埃索美拉唑在酸相关性消化疾病治疗中的作用

质子泵抑制剂（proton pump inhibitor，PPI）是20世纪80～90年代以来酸相关性消化疾病治疗的一大突破。这类药物能迅速控制症状，也是治愈食管炎和消化性溃疡病最有效的药物。患者对PPI治疗的满意度比H2受体阻滞剂（H2RA）要高。其经典代表——奥美拉唑（Ome）的疗效已被广泛认可。2003年在国内上市的埃索美拉唑（Eso），是奥美拉唑的S异构体，是第一个发展为异构体的PPI。     

新型质子泵抑制剂——埃索美拉唑

质子泵抑制剂穴PPI雪是20世纪80～90年代治疗酸相关性疾病的一个重要进展,对溃疡病、胃食管反流病穴GERD雪和胃泌素瘤等的内科治疗是一个突破。埃索美拉唑,商品名耐信。它是奥美拉唑的S型光学异构体,由于其药代动力学的特点,治疗GERD优于目前已有的4种PPI眼1演。1.药代动力学奥美拉唑是R型和S型两种光学异构体1押1的混合物,而埃索美拉唑是单一的S型异构体,其特点为口服后的首过效应少,生物利用度和血浓度较奥美拉唑或R型异构体为高,因此,药效较奥美拉唑高而持久。本品在小肠内吸收,单次口服本品的血药浓度达峰时间穴Tmax雪为1～2h,…     

埃索美拉唑治疗胃食管反流病31例疗效观察

质子泵抑制剂(PPI)是目前治疗胃食管反流病(GERD)最有效的药物之一，但是不同的PPI疗效有差别，埃索美拉唑(Eso)是纯左旋异构体的PPI，我们分别用Eso及奥美拉唑(Ome)对61例GERD治疗，应用反流性疾病问卷(RDQ，又称耐信量表)，帮助诊断及判断疗效差别，疗效观察如下。     

三联药物1周治疗十二指肠球部溃疡合并幽门螺杆菌的疗效观察

幽门螺杆菌(Hp)感染是消化性溃疡最主要的致病因子,成功根除Hp能显著降低溃疡的复发率,因此众多指南均主张Hp相关的消化性溃疡应作根除治疗。奥美拉唑 克拉霉素 阿莫西林现为常用的一线治疗方案。埃索美拉唑是奥美拉唑的纯左旋光学异构体,胃食管反流病(GERD)的早期临床表明,埃索美拉唑20mg和40mg比奥美拉唑20mg的抑酸作用更强,更持久,而耐受性无差异。传统的治疗十二指肠溃疡(DU)基本策略是在Hp根除后继续3周质子泵抑制剂(PPI)以确保溃疡的愈合和症状缓解。本研究采用埃索美拉唑 阿莫西林 克拉霉素三联1周疗法治疗Hp阳性的DU,对其溃…     

质子泵抑制剂诱发癫痫1例

<正>质子泵抑制剂(proton pump inhibitor,PPI)是目前临床上广泛用于酸相关性疾病和根除幽门螺杆菌的药物,其通过阻碍胃壁细胞H~+-K~+-ATP酶发挥抑制胃酸分泌的作用,抑酸作用强,特异性高。目前常用的PPI有奥美拉唑、兰索拉唑、雷贝拉唑、泮托拉唑和埃索美拉唑。埃索美拉唑作为奥美拉唑的     

