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亚砜咪瞍(Omeprazole)为苯井咪唑的取代物,可通过抑制质子泵、H~+K~+-ATP 酶的作用而减低胃酸分泌。此酶几乎只存于胃中,而亚砜咪唑可与其结合。本药从血浆中迅速消失,但放射自显影研究表明在胃粘膜内可存留16～48小时。本药的剂量-效应相关范围较宽;多数研究表明在正常人及十二指肠溃疡(DU)患者中,胃液分泌及酸度几乎全受抑制。每天用20～60mg,24小时胃液 pH 右上升至5.0,但少数患者效果稍差。本药抗分泌作用大于 H_2受体拮抗剂,且其活性在头几天中增加,因通过抑制胃液分泌后可增加其本身的生物利用度。停药后胃液分泌抑制作用可持续5天。
Omeprazole, a substituted benomyl imidazole, can reduce gastric acid secretion by inhibiting the action of proton pump and H ~ + K ~ + -ATPase. This enzyme resides almost exclusively in the stomach, whereas sulfoxide imidazole binds to it. The drug rapidly disappears from the plasma, but autoradiography studies have shown that the gastric mucosa can remain in 16 to 48 hours. The drug dose-effect wide range; most studies have shown that in normal and duodenal ulcer (DU) patients, gastric secretion and acidity almost completely inhibited. Daily use of 20 ~ 60mg, 24-hour gastric pH rose to 5.0 right, but a few patients less effective. The antisecretory effect of the drug is greater than that of the H 2 receptor antagonist, and its activity increases in the first few days because its bioavailability can be increased by inhibiting gastric juice secretion. Gastric juice secretion inhibition after stopping for 5 days.