Mexidol emoxypine - detailed description of the substance

Emoxypine, also known by its trade name Mexidol or Mexifin in succinate form, is a new compound developed by Pharmasoft Pharmaceuticals. It is known for its therapeutic and industrial applications due to its diverse properties, including antihypoxic, antioxidant, neuroprotective and cardioprotective [1]. Interestingly, scientific studies have also reported beneficial effects of emoxipine in the treatment of neurodegenerative conditions such as Alzheimer's disease, as well as blood disorders such as thalassemia and hemochromatosis [1].

Note: Studies on emoxipine refer to several of its forms, basic emoxipine, emoxipine succinate, which is its most advanced form and has the trade name Mexidol, and several others.

History and key features of emoxipine action

Emoxypine was introduced to the Russian market by Smirnov and Kuzmin under the brand name Mexidol. Although well known in Russia, the drug has not received approval in the United States or Europe, mainly because of its Russian origin [1]. Nevertheless, there is growing curiosity about its properties and possible applications around the world. Companies intend to conduct tests using internationally recognized animal models to discover treatments for new conditions.

One of the key pharmacokinetic advantages of emoxypine is its ability to penetrate the blood-brain barrier due to its small size and low molecular weight. Researchers Biryukov, Dmitri Valerievich and POMYTKIN's Igor Anatolievich worked on emoxypine to improve its delivery to the brain and neural tissues [1]. Because emoxypine is hydrophilic, it had difficulty effectively penetrating the blood-brain barrier. To solve this problem, they created derivatives with higher lipophilicity. Their goal was to increase the drug's absorption into the central nervous system and increase its efficacy.

Moreover, the unique combination of 2-ethyl-6-methyl-3-hydroxypyridinium cation and succinate ion in emoxypine succinate offers a wide range of pharmacological effects [1]. This combination not only copes with metabolic diseases associated with problems in the blood vessel lining, but also helps maintain an adequate thickness of the lipid bilayer, which is crucial for controlling the movement and absorption of the drug in the body.

Anti-anxiety and antidepressant properties of Mexidol in studies

Studies have shown that emoxipine (known commercially as Mexidol) can help alleviate anxiety and depression in a variety of medical settings. In one study involving 32 older adults experiencing anxiety and mild cognitive decline, participants reported high levels of anxiety and some cognitive impairment at baseline. However, after taking Mexidol daily for four weeks, participants reported improved well-being, especially those with some cognitive problems, suggesting that Mexidol may be effective in reducing anxiety. The results were particularly notable for those with certain types of cognitive impairment, as they experienced more significant improvements. Additionally, the drug appeared to improve attention and overall nervous system function [2]. In another study focused on women with rheumatoid arthritis - a condition that leads to joint pain and potential mental health impacts - adding Mexidol to their treatment regimen resulted in reduced inflammation, reduced depressive symptoms and improved quality of life [3]. Notably, it works by targeting and improving certain brain functions and has the potential to improve attention and stabilize the body's automatic neural responses, contributing to a better sense of well-being. During an animal study, results revealed that administration of mexidol to rats reduced the time they showed signs of despair in the swim test, indicating potential antidepressant effects. The antidepressant effects of these drugs were similar to known therapies such as amitriptyline and alpha-lipoic acid. In addition, the effects of these drugs on depressive behavior appeared to be related to their effects on rat activity in the open field test [4].

In addition, the researchers studied 70 patients with panic disorder, including 30 men and 40 women, with a mean age of 34.5 years, all suffering from insomnia. Clinical and instrumental tests, including polysomnography, showed that the addition of mexidol significantly reduced anxiety, autonomic disorders and insomnia, improving the patients' quality of life. This study underscores the potential of mexidol as an effective addition to antidepressant therapy for patients with panic disorder, especially those with severe insomnia [6]. Interestingly, the study found that the antidepressant effects of mexidol and emoxipine may be related to their ability to improve the body's response to insulin [5]. When administered in appropriate doses, these drugs improved insulin sensitivity in rats. This improvement was associated with a reduction in the despair-like behavior observed in the Porsolt swim test. This suggests that mexidol and emoxipine may be effective in treating depression and anxiety not only through their direct effects on mood-related brain chemistry, but also by improving insulin sensitivity.

Studies of the effect of emoxipine in diabetic obesity

An animal study examined the potential of Mexidol and emoxipine to alleviate depression and anxiety, particularly in diabetic conditions, which are known to worsen mood disorders.

