Emoxypine Mexidol - Educational material

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 properties [1]. Interestingly, scientific studies have also reported beneficial effects of emoxypine in the treatment of neurodegenerative conditions such as Alzheimer's disease, as well as blood disorders such as thalassaemia and haemochromatosis [1].

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

History and key features of the action of emoxipine

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 recognised 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, Igor Anatolievich, worked on emoxypine to improve its delivery to the brain and neural tissues [1]. Because emoxypine is hydrophilic, it had difficulty penetrating the blood-brain barrier effectively. To overcome this problem, they created derivatives with higher lipophilicity. Their aim was to increase the uptake of the drug into the central nervous system and increase its efficacy.

Furthermore, 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 manages metabolic diseases associated with problems in the blood vessel lining, but also helps to maintain an adequate thickness of the lipid bilayer, which is crucial for controlling drug movement and absorption 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 wellbeing, particularly 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]. It is notable that it works by targeting and improving certain brain functions and has the potential to improve attention and stabilise the body's automatic neural responses, contributing to a better sense of wellbeing. 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 behaviour 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 dysfunction and insomnia, improving patients' quality of life. This study highlights the potential of mexidol as an effective addition to antidepressant therapy for patients with panic disorder, particularly those with severe insomnia [6]. Interestingly, the study showed that the antidepressant effects of mexidol and emoxipine may be related to their ability to improve the body's response to insulin [5]. When given in appropriate doses, these drugs improved insulin sensitivity in rats. This improvement was associated with a reduction in the despair-like behaviour 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 on the effect of emoxipine in diabetic symptoms

An animal study investigated 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 clearly reduced anxiety and depression scores in rats with diabetes. This indicates that they are effective in treating similar mood disorders in patients with diabetes. In addition, both drugs significantly reduced high blood sugar levels in rats with diabetes, presenting an additional benefit to individuals [7]. Furthermore, a separate study with 30 diabetic patients treated with mexidol showed improvements in cognitive function, mood (reduction of asthenia and depression), sleep disturbances and normalisation of blood tests. This indicates that mexidol may be an effective adjunctive therapy for the management of 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 rapid solution for the acute management of depressive symptoms. Additionally, 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 reduced blood sugar levels after two weeks. It is notable that mexidol is particularly beneficial for patients with diabetes, combining the ability to alleviate depression with improved blood sugar control, presenting a unique dual therapy approach. This makes mexidol and emoxipine promising for rapidly managing symptoms of depression and improving quality of life in people with diabetes [10]. 

Mexidol and emoxipine have been investigated 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 a significant reduction in neurological symptoms and a reduction in anxiety and depressive disorders, highlighting their effectiveness as an adjunctive treatment 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 disease indicated that the inclusion of 3-oxypyridine derivatives, such as mexidol, in their treatment could 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 wellbeing 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 ischaemia, treatment with mexidol together 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 ischaemia [16]. Another study assessed the effects of emoxipine and mexidol on depressive symptoms in patients with type 2 diabetes, together 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 outcomes 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 ischaemia [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 been shown 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 assess 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, randomised trial evaluated the effects of these drugs during a 14-day inpatient treatment period for AWS. The results revealed that all drugs tested reduced the duration of specific symptoms of anxiety and depression associated with AWS, with the extent of the effect varying according to the drug formulation. Mexidol significantly reduced the 'terror', 'respiratory' and 'cardiovascular' symptoms of anxiety by 25-50% and improved the symptoms of 'decreased appetite' and 'difficulty concentrating' by 28.5%. Reamberin reduced the length of 'gastrointestinal' and 'respiratory' anxiety symptoms by 17-50% and 'internal tension' by 7%. Emoxipine provided relief of '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 results 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 versus 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 behavioural interventions for the treatment of 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 concentrations after treatment. The results indicate that mexidol, together with cytisine and behavioural interventions, helps to reduce nicotine intake and significantly improves their clinical outcomes and lung function. This suggests that mexidol in combination with cytisine and behavioural strategies may be an effective component of a treatment regimen for smoking cessation and reduction of nicotine dependence in patients with TB and COPD.

Emoxypine (Mexidol) and ischaemia and stroke (brain health)

Mexidol (emoxypine), administered both intravenously and orally, has been shown to be highly effective and safe in the management of chronic cerebral ischaemia (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 a fortnight, 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 had suffered a carotid artery ischaemic 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 ischaemic stroke (IS) patients showed that Mexidol consistently supported 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 a 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 years, 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. This is 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 ischaemia, 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]. Additionally, studies by Konorev et al. have demonstrated the ability of Emoxypine to alleviate chest pain and promote myocardial healing after myocardial infarction by activating cardiac repair processes [1]. In studies focusing on heart health during severe pancreatitis, Mexidol has been shown to enhance the heart's natural defences against oxidative stress, reduce fat accumulation in cardiac tissue and prevent cardiac damage in experiments involving adult hybrid dogs, as noted by Polozova [1]. In addition, a study by Konoplji et al. investigated how alcohol consumption after pancreatitis affects red blood cells [1]. They found that treatment with Mexidol helped to maintain the stability of these cells and reduced damage to the heart, highlighting its effectiveness in protecting heart health under difficult conditions.

Dosage of Emoxipine (MexidolTM)

The dose of mexidol/emoxipine ranges from 250 to 1000 mg daily. However, the dose of emoxipine/mexidol varies according to medical conditions. Based on various human studies, some of the dosage regimens used for different medical conditions are outlined below:

- 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 ischaemia: Patients were treated with 500 mg of Mexidol intravenously once daily for 14 days and then switched to oral Mexidol FORTE 250 - 250 mg three times daily for 60 days.

- Ischaemic stroke (IS) management: Treatment consisted of intravenous 500 mg/day of mexidol for 10 days, followed by oral 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 years were treated with Mexidol film-coated tablets, 125 mg, twice daily, 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 results highlight the wide range of uses 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

Emoxyipine 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 US and Europe. Particularly noteworthy is its action in the management of anxiety and depression, with studies demonstrating its efficacy in improving the quality of life of patients with a variety of 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, highlights a dual-therapeutic approach that could revolutionise 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 symptoms of anxiety and depression associated with withdrawal. 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 develop, the potential for wider adoption and use of Mexidol in international medical practices continues to be explored, highlighting the importance of further clinical trials and regulatory reviews to fully recommend its benefits for global health improvement.

Disclaimer

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

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