质子泵抑制剂的研究进展

本文通过回顾国内外近 2 0a有关质子泵抑制剂的研究及临床应用 ,就奥美拉唑、兰索拉唑、泮托拉唑、雷贝拉唑等新型质子泵抑制剂的作用机制及临床应用进行综述 ,旨在探讨质子泵抑制剂国内外研究进展及临床疗效比较     

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。     

五种常用质子泵抑制剂前景及国内立项分析

消化性溃疡是一种常见病和多发病,质子泵抑制剂是目前治疗消化性溃疡病抑制胃酸分泌最为有效的药物,质子泵抑制剂的前景以及能否在国内立项是人们关注的热点。本文调研了五种常用质子泵抑制剂在国内外的上市情况,检索这些质子泵抑制剂在中国的专利状态并进行分析。结果表明,奥美拉唑、泮托拉唑、埃索美拉唑、雷贝拉唑和兰索拉唑(含右旋兰索拉唑)前景良好,其中有一些品种涉及专利问题,需注意。     

近年来长江流域上海等六市医院质子泵抑制剂应用分析

目的:了解近年来长江流域六市医院质子泵抑制剂用药的情况和变化趋势。方法:调查2009-2011年长江流域上海、杭州、南京、武汉、成都、重庆六城市样本医院质子泵抑制剂品种用药金额、占比、生产厂商及临床评价。结果:常用品种为奥美拉唑、泮托拉唑、埃索美拉唑、雷贝拉唑和兰索拉唑,用药金额名列第1是奥美拉唑,第2是泮托拉唑。结论:质子泵抑制剂市场前景看好。     

质子泵抑制剂致过敏性休克84例文献分析

目的 探讨质子泵抑制剂致过敏性休克的规律及特点,为其临床合理应用提供依据。方法 检索中国知网总库、万方数据总库、维普网、中国生物医学文献服务系统和PubMed、Web of Science数据库收录的1990—2022年间发表的质子泵抑制剂致过敏性休克相关案例报道文献,对符合要求的病例进行统计和分析。结果 共收集到82篇文献,共计84例质子泵抑制剂致过敏性休克。男女比例约为1∶1,以41～60岁和61～80岁患者居多,均占36.47%;具有食物或药物过敏史者占28.57%;共涉及5种药物,奥美拉唑、泮托拉唑、兰索拉唑分别位居前3位,占90.49%;以静脉方式给药的发生率最高,占60.71%;主要发生于首次用药,用药60 min内,占78.57%,其中最快为用药后几秒钟;主要临床表现为血压下降、大汗淋漓、心率加快、皮肤瘙痒、皮疹等;预后良好;不同的质子泵抑制剂间可能存在交叉过敏。结论 多种质子泵抑制剂均可引起过敏性休克,应引起广大医务工作者的关注,加强用药监护,保证患者用药安全。     

质子泵抑制剂合理用药分析及专项整治工作建议

目的：回顾性分析我院住院患者2016年质子泵抑制剂（PPIs）的使用情况,了解PPIs在我院的合理应用情况,针对PPIs专项整治活动的开展提出建议。方法：调取2016年住院患者PPIs用药数据,包括药品名称、使用金额、临床诊断、用法用量、疗程、使用人数等,并对PPIs使用率排名前10位的临床科室随机抽取500份病历（50份/科）进行用药合理性分析。结果：我院PPIs的不合理使用存在的主要问题有无指征用药、品种选择不当、疗程过长、用法用量不合理、存在药物相互作用等。结论：应尽快开展PPIs专项整治活动。由行政部门制定点评方案并实施;由药剂科临床药学室具体开展PPIs专项整治工作,确定评价内容和抽检病历方案,并对不合理病历进行干预和点评后再干预工作;在PPIs专项整治工作早期开展宣传和培训工作,以期推动我院PPIs的合理应用。     

新一代的质子泵抑制剂——兰索拉唑

兰索拉唑是一种新一代的质子泵抑制剂，对胃酸分泌有显著的抑制作用。口服兰索拉唑３０ｍｇ／ｄ治疗酸相关性消化系疾病，如十二指肠溃疡、胃溃疡和反流性食管炎，４￣６ｗｋ溃疡的愈合率达９０％以上，效果优于Ｈ２受体拮抗剂。用较大剂量可治疗对Ｈ２受体拮抗剂无效的顽固性消化性溃疡和胃泌素瘤，也有相当好的疗效。兰索拉唑与１种或２种抗生素联合治疗幽门螺杆菌阳性的溃疡病，根治率为６０％￣９０％。本品安全性较高，不良反应     