When administered in doses comparable to human consumption, both drugs markedly reduced anxiety and depression ratings in rats with diabetes. This indicates their effectiveness in treating similar mood disorders in diabetic patients. In addition, both drugs significantly lowered high blood sugar levels in rats with diabetes, presenting an additional benefit to individuals [7]. Moreover, a separate study with 30 diabetic patients treated with mexidol showed improvements in cognitive function, mood (reduction in asthenia and depression), sleep disorders and normalization of blood tests. This indicates that mexidol may be an effective adjunctive therapy for managing diabetes-related complications, including mood disorders [8]. These findings revealed that mexidol and emoxipine show promise not only in reducing anxiety and depression in diabetic conditions, but also in improving the overall management of diabetes by lowering blood sugar levels. 

Studies have shown that mexidol and emoxipine can exhibit antidepressant properties as early as 30 to 45 minutes after administration, offering a quick fix for acute management of depressive symptoms. In addition, an animal study revealed that emoxipine not only reduces signs of depression, but can also increase physical activity, indicating a possible stimulant effect [9]. In the case of diabetes, an animal study showed that mexidol lowered blood sugar levels after two weeks. It is noteworthy that mexidol is particularly beneficial for patients with diabetes, combining the ability to relieve depression with improved blood sugar control, presenting a unique dual therapy approach. This makes mexidol and emoxipine promising for rapidly controlling symptoms of depression and improving the quality of life of people with diabetes [10]. 

Mexidol and emoxipine have been studied for their potential benefits in treating the clinical symptoms of diabetic neuropathy, which often includes distressing sensations such as pain and numbness in the extremities, as well as associated anxiety and depression in patients with diabetes. In a study involving 120 patients with diabetes and diabetic foot syndrome, both emoxipine and mexidol contributed to significant reductions in neurological symptoms and anxiety and depressive disorders, underscoring their effectiveness as adjunctive treatments to primary diabetes therapy [11]. Similarly, another study compared the effects of alpha-lipoic acid and mexidol in the early stages of diabetic foot syndrome. The results revealed that mexidol not only reduced depression associated with neuropathy, but also relieved symptoms such as cramps and paresthesias more effectively than alpha-lipoic acid, without affecting blood sugar and lipid levels [12].

Further studies on women with recurrent uterine inflammatory diseases have indicated that including 3-oxypyridine derivatives, such as mexidol, in their treatment can reduce symptoms of depression, anxiety and systemic inflammation. In particular, mexidol significantly improved both mood disorders and inflammatory markers [13]. Also, in patients recovering from spinal surgery, a two-week course of mexidol showed efficacy in reducing depression. This benefit was accompanied by a reduction in pain levels and an improvement in psychological well-being and overall quality of life, highlighting the strong effect of mexidol on the physical and emotional aspects of postoperative recovery [14]. In an animal study, emoxipine and mexidol were observed to not only improve mood, but also lower blood sugar levels in diabetic rats. In particular, emoxipine showed more pronounced sedative effects at higher doses, but was not as effective as mexidol in relieving depression at lower doses [15]. 

In a separate study involving 67 patients with chronic cerebral ischemia, treatment with mexidol along with standard therapy (vinpocetine and piracetam) showed significant benefits. Patients receiving mexidol experienced a marked decrease in anxiety, improved autonomic balance and positive changes in adaptive blood responses, indicating activation of the adrenal cortex. In addition, the study noted a decrease in mean plasma molecules and an improvement in the ability of red blood cells to absorb the substance. This indicates differential effects of mexidol in reducing stress in cases of chronic cerebral ischemia [16]. Another study evaluated the effects of emoxipine and mexidol on depressive symptoms in patients with type 2 diabetes, along with the dynamics of blood lipoperoxidation. Both emoxipine and mexidol, administered for 14 days, were effective in lowering the lipoperoxidation products present in the circulation and reducing depressive symptoms, leading to improved cognitive function and increased quality of life. These positive clinical results of 3-oxypyridine derivatives occurred independently of changes in blood sugar and lipid levels, highlighting their potential therapeutic benefits in the management of depression associated with diabetes and cerebral ischemia [17]. 

In a study involving 162 patients suffering from SARS-CoV-2 infections and showing signs of pocovid syndrome, the mexidol treatment regimen significantly alleviated both subjective and objective symptoms associated with pocovid syndrome, including asthenia (weakness), anxiety and depression. In addition, there was a marked improvement in patients' quality of life. Selective mexidol therapy, starting with injections and then switching to oral Mexidol FORTE 250, has proven to be both highly effective and safe for those struggling with pocovid syndrome [18].

