Thioctic acid: antioxidant therapy for neurological diseases. Thioctic acid: antioxidant therapy for neurological diseases Dietary supplements with lipoic acid
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Alpha lipoic acid is one of the most powerful antioxidants that few people have heard of. It is also called a superantioxidant, the closest to ideal. It serves as an antioxidant for other antioxidants
Alpha-lipoic acid, also known as thioctic or vitamin N, belongs to a group of conditional vitamins that can resist active oxygen ions that destroy cell membranes. Also, this substance enhances the action of insulin.
Alpha Lipoic Acid helps fight premature wrinkles, glaucoma, diabetic neuropathy, and radiation sickness. It is also recommended to take its preparations for poisoning with poisonous mushrooms or alcohol, restoration of liver cells after hepatitis, for weight loss, for HIV infection and cardiovascular diseases.
Due to the small size of the molecules, it easily overcomes the barrier between the blood and brain tissues, entering directly into the brain cells. It is the only antioxidant capable of reaching the brain directly;
Due to its special chemical structure, it can dissolve both in water and in fat, and, accordingly, it works equally effectively in both the water and fatty parts of the brain;
This is the only antioxidant capable of regenerating not only itself, but also several other important antioxidants - vitamins C and E, coenzyme Q10 and glutathione, restoring their antioxidant potential;
It is able to neutralize the most dangerous nitrogen radicals for brain cells, including nitric oxide. Previously, the focus was on the fight against oxygen radicals, but recent research has revealed the presence of another type of free radicals - nitrogen, which pose the most serious threat to brain cells;
Increases the efficiency of mitochondria - energy factories of cells. With age, the efficiency of mitochondria decreases, glucose and oxygen are consumed worse, and more free radicals are released. Laboratory studies at the University of California showed that alpha-lipoic acid reduced the rate of decline in mitochondrial energy production in old rats by more than 50%, and their activity increased to the level of young ones;
It regulates insulin and blood sugar levels and reduces the production of sugar-damaged proteins (glycation end products) that accelerate aging and are found in large numbers in the blood of diabetics.
Alpha-lipoic acid can protect you from a stroke, and if it does occur, it will limit its consequences and significantly speed up recovery.
Laboratory studies have shown that animals treated with alpha-lipoic acid recovered faster from a stroke. Scientists artificially caused a stroke in rats by squeezing the carotid artery and blocking the access of blood and oxygen to the brain.
The main danger of a stroke is that after the restoration of blood flow, along with the blood, a flow of oxygen falls on the brain (reperfusion). It causes the formation of a large number of free radicals and the usual antioxidant defense can not cope with them. As a result, brain cells die, which can lead to temporary or even permanent disability, and in some cases, death.
In the experiments of scientists, up to 80% of rats died in the first day after the restoration of oxygen supply to the brain.
When alpha-lipoic acid was administered to the rats before restoring the normal flow of blood and oxygen to the brain, the mortality of animals was reduced to 25%, and all surviving individuals recovered without obvious visible consequences.
Further research has shown that alpha-lipoic acid is able to prevent free radicals from destroying vulnerable areas of the brain. Autopsies of rats not treated with alpha-lipoic acid showed brain damage from free radicals. The same rats that received the acid showed no such damage.
But that's not all that alpha-lipoic acid is capable of. It prevents age-related memory impairment. Researchers at the Clinical Institute for Psychiatry Mannheim added alpha-lipoic acid to the water of old but healthy mice. Just like humans, the memory of animals weakens with age. A few weeks after the start of administration, the mice were run into a maze. And the mice, in whose drinking water added alpha-lipoic acid, coped with the task much better. This suggests that due to its antioxidant activity, alpha-lipoic acid slows down the aging process of the brain.
It is worth noting, however, that alpha-lipoic acid does not affect the growth of new nerve cells and nerve connections. It is believed that the aggravation of memory as a result of taking alpha-lipoic acid occurs due to the renewal of receptors in the shells of nerve cells that regulate signal transmission in the brain.
But memory enhancement with alpha-lipoic acid has not been observed in young animals, since it only repairs and revitalizes neuronal circuits, and does not give any super powers.
