[Current status and prospects of using potassium-competitive acid blockers in gastroenterology].

IF 0.3 4区 医学 Q3 MEDICINE, GENERAL & INTERNAL
I V Maev, D N Andreev, A V Zaborovsky, A K Fomenko
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引用次数: 0

Abstract

Over the past decades, acid production in the stomach has been regulated mainly by proton pump inhibitors (PPIs). However, despite their widespread use and solid evidence base for efficacy, PPIs have pharmacokinetic and pharmacodynamic limitations, such as a slow onset of action, response variability (dependent on CYP2C19 polymorphisms), and the need for activation in an acidic environment. These restrictions underscore the need for innovative molecular approaches to inhibiting acid production, which led to the development of a fundamentally different mechanism of action - potassium-competitive acid blockers (P-CABs), first introduced into clinical practice in 2015. The mechanism of action of P-CABs is based on a reversible ionic interaction with hydrogen potassium adenosine triphosphatase (H+/K+ ATPase) in parietal cells of the stomach. Direct inhibition of the active enzyme enables more rapid and sustained control of gastric secretion, including nocturnal and postprandial acid production, making this class of drugs particularly relevant in the treatment of gastroesophageal reflux disease, peptic ulcers, and in the eradication of Helicobacter pylori. Recent meta-analyses demonstrate the clinical benefits of P-CABs over PPIs for these indications.

[在胃肠病学中使用钾竞争酸阻滞剂的现状和前景]。
在过去的几十年里,胃中的酸产生主要由质子泵抑制剂(PPIs)调节。然而,尽管PPIs被广泛使用,且疗效有坚实的证据基础,但它具有药代动力学和药效学上的局限性,如起效缓慢、反应变异性(依赖于CYP2C19多态性)以及需要在酸性环境中激活。这些限制强调了抑制酸生成的创新分子方法的必要性,这导致了一种完全不同的作用机制的发展-钾竞争酸阻滞剂(p - cab),于2015年首次引入临床实践。p - cab的作用机制是基于与胃壁细胞中氢钾腺苷三磷酸酶(H+/K+ atp酶)的可逆离子相互作用。直接抑制这种活性酶可以更快速、更持久地控制胃液分泌,包括夜间和餐后的胃酸分泌,这类药物在治疗胃食管反流病、消化性溃疡和根除幽门螺杆菌方面尤为重要。最近的荟萃分析表明,在这些适应症中,p - cab优于PPIs。
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来源期刊
Terapevticheskii Arkhiv
Terapevticheskii Arkhiv 医学-医学:内科
CiteScore
1.40
自引率
33.30%
发文量
171
审稿时长
3-8 weeks
期刊介绍: Терапевтический архив The journal was founded by the prominent Russian therapists M.P. Konchalovsky and G.F. Lang in 1923. Then its editors-in-chief were Professors V.N. Vinogradov and A.G. Gukasyan. Since 1972, E.I. Chazov, Academician of the Russian Academy of Sciences, has been heading the editorial board of the journal. Over 90 years, there have been more than 1000 issues where the authors and editorial staff have done their best for readers to keep abreast of current advances in medical science and practice and for physicians to master the advanced principles of recognition and treatment of a wide spectrum of visceral diseases. The papers published in the journal (editorials, original articles, lectures, reviews, etc.) cover both current scientific achievements and practical experience in diagnosing, treating, and preventing visceral diseases. The authors of publications are not only Russian, but also foreign scientists and physicians. All papers are peer-reviewed by highly qualified Russian specialists. The journal is published monthly. Traditionally, each issue has predominantly certain thematic areas covering individual therapy specializations. Every year, one of the issues is devoted to related problems in practical medicine (allergology and immunology, neurology and psychiatry, obstetrics, oncology, etc.). This all draws the attention of the reading public to the journal. The journal is indexed in RSCI (Russian Science Citation Index), PubMed/Medline, Index Medicus, Scopus/EMBASE, Web of Science Core Collection (Science Citation Index Expanded), Web of Science (Russian Science Citation Index - RSCI, Current Contents Connect, BIOSIS Previews), Google Scholar, Ulrich''s Periodicals Directory. The journal is included in the list of periodicals recommended by the Higher Attestation Committee for publishing the papers containing the basic materials of doctoral and candidate dissertations. By the decision of the Presidium of the Russian Academy of Medical Sciences, the “Therapevticheskiy Arkhiv” was awarded the Botkin medal. It was admitted to the European Association of Sciences Editors (EASE). The journal was honored with the Golden Press Fund decoration at the 13th International Press Professional Exhibition.
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