质子泵抑制剂的分类及药理学特性

选择性抑制胃壁细胞上H^＋/-ATP酶的药物-质子泵抑制剂已成为一代新型抑酸药物,是目前治疗酸相关疾病（消化性溃疡、反流性食管炎等）以及非甾体类抗炎药相关胃肠病变的首选药物。自1988年第一个质子泵抑制剂奥美拉唑上市以来,全球共相继上市了兰索拉唑、泮托拉唑、雷贝拉唑、埃索美拉唑等8个品种,而现在国内上市的质子泵抑制剂有5个。尽管各个质子泵抑制剂拥有共同的苯并咪唑内核及吡啶环的化学结构,但它们在药代动力学和药效学上仍有细微差异。本文就国内已上市的质子泵抑制剂的药理学特性作一简要概述,以期促进质子泵抑制剂在临床上的合理选用。     

苯并咪唑类质子泵抑制剂的药理和临床研究进展

从药理作用、药动学、临床应用及安全性等方面综述质子泵抑制剂（PPIs）的研究进展，比较了各种不同PPIs包括奥美拉唑、兰索拉唑、泮托拉唑、雷贝拉唑、莱米诺拉唑和吡帕拉唑等的相应特点。     

质子泵抑制剂的临床研究

目的 探讨质子泵抑制剂的临床应用及研究.方法 选取临床近年来临床常用质子泵抑制剂药物,进行研究.结果 奥美拉唑、兰索拉唑、泮妥拉唑、雷贝拉唑钠、依索拉唑、莱米诺拉唑进行药物的生物利用度、血浆药物浓度达峰时间、血浆半衰期、排泄途径进行观察.结论 质子泵抑制剂随着药学的发展,已经成为种类齐全,药理更趋合理,临床应用更方便的抑酸类药物.     

克里唑替尼的药理作用及临床评价

克里唑替尼是一种口服间变型淋巴瘤激酶(ALK)抑制剂,用于治疗通过FDA批准的检测方法诊断为ALK阳性的局部晚期或转移非小细胞肺癌。现对其药理作用、药代动力学、临床安全性评价及药物相互作用等做一综述。     

埃索美拉唑——质子泵抑制剂的新成员

综述了新的质子泵抑制剂--埃索美拉唑的药物动力学、药效学、安全性及临床应用等方面的研究进展.     

雷贝拉唑在出血性胃病中的应用进展

讨论新型质子泵抑制剂雷贝拉唑的药理机制、药代动力学及应用于出血性胃病中的研究进展.检索近5年来国内外相关研究进行分析.雷贝拉唑作为第2代苯并咪唑类质子泵抑制剂,能有效抑制胃酸分泌,清除幽门螺杆菌,促进血小板凝聚,改善胃出血.     

二肽基肽酶-4(DPP-4)抑制剂西格列汀在2型糖尿病治疗中的作用

目的:介绍新型口服降糖药二肽基肽酶-4(DPP-4)抑制剂西格列汀及其最新研究进展。方法 :对西格列汀的药理作用、药代动力学、不良反应及药物相互作用等方面的临床研究进行论述。结果和结论 :西格列汀是一种安全、有效的新型口服降糖药,具有良好的临床应用前景。     

2010年～2012年我院口服质子泵抑制剂的临床应用分析

目的了解2010年~2012年连续3年质子泵抑制剂在我院的应用情况及用药趋势。方法收集2010年~2012年我院质子泵抑制剂的品种、消耗量,并将其分类,求其消耗金额,按限定日剂量及金额排序法计算用药频度(DDDs)、日用药金额(DDDc)并进行分析。结果第二代质子泵抑制剂在抗溃疡药消耗金额中占60%,口服质子泵抑制剂(PPI)中埃索美拉唑消耗量最大。结论 3年来我院质子泵抑制剂消耗金额逐年递增,患者口服抗溃疡药以PPI为主。第二代逐步取代第一代质子泵抑制剂。新型抗溃疡药有被临床看好的趋势。     

