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(10):1503-38. doi: 10.2165/00003495-200262100-00006.
Esomeprazole (S-isomer of omeprazole), the first single optical isomer proton pump inhibitor, generally provides better acid control than current racemic proton pump inhibitors and has a favourable pharmacokinetic profile relative to omeprazole. In a large well designed 8-week trial in patients (n >5000) with erosive oesophagitis, esomeprazole recipients achieved significantly higher rates of endoscopically confirmed healed oesophagitis than those receiving lansoprazole. Respective healed oesophagitis rates with once-daily esomeprazole 40mg or lansoprazole 30mg were 92.6 and 88.8%. Overall, esomeprazole was also better than omeprazole, although these differences were not always statistically significance. Ninety-two to 94% of esomeprazole recipients (40mg once daily) achieved healed oesophagitis versus 84 to 90% of omeprazole recipients (20mg once daily). Esomeprazole was effective across all baseline grades of oesophagitis; notably, relative to lansoprazole, as baseline severity of disease increased, the difference in rates of healed oesophagitis also increased in favour of esomeprazole. Resolution of heartburn was also significantly better with esomeprazole 40mg than with these racemic proton pump inhibitors. Long-term (up to 12 months) therapy with esomeprazole effectively maintained healing in these patients. Once-daily esomeprazole 20 or 40mg for 4 weeks resolved symptoms in patients with symptomatic gastro-oesophageal reflux disease (GORD) without oesophagitis. Symptoms were effectively managed in the long-term with symptom-driven on-demand esomeprazole (20 or 40mg once daily). Eradicating Helicobacter pylori infection is considered pivotal to successfully managing duodenal ulcer disease. Seven days' treatment (twice-daily esomeprazole 20mg plus amoxicillin 1g and clarithromycin 500mg) eradicated H. pylori in >/=86% of patients (intention-to-treat), a rate that was similar to equivalent omeprazole-based regimens. Esomeprazole is generally well tolerated, both as monotherapy and in combination with antimicrobial agents, with a tolerability profile similar to that of other proton pump inhibitors. Few patients discontinued therapy because of treatment-emergent adverse events (<3% of patients), with very few (<1%) drug-related serious adverse events reported.
Esomeprazole is an effective, 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 healed oesophagitis and resolved symptoms in patients with endoscopically confirmed erosive oesophagitis and overall, provided better efficacy than omeprazole. Notably, in a large (n >5000 patients) double-blind trial, esomeprazole 40mg provided significantly better efficacy than lansoprazole in terms of healing rates and resolution of symptoms. Long-term therapy with esomeprazole maintained healed oesophagitis in these patients. Esomeprazole also proved beneficial in patients with symptomatic GORD without oesophagitis. Thus, esomeprazole has emerged as an option for first-line therapy in the management of acid-related disorders.
埃索美拉唑（奥美拉唑的S-异构体）是首个单一光学异构体质子泵抑制剂，通常比目前的消旋质子泵抑制剂能更好地控制胃酸，并且相对于奥美拉唑具有良好的药代动力学特征。在一项针对侵蚀性食管炎患者（n>5000）的大型精心设计的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兰索拉唑治疗的患者。每日一次服用40mg埃索美拉唑或30mg兰索拉唑时，食管炎愈合率分别为92.6%和88.8%。总体而言，埃索美拉唑也优于奥美拉唑，尽管这些差异并不总是具有统计学意义。92%至94%接受埃索美拉唑治疗的患者（每日一次40mg）实现了食管炎愈合，而接受奥美拉唑治疗的患者（每日一次20mg）这一比例为84%至90%。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增加，食管炎愈合率的差异也增大，且更有利于埃索美拉唑。服用40mg埃索美拉唑缓解烧心症状的效果也显著优于这些消旋质子泵抑制剂。埃索美拉唑长期（长达12个月）治疗可有效维持这些患者的愈合状态。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4周可缓解症状。通过症状驱动按需服用埃索美拉唑（每日一次20mg或40mg）可长期有效控制症状。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。7天治疗（每日两次服用20mg埃索美拉唑加1g阿莫西林和500mg克拉霉素）使≥86%的患者（意向性治疗）根除了幽门螺杆菌，这一比率与基于奥美拉唑的等效方案相似。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，耐受性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），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有效且耐受性良好的药物。在8周双盲试验中，埃索美拉唑使经内镜确认的侵蚀性食管炎患者的食管炎愈合并缓解症状，总体而言，其疗效优于奥美拉唑。值得注意的是，在一项大型（n>5000例患者）双盲试验中，就愈合率和症状缓解而言，40mg埃索美拉唑的疗效显著优于兰索拉唑。埃索美拉唑长期治疗可维持这些患者的食管炎愈合状态。埃索美拉唑对无食管炎的有症状GORD患者也有益。因此，埃索美拉唑已成为治疗酸相关疾病一线疗法的一个选择。
