Sachs G
Department of Medicine, University of California at Los Angeles, USA.
Pharmacotherapy. 1997 Jan-Feb;17(1):22-37.
Proton pump inhibitors (PPIs) are targeted to the gastric acid pump, H+, K(+)-adenosine triphosphatase (ATPase). The drugs accumulate in the acid space of the parietal cell and convert to active sulfenamide by an acid-catalyzed reaction. Consequent covalent inhibition of H+, K(+)-ATPase blocks the final step of acid secretion, hence the PPIs omeprazole, lansoprazole, and pantoprazole are more effective than histamine2-receptor antagonists (H2RAs) in controlling acid secretion. Preclinical short- and long-term clinical surveillance data show these drugs to be well tolerated and safe. The PPIs heal the lesions of gastroesophageal reflux disease and lessen symptoms more effectively and more quickly than the H2RAs, and are effective and faster acting for peptic ulcer disease. Helicobacter pylori is causally implicated in the majority of peptic ulcers and in atrophic gastritis. Since PPIs, but not H2RAs, are synergistic with antibiotics in eradicating H. pylori, their use is appropriate in all acid-related diseases since all patients who are H. pylori positive require eradication as well as healing.
质子泵抑制剂(PPIs)作用于胃酸泵,即H⁺,K⁺ - 腺苷三磷酸酶(ATP酶)。这些药物在壁细胞的酸性空间中蓄积,并通过酸催化反应转化为活性亚磺酰胺。随后对H⁺,K⁺ - ATP酶的共价抑制作用阻断了胃酸分泌的最后一步,因此,奥美拉唑、兰索拉唑和泮托拉唑等质子泵抑制剂在控制胃酸分泌方面比组胺2受体拮抗剂(H2RAs)更有效。临床前短期和长期临床监测数据表明这些药物耐受性良好且安全。与H2RAs相比,质子泵抑制剂能更有效、更快速地治愈胃食管反流病的病变并减轻症状,对消化性溃疡病也有效且起效更快。幽门螺杆菌与大多数消化性溃疡和萎缩性胃炎的病因有关。由于质子泵抑制剂而非H2RAs在根除幽门螺杆菌方面与抗生素具有协同作用,因此它们适用于所有与酸相关的疾病,因为所有幽门螺杆菌阳性的患者都需要根除幽门螺杆菌以及治愈疾病。