不同质子泵抑制药治疗十二指肠溃疡伴出血的临床效果

目的比较不同质子泵抑制药治疗十二指肠溃疡伴出血的临床效果。方法选择2018年1月-2020年1月福建省泉州市妇幼保健院儿童医院消化内科收治的十二指肠溃疡伴出血患者80例,根据应用不同的质子泵抑制药分为A组、B组、C组及D组,每组20例。A组采用奥美拉唑治疗,B组采用泮托拉唑治疗,C组采用兰索拉唑治疗,D组采用埃索美拉唑治疗。比较4组临床疗效、止血时间、治疗成本、血清炎性指标[肿瘤坏死因子-α(TNF-α)、降钙素原(PCT)及白细胞介素-8(IL-8)]及不良反应。结果4组患者的总有效率无显著差异(P>0.05);4组患者的平均止血时间无显著差异(P>0.05),但B组的治疗总成本显著低于A组、C组及D组(P<0.05);治疗前,4组患者的TNF-α、PCT及IL-8水平均无显著差异(P>0.05);治疗后,4组患者的TNF-α、PCT及IL-8水平均较治疗前显著降低(P<0.05),但各组TNF-α、PCT及IL-8水平仍无显著差异(P>0.05);4组患者在治疗过程中均未出现严重不良反应。结论对于十二指肠溃疡伴出血患者,各类质子泵抑制药均可发挥较佳的临床疗效,而泮托拉唑的成本最低,属于一种最经济有效的质子泵抑制药。     

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.     

住院患者质子泵抑制剂临床应用横断面调查分析

<正>为了解质子泵抑制剂(PPI)在此院的应用情况及其合理性,笔者采用横断面调查方法,对住院患者1日的医嘱PPI应用情况进行统计分析,结果如下。1资料与方法1.1调查对象:原始资料与数据来源于某院住院医师数据     

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.     

Pharmacokinetics and effect on caffeine metabolism of the proton pump inhibitors, omeprazole, lansoprazole, and pantoprazole

Aims To study the pharmacokinetics of three proton pump inhibitors, omeprazole, lansoprazole, and pantoprazole, as well as any potential influence on CYP1A2 activity (measured by means of rate of caffeine metabolism) of these compounds at single dose and repeated dose administration.
Methods Fourteen healthy males, classified as 12 extensive metabolizers (EMs) and two poor metabolizers (PMs) according to the urinary S/R mephenytoin ratio, completed this open, randomized, three-way cross-over study. In each of the three 7-day treatment periods either omeprazole (20  mg), lansoprazole (30  mg) or pantoprazole (40  mg) in therapeutically recommended doses was administered once daily, and the pharmacokinetics of the proton pump inhibitors as well as the rate of caffeine metabolism was measured on days 1 and 7.
Results In the EMs there was an increase in AUC from day 1 to day 7 for omeprazole. In the PMs the AUC of both omeprazole and lansoprazole was unchanged during repeated dosing, while for pantoprazole there was a tendency to a slight decrease. The AUC at steady state was for all three proton pump inhibitors 5 fold higher in PMs compared with EMs, indicating that the same proportion of the dose, irrespective of compound, is metabolized by CYP2C19. No induction of CYP1A2 was evident for any of the compounds in either EMs or PMs.
Conclusions The ∼5 fold difference in AUC between EMs and PMs indicates that approximately 80% of the dose for all three proton pump inhibitors is metabolized by the polymorphically expressed CYP2C19. None of the three proton pump inhibitors, administered in therapeutically recommended doses, is an inducer of CYP1A2—neither in PMs nor in EMs.     