Use of emoxipine to reduce alcohol withdrawal symptoms

Emoxipine and Mexidol offer significant benefits in the management of Alcohol Withdrawal Syndrome (AWS). In this regard, a study was conducted to evaluate the efficacy of 3-oxypyridine and succinic acid derivatives (emoxipine, reamberin and mexidol) in reducing symptoms of anxiety and depression during the treatment of Alcohol Withdrawal Syndrome (AWS) [19]. This short-term, double-blind, placebo-controlled, randomized study evaluated the effects of these drugs during a 14-day inpatient treatment period for AWS. The results revealed that all of the drugs tested reduced the duration of specific anxiety and depression symptoms associated with AWS, with the extent of the effect varying depending on the drug's formulation. Mexidol significantly reduced "terror," "respiratory," and "cardiovascular" symptoms of anxiety by 25-50%, and improved symptoms of "decreased appetite" and "difficulty concentrating" by 28.5%. Reamberin shortened the length of "gastrointestinal" and "respiratory" anxiety symptoms by 17-50% and "internal tension" by 7%. Emoxipine provided relief from "insomnia" and "respiratory" symptoms, but had no effect on the duration of objective depressive symptoms. Both emoxypine and reamberin reduced the intensity of affective and cognitive symptoms by 32-37%, although they had no effect on self-reported anxiety. These findings suggest a potential role for emoxipine and mexidol in offering targeted relief and support during the difficult process of alcohol withdrawal.

Smoking cessation and nicotine reduction vs. mexidol support

Mexidol (Emoxypine) is also helpful in smoking cessation and nicotine reduction in addicts. A study evaluated the effect of integrating cytisine (a nicotinic acetylcholine receptor agonist), mexidol and behavioral interventions to treat nicotine dependence in patients with tuberculosis (TB) and Chronic Obstructive Pulmonary Disease (COPD) [20]. It included 91 patients, comparing their health status before and after a 3-month regimen. Initially, patients showed low levels of nicotine dependence and motivation to quit smoking. However, the intervention led to significant improvements in health: 16% of the first group quit smoking, and 60% reduced their nicotine intake. Remarkably, improvements in chest X-ray results, sputum conversion rates and pulmonary function tests further indicated better lung health and reduced blood carbon dioxide levels after treatment. The results indicate that mexidol, together with cytisine and behavioral interventions, helps reduce nicotine intake and significantly improves their clinical outcomes and lung function. This suggests that mexidol combined with cytisine and behavioral strategies may be an effective component of a treatment regimen for smoking cessation and reducing nicotine dependence in patients with TB and COPD.

Eloxipine (Mexidol) and ischemia and stroke (brain health)

Mexidol (emoxipine), administered both intravenously and orally, has been shown to be highly effective and safe in the management of chronic cerebral ischemia (CCI) and stroke, which are often caused by high blood pressure and hardening of the arteries. Studies on people with CCI have shown that starting treatment with 500 mg of Mexidol administered intravenously each day for two weeks, followed by taking Mexidol Forte 250 orally at a dose of 250 mg three times a day for two months, leads to significant improvements in CCI symptoms. This treatment significantly improves patients' emotional health, thinking skills and physical coordination [21, 22]. In one study focusing on patients who suffered a carotid ischemic stroke, those who received Mexidol treatment showed significant progress [23]. Patients treated with Mexidol reported higher scores on cognitive tests, improved abilities in motor tasks and spatial awareness, and better memory function. In addition, a significant number of those treated with Mexidol showed levels of cognitive function indicating the absence of moderate cognitive impairment, a decrease in their National Institutes of Health Stroke Scale (NIHSS) scores and a reduced range of disability.

Another study in ischemic stroke (IS) patients showed that Mexidol consistently aided recovery from IS in all age groups, demonstrating that its efficacy is not limited by patient age [24]. Particularly noteworthy was that those aged 76-90 years showed significant improvement in their modified Rankin Scale (mRS) scores compared to the placebo group, showing a significant reduction in disability. This effect was particularly higher in patients aged 60-65, including those with diabetes mellitus (DM), who reported a significant reduction in cognitive-affective depression symptoms along with improvements in daily activities and overall quality of life. These results show that Mexidol is very good at helping people feel better after a stroke, making it easier for them to perform daily tasks, remember things better and move more easily. That's why doctors recommend Mexidol, including its tablet form Mexidol Forte 250, as part of a treatment plan for people who have suffered a stroke or chronic cerebral ischemia, which can lead to strokes. This offers great hope to better help patients recover and improve their quality of life.