Currently, alpha lipoic acid is the most powerful antioxidant known to man.
It is found in the greatest quantities in tomatoes, spinach, and broccoli.
daily requirement of the body
Since the synthesis of alpha-lipoic acid by the intestinal microflora is not always carried out in sufficient quantities, it must be additionally obtained from food. The need for thioctic acid per day may increase:
in violation of liver function up to 75 mg;
during pregnancy up to 70 mg;
in diabetes - from 200 mg to 600 mg.
For children under 12 years old, 1-10 mg of a substance is enough per day, for adolescents - up to 20 mg, and for adults - from 10 to 50 mg, depending on body weight, the level of physical, mental and psychological stress.The quality of alpha lipoic acid is determined by several factors:
The following is a table of foods that contain the highest amount of alpha lipoic acid.
NAME OF PRODUCTS CONTENT OF THIOCTIC K-TY, MG/KG
Meat beef 1233
Beef liver 629
Lungs, heart, beef kidneys 660
Pork 450
Oats 523
Buckwheat 347
Rice 333
Spinach 49
Walnut 346
Legumes 407
Cashew 593
Medicines
Alpha-lipoic acid preparations are available in the form of tablets and capsules, the dosage of the active substance in which is 100 mg, 200 mg or 600 mg.
Common drugs of alpha-lipoic acid, which are sold in pharmacies:
Berlition;
Lipamide;
Lipothioxone;
Neurolipon;
Octolipen;
Thiogamma;
Thioctacid;
Thiolepta
Known by various names - lipoic acid, lipoate, alpha-lipoic acid or thioctic acid - the substance is involved as a coenzyme (auxiliary compound) in many reactions in our body, one of which is called glycolysis, or the conversion of sugars into energy. Lipoic acid enhances this process by supporting the activity of mitochondria - small structures located inside each muscle cell and acting as an energy station.
Lipoic acid does not belong to the category of “essential” substances, it is produced by our body. However, studies have shown that the addition of lipoic acid to the diet of individuals who do not require insulin therapy significantly enhances the body's ability to utilize sugar from the blood. Since most of the sugar is consumed by the muscles, it seems that lipoic acid helps the muscles take sugar out of the bloodstream and increases the process of glycogen synthesis.
The human body itself produces lipoic acid, but less and less with age. Foods rich in lipoic acid and nutritional supplements can correct the situation. From meat and vegetables it will definitely not be worse. As for lipoic acid in powders and tablets, scientists still have not agreed on what dose can be considered safe and effective. It is only known that 300-600 mg of lipoic acid per day will not cause side effects. However, higher doses can harm cells. No scientific studies have been conducted to support or refute the claim that lipoic acid supplements prevent or stop cancer.
In Germany, this drug has long been used as a remedy for diabetics. A group of doctors from Munich, led by Dr. Hans Tritschler, made a presentation at an international conference on diabetes, in which, in particular, it was noted that lipoic acid not only increases the susceptibility of muscle cells to glucose, but also simultaneously reduces the consumption of glucose by adipose tissues. The result of this action of the drug is increased energy production in the muscles and a decrease in fat deposition in the body.
Lipoic acid is also considered a powerful antioxidant. Research results show that lipoic acid helps protect red blood cells and fatty acids from both oxidative damage (seen with intense exercise) and the damaging effects of ultraviolet light.
Targeted studies have not yet been carried out on physically healthy people involved in sports. However, it is well known that a large (and growing) number of Americans suffer from insulin resistance, especially those with significant body fat and those whose diets are high in saturated fat (that is, more than half of the nation's population). If you are an insulin sensitive person and want to build muscle as well as lose body fat, then taking lipoic acid will help increase your stamina and give you bigger, leaner muscles.
Today, one of the most difficult issues in medicine is the effective treatment of viral hepatitis. First of all, this applies to the most severe chronic viral and, the outcome of which is very often. The incidence of hepatitis is constantly growing, mainly young, able-bodied people get sick. Given the biological properties of a-lipoic acid, it has become widely used in the treatment of chronic forms of hepatitis B and C, along with traditional therapy.
