Nakashima M, Kanamaru M
Department of Pharmacology, Hamamatsu University School of Medicine.
Nihon Rinsho. 1992 Jan;50(1):60-7.
We evaluated the safety, tolerance, pharmacokinetics and pharmacodynamics of omeprazole, a new anti-ulcer agent chiefly on the basis of our studies in healthy male volunteers. The type and incidence of side effects of omeprazole have been reported to be similar to those of H2-antagonists, and in our studies too, omeprazole was estimated to be safe and tolerable. Following single doses, the increase in AUC was not proportional to the increase in dosage. In the multiple-dose study, the AUC was greater on day 7 than on day 1. This finding may be due to a partial saturation of first pass elimination. Repeated omeprazole treatment (20 mg once daily for 4 days) inhibited the basal and stimulated acid secretion. Though H2-blockers inhibit the basal and stimulated pepsin secretion, omeprazole inhibited the stimulated pepsin secretion only.
我们主要基于对健康男性志愿者的研究，评估了一种新型抗溃疡药物奥美拉唑的安全性、耐受性、药代动力学和药效学。据报道，奥美拉唑副作用的类型和发生率与H2拮抗剂相似，在我们的研究中，奥美拉唑也被认为是安全且可耐受的。单次给药后，AUC的增加与剂量的增加不成比例。在多剂量研究中，第7天的AUC高于第1天。这一发现可能是由于首过消除部分饱和所致。重复使用奥美拉唑治疗（每日一次，每次20mg，共4天）可抑制基础胃酸分泌和刺激胃酸分泌。虽然H2阻滞剂可抑制基础胃蛋白酶分泌和刺激胃蛋白酶分泌，但奥美拉唑仅抑制刺激胃蛋白酶分泌。
