Effect of esomeprazole 40 mg vs omeprazole 40 mg on 24-hour intragastric pH in patients with symptoms of gastroesophageal reflux disease

Maintenance of intragastric pH > 4 is vital for effective management of gastroesophageal reflux disease (GERD). Esomeprazole 40 mg, the first proton pump inhibitor developed as an optical isomer, demonstrates improved acid inhibition over omeprazole 20 mg. Our aim was to compare esomeprazole 40 mg with omeprazole 40 mg, once-daily, on intragastric acidity in patients with symptoms of GERD. In this open-label, crossover study, 130 patients with symptoms of GERD received esomeprazole 40 mg or omeprazole 40 mg once-daily for five days. The 24-hr intragastric pH was monitored on days 1 and 5 of each treatment period. The mean percentage of the 24-hr period with intragastric pH > 4 was significantly greater (P < 0.001) with esomeprazole 40 mg than with omeprazole 40 mg on days 1 (48.6% vs 40.6%) and 5 (68.4% vs 62.0%). Interpatient variability was significantly less with esomeprazole than omeprazole. Esomeprazole was well tolerated. In conclusion, esomeprazole 40 mg provides more effective acid control than twice the standard dose of omeprazole.     

埃索美拉唑联合丽珠胃三联治疗HP阳性慢性浅表性胃炎临床观察

[目的]观察埃索美拉唑联合丽珠胃三联治疗Hp阳性慢性浅表性胃炎的临床疗效。[方法]Hp阳性的慢性浅表性胃炎90例，随机分为治疗组（45例）、对照组（45例），治疗组采用埃索美拉唑联合丽珠胃三联口服治疗，对照组采用奥美拉唑联合丽珠胃三联口服治疗，分别于治疗第2、3、4周观察临床症状改善情况及胃镜下胃炎愈合情况。[结果]症状改善情况及胃炎愈合情况，治疗组疗效均优于对照组（P〈0．05）。[结论]埃索美拉唑联合丽珠胃三联治疗HP阳性慢性浅表性胃炎有较好的临床疗效。     

埃索美拉唑治疗胃食管反流病的临床观察

目的探讨不同剂量埃索美拉唑对胃食管反流病(GERD)的治疗效果。方法选择63例门诊及住院经电子胃镜证实为GERD患者(洛杉矶分级为A级和B级)随机分为三组。A组20例予以埃索美拉唑20mg,每日2次;B组21例予以埃索美拉唑40mg,每日2次;C组22例予以埃索美拉唑20mg,每日2次,睡前40mg,分别观察患者治疗前及治疗后8周临床症状改善情况;治疗8周后行电子胃镜检查观察愈合率。结果三组临床症状均有明显改善,症状记分较治疗前显著下降(P均<0.01)。C组在症状消失率、总有效率以及内镜下食管炎愈合率和总有效率方面均高于A、B组,但差异无显著性。结论埃索美拉唑是治疗轻、中度GERD患者有效的药物,尤其加用夜间酸突破治疗,效果更佳。     

埃索美拉唑治疗胃食管反流病的系统评价

目的：评价埃索美拉唑与其它质子泵抑制剂（PPI）比较治疗胃食管反流病的疗效。方法：文献检索并收集埃索美拉唑与其它PPI相比较的随机对照试验文献，按Cochrane协作网提供的方法对纳入文献进行质量评价。结果：共纳入14个随机对照研究（RCT）。对于非糜烂性食管炎埃索美拉唑与潘索拉唑比较在6个月后症状缓解率差异有统计学意义。对于糜烂性食管炎，埃索美拉唑与其他PPI比较均有统计学意义。结论：对于非糜烂性食管炎，埃索美拉唑比潘索拉唑疗效好；对于糜烂性食管炎，埃索美拉唑比其他PPI疗效好。     

埃索美拉唑相关药物性肝损害

1名54岁女性患者，因十二指肠球部溃疡口服埃索美拉唑20mg，1次／d、吉法酯50mg，3次／d、铝碳酸镁500mg，3次／d。服药近半月后逐渐出现食欲减退、尿色加深，继续服用1月余后出现巩膜黄染、伴皮肤瘙痒。门诊检查肝功能示：AST890 U／L，ALT 1123 U／L，ALP 204 U／L，,γ-GT 277 U／L，TBil 169．7μmol／L，DBil 99．7iμmol／L，IBil 70．0 μmol／L，TBA 234．6μmol／L。入院后停用埃索关拉唑，给予还原型谷胱甘肽和硫普罗宁治疗，1周后患者巩膜黄染逐渐消退，尿色恢复正常，3周后复查肝功能，明显好转出院。     