It was shown that after 4 weeks of taking the drug a-lipoic acid in these patients, the functional parameters of the liver are significantly improved. The most favorable results in the form of improvement in functional parameters were noted in patients with latent hepatitis and alcoholic fatty degeneration of the liver. A very important clinical effect was the inhibition of the development of fibrosis and a decrease in the risk of malignant transformation of liver cells due to the antioxidant ability of a-lipoic acid. In patients with non-alcoholic steatohepatitis, which often proceeds aggressively with the transition to cirrhosis and liver failure, a-lipoic acid also has a positive effect. It has been shown that the inclusion of a-lipoic acid in complex therapy normalizes lipid metabolism in liver cells and reduces inflammation in the liver.
Lipoic acid is essential for:
- chronic fatigue syndrome
- pathology of the cardiovascular system
- Alzheimer's disease
- diabetes
- alcoholism;
By nature, lipoic acid is considered an antioxidant. It creates additional protection for vitamin C and E, which have similar properties. In parallel, it removes all heavy metals from the human body and breaks down toxins. This substance was first discovered in 1948.
Almost immediately, it began to be produced in the laboratory, where it was also found that it can reduce blood sugar levels and have a beneficial effect on liver health. Because of this, this ingredient began to be included in dietary supplements and nutrition for athletes.
Health impact
Athletes who suffer from liver dysfunction due to the frequent use of synthetic supplements are forced to constantly fight free radicals. These substances trigger oxidative processes that negatively affect the condition of the skin and muscles. To neutralize them, you need to use lipoic acid. It helps break down all these substances and helps to restore the overall integrity of the liver.
Also, this acid plays the role of a coenzyme for a number of enzymes that regulate the metabolism of fats and carbohydrates. If its amount in the body fluctuates within the normal range, then the liver remains reliably protected from fatty degeneration. This property of the acid is often used in fat burners, as it allows you to further protect the liver from destruction.
This substance can reduce consumption of glutathione in the human body. This hepatic antioxidant is quickly destroyed in the human body during severe physical exertion, so it needs to be quickly restored. Lipoic acid protects it from destruction, so the liver remains healthy for a long time.
Indications for use
Alpha lipoic acid should be used in bodybuilding. The fact is that intense training can stimulate the formation of free radicals, which will increase the stress of muscle tissue. The intake of this substance helps to reduce the amount of these harmful compounds in the muscles, which additionally protects them from damage, and also allows you to recover faster after exercise.
This substance has good insulin-like properties. Because of this, it can be used by people who have problems with the secretion of this hormone. Insulin helps stimulate the process of storing glycogen, which is used as "fuel" in training. Gradually, more glucose from food begins to accumulate in muscle tissue. It will also be used as an important energy source.
In some cases, alpha-lipic acid is prescribed as a prophylactic. First of all, this applies to people who constantly take synthetic sports supplements, or are at risk for cirrhosis and hepatitis.
It is also used against diabetic neuropathy:
Instructions for use and dosage
The daily allowance of alpha-lipoic acid for a healthy athlete varies 10 to 50 mg. People with liver problems should take 75 mg of alpha-lipoic acid per day, and for diabetics this dose increases to 200-600 mg.
What foods or preparations contain
Acid is found in many foods familiar to athletes: by-products, beef, beef liver, milk, rice, spinach and cabbage. A lower concentration of acid can be found in broccoli, potatoes, carrots, beets and yeast.
The body of an athlete is able to independently produce a certain amount of this acid, but with liver diseases, an acute deficiency of this substance begins to be observed, so you have to get it from medicines.
This acid can be obtained from Opti-Men and Opti-Women from Optimum Nutrition, Cell-Tech and Aplodan from MuscleTech and Cheaters Relief from BSN.
Contraindications
Alpha lipoic acid is contraindicated in pregnant and lactating women. It should not be used by people taking iron, magnesium, calcium, or cisplatin supplements. Also, do not combine the intake of supplements with this substance with the constant use of alcoholic beverages.
Consequences
Lipoic acid is considered a strong antioxidant, therefore, when it enters the human body normally, it immediately begins to cleanse it of all toxic substances. First of all, it has a beneficial effect on the functioning of the liver. This organ receives additional protection from fatty destruction, cirrhosis and hepatitis. In addition, the athlete accelerates carbohydrate, lipid and protein metabolism, which makes it possible to quickly bring his body into the desired physical shape.
