Mexidol, Cytoflavin, and succinic acid derivatives as antihypoxic, anti‐ischemic metabolic modulators, and ergogenic aids in athletes and consideration of their potential as performance enhancing drugs,Drug Testing and Analysis

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Mexidol, Cytoflavin, and succinic acid derivatives as antihypoxic, anti‐ischemic metabolic modulators, and ergogenic aids in athletes and consideration of their potential as performance enhancing drugs
Drug Testing and Analysis ( IF 2.6 ) Pub Date : 2024-02-26 , DOI: 10.1002/dta.3655
Karol Jędrejko ₁ , Oliver Catlin ₂ , Timothy Stewart ₂ , Bożena Muszyńska ₁

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Emoxypine (ethylmethylhydroxypyridine) is a synthetic derivative of vitamin B6. Emoxypine succinate is a registered drug in Russia and Ukraine under various trade names including Mexidol, Mexicor, and Armadin Long. Mexidol demonstrates antihypoxic and anti‐ischemic effects and also modulates metabolism. The use of Mexidol by Russian athletes has been confirmed in the past. Current use by athletes is unknown as this drug is not monitored or included in drug testing protocol. Metabotropic and antihypoxic effects of Mexidol were compared to the effects of meldonium or trimetazidine, both of which are included on the World Anti‐Doping Agency (WADA) Prohibited List in category S4.4. Metabolic Modulators. The conjugation of emoxypine with succinate elevates the therapeutic effectiveness of the Mexidol formulation as succinic acid itself has important impacts to consider despite being a common food additive and drug excipient. Other succinic acid salts like ammonium succinate, found as dietary supplement, have been patented as performance enhancers. Available research on healthy subjects suggests that combinations of selected 3‐substituted pyridine derivatives with succinate including Mexidol and a related drug Cytoflavin can enhance the performance of athletes. Cytoflavin is a multi‐component formula containing meglumine sodium succinate, nicotinamide (vitamin B3), inosine (riboxin), and riboflavin. Other related succinate‐based drugs include Remaxol, Reamberin, and Cogitum. Mexidol and Cytoflavin and related substances exhibit similar biological effects as drugs on the WADA Prohibited List, and if they are used for performance enhancement by athletes, they could be worthy of consideration as prohibited substances in sport.

中文翻译：

Mexidol、细胞黄素和琥珀酸衍生物作为运动员的抗缺氧、抗缺血代谢调节剂和增效剂，并考虑它们作为性能增强药物的潜力

Emoxypine（乙基甲基羟基吡啶）是维生素 B 的合成衍生物6 。 Emoxypine succinate 是在俄罗斯和乌克兰注册的药物，商品名为 Mexidol、Mexisr 和 Armadin Long。 Mexidol 具有抗缺氧和抗缺血作用，还可以调节新陈代谢。俄罗斯运动员使用 Mexidol 的情况过去已得到证实。目前运动员的使用情况尚不清楚，因为该药物未受到监控或包含在药物测试方案中。将 Mexidol 的代谢和抗缺氧作用与米曲肼或曲美他嗪的作用进行了比较，两者均被列入世界反兴奋剂机构 (WADA) 禁用清单的 S4.4 类。代谢调节剂。 Emoxypine 与琥珀酸盐的结合提高了 Mexidol 制剂的治疗效果，因为琥珀酸本身具有重要的影响需要考虑，尽管它是一种常见的食品添加剂和药物赋形剂。其他琥珀酸盐，如琥珀酸铵，作为膳食补充剂被发现，已作为性能增强剂获得专利。对健康受试者的现有研究表明，选定的 3-取代吡啶衍生物与琥珀酸盐（包括 Mexidol 和相关药物细胞黄素）的组合可以提高运动员的表现。细胞黄素是一种多成分配方，含有葡甲胺琥珀酸钠、烟酰胺（维生素 B 3 ）、肌苷（核糖蛋白）和核黄素。其他相关的琥珀酸盐药物包括 Remaxol、Reamberin 和 Cogitum。 Mexidol和细胞黄素及相关物质与世界反兴奋剂机构禁用清单上的药物表现出相似的生物作用，如果它们用于运动员提高成绩，则值得考虑将其列为体育运动中的禁用物质。

更新日期：2024-02-26

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