Ethnic differences in drug therapy: a pharmacogenomics perspective

This study was presented at the American College of Chest Physicians meeting in Pittsburgh (PA, USA) in October 2011. The study objective was to evaluate the association of proton pump inhibitors (PPIs) and community-acquired pneumonia (CAP). The design was a meta-analysis of nine case–controlled and cohort studies. 120,863 pneumonia cases from 1987 to 2006 were included in the meta-analysis. PubMed and Ovid Medline were searched from inception through May 2011 by two investigators independently using keywords: PPI, pneumonia, CAP, anti-ulcer, antacid, omeprazole, esomeprazole, lansoprazole, pantoprazole and rabeprazole. This meta-analysis only included case–controlled and cohort studies that were published in full in English and evaluated PPI use and CAP incidence. Studies were excluded if they included the following patients: pediatric, Helicobacter pylori treatment and critically ill. Bibliographies of recent review articles and systematic reviews were hand-searched. Quality of studies was assessed using the Newcastle–Ottawa Quality Assessment Scale. Two investigators independently extracted data into standardized data collection forms that were confirmed by a third investigator. Data were analyzed based on current use of PPIs, duration of PPI use (<30 days or >180 days) and PPI dose (high vs low). Overall association of PPI and CAP was analyzed using the random effects model (Comprehensive Meta analysis^® Version 2.0). Nine studies met all criteria for the primary outcome. Newcastle–Ottawa Quality Assessment Scale scores ranged from 4 to 8 out of 9. Current use of PPIs (odds ratio [OR]: 1.39; 95% CI: 1.09–1.76), PPI use <30 days (OR: 1.65; 95% CI: 1.25–2.19), PPI high dose (OR: 1.50; 95% CI: 1.33–1.68) and PPI low dose (OR: 1.17; 95% CI: 1.11–1.24) were significantly associated with CAP. There was no association between CAP and PPI use >180 days (OR: 1.10; 95% CI: 1.00–1.21). In conclusion, patients currently receiving PPIs, particularly <30 days or high dose, showed an association with CAP. Practitioners need to be vigilant about adverse effects of PPIs and consider alternative therapies.     

Impact of proton pump inhibitors on efficacy of clopidogrel: Review of evidence

Clopidogrel is a prodrug which requires cytochrome P450 2C19 (CYP 2C19) enzyme for its conversion to an active thiol metabolite. Proton pump inhibitors (PPIs) inhibits enzyme CYP 2C19 interfering with the conversion of clopidogrel into its active metabolite. Studies document the possible interaction of clopidogrel and PPIs leading to a decrease in the antiplatelet efficacy of clopidogrel. A PubMed/MEDLINE database literature search was carried out and the bibliographies of found articles were checked for other relevant literature. Most retrospective cohort studies and studies using platelet markers found a significant association between PPI use especially omeprazole and decreased efficacy of clopidogrel while few comparative trials using clinical outcomes found no association between the same. Pantoprazole was not associated with the decrease in the antiplatelet efficacy of clopidogrel. Patients on dual antiplatelet therapy and/or with a history of gastrointestinal bleed will require gastroprotection in the form of PPIs. In such cases, pantoprazole should be the preferred PPI. Rabeprazole can be used as an alternative.     

可逆型质子泵抑制剂的研究进展

酸相关性疾病是消化道由于胃酸作用而诱发或导致的疾病,包括消化性溃疡、胃食道反流病等常见多发病。自第一个质子泵抑制剂奥美拉唑于1988年上市以来,质子泵抑制剂已成为酸相关性疾病治疗的首选药物,其缺点是起效慢、抑酸不彻底。可逆型的质子泵抑制剂口服起效快,疗效与剂量线性相关,副作用少成为了治疗消化性溃疡疾病的新方向。文中主要对近年来有关可逆性质子泵抑制剂的研究情况作一介绍。     

氯吡格雷与质子泵抑制剂的相互作用

氯吡格雷能够降低冠心病患者再次发生心肌梗死的风险,故广泛用于急性冠脉综合征和经皮冠脉介入术后的患者。临床相关指南建议,氯吡格雷应与质子泵抑制剂（proton pump inhibitor,PPI）合用以减少氯吡格雷的胃肠道不良反应。但是,氯吡格雷需经肝脏细胞色素P450酶的同功酶CYP2C19代谢才能转化为活性产物发挥作用,而PPI同样主要由CYP2C19代谢。药代动力学研究显示,氯吡格雷与奥美拉唑合用会发生药物相互作用、由此降低氯吡格雷的抗血小板作用,而泮托拉唑与氯吡格雷的相互作用不明显。发表于2009年的系列回顾性病例对照研究表明,氯吡格雷与PPI合用会增加心血管不良事件的发生风险。但这一研究结果并未得到前瞻性的随机、对照研究和荟萃分析的证实。因此,目前仍需进行大规模的前瞻性的随机、对照试验来分析氯吡格雷和PPI合用与心血管不良事件风险间的相关性。鉴于临床上有大量服用氯吡格雷的患者需合用PPI来降低胃肠道出血风险,建议现最好选用与氯吡格雷相互作用较小的泮托拉唑。