Poole P
Department of Pharmaceutical Services, University of California Davis Medical Center, Sacramento, CA, USA.
Am J Health Syst Pharm. 2001 Jun 1;58(11):999-1008. doi: 10.1093/ajhp/58.11.999.
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of pantoprazole are reviewed. Pantoprazole is a gastric hydrogen-potassium adenosine triphosphatase (H+/K(+)-ATPase) inhibitor. It shares the same core structure as other currently available proton-pump inhibitors (PPIs). The FDA-labeled indication is the short-term treatment of erosive esophagitis. PPIs act by selectively inhibiting H+/K(+)-ATPase in the secretory canaliculus of the stimulated parietal cell. Understanding the pharmacodynamics of PPIs is more relevant than knowing their pharmacokinetics, since the duration of action depends on the rate of de novo proton-pump regeneration, not the duration of drug circulation in the body. Pantoprazole is well absorbed, undergoes little first-pass metabolism, and has an absolute bioavailability of approximately 77%. Pantoprazole has been evaluated in more than 100 clinical trials involving more than 11,000 patients. It is effective in treating erosive esophagitis and duodenal and gastric ulcers. It is also effective as adjunctive treatment with antimicrobials in patients infected with Helicobacter pylori. Pantoprazole has been shown to control acid production in Zollinger-Ellison syndrome. Pantoprazole is well tolerated. The most commonly reported adverse effects are headache, diarrhea, and abdominal pain. The recommended oral dosage for erosive esophagitis is 40 mg once a day for up to eight weeks. The recommended i.v. dose is 40 mg given over 15 minutes once a day in patients with gastroesophageal reflux disease who are unable to take oral medication. Pantoprazole appears to be as safe and effective as other PPIs in acid-related disorders.
本文综述了泮托拉唑的药理学、药代动力学、临床疗效、不良反应以及用法用量。泮托拉唑是一种胃氢钾三磷酸腺苷酶(H+/K(+)-ATP酶)抑制剂。它与其他现有的质子泵抑制剂(PPI)具有相同的核心结构。美国食品药品监督管理局(FDA)批准的适应证为糜烂性食管炎的短期治疗。PPI通过选择性抑制受刺激壁细胞分泌小管中的H+/K(+)-ATP酶发挥作用。了解PPI的药效学比了解其药代动力学更重要,因为作用持续时间取决于质子泵重新生成的速率,而非药物在体内的循环时间。泮托拉唑吸收良好,首过代谢少,绝对生物利用度约为77%。泮托拉唑已在100多项涉及11000多名患者的临床试验中进行了评估。它对治疗糜烂性食管炎、十二指肠溃疡和胃溃疡有效。在感染幽门螺杆菌的患者中,作为抗菌药物的辅助治疗也有效。泮托拉唑已被证明可控制卓-艾综合征中的胃酸分泌。泮托拉唑耐受性良好。最常报告的不良反应是头痛、腹泻和腹痛。糜烂性食管炎的推荐口服剂量为每日40mg,最多服用8周。对于无法口服药物的胃食管反流病患者,推荐的静脉注射剂量是每日一次,40mg在15分钟内输注完毕。在与酸相关的疾病中,泮托拉唑似乎与其他PPI一样安全有效。