Lipoic acid has no side effects. Only in some cases, minor allergic reactions are possible. Some athletes notice indigestion, nausea and vomiting, which are aggravated by an overdose of this substance. The maximum allowable dose is 1800 mg of acid per day. If this threshold is systematically exceeded, typical symptoms of toxicosis. Therefore, do not forget about how to take alpha lipoic acid.
Conclusion
Alpha Lipoic Acid is a powerful antioxidant that can protect the liver from damage caused by frequent exercise. This substance takes part in almost all biochemical reactions that occur in the human body, therefore, when it enters, muscle mass gain improves and accelerated burning of subcutaneous fat is provoked. Companies such as Optimum Nutrition, MuscleTech and BSN now use this acid as a main ingredient.
For citation: Shavlovskaya O.A. Thioctic acid: antioxidant therapy for neurological diseases // BC. 2014. No. 13. S. 960
Thioctic (alpha-lipoic) acid is synthesized in the body and acts as a coenzyme in the oxidative decarboxylation of alpha-keto acids. It is an ethylenediamine salt of alpha-lipoic acid, which, being a prosthetic group of multienzyme complexes, plays an important role in cell metabolism. Thioctic (alpha-lipoic) acid is an endogenous antioxidant (binds free radicals), it is formed in the body during oxidative decarboxylation of alpha-keto acids. It is this fact that, first of all, is due to the growing interest of clinicians in thioctic acid, which opens up new possibilities for the use of thioctic acid in the treatment of diseases and pathological conditions, which are based on an imbalance of oxidative-antioxidant homeostasis. The property of normalizing the cellular metabolism of utioctic acid is realized as a result of the direct inactivation of free radicals due to their binding by the SH-groups of the drug. Uthioctic acid also has properties that potentiate the anti-inflammatory effect of glucocorticosteroids, and an immunostimulating effect. In addition, thioctic acid is similar in pharmacological properties to vitamines of the Vio group, it has the ability to reduce blood sugar levels and increase liver glycogen content.
The use of thioctic acid in medical practice is largely associated with the development of ideas about "oxidative stress" and lipid peroxidation as a fairly universal pathogenetic mechanism of cell and tissue damage. The antioxidant effect of thioctic acid is due to the presence of two thiol groups in the molecule (hence the prefix "thio"), as well as the ability to bind free radicals and free tissue iron (preventing its participation in lipid peroxidation). Thioctic acid not only has an independent antioxidant potential, but also provides powerful support for the work of other antioxidant links in the body. In this regard, its protective action is closely related to homeostasis in the system of glutathione and ubiquinone. The production of reactive oxygen species increases significantly with inflammation, immunological disorders, hypoxia, hyperoxia, exposure to drugs, radiation, and antioxidant deficiency.
Thioctic acid is one of the strongest antioxidants used in the treatment of diabetic neuropathy. Thioctic acid is a coenzyme of key enzymes of the Krebs cycle, which explains its effectiveness. An additional advantage in the mechanism of action of thioctic acid is its well-documented effect of glucose utilization. High efficiency and pathogenetic action of thioctic acid have been proven by numerous experimental and clinical studies. The adequate and rational use of thioctic acid preparations is based on the results of numerous studies (ALADIN I, ALADIN II, ALADIN III, ORPIL, NATHAN, DECAN, SYDNEY), in which the dose, frequency of administration and duration of the course were worked out (Table 1).
