质子泵抑制剂在酸相关性疾病中的临床应用

目的探讨质子泵抑制剂在酸相关性疾病中的临床应用。方法通过查找文献资料，分析、总结质子泵抑制剂在酸相关性疾病中的临床应用。结果质子泵抑制剂治疗酸相关性疾病疗效较好。结论质子泵抑制剂治疗酸相关性疾病，是近十几年来临床应用广泛、疗效较好的药物。     

质子泵抑制剂在临床中的应用

目的 探讨质子泵抑制剂在临床应用情况及疗效.方法 通过收集本院的使用情况、查找文献资料,分析、总结质子泵抑制剂在临床中的应用.结果 质子泵抑制剂在治疗酸相关性疾病及联合根治幽门螺杆菌(Hp)疗效好.结论 质子泵抑制剂治疗酸相关性疾病和根治Hp已广泛应用,是疗效确切、安全可靠的药物.     

消化性溃疡的药物治疗进展

消化性溃疡可分为胃溃疡和十二指肠溃疡,是具有反复发作倾向的消化系统疾病。治疗药物主要包括抑酸剂、质子泵抑制剂、H2受体拮抗剂和铋剂等,目前以质子泵抑制剂加两种抗生素的三联方案和三联方案加铋剂的四联方案为公认的治疗方法。     

几种质子泵抑制剂的优劣势对比分析

质子泵抑制剂为苯并咪唑类衍生物，特异性和非竞争性的作用于H^＋／K^＋-ATP酶，治疗消化性溃疡，目前其疗效已得到肯定。具有起效快、作用强和持续时间长的特点，是治疗酸相关疾病的首选药物，在根除幽门螺杆菌感染联合治疗中发挥重要的作用。     

关于质子泵抑制剂的研究

目的:探讨质子泵抑制剂(PPIS)作为抑制胃酸分泌药物的作用机理,药理作用并探讨其不良反应,从而为临床应用提供科学依据,使质子泵抑制剂发挥其最佳的治疗效果。方法:阐述质子泵抑制剂的作用机理、药理作用、不良反应。结果:质子泵抑制剂是目前最先进的治疗消化性溃疡的一类药物,通过迅速抑制胃酸的分泌来达到快速治愈溃疡性疾病,但必须注意合理用药,减少不良反应现象的发生。结论:质子泵抑制剂的特殊抑酸作用使其成为了临床不可或缺的重要药品之一。     

大剂量质子泵抑制剂使用的稳定性

1988年首个质子泵抑制剂（protonpumpinhibitors,PPI）奥美拉唑上市后,先后有兰索拉唑、泮托拉唑、雷贝拉唑和埃索美拉唑等上市并在我国销售。PPI已成为大多数酸相关性疾病治疗的首选用药,临床上主要用于消化性溃疡、胃食管反流病、     

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。     

抗消化性溃疡药物临床治疗的研究近况

消化性溃疡是1种常见的消化系统疾病,其治疗的愈合率较低、复发率较高;抗消化性溃疡的治疗药物主要包括抗酸药、H2受体拮抗剂、质子泵抑制剂和根除幽门螺旋杆菌的药物,而质子泵抑制剂联合2种抗生素的三联治疗方案为目前公认的效果较好的治疗方法,三联方案加铋剂的四联方案也取得了公认疗效.综述近年来抗消化性溃疡药物在临床使用的文献资料,并对其治疗进展近况作一分析.     

质子泵抑制剂诱发感染危险性研究进展

<正>质子泵抑制剂是目前治疗消化性溃疡首选药物,质子泵抑制剂是通过快速有效地抑制胃酸的分泌和清除幽门螺旋杆菌从而有效的治疗溃疡。其也是治疗酸性相关疾病的首选药物,在临床上已经广泛地应用于抑酸治疗当中。质子泵抑制剂的抑酸作用十分显著,而且抑酸持续的时间长,与H2受体拮抗剂比较,有着明显的优点,主要是夜间抑酸作用十分良好,起效时间快,抑酸作用强且时间常,服药方法简单[1]。但是相关研究表明,质子泵     

质子泵抑制剂族的新药--埃索美拉唑

酸相关性疾病的药物治疗,于20世纪70年代首先推出的第1个H2受体拮抗剂西咪替丁,又于上世纪的80年代研究发现了质子泵抑制剂,明显改变了酸相关性疾病如消化性溃疡(包括应激性溃疡)、胃食管反流病(包括反流性食管炎)、胃泌素瘤、部分功能性消化不良等的临床疗效,使该类疾病的控制     