重点监控药品政策对样本地区质子泵抑制剂使用的影响研究

目的:探究安徽省、四川省重点监控药品政策对样本医院质子泵抑制剂(PPI)使用的影响,为减少质子泵抑制剂滥用现象、促进质子泵抑制剂合理使用、完善与推进重点监控药品管理政策提供依据。方法:以全国各省份监控目录形成的重点监控药品库为基础,结合安徽省、四川省的重点监控药品目录,综合考虑药品典型性及临床替代品等因素,遴选出安徽省奥美拉唑被监控品种(商品名)作为样本药品,奥美拉唑未被监控品种及4种PPI(通用名)作为对照药品,另外四川省纳入5种PPI(通用名)作为研究对象,进一步提取安徽省3家三级医院2014年11月至2017年9月的月度数据、四川省成都市9家三级医院2014年一季度至2017年一季度的季度数据。研究通过有对照的间断时间序列(interrupted time series,ITS)模型,分析样本药品及对照药品用量与金额的变化。结果:(1)安徽省、四川省实施重点监控政策后,除四川省埃索美拉唑使用下降趋势不显著外,被纳入监控目录的PPI品种的用量、金额均出现显著下降(P值均小于0.05);(2)安徽实施重点监控政策后,奥美拉唑未被监控品种(商品名)使用显著上升,所有奥美拉唑(通用名)使用显著下降(P值均小于0.05)。(3)安徽省将奥美拉唑纳入监控目录后,其他PPI品种(通用名)的使用显著下降,PPI类药品的整体使用受到有效限制(P值均小于0.05)。结论:安徽省重点监控药品政策有效限制了奥美拉唑的使用,同时使PPI类药品的整体使用显著下降。四川省重点监控药品政策使纳入监控目录的5种PPI整体的使用受到有效限制,政策效果显著。     

我院住院患者质子泵抑制剂的使用分析

目的分析我院2015年住院患者质子泵抑制剂(proton pump inhibitor,PPI)的使用情况。方法对我院2015年住院患者PPI的品种、销售量、消耗金额、用药频度(DDDs)和日均费用(DDC)等情况进行统计分析。结果我院PPI品种DDDs排序前3位的为雷贝拉唑肠溶胶囊、注射用奥美拉唑和注射用泮托拉唑;销售金额排序前3位的为注射用兰索拉唑、注射用奥美拉唑和注射用泮托拉唑;以雷贝拉唑肠溶胶囊序号比值>1的情况最为突出,其余大多数药品的序号比值为1;住院患者使用PPI病例数占首位的为消化内科;DDDs占首位的为心血管内科。结论 PPI在我院临床使用基本合理,但存在无适应证使用、盲目预防性使用等不合理现象,特别是外科;医院应加强对PPI使用的监管,促进合理用药。     

174张门急诊处方超适应证使用质子泵抑制剂的合理性分析

目的对口服质子泵抑制剂(PPI)的超适应证使用情况进行分析,为合理用药提供参考。方法调取我院2011年11月12日-15日期间含PPI的门、急诊处方,分析PPI超适应证使用情况,并对PPI在消化与非消化内科间超适应证使用的合理性进行比较。结果超适应证处方174张,其中合理处方134张(占77.0%)。超适应证处方中的PPI以奥美拉唑肠溶胶囊为主(76张,占43.7%),埃索美拉唑镁肠溶片次之(40张,占23.0%)。非消化内科超适应证使用PPI以奥美拉唑肠溶胶囊为主(占67.1%),消化内科以其他PPI为主(占62.2%),两者的品种选择差异有统计学意义(χ2=14.456,P<0.01)。消化内科超适应证使用PPI的合理性优于非消化内科(χ2=6.788,P<0.01)。结论超适应证使用口服PPI,消化内科处方更合理。     

我院注射用质子泵抑制剂临床使用合理性评价

目的 了解我院注射用质子泵抑制剂(PPI)的临床使用情况.方法 回顾性调查2020年10月份使用注射用PPI制剂病历1316份,随机抽取外科系统100份病历进行预防性应用的合理性评价.结果 注射用雷贝拉唑钠使用量最多,占比达73.71％,其次为注射用艾司奥美拉唑钠(16.41％)、注射用奥美拉唑钠(7.22％)、注射用...     

FDA批准奥美拉唑口服干混悬剂（Zegerid）上市

美国FDA批准Santarus公司的40mg奥美拉唑口服混悬剂(Zegerid)上市。该药用于减少危重患者上消化道出血、短期(4～6周)治疗良性活动期胃溃疡。本品是首个和唯一的质子泵抑制剂(PPI)口服迅速释放制剂，是唯一获准用于临床危重患者使用的口服PPI。     