2006年—2008年长江流域6市质子泵抑制剂利用分析

目的:分析质子泵抑制剂应用情况。方法:调查长江流域6市178家医院中,对应用质子泵抑制剂的常用品种、销售金额等,并结合临床应用和国内外医药动态进行分析。结果:质子泵抑制剂的常用品种为奥美拉唑、泮托拉唑、埃索美拉唑、雷贝拉唑、兰索拉唑,2008年销售总金额分别为33218万(上海)、11733万(杭州)、8947万(南京)、6583万(武汉)、5641万(成都)、5338万(重庆);单品种用药金额居首位是奥美拉唑,其次是泮托拉唑。结论:质子泵抑制剂在长江流域6市利用前景看好。     

2013～2015年某肿瘤医院质子泵抑制剂的应用分析

目的了解新疆医科大学附属肿瘤医院质子泵抑制剂的应用现状和趋势。方法对医院2013~2015年质子泵抑制剂的品种、销售金额、用药频度(DDDs)和限定日费用(DDC)等进行分析和统计。结果医院2013~2015年质子泵抑制剂(PPI)的使用品种基本固定,购药金额呈逐年递增趋势,用药频度及销售金额排前3位的药物是注射用奥美拉唑钠(奥西康)、注射用兰索拉唑(兰川)和注射用兰索拉唑(悦康),各药用药频度呈平稳趋势。结论医院2013~2015年质子泵抑制剂使用广泛,存在盲目预防性应用和倾向于使用注射剂等不合理现象,需进一步完善质子泵抑制剂的临床应用和管理制度,促进质子泵抑制剂的合理应用。     

艾普拉唑的作用机制与临床评价

目的：分析艾普拉唑的作用机制并评价其临床特点与疗效。方法：查阅国内外期刊文献,综述相关的药理学、药动学研究结果。结果：艾普拉唑抑酸能力强于奥美拉唑,其不通过CYP2C19代谢,在治疗胃食管反流病及消化性溃疡的疗效要强于其它质子泵抑制剂。结论：艾普拉唑相对前几代的质子泵抑制剂在药理学、药动学方面都具有一定的优势,其在临床疗效上有所提高,可成为临床抑酸治疗新的用药选择。     

Drug interactions between proton pump inhibitors and antiretroviral drugs

Gastroesophageal reflux disease and other related symptoms are common comorbidities for HIV-infected patients. Therefore, concurrent use of proton pump inhibitors and antiretrovirals is a common practice in the clinical setting. However, this practice may alter antiretroviral pharmacokinetics and lead to treatment failure due to inadequate drug exposure. Clinician awareness of these complex interactions is essential for optimal HIV management. This review summarizes the current knowledge on the interactions between proton pump inhibitors and antiretrovirals, and makes recommendations for the coadministration of proton pump inhibitors.     

质子泵抑制剂和化疗药物的协同效应

质子泵抑制剂（PPIs）,H+/K+-ATPase抑制剂,是治疗胃食管反流征和消化性溃疡的最常用药物,它们很安全,而且耐受性好。由于PPIs经常被用于癌症患者,研究PPIs和抗癌药物之间的相互作用对于实现有效和安全的癌症化疗具有特别重要的意义。研究表明,PPIs不仅抑制胃壁细胞中H+/K+-ATPase,还抑制肿瘤细胞中表达的空泡型ATP酶（V-ATPase）,以及与药代动力学和/或各种肾脏药物蓄积相关的有机阳离子转运蛋白2（OCT2）,对化疗有减毒和增效作用。本文总结了PPIs对于化疗安全性和有效性的影响,为质子泵抑制剂更广的临床研究提供参考。     

Gastroesophageal reflux in children: pathogenesis,prevalence, diagnosis,and role of proton pump inhibitors in treatment