Review of pharmacokinetic and pharmacodynamic modeling and safety of proton pump inhibitors and aspirin

The efficacy of aspirin in primary and secondary prevention of cardiovascular diseases has been convincingly demonstrated. Gastrointestinal (GI) adverse effects with aspirin may lead to poor adherence and/or discontinuation of treatment. Proton pump inhibitors (PPIs) have been used for more than 20 years as the first choice for treating peptic ulcers and their bleeding complications, gastroesophageal reflux disease, non-steroidal anti-inflammatory drug-induced GI lesions and dyspepsia. Adherence becomes a major concern when aspirin is co-prescribed with PPIs to prevent GI adverse effects. Combining aspirin and PPIs into one tablet is an effective approach to address aspirin-related GI adverse effects and increase adherence to aspirin therapy for the prevention of cardiovascular diseases.     

Lansoprazole inhibits the cysteine protease legumain by binding to the active site

Proton pump inhibitors (PPIs) are prodrugs used in the treatment of peptic ulcer diseases. Once activated by acidic pH, the PPIs subsequently inhibit the secretion of gastric acid by covalently forming disulphide bonds with the SH groups of the parietal proton pump, that is the H⁺/K⁺‐ATPase. Long‐term use of PPIs has been associated with numerous adverse effects, including bone fractures. Considering the mechanism of activation, PPIs could also be active in acidic micro‐environments such as in lysosomes, tumours and bone resorption sites. We suggested that the SH group in the active site of cysteine proteases could be susceptible for inhibition by PPIs. In this study, the inhibition by lansoprazole was shown on the cysteine proteases legumain and cathepsin B by incubating purified proteases or cell lysates with lansoprazole at different concentrations and pH conditions. The mechanism of legumain inhibition was shown to be a direct interaction of lansoprazole with the SH group in the active site, and thus blocking binding of the legumain‐selective activity‐based probe MP‐L01. Lansoprazole was also shown to inhibit both legumain and cathepsin B in various cell models like HEK293, monoclonal legumain over‐expressing HEK293 cells (M38L) and RAW264.7 macrophages, but not in human bone marrow‐derived skeletal (mesenchymal) stem cells (hBMSC‐TERT). During hBMSC‐TERT differentiation to osteoblasts, lansoprazole inhibited legumain secretion, alkaline phosphatase activity, but had no effects on in vitro mineralization capacity. In conclusion, lansoprazole acts as a direct covalent inhibitor of cysteine proteases via disulphide bonds with the SH group in the protease active site. Such inhibition of cysteine proteases could explain some of the off‐target effects of PPIs.     

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。     

质子泵抑制剂致肾脏不良反应研究进展

随着质子泵抑制剂在临床的广泛应用,近年来质子泵抑制剂致急性间质性肾炎和慢性肾脏病的不良反应报道也越来越多,引起了专家的广泛关注。本文主要对质子泵抑制剂致肾脏不良反应的研究进展进行综述。从案例报道和病例回顾角度总结了近年来质子泵抑制剂致肾脏不良反应的临床特点、发病率、发病机制及治疗等,为临床安全用药提供依据。     

Proton pump inhibitors in the treatment of gastro-oesophageal reflux disease

Gastro-oesophageal reflux disease (GERD) is the most common peptic acid disease in the western world and is the commonest indication for acid suppression therapy. Major advances have been made over the past 30 years in the understanding of lower oesophageal sphincter function and the mechanism of acid secretion. Developments in surgical and pharmacological therapy have paralleled these advances. Pharmacotherapy for GERD has evolved from antacids to H₂-receptor antagonists (H₂RAs) to prokinetics to proton pump inhibitors (PPIs). The H₂RAs, while modestly effective in symptom relief and healing of GERD, are limited by pharmacological tolerance. The prokinetics (metoclopramide and cisapride) are limited by low efficacy, pharmacological tolerance and toxicity. The PPIs have emerged as the most effective therapy for symptom relief, healing and long-term maintenance. They have also proved to be remarkably safe and cost-effective in long-term therapy. This review evaluates the pharmacology, efficacy, tolerability, safety and cost-effectiveness of the four currently available PPIs, lansoprazole, omeprazole, pantoprazole and rabeprazole, in the treatment of GERD.     