Emoxypine (Mexidol) for cardiovascular health

Studies have shown that Emoxypine significantly improves blood flow in the arteries of the heart without affecting overall blood pressure [1]. In addition, studies by Konorev et al. demonstrated Emoxypine's ability to relieve chest pain and promote myocardial healing after myocardial infarction by activating the heart's repair processes [1]. In studies focusing on heart health during severe pancreatitis, Mexidol has been shown to enhance the heart's natural defenses against oxidative stress, reduce fat accumulation in cardiac tissue and prevent heart damage in experiments involving adult hybrid dogs, as noted by Polozova [1]. In addition, a study by Konoplji et al. examined how alcohol consumption after pancreatitis affects red blood cells [1]. They found that treatment with Mexidol helped maintain the stability of these cells and reduced the damage to the heart, underscoring its effectiveness in protecting heart health under difficult conditions.

Dosage of Emoxipine (MexidolTM).

The dose of mexidol/emoxypine is 250 to 1,000 mg per day. However, the dose of emoxipine/mexidol varies depending on medical conditions. Based on various human studies, the following are some of the dosage regimens used for different medical conditions:

- Treatment of carotid artery stroke: Patients received 500 mg of mexidol intravenously once daily for 14 days, followed by oral Mexidol FORTE 250, taking 250 mg tablets three times daily for 60 days.

- Therapy for chronic cerebral ischemia: Patients were treated with 500 mg of Mexidol intravenously once a day for 14 days, and then switched to oral Mexidol FORTE 250 - 250 mg three times a day for 60 days.

- Ischemic stroke (IS) management: Treatment consisted of intravenous administration of 500 mg/day of mexidol for 10 days, followed by oral administration of 125 mg three times a day (375 mg/day) for 8 weeks.

- Intervention in diabetic neuropathy (DN) and diabetic foot syndrome (DFS): Treatment included alpha-lipoic acid (600 mg/day) and mexidol (300 mg/day) for 14 days, showing significant improvement in clinical symptoms.

- Attention deficit disorder with hyperactivity (ADHD) in children: In the study, children aged 6 to 12 were treated with Mexidol film-coated tablets, 125 mg, twice a day, or in combination with placebo, for a total treatment duration of 42 days.

- Panic disorder with insomnia: Patients were given 375 mg of mexidol daily, along with standard antidepressant therapy, for a treatment period of two weeks, resulting in significant improvements in anxiety, autonomic dysfunction and quality of life.

These findings underscore the wide range of applications and efficacy of emoxipine/mexidol in the treatment of a variety of conditions, from cardiovascular and neurological disorders to mental health and chronic illness, indicating the potential of emoxipine/mexidol as a beneficial therapeutic agent in diverse medical fields.

Summary

Emoxipine succinate, marketed as Mexidol or Mexifin, represents a significant advance in pharmaceutical development, offering a wide range of therapeutic effects. Developed by Pharmasoft Pharmaceuticals, its pharmacological properties, including antihypoxic, antioxidant, neuroprotective and cardioprotective properties, make it of growing interest to the global health communities. Despite its initial popularity in Russia, it lacks official approval in the United States and Europe. Particularly noteworthy is its effect in managing anxiety and depression, with studies showing its efficacy in improving the quality of life of patients with various health conditions, including panic disorder, rheumatoid arthritis and cognitive impairment. In addition, its potential to address depression and anxiety in diabetic conditions, combined with its ability to regulate blood sugar levels, underscores a dual-therapeutic approach that could revolutionize treatment strategies for diabetic patients experiencing mood disorders. In addition to mental health, emoxipine and mexidol have shown promise in treating alcohol withdrawal symptoms, offering relief from specific withdrawal-related symptoms of anxiety and depression. In addition, their use in aiding smoking cessation and reducing nicotine intake in patients with TB and COPD exemplifies their diversity and effectiveness in managing addiction-related problems, improving clinical outcomes and lung function. As research continues to expand, the potential for wider adoption and use of Mexidol in international medical practices continues to be explored, underscoring the importance of further clinical trials and regulatory reviews to fully recommend its benefits for global health improvement.

Disclaimer

This article was written for educational purposes and is intended to raise awareness of the substance being discussed. It is important to note that the substance discussed is a substance, not a specific product. The information contained in the text is based on available scientific research and is not intended to serve as medical advice or promote self-medication. The reader should consult any health and treatment decisions with a qualified health professional

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