As part of a multicenter randomized double-blind study (SYDNEY II), the effectiveness of thioctic acid in the treatment of patients with diabetic polyneuropathy (DPN) was evaluated. The study was conducted in the period from 2004 to 2006, it involved 87 patients with diabetes mellitus (DM) of the 1st and 2nd types, who were on inpatient (Nuzik Central Clinical Hospital No. 1 of Russian Railways) and outpatient treatment (Department Endocrinology GOU DPO RMAPO Roszdrav). The SYDNEY study concluded that intravenous administration of alpha-lipoic acid for 3 weeks. causes a significant weakening of painful neuropathic symptoms for patients and objective neurological symptoms. Given the dose-dependent effect of the development of side effects, the optimal dosage is 600 mg of thioctic acid. The authors concluded that as a result of a comprehensive clinical and neurophysiological study of patients with type 1 and type 2 diabetes, it was noted that the earliest EMG indicator of sensory nerve damage in diabetes is a decrease in the action potential. Pain reduction occurred from the 2nd week. taking thioctic acid at a dose of 1800 mg / day, from the 4th week. reception - at a dose of 1200 mg and only by the 5th week. - while taking 600 mg of thioctic acid. In patients with DPN (n=24) participating in the study, when using thioctic acid at a dose of 1800 mg / day for 3 weeks. decreased neuropathic symptoms and neurological deficit, in terms of the incidence of side effects, these are comparable to the placebo group.
In medical practice, for therapeutic purposes, a number of preparations of thioctic acid are used, which are represented by its three main salts: ethylenediamine, trometamol and megluminic. One of the drugs, the active substance of which is thioctic (alpha-lipoic) acid, is Thiogamma® (pharmaceutical company "Verwag Pharma" (Germany)). Thiogamma® is a meglumine salt of alpha-lipoic acid, polyethylene glycol is used as a solubilizer, their advantages are to suppress the formation of free radicals, improve the energy metabolism of neurons, and restore impaired endoneural blood flow. The drug is available in the form of tablets containing 600 mg of the drug, a solution for intravenous infusion in vials containing 600 mg of the drug in the form of meglumine salt, and ampoules. Meglumine (N-methyl-D-glucamine) is known to be used as a stabilizer in many pharmaceutical products. Meglumine is also used to reduce the toxicity of gadolinium in magnetic resonance contrast media. It is used as meglumine antimonate for the treatment of leishmaniasis. It has been demonstrated that in the experiment, mice took doses up to 1 g/kg intraperitoneally without side effects. There is only one report of the development of an anaphylactic reaction in a patient with osteoid osteoma after the use of gadoteric and gadopentetic acid during an MRI study. Descriptions of other negative effects of meglumine could not be found. Thus, it can be concluded that of all the stabilizers used for the manufacture of dosage forms of thioctic acid, meglumine is the least toxic.
Instructions for use of the drug Thiogamma® was approved on 04/15/1999 by the Pharmacological State Committee of the Ministry of Health of Russia, re-registration on 05/24/2010 (for tablet forms), 02/29/2012 (for injection forms). The drug is prescribed 1 r./day 300-600 mg, take it without chewing, drinking a small amount of liquid. According to the ALADIN I study, the effect of alpha-lipoic acid on positive neuropathic symptoms at doses of 600 and 1200 mg is almost the same. In a clinical study with 3-week intravenous administration of alpha-lipoic acid, side effects (headache, nausea, vomiting) developed more often at a dosage of 1200 mg (32.6%) than 600 mg (19.8%) with placebo (20.7%) . It was concluded that the dosage of alpha-lipoic acid at 600 mg, both in terms of clinical efficacy and the possibility of side effects, is optimal.
The clinical use of thioctic (alpha-lipoic) acid (in particular Thiogamma®) is based on the many biochemical and physiological effects of this substance. The main mechanisms of action of Thiogamma®, according to the Methodological recommendations of V. V. Gorodetsky (2004), can be presented as follows:
- influence on energy metabolism, glucose and lipid metabolism (participation in oxidative decarboxylation of keto acids) with activation of the Krebs cycle; increased uptake and utilization of glucose by the cell and oxygen consumption; increase in basal metabolism; normalization of gluconeogenesis and ketogenesis; inhibition of cholesterol formation;
- cytoprotective action: increased antioxidant activity (direct and indirect through the system of vitamins C/E, cystine/cysteine and glutathione); stabilization of mitochondrial membranes;
- influence on the reactivity of the body: stimulation of the reticuloendothelial system; immunotropic action; anti-inflammatory and analgesic activity (associated with antioxidant action);
- neurotropic effects: stimulation of axon growth, a positive effect on axonal transport, a decrease in the harmful effects of free radicals on nerve cells, normalization of abnormal glucose supply to the nerve, prevention and reduction of nerve damage in experimental diabetes;
- hepatoprotective action: accumulation of glycogen in the liver, inhibition of lipid accumulation in the liver (under certain pathological conditions), increased activity of a number of enzymes, improvement of the functional activity of the liver;
- detoxification effect (FOS, lead, arsenic, mercury, sublimate, cyanides, phenothiazides, etc.).