凝血酶联合奥美拉唑治疗上消化道出血80例效果分析

目的观察凝血酶联合奥美拉唑治疗上消化道出血的效果研究。方法选取2009年3月至2009年12月因上消化道出血的住院80例患者,随机分为常规奥美拉唑治疗组和凝血酶联合奥美拉唑治疗组,常规奥美拉唑治疗组病例给予扩容及调整水电解质紊乱,静脉滴注奥美拉唑40mg,2次/d;静脉滴注止血芳酸0.5g,1次/d,重度贫血者予输血。凝血酶联合奥美拉唑治疗组再应用凝血酶2000单位加生理盐水15mL口服,2次/d,常规奥美拉唑治疗组用去甲肾上腺素8mg加生理盐水100mL,3次/d口服。结果通过观察证实凝血酶联合奥美拉唑治疗组可更有效地控制患者上消化道出血,且无明显的不良反应。结论凝血酶联合奥美拉唑治疗上消化道出血是一种有效的、安全的治疗方法,比常规奥美拉唑治疗的方法临床治疗效果更好,更为有效。     

奥美拉唑治疗非静脉曲张性上消化道出血的疗效观察

目的：观察奥美拉唑治疗非静脉曲张性上消化道出血的疗效。方法：将246例非静脉曲张性上消化道出血患者作为研究对象,随机分为3组,分别为奥美拉唑静脉滴注组、奥美拉唑80 mg泵入组、奥美拉唑160 mg泵入组,各组患者数均为82例,然后比较各组治疗方法的临床疗效。结果：不同给药治疗方法疗效有显著性差别（P〈0.05）。结论：奥美拉唑持续静脉泵入治疗非静脉曲张性上消化道出血效果好于奥美拉唑分次静脉滴注,且大剂量奥美拉唑持续泵入治疗能够达到更好的止血效果。     

微分脉冲伏安法测定奥美拉唑片中主药含量

目的:建立以微分脉冲伏安(DPV)法测定奥美拉唑片中奥美拉唑含量的方法。方法:分析了奥美拉唑不同电化学分析方法下的不同伏安行为,确定最佳分析方法及条件。结果:最佳分析方法为DPV法,在0.1mol/L醋酸-醋酸钠(HAc-NaAc)缓冲液中奥美拉唑检测浓度在1.0～40.0mg/L范围内与该峰电流值呈良好的线性关系(r=0.9904),其最低检测限为0.19mg/L,回收率为99.3%～102.0%。结论:DPV法测定奥美拉唑含量灵敏度较高,检测限较低,可望成为标准测试方法。     

Omeprazole (20 mg) daily given in the morning or evening: a comparison of effects on gastric acidity, and plasma gastrin and omeprazole concentration

Although omeprazole has a long duration of action and has usually been given in the morning, there are theoretical advantages in administering antisecretory drugs in the evening as has been shown for the H2-receptor antagonists. The aim of this study was to compare the effects of placebo and 20 mg omeprazole given either in the morning or evening, on gastric acidity, plasma gastrin levels and plasma omeprazole in 6 duodenal ulcer patients. The 24-hour mean pH (+/- S.E.M.) was: placebo 1.7 +/- 0.1; morning doing, 3.9 +/- 1.8 (P less than 0.01); evening dosing, 2.9 +/- 1.1 (N.S.). There was a large inter-individual variability of intragastric acidity in response to omeprazole, which was reflected both in the plasma gastrin and in the area under the plasma omeprazole concentration-time curve. Morning administration of omeprazole is optimal, but variability in the patient response to 20 mg omeprazole is still seen.     

Identification of human liver cytochrome P450 isoforms mediating secondary omeprazole metabolism.

1. The in vitro metabolism of omeprazole was studied in human liver microsomes in order to define the secondary metabolic pathways and identify the cytochrome P450 (CYP) isoforms responsible for the formation of the secondary metabolites of omeprazole. 2. The major secondary omeprazole metabolite was the hydroxysulphone, which was formed during incubation with both hydroxyomeprazole and omeprazole sulphone. A second metabolite, tentatively identified as pyridine-N-oxide omeprazole sulphone, was also formed during incubation with omeprazole sulphone. The formation kinetics of these two metabolites from omeprazole sulphone were biphasic suggesting the involvement of multiple CYP isoforms in each case. In contrast, the formation kinetics of hydroxysulphone from hydroxyomeprazole were linear. 3. Inhibition studies, performed with omeprazole sulphone as substrate at concentrations at which the high affinity activities predominated, with a series of isoform selective inhibitors as well as with an anti-CYP2C3 antibody suggested a dominant role of S-mephenytoin hydroxylase in the formation of hydroxysulphone from omeprazole sulphone. By contrast, CYP3A activities were predominant in the formation of hydroxysulphone from hydroxyomeprazole as well as in the formation of pyridine-N-oxide omeprazole sulphone from omeprazole sulphone.     

