[伊美乐明:作用机制特点及潜在益处]。

Q4 Medicine
K O Kuznetsov, A A Saetova, E I Mahmutova, A G Bobrik, D V Bobrik, I R Nagaev, A D Khamitova, A M Arapieva
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引用次数: 0

摘要

依米明是一类新的含四氢三嗪的口服降糖药中的第一种药物,称为“glimines”。其作用机制旨在达到双重效果,一是改善胰腺β细胞的功能,二是增强胰岛素在关键组织中的作用,包括肝脏和骨骼肌。在细胞水平上,imimimin调节线粒体功能,从而改善细胞能量代谢,并在活性氧过度积累的条件下保护细胞免于死亡。值得注意的是,伊米明的作用机制不同于现有治疗2型糖尿病的药物。与胰高血糖素样肽-1受体激动剂一样,伊米霉素以完全依赖葡萄糖的方式增强胰岛素分泌,但它们在细胞水平上的作用机制不同。磺脲类药物和格列尼德类药物通过关闭atp敏感的钾通道来释放胰岛素,这也不同于伊米霉素。与二甲双胍相比,依米列明的效果也有显著差异。其他主要类型的口服降压药,如钠-葡萄糖转运蛋白-2抑制剂、噻唑烷二酮类和α葡萄糖苷酶抑制剂,其作用机制与依米列明不重叠。鉴于这种作用机制的差异,依米明可作为联合治疗的一部分,例如与西格列汀和二甲双胍联合使用。依米列明分子吸收良好(Tmax-4),半衰期为5-6小时,大部分通过肾脏排出,与二甲双胍或西格列汀均无临床显著相互作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

[Imeglimin: features of the mechanism of action and potential benefits].

[Imeglimin: features of the mechanism of action and potential benefits].

Imeglimin is the first drug in a new class of tetrahydrotriazine-containing oral hypoglycemic agents called «glimines». Its mechanism of action is aimed at achieving a double effect, firstly, to improve the function of beta cells of the pancreas, and secondly, to enhance the action of insulin in key tissues, including the liver and skeletal muscles. At the cellular level, imeglimin modulates mitochondrial function, which leads to an improvement in cellular energy metabolism, as well as to the protection of cells from death in conditions of excessive accumulation of reactive oxygen species. It is important to note that the mechanism of action of imeglimin differs from existing drugs used for the treatment of type 2 diabetes mellitus. Like glucagon-like peptide-1 receptor agonists, imeglimin enhances insulin secretion in an exclusively glucose-dependent manner, but their mechanism of action at the cellular level diverges. Sulfonylureas and glinides function by closing ATP-sensitive potassium channels to release insulin, which is also different from imeglimin. Compared with metformin, the effect of imeglimine is also significantly different. Other major classes of oral antihypertensive agents, such as sodium-glucose transporter-2 inhibitors, thiazolidinediones and α glucosidase inhibitors mediate their action through mechanisms that do not overlap with imeglimine. Given such differences in the mechanisms of action, imeglimin can be used as part of combination therapy, for example with sitagliptin and metformin. The imeglimine molecule is well absorbed (Tmax-4), and the half-life is 5-6 hours, is largely excreted through the kidneys, and also has no clinically significant interactions with either metformin or sitagliptin.

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来源期刊
Problemy endokrinologii
Problemy endokrinologii Medicine-Endocrinology, Diabetes and Metabolism
CiteScore
1.40
自引率
0.00%
发文量
59
期刊介绍: Since 1955 the “Problems of Endocrinology” (or “Problemy Endocrinologii”) Journal publishes timely articles, balancing both clinical and experimental research, case reports, reviews and lectures on pressing problems of endocrinology. The Journal is aimed to the most topical issues of endocrinology: to chemical structure, biosynthesis and metabolism of hormones, the mechanism of their action at cellular and molecular level; pathogenesis and to clinic of the endocrine diseases, new methods of their diagnostics and treatment. The Journal: features original national and foreign research articles, reflecting world endocrinology development; issues thematic editions on specific areas; publishes chronicle of major international congress sessions and workshops on endocrinology, as well as state-of-the-art guidelines; is intended for scientists, endocrinologists diabetologists and specialists of allied trade, general practitioners, family physicians and pediatrics.
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