Keating Gillian M, Figgitt David P
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2004;64(8):875-82; discussion 883. doi: 10.2165/00003495-200464080-00008.
The proton pump inhibitor esomeprazole comprises the S-isomer of omeprazole. An intravenous formulation of the drug has been developed for use in patients not able to take oral drugs. The level of gastric acid control was similar with intravenous and oral esomeprazole in two studies in healthy volunteers receiving 20 or 40 mg once daily for 5 days. In addition, a similar level of gastric acid control occurred with intravenous esomeprazole 40 mg administered by infusion or injection once daily for 10 days. In healthy volunteers, intravenous esomeprazole provided faster and more effective gastric acid control than intravenous pantoprazole (40 mg once daily for 5 days). In addition, control of basal and pentagastrin-stimulated gastric acid secretion was better with intravenous esomeprazole 40 mg than with intravenous omeprazole 40 mg (single-dose study). Healing rates at 4 weeks were approximate, equals 80% in a well designed study in patients with erosive oesophagitis (n = 246) who received esomeprazole 40 mg once daily intravenously (by injection or infusion) or orally. Intravenous therapy was administered for the first week, after which all patients received oral esomeprazole. Intravenous esomeprazole was generally well tolerated in patients with erosive oesophagitis, with a tolerability profile similar to that of the oral formulation.
质子泵抑制剂埃索美拉唑是奥美拉唑的S-异构体。已开发出该药物的静脉制剂，用于无法口服药物的患者。在两项针对健康志愿者的研究中，每天一次给予20或40毫克，持续5天，静脉注射和口服埃索美拉唑对胃酸的控制水平相似。此外，每天一次静脉输注或注射40毫克埃索美拉唑，持续10天，对胃酸的控制水平也相似。在健康志愿者中，静脉注射埃索美拉唑比静脉注射泮托拉唑（每天一次40毫克，持续5天）能更快、更有效地控制胃酸。此外，在单剂量研究中，40毫克静脉注射埃索美拉唑对基础胃酸分泌和五肽胃泌素刺激的胃酸分泌的控制比40毫克静脉注射奥美拉唑更好。在一项设计良好的针对糜烂性食管炎患者（n = 246）的研究中，接受每天一次40毫克静脉注射（通过注射或输注）或口服埃索美拉唑的患者，4周时的愈合率相近，约为80%。静脉治疗持续第一周，之后所有患者接受口服埃索美拉唑。糜烂性食管炎患者对静脉注射埃索美拉唑的耐受性通常良好，其耐受性与口服制剂相似。