黛力新辅助奥美拉唑、莫沙必利治疗老年患者胃食管反流病的临床研究(129例)

目的:观察黛力新辅助奥美拉唑、莫沙必利治疗老年人胃食管反流病的临床疗效。方法:选取我院收治的129例老年胃食管反流病患者,随机分为观察组70例和对照组59例,对照组采用奥美拉唑联合莫沙必利治疗,观察组在对照组基础上加用黛力新。观察治疗后两组患者临床疗效以及反酸、烧心症状评分。结果:治疗后观察组总有效率为94.28%,对照组为61.02%,观察组总有效率明显高于对照组(P<0.05);两组患者治疗后反酸和烧心等症状均有所改善,其中观察组4周后反酸症状评分明显低于对照组(P<0.05);2周末烧心症状评分观察组优于对照组(P<0.05)。结论:黛力新辅助奥美拉唑、莫沙必利治疗老年人胃食管反流病临床疗效明显,对反酸、烧心等症状有明显改善作用,值得临床推广应用。     

Omeprazole: a pharmacoeconomic evaluation of its use in duodenal ulcer and reflux oesophagitis

Omeprazole regulates gastric acid secretion and is an effective treatment of acute duodenal ulcer and reflux oesophagitis, achieving more rapid healing and symptomatic relief than histamine H 2-receptor antagonists. When administered as maintenance therapy, omeprazole reduces the incidence of relapse. The drug is also highly effective in patients poorly responsive to histamine H 2-receptor antagonists. The daily acquisition cost of omeprazole is higher than that of histamine H 2-receptor antagonists in many countries, and thus it is important to evaluate the pharmacoeconomic impact of omeprazole in the short and long term treatment of duodenal ulcer and reflux oesophagitis. Pharmacoeconomic analyses have been performed in several clinical settings using pooled data from clinical trials or simulated models of clinical practice. In a single analysis using Finnish cost data, omeprazole was more cost effective than ranitidine in the treatment of duodenal ulcer disease over a 6-month period. The cost effectiveness of omeprazole was comparable to that of sucralfate-containing regimens, with patients receiving omeprazole being healed more quickly and experiencing a greater number of healthy days. Using a computer-model simulation and Swedish cost data, omeprazole was more cost effective than ranitidine when administered as intermittent treatment of duodenal ulcer over 5 years. Preliminary reports indicate that regimens which eradicate Helicobacter pylori are more cost effective than those which do not. As short term treatment of reflux oesophagitis, omeprazole 20 to 40 mg/day was the dominating treatment strategy, being less costly and more effective than ranitidine 300 to 1200 mg/day. Omeprazole 20 mg/day produced symptom-free days more cost effectively than either cimetidine 1.6 g/day or ranitidine 300 mg/day. More importantly, as long term (maintenance or intermittent) treatment of reflux oesophagitis, omeprazole 20 mg/day was more cost effective than both ranitidine 150 mg twice daily and 'phase 1' therapy (diet and antacids) over 6 and 12 months. Thus, based on analyses evaluated, omeprazole appears to be more cost effective than ranitidine in the short term treatment of duodenal ulcer. Results for long term treatment are less clear cut, but full details from some studies are not yet available. For the short term treatment of reflux oesophagitis omeprazole is more cost effective than ranitidine or cimetidine and for long term treatment omeprazole is more cost effective than ranitidine. As treatment for reflux oesophagitis, omeprazole is considered to be the dominating treatment strategy.     