The main indications for the use of Thiogamma® in the treatment of diseases accompanied by neurological symptoms are focused on diabetic and alcoholic polyneuropathy. Currently, thioctic (alpha-lipoic) acid, in particular Thiogamma®, is the most effective agent in the treatment of peripheral polyneuropathy, which has been confirmed by large-scale multi-center long-term studies, such as the ALADIN Study (Alpha-Lipoic Acid in Diabetic Neuropathy) . However, the antioxidant activity of thioctic acid is used in many areas of medicine (Table 2).
Thioctic (alpha-lipoic) acid is a powerful lipophilic antioxidant and is rightfully considered the "gold standard" of the pathogenetic treatment of diabetic polyneuropathy (DPN). A number of studies have shown that the use of alpha-lipoic acid at a dose of 600 mg / day intravenously or orally for 3 weeks. up to 6 months reduces to a clinically significant extent the main symptoms of DPN, including pain, paresthesia and numbness. Oxidative stress is known to cause a 50–70% decrease in the rate of insulin-dependent transmembrane glucose transport in DM. The basis for the treatment of DPN with thioctic (alpha-lipoic) acid preparations is the fact that in diabetes there is a deficiency of alpha-lipoic acid, and alpha-lipoic acid (which has a powerful antioxidant effect), in turn, increases the bioavailability of glucose in insulin-dependent and insulin-independent tissues , increases the absorption of glucose by peripheral nerves to a normal level, and also contributes to an increase in endoneural glucose reserves, which favorably affects the restoration of the energy metabolism of the nerves. It is believed that the appointment of thioctic acid is appropriate for insulin-resistant forms of diabetes. In this case, the appointment of an intravenous drip of a solution of alpha-lipoic acid for 3 weeks is considered optimal in this case. (15 droppers) followed by taking 600 mg of the drug in the form of tablets (1 p./day 30-40 minutes before meals) for 1-2 months. .
The effectiveness of Thiogamma® in DPN has been convincingly demonstrated in many clinical studies. At Sofia Medical University (Bulgaria) T. Tankova et al. (2000) conducted a randomized open placebo-controlled study to evaluate the effectiveness of the drug Thiogamma® according to a 2-stage regimen: after a period of intravenous infusion, the drug was administered orally. A constant dose of 600 mg/day was used, intravenous administration was carried out for 10 days, oral administration for another 50 days. A pronounced clinical effect appears after the first 10 days of therapy. When compared with the control group in patients treated with Thiogamma®, the intensity of spontaneous pain sensations in the legs decreased by 40%, the vibration sensitivity significantly reduced before treatment, which was determined in various areas of the foot, increased by 35%. By the end of the course of therapy, there was a positive trend in reducing the severity of pain according to VAS, increasing vibration sensitivity. Also, a positive dynamics of indicators characterizing the severity of damage to the autonomic nervous system was obtained: over 60 days of therapy, the manifestations of autonomic neuropathy decreased by 40% and the drop in systolic blood pressure decreased by 2.5 times during the orthostatic test, which indicates an improvement in the function of the autonomic nervous system.
As part of another single-center, randomized, double-blind, placebo-controlled study, 120 patients with type 1 and type 2 diabetes were examined, of which 60 people received placebo and 60 received alpha-lipoic acid (at a dose of 600 mg in 225 ml of saline at intravenous time). drip injection 30–40 min). The effect of this drug on the clinical manifestations of DPN, electromyographic (EMG) indicators, indicators of quantitative sensory and autonomous testing in 60 patients with type 1 and type 2 diabetes was studied. The duration of the study was 4 weeks. Positive neuropathic symptoms were chosen as the main criterion for the clinical efficacy of the study drug due to the fact that they primarily impair the patient's quality of life. The improvement in the distal latency index in the EMG study indicates that the main unpleasant sensations (pain, burning, numbness, paresthesias), which worsen the quality of life of the patient, decreased during therapy with alpha-lipic acid, due to the improvement in the function of peripheral nerves. Thus, the high efficacy of the drug in relation to most of the studied indicators of the state of peripheral nerves was shown. It was concluded that thiocotic (alpha-lipoic) acid preparations can be successfully used in the treatment of symptomatic DPN.
