Boeckxstaens G E
Catholic University of Leuven, University Hospital Leuven, Dept Gastroenterology, Herestraat 49, Leuven 3000, Belgium.
Expert Opin Emerg Drugs. 2009 Sep;14(3):481-91. doi: 10.1517/14728210903133807.
Proton pump inhibitors (PPIs) are very effective and safe drugs for the treatment of erosive and non-erosive gastroesophageal reflux disease (GERD). Nevertheless, a significant proportion of GERD patients (30 - 40%) continue to suffer from symptoms during PPI treatment, which has stimulated the search for better drugs. Improvement of PPI pharmacokinetics and pharmacodynamics has been the main focus of drug development in the past decade with the ultimate goal of optimizing acid inhibition. New inhibitors of the proton pump with a longer half-life, acting faster and longer, have been developed, including potassium-competitive acid blockers. Recent data, however, suggest that the therapeutic efficacy of acid suppression may have reached its maximum and other mechanisms may have to be targeted to further improve symptom control. Potential drugs interacting with different targets are reflux inhibitors such as GABA(B) receptor agonists and mGluR5 antagonists. These agents reduce the number of transient lower esophageal sphincter relaxation thereby reducing both acid and non-acid reflux. Theoretically, visceral analgesics to modulate visceral perception or even growth factors to enhance mucosal healing may be other emerging drugs to treat GERD.
质子泵抑制剂(PPIs)是治疗糜烂性和非糜烂性胃食管反流病(GERD)非常有效且安全的药物。然而,相当一部分GERD患者(30%-40%)在接受PPI治疗期间仍有症状,这促使人们寻找更好的药物。在过去十年中,改善PPI的药代动力学和药效学一直是药物研发的主要重点,最终目标是优化胃酸抑制作用。已经开发出了半衰期更长、起效更快且作用时间更长的新型质子泵抑制剂,包括钾离子竞争性酸阻滞剂。然而,最近的数据表明,胃酸抑制的治疗效果可能已达到极限,可能需要针对其他机制来进一步改善症状控制。与不同靶点相互作用的潜在药物包括反流抑制剂,如GABA(B)受体激动剂和mGluR5拮抗剂。这些药物可减少下食管括约肌一过性松弛的次数,从而减少酸反流和非酸反流。从理论上讲,调节内脏感觉的内脏镇痛药甚至促进黏膜愈合的生长因子可能是其他正在出现的治疗GERD的药物。