的抑制作用最初增强，并在约4天内稳定下来。十二指肠溃疡患者和健康受试者的剂量反应研究表明，每天服用20-40mg可使五肽胃泌素刺激的胃酸分泌在服药后6小时达到最大减少量（80-100%）。对十二指肠溃疡患者24小时胃内酸度的研究表明，每日一次服用20mg奥美拉唑治疗4周，可使胃内酸度中位数降低97%，优于同一患者每日两次服用150mg雷尼替丁治疗4周所达到的57%的中位数降低幅度。在奥美拉唑治疗期间，空腹血浆胃泌素随胃酸分泌抑制程度的增加而升高。停药后，血浆胃泌素恢复正常。服用20mg奥美拉唑治疗可使24小时血浆胃泌素升高至与高选择性迷走神经切断术后相同的程度。长期服用20-40mg奥美拉唑长达2年，空腹血浆胃泌素未出现任何进行性升高。