In the study by I. I. Matveeva et al. 126 patients with newly diagnosed type 2 diabetes (screening) were examined, who were prescribed thioctic acid for 10 days intravenously at 600 mg, followed by 600 mg tablets daily in within 8–10 weeks. Based on the results of the study, it was concluded that thioctic acid is highly effective in the treatment of distal DPN, improves clinical symptoms, the state of peripheral nerves, reduces oxidative stress, and insulin resistance.
In another study, 50 patients with diabetic and hypothyroid distal symmetric sensorimotor polyneuropathy were prescribed Thiogamma® initially at a dose of 600 mg (equivalent to 1167.70 meglumine salt of alpha-lipoic acid) intravenously, drip for 10 days, 1 injection per day, the rate of administration was not more than 50 mg/min. It is also important to note that a distinctive feature of the drug Thiogamma® is the release form, which allows you to administer the drug intravenously, drip, without requiring preliminary dilution. Then, for 30 days, patients took Thiogamma® 600 mg in the morning and on an empty stomach. In the course of the study, the author came to the conclusion that among all forms of DPN, the greatest effect of the use of Thiogamma® was noted in the treatment of acute sensory polyneuropathy and radiculoplexopathy; in the treatment of progressive sensorimotor polyneuropathy, the use of Thiogamma® also showed a statistically significant therapeutic result. With regard to hypothyroid polyneuropathy, Thiogamma® showed high efficiency, in particular, to reduce and eliminate pain, however, the positive dynamics in the treatment of Thiogamma® clearly correlated with adequate replacement therapy with thyroid hormones.
In a study by E. Yu. Komelagina et al. (2006) presents the results of comparing the effectiveness of two options for treating DPN with thioctic acid preparations: option 1 - oral administration of 1800 mg / day (600 mg 3 times / day) for 4 weeks. (n=15) and the 2nd option - oral administration of 600 mg/day for 3 months. (n=15). The study showed that in both modes of application, the thioctic acid preparation provides a significant reduction in the severity of neuropathic complaints in patients with diabetes with a satisfactory level of carbohydrate metabolism compensation. Based on the results of the study, the authors came to the conclusion: “... the choice of a regimen for DPN therapy using thioctic acid preparations is individual and depends on the specific situation: with severe pain symptoms, a shorter course with a high dosage of the drug (1800 mg / day for 4 weeks) ), with unexpressed symptoms - a longer course with a lower daily dosage (600 mg / day for 3 months) ... ".
The range of use of drugs containing thioctic acid, both as monotherapy and as part of complex therapy, is constantly expanding. In a comparative open randomized study conducted at the Department of Occupational Diseases of the St. Petersburg State Medical Academy. I. I. Mechnikov, the effectiveness of the drug, the active substance of which is thioctic acid, in the complex therapy of manifestations of vibration disease (syndrome of autonomic-sensory polyneuropathy of the extremities, angiodystonic syndrome) was evaluated. The use at a dosage of 600 mg daily as part of complex therapy for 21 days significantly reduces the frequency of subjective complaints of patients, leads to a steady decrease in the recurrence of pain in the extremities, a decrease in the frequency of angiospasm attacks, enhancing the effect of therapy as a whole. Thus, the effectiveness of this drug in relation to vascular tone, blood filling and venous outflow was shown, which, according to the authors, causes the development of anti-inflammatory, anti-edematous, analgesic effects and contributes to the normalization of homeostasis.