泮托拉唑奥美拉唑与法莫替丁治疗消化性溃疡的疗效观察

目的:探讨泮托拉唑、奥美拉唑与法莫替丁治疗消化性溃疡的临床效果.方法:将2007年1月～2008年1月在我院住院治疗的消化性溃疡患者随机分为泮托拉唑组、奥美拉唑组和法莫替丁组并接受相应的药物治疗,同时三组均给予常规抗菌药物治疗,评估三组治疗效果与安全性.结果:泮托拉唑组第一周疼痛消失例数占65.63%,第四周占1.56%;奥美拉唑组第一周疼痛消失人数占67.19%,第四周占1.56%;法莫替丁组第一周疼痛消失例数占46.88%,第四周占14.06%,两组与法莫替丁组分别比较差异具有统计学意义(P<0.05).泮托拉唑组HP清除率为96.30%,奥美拉唑组为94.64%,法莫替丁组为80.00%,两组分别与法莫替丁组比较差异具有统计学意义(P<0.05).泮托拉唑组总有效率为96.88%,奥美拉唑组为96.88%,法莫替丁组为87.50%,两组分别与法莫替丁组比较差异具有统计学意义(P<0.05).三种药物临床不良反应发生率比较差异无统计学意义(P>0.05).结论:泮托拉唑、奥美拉唑治疗消化性溃疡的临床效果相似,优于法莫替丁,不良反应少,值得推荐应用.     

Twenty-four-hour intragastric acidity: 300 mg ranitidine b.d., 20 mg omeprazole o.m., 40 mg omeprazole o.m. vs. placebo

Background: There is considerable controversy about the degree of acid suppression that is optimal for the treatment of peptic disorders. Aim: To compare the effects of three different regimens that are reported to strongly inhibit acid secretion. Methods: Intragastric 24-hour pH monitoring was performed in 11 healthy subjects in a randomized, multiple, cross-over, double-blind study. Each subject received four dose regimens, each for 2 weeks, in a random order. The regimens were: 300 mg ranitidine b.d., 20 mg omeprazole o.m., 40 mg omeprazole o.m., and placebo. Results: The decrease in gastric acidity during the daytime and during the total 24-hour period by all three treatments was significantly greater than after placebo: a significant difference in acid inhibition was found between ranitidine and 40 mg omeprazole, but not between ranitidine and 20 mg omeprazole, nor between the two doses of omeprazole. During the night-time the decrease in gastric acidity by all three treatments was significantly greater than after placebo: no difference was seen between the two doses of omeprazole and ranitidine. For the time of pH greater than 3 we found no statistical difference between the various acid decreasing regimens. The pH remained significantly longer above 4 after ranitidine and the two doses of omeprazole compared with placebo, and also longer above 4 after 40 mg omeprazole compared with ranitidine, but not after 20 mg omeprazole compared with ranitidine, nor after the two different doses of omeprazole. Conclusions: Dosing with 300 mg ranitidine b.d., 20 mg omeprazole or 40 mg omeprazole is superior in gastric acid inhibition compared with placebo, when measured using 24-hour pH monitoring.     

Stereospecific analysis of omeprazole in human plasma as a probe for CYP2C19 phenotype

Omeprazole is a class referred to as proton pump inhibitor; it acts to regulate acid production in the stomach and is used to treat various acid-related gastrointestinal disorders. In the liver, it is metabolized to varying degrees by several cytochrome P-450 (CYP) isoenzymes which are further categorized into subfamilies of related polymorphic gene products. The metabolism of omeprazole is to a large extent dependent on CYP3A4 and CYP2C19. Omeprazole is metabolized to two major metabolites, 5-hydroxyomeprazole (CYP2C19) and omeprazole sulfone (CYP3A4). Minor mutations in CYP2C19 affect its activity in the liver and, in turn, the metabolic and pharmacokinetic profiles of omeprazole. The frequency of CYP2C19 poor metabolizers in population of Asian descent has been reported to range from 10 to 20%. Accordingly, results from population studies indicate that omeprazole can be used as a probe drug for phenotyping CYP2C19. The optical isomers of omeprazole show a clear difference in their metabolism by human liver microsomes. This study demonstrates the stereospecific analysis of omeprazole in human plasma as a probe drug of CYP2C19 phenotyping. The chiral separation of omeprazole was achieved on a chiral column with circular dichroism (CD) detection and LC/MS. A good resolution of enantiomers was obtained. The column used for chiral separation was CHIRALPAK AD-RH column (4.6×150 mm) using phosphate buffer and (or ammonium acetate) acetonitrile as an eluent. After a single oral dose of omeprazole (20 mg), the plasma concentrations of the separate enantiomers of omeprazole were determined for 3.5 h after drug intake. The present study is useful because of the part polymorphism plays in the therapeutic effectiveness of proton pump inhibitors during the treatment of acid-related diseases.