Scott Lesley J, Dunn Christopher J, Mallarkey Gordon, Sharpe Miriam
Adis International Limited, 41 Centorian Drive, PB 65901, Mairangi Bay, Auckland 10, New Zealand.
Drugs. 2002;62(7):1091-118. doi: 10.2165/00003495-200262070-00006.
Esomeprazole, the S-isomer of omeprazole, is the first proton pump inhibitor to be developed as a single optical isomer. It provides better acid control than current racemic proton pump inhibitors and has a favourable pharmacokinetic profile relative to omeprazole. In large well designed 8-week trials in patients with erosive oesophagitis, esomeprazole recipients achieved significantly higher rates of endoscopically confirmed healed oesophagitis than those receiving omeprazole or lansoprazole. Esomeprazole was effective across all baseline grades of oesophagitis; notably, relative to lansoprazole, as the baseline severity of disease increased, the difference in rates of healed oesophagitis also increased in favour of esomeprazole. In two trials, 94% of patients receiving esomeprazole 40mg once daily achieved healed oesophagitis versus 84 to 87% of omeprazole recipients (20mg once daily). In a study in >5000 patients, respective healed oesophagitis rates with once-daily esomeprazole 40mg or lansoprazole 30mg were 92.6 and 88.8%. Resolution of heartburn was also significantly better with esomeprazole than with these racemic proton pump inhibitors. Long-term (up to 12 months) therapy with esomeprazole effectively maintained healed oesophagitis in these patients. Esomeprazole 20 or 40mg once daily for 4 weeks proved effective in patients with symptomatic gastro-oesophageal reflux disease (GORD) without oesophagitis. Eradicating Helicobacter pylori infection is considered pivotal to successfully managing duodenal ulcer disease. Ten days' triple therapy (esomeprazole 40mg once daily, plus twice-daily amoxicillin 1g and clarithromycin 500mg) eradicated H. pylori in 77 to 78% of patients (intention-to-treat) with endoscopically confirmed duodenal ulcer disease. Esomeprazole is generally well tolerated, both as monotherapy and in combination with antimicrobial agents. The tolerability profile is similar to that of other proton pump inhibitors. Few patients discontinued therapy because of treatment-emergent adverse events (<3% of patients) and very few (<1%) drug-related serious adverse events were reported.
Esomeprazole is an effective and well tolerated treatment for managing GORD and for eradicating H. pylori infection in patients with duodenal ulcer disease. In 8-week double-blind trials, esomeprazole effectively healed oesophagitis and resolved symptoms in patients with endoscopically confirmed erosive oesophagitis. Notably, in large (n >1900 patients) double-blind trials, esomeprazole provided significantly better efficacy than omeprazole or lansoprazole in terms of both healing rates and resolution of symptoms. Long-term therapy with esomeprazole effectively maintained healed oesophagitis in these patients. Esomeprazole was also effective in patients with symptomatic GORD. Thus, esomeprazole has emerged as an effective option for first-line therapy in the management of acid-related disorders.
埃索美拉唑是奥美拉唑的S-异构体，是首个作为单一光学异构体开发的质子泵抑制剂。与目前的消旋质子泵抑制剂相比，它能更好地控制胃酸，并且相对于奥美拉唑具有良好的药代动力学特征。在针对糜烂性食管炎患者进行的精心设计的大型8周试验中，接受埃索美拉唑治疗的患者经内镜确认的食管炎愈合率显著高于接受奥美拉唑或兰索拉唑治疗的患者。埃索美拉唑对所有基线食管炎分级均有效；值得注意的是，相对于兰索拉唑，随着疾病基线严重程度的增加，食管炎愈合率的差异也更有利于埃索美拉唑。在两项试验中，每日一次服用40mg埃索美拉唑的患者中有94%实现了食管炎愈合，而接受奥美拉唑（每日一次20mg）治疗的患者这一比例为84%至87%。在一项超过5000例患者的研究中，每日一次服用40mg埃索美拉唑或30mg兰索拉唑的患者食管炎愈合率分别为92.6%和88.8%。与这些消旋质子泵抑制剂相比，埃索美拉唑缓解烧心症状的效果也显著更好。在这些患者中，埃索美拉唑长期（长达12个月）治疗有效地维持了食管炎的愈合。对于无食管炎的有症状胃食管反流病（GORD）患者，每日一次服用20mg或40mg埃索美拉唑，持续4周被证明是有效的。根除幽门螺杆菌感染被认为是成功治疗十二指肠溃疡病的关键。为期10天的三联疗法（每日一次40mg埃索美拉唑，加每日两次1g阿莫西林和500mg克拉霉素）使经内镜确认患有十二指肠溃疡病的患者中77%至78%（意向性治疗）的幽门螺杆菌得到根除。埃索美拉唑作为单一疗法或与抗菌药物联合使用时，一般耐受性良好。其耐受性特征与其他质子泵抑制剂相似。很少有患者因治疗中出现的不良事件而停药（<3%的患者），并且报告的与药物相关的严重不良事件极少（<1%）。
埃索美拉唑是治疗GORD以及根除十二指肠溃疡病患者幽门螺杆菌感染的一种有效且耐受性良好的药物。在8周的双盲试验中，埃索美拉唑有效地治愈了经内镜确认的糜烂性食管炎患者的食管炎并缓解了症状。值得注意的是，在大型（n>1900例患者）双盲试验中，就愈合率和症状缓解方面，埃索美拉唑比奥美拉唑或兰索拉唑具有显著更好的疗效。埃索美拉唑长期治疗有效地维持了这些患者食管炎的愈合。埃索美拉唑对有症状的GORD患者也有效。因此，埃索美拉唑已成为治疗酸相关疾病一线疗法的有效选择。