Clinical pharmacology and safety profile of esomeprazole, the first enantiomerically pure proton pump inhibitor

Awareness of important differences in the pharmacological profile of individual optical isomers of chiral drugs led to the development of esomeprazole, the S-isomer of omeprazole, a new pharmacological entity designed to improve the clinical outcome of available proton pump inhibitors in the management of acid-related disorders. The superior acid control achieved by esomeprazole is mainly due to an advantageous metabolism compared with racemate omeprazole, leading to improved bioavailability and to enhanced delivery of the drug to the gastric proton pump.     

埃索美拉唑、左氧氟沙星与奥硝唑联用治疗慢性胃炎效果

目的观察埃索美拉唑、左氧氟沙星与奥硝唑联用治疗幽门螺杆菌阳性慢性胃炎病人的效果及安全性。方法选取97例幽门螺杆菌阳性慢性胃炎病人,随机分为治疗组50例与对照组47例。治疗组采用埃索美拉唑、左氧氟沙星与奥硝唑治疗;对照组采用埃索美拉唑、克拉霉素、阿莫西林治疗,均治疗7d,疗程结束4～6周后行^13C-尿素呼气试验检查。结果治疗组和对照组的幽门螺杆菌根治率分别为82．00％和63．83％,两组比较差异有显著性（χ^2=4．08,P〈0．05）。结论埃索美拉唑、左氧氟沙星与奥硝唑联用治疗幽门螺杆菌阳性慢性胃炎病人效果可靠,安全性好。     

Effect of esomeprazole and rabeprazole on intragastric pH in healthy Chinese: an open, randomized crossover trial

BACKGROUND AND AIM: Esomeprazole is the S-isomer of omeprazole, with a stronger acid suppressive effect than omeprazole. This open, randomized crossover study was designed to evaluate the effect of esomeprazole and another proton-pump inhibitor, rabeprazole, on intragastric pH in healthy Chinese. METHODS: Thirty-six healthy volunteers (26 men and 10 women, aged between 20 and 31 years) were enrolled. Subjects were given either esomeprazole 40 mg (n = 18) or rabeprazole 10 mg (n = 18) orally once daily for 5 days during the first dosing period, then the other medicine at the set dosage for the second dosing period. The two periods were separated by a 14-day washout phase. The doses were chosen according to the State Food and Drug Administration of China for the treatment of acid-related diseases. Intragastric pH was continuously monitored for 24 h on days 1 and 5 of each dosing period. CYP2C19 genotypes were analyzed to identify the extensive metabolizers (EM) and poor metabolizers (PM). RESULTS: The percentage of time with intragastric pH >4 was significantly higher (P < 0.001) in subjects receiving esomeprazole than in those receiving rabeprazole in the first 4 h after administration of the first dose (70.65% vs 44.87%), at 24 h on day 1 (73.7% vs 54.8%) and at 24 h on day 5 (84.2% vs 76.2%). The median intragastric pH was also higher in subjects receiving esomeprazole than in those receiving rabeprazole in the first 6 h, day 1 and day 5 (P 4 for at least 16 h on day 1 (63.9% vs 33.3%) and on day 5 (88.9% vs 61.1%) was higher after administration of esomeprazole than after rabeprazole (both P < 0.05). On genotype analysis, 28 of the subjects were EM and eight were PM. Those who were PM tended to have a higher, albeit not statistically significant, percentage of time with intragastric pH >4 and the median 24-h intragastric pH than those who were EM. Both drugs were well tolerated. CONCLUSIONS: Esomeprazole 40 mg orally once daily is more effective and faster in increasing intragastric pH than rabeprazole 10 mg orally once daily, and thus offers a potential for improved efficacy in acid-related diseases.     

Severe systemic adverse reaction to proton pump inhibitors in an infant

Episodes of respiratory distress with chest retraction and wheezing, sometimes associated with facial edema, were noted after administering the proton pump inhibitors omeprazole and esomeprazole in an infant with gastroesophageal reflux. The disturbances relieved dramatically after withdrawing the proton pump inhibitor.