质子泵抑制剂对大剂量甲氨蝶呤排泄延迟影响的研究现状

甲氨蝶呤为广谱抗叶酸类抗肿瘤药,大剂量甲氨蝶呤主要用于急性淋巴细胞白血病等肿瘤的治疗。临床实际工作中常合并使用质子泵抑制剂以预防甲氨蝶呤导致的胃肠道相关不良反应。有研究发现,合并使用质子泵抑制剂可能导致甲氨蝶呤血药浓度升高及延迟消除,但该结果仍存在争议。本文通过分析已报告的质子泵抑制剂与甲氨蝶呤相互作用有关的文献,并进行总结,对质子泵抑制剂与大剂量甲氨蝶呤排泄延迟的相关性及可能机制进行综述,提高甲氨蝶呤临床用药的合理性与安全性,降低药物不良反应的发生率。     

临床药师参与的处方点评与医保控费及DRGs干预前后我院住院患者质子泵抑制剂应用情况分析

目的：探讨临床药师参与的处方点评与医保控费及DRGs对我院质子泵抑制剂干预效果。方法：对医院干预前（2017年4月至2017年6月）、干预第一阶段（2017年7月至2017年9月）、干预第二阶段（2017年10月至2017年12月）、干预第三阶段（2018年1月至2018年3月）质子泵抑制剂的人均消费金额和用药合理性进行对比和分析。结果：我院外科住院患者人均PPIs费用干预第一阶段平均增长率为-49.86%,干预第二阶段平均增长率为-42.33%,干预第三阶段平均增长率为-69.59%;内科住院患者人均PPIs费用干预第一阶段平均增长率为-12.29%,干预第二阶段平均增长率为-23.28%,干预第三阶段平均增长率为-35.74%。不合理使用率由干预前的47.5%降至第一阶段干预后的21.5%,并进一步降至第二阶段干预后的13.0%,至第三阶段干预后的4.5%。结论：临床药师参与的处方点评与医保控费及DRGs促进了我院质子泵抑制剂的合理使用,降低了我院质子泵抑制剂的使用费用,为患者减轻了经济负担。     

Proton pump inhibitors for preventing non-steroidal anti-inflammatory drug induced gastrointestinal toxicity: a systematic review

Objective: Proton pump inhibitors (PPIs) are recommended for preventing gastrointestinal lesions induced by non-steroidal anti-inflammatory drugs (NSAIDs). We performed this study: (1) to evaluate the effectiveness and safety of PPIs, (2) to explore the association between effectiveness and potential influential factors, and (3) to investigate the comparative effect of different PPIs.

Methods: MEDLINE, EMBASE, and the Cochrane Library were searched to identify randomized controlled trials comparing different classes of PPIs, or comparing PPIs with placebo, H₂ receptor antagonists or misoprostol in NSAIDs users. Both pairwise meta-analysis and Bayesian network meta-analysis were performed.

Results: Analyses were based on 12,532 participants from 31 trials. PPIs were significantly more effective than placebo in reducing ulcer complications (relative risk [RR]?=?0.29; 95% confidence interval [CI], 0.20 to 0.42) and endoscopic peptic ulcers (RR?=?0.27; 95% CI, 0.22 to 0.33), with no subgroup differences according to class of NSAIDs, ulcer risk, history of previous ulcer disease, Helicobacter pylori infection, or age. To prevent one ulcer complication, 10 high risk patients and 268 moderate risk patients need PPI therapy. Network meta-analysis indicated that the effectiveness of different PPIs in reducing ulcer complications and endoscopic peptic ulcers is generally similar. PPIs significantly reduced gastrointestinal adverse events and the related withdrawals compared to placebo; there is no difference in safety between different PPIs.

Conclusions: PPIs are effective and safe in preventing peptic ulcers and complications in a wide spectrum of patients requiring NSAID therapy. There is no major difference in the comparative effectiveness and safety between different PPIs.     

质子泵抑制剂临床超适应证使用的医疗大数据分析

目的 探讨国内住院患者质子泵抑制剂（PPIs）过度使用的主要原因。方法 分析20家综合性医院2015年1月1日至2018年3月31日的患者电子病历信息,统计PPIs的适应证分布,不同品种PPIs的使用分布以及超适应证用药患者的高频疾病、手术、合并用药等。结果 PPIs使用人数最高的适应证为非甾体抗炎药(NSAIDs)相关溃疡的预防,占使用患者的40.9%;34.2%的患者为超适应证用药;超适应证用药患者中,兰索拉唑使用比例最高,占48.1%;使用PPIs患者人数最高的疾病、手术和伴随用药分别是食管、胃和十二指肠疾病、胆囊胆道手术和矿物质补充剂。结论 药物性溃疡的预防和超适应证用药是PPIs用量巨大的主要原因;兰索拉唑的应用不够规范;超适应证用药通常发生在肿瘤和消化道疾病的患者,消化道不适、禁食、手术和使用糖皮质激素是其发生的主要原因。