A substantial percentage of infants, children and adolescents experience gastroesophageal reflux disease (GERD) and its accompanying symptoms, as well as disease complications. The diagnosis of GERD in children is made based upon the child's history, and data derived primarily from pH monitoring tests and endoscopy. In those children with confirmed reflux disease, the options for management parallel those recommended in adult patients, with the first step consisting of lifestyle changes. Surgical procedures may also be performed; however, these are rarely recommended prior to an adequate course of pharmacologic therapy, and appropriate case selection is important. Among the current pharmacotherapeutic options available in the US, the prokinetic agents and the acid-inhibitory agents (histamine-2 receptor antagonists, proton pump inhibitors) are the most widely used. The clinical utility of the prokinetic agents has been limited by the recent withdrawal of cisapride from the US marketplace and the potential for irreversible central nervous system complications with metoclopramide. Numerous clinical studies performed in adults, and several studies involving children, have demonstrated that the proton pump inhibitors are more effective than the histamine-2 receptor antagonists in the relief of GERD symptoms and healing of erosive esophagitis. In children, omeprazole and lansoprazole may be administered as the intact oral capsule, or in those who are unable or unwilling to swallow, the granule contents of the capsule may be mixed with soft foods (e.g. apple sauce) or fruit drinks/liquid dietary supplements prior to oral administration with no detrimental effects on pharmacokinetics, bioavailability, or pharmacodynamics. Studies performed with omeprazole and lansoprazole in children have shown pharmacokinetic parameters that closely resemble those observed in adults. In over a decade of use in adults, the proton pump inhibitor class of agents has been found to have a good safety profile. Studies involving children have also shown these agents to be well tolerated. In numerous drug-drug interaction studies performed with these two proton pump inhibitors, relatively few clinically significant interactions have been observed.     

我院住院患者注射用质子泵抑制剂使用情况调查及不合理用药分析

目的：分析我院住院患者注射用质子泵抑制剂的临床合理用药情况。方法：制定质子泵抑制剂用药评价标准,组织抽查小组,现场抽查病例．对注射用质子泵抑制剂的适应症、用法用量等进行合理性分析。结果：共抽查6个重点病房91份病例,涉及奥美拉唑钠针（洛赛克针、奥克针）、泮托拉唑针（泮立苏针、韦迪针）,存在注射用质子泵抑制剂不合理用药的病例21例,合格率为76.92％。外科病房不合理使用情况较内科病房严重。多数不合理为使用无明确指征,部分存在使用疗程偏长现象。结论：住院患者注射用质子泵抑制剂存在不合理用药情况,医院应制定注射用质子泵抑制剂使用规范．临床使用中应严格把握用药指征,避免过度使用。     

Pharmacokinetics of intravenous omeprazole in critically ill paediatric patients

The proton pump inhibitors are first-line drugs for the treatment of a number of gastrointestinal diseases. These drugs have a good safety profile, making it possible to use them in paediatric patients. Although their pharmacokinetics in children has not been extensively studied, research performed suggests that the dose used should be varied as a function of age, as this factor affects the drug’s metabolism. Proton pump inhibitors can be used in critically ill children for the prophylaxis and treatment of gastrointestinal haemorrhage, although there is still little experience with this. The most widely used proton pump inhibitor at the present time is omeprazole. As there are specific characteristics of these patients that could alter the pharmacokinetics of the drugs, studies need to be performed to determine the most suitable dose and dosage interval.     

近年来质子泵抑制剂的研究进展

概述了质子泵抑制剂（PPIs)作为临床应用最广泛的抗酸药物的作用机制,以及各种不同PPIs包括奥美拉唑、兰索拉唑、泮托拉唑、雷贝拉唑、莱米诺拉唑和吡帕拉唑等的临床应用特点。     

Recent advances in proton pump inhibitors

Mechanism of action and shortcomings of the approved proton pump inhibitors are reviewed. Advances in the design of new proton pump K(+) and S site inhibitors are presented. Design criteria incorporated into the structure of investigational proton pump inhibitors to address these drawbacks are discussed.