Studies by M. Senoglu et al. (2009) showed the effectiveness of alpha-lipoic acid in relation to clinical symptoms such as pain, paresthesia, hypoesthesia in patients with compression radiculopathy due to discorradicular conflict. The results of this study correlate with the study in which M. Ranieri et al. (2009) evaluated the effectiveness of the additional use of a combination of alpha-lipoic and gamma-linolenic acid in a 6-week rehabilitation program for patients with discogenic radiculopathy compared with a similar group of patients who received only a rehabilitation program. A case of the effective use of the drug thioctic acid (600 mg/day for 1 month) as part of complex therapy in a patient with stage III Lyme disease (neuroborreliosis, CNS changes, cranial insufficiency, peripheral polyneuropathy by neuroborreliosis) is described.
Employees of the clinic of neurology and neurosurgery of the medical faculty of the Russian State Medical University (now RNIMU) E. I. Chukanova et al. (2001-2014) conducted a number of studies to evaluate the effectiveness of the use of thioctic acid in the treatment of patients with dyscirculatory encephalopathy (DE) and when prescribed in the complex pathogenetic therapy of vascular cognitive impairment. On the example of a study of 49 patients with DE, it was shown that when prescribing a thioctic acid preparation in a dosing regimen of 600 mg 2 times a day for 7 days, switching to 600 mg 1 time a day for 53 days orally 30 minutes before meals allows to achieve a positive effect by the 7th day of treatment (at a dose of 1200 mg / day), with a dose reduction to 600 mg / day (from the 8th day of treatment), the positive effect of the drug on the dynamics of the neurological status remains and is most pronounced by the 60th day Positive dynamics in the neurological and neuropsychological status of patients with DE was noted. Based on the results of the study, it was concluded that thioctic acid is effective not only in the treatment of patients with DE with elevated glucose levels, but also in patients with cerebrovascular insufficiency without DM. In the study of a group of 128 patients with DE, a pharmacoeconomic analysis of the effectiveness of treatment with thioctic acid in patients with different stages of chronic cerebral vascular insufficiency was carried out. The preparation of thioctic acid was administered orally at a daily dose of 600 mg 2 times a day for 7 days with a transition to 600 mg 1 time a day for 23 days 30 minutes before meals. The study found: in patients with DE I st. - regression of asthenic syndrome, vestibular ataxia, axial reflexes; in patients with DE II Art. - increasing the effectiveness of influencing the indicators of the "movement" scale, ataxia, pseudobulbar syndrome; in patients with DE III Art. - a positive effect on the indicators of the "movement" scale, ataxia (frontal and cerebellar), pseudobulbar syndrome, which persisted until the 12th month. observations, as well as showing a statistically significant effect on the dynamics of the score of the amyostatic syndrome. The authors of the study concluded that treatment with thioctic acid in patients with DE leads to significant clinical improvement, reduces the risk of stroke during the course of the disease, and reduces the percentage of disease progression in patients with DE I and II stage. A small percentage of side effects were noted. Thioctic acid is well tolerated by patients, including patients of older age groups. Therapy with thioctic acid is preferable from an economic point of view compared to the cost of treating patients in the control group who received antihypertensive and antithrombotic therapy, which is associated with its high effectiveness in influencing the risk of TIA, stroke, and the progression of DE.
Conclusion
The data available today allow us to recommend the prescription of Thiogamma® by a doctor in the treatment of patients with neuropathy of somatogenic origin. With a high degree of efficiency, the developed scheme for the 2-stage administration of the drug Thiogamma® is successfully used: intravenous infusions of the finished solution of the drug Thiogamma® for 10 days (in vials of 50 mg solution for infusion 12 mg / ml, which is equivalent to 600 mg of thioctic acid, at the time of intravenous drip injection 30-40 min) followed by the appointment of the tablet form of the drug (600 mg / day) for 50 days. From the point of view of clinical efficacy and taking into account the possibility of developing side effects, the dosage of thioctic (alpha-lipoic) acid at 600 mg / day is optimal. Individual approach to the dosing regimen: with severe pain symptoms - a shorter course with a high dosage of the drug (1800 mg / day for 4 weeks), with less severe symptoms - a longer course with a lower daily dosage (600 mg / day for 3 months).
It is important to note that a distinctive feature of the drug Thiogamma® is the release form, which allows you to administer the drug intravenously, drip, without requiring preliminary dilution.
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We live on the brink of systemic death.
Life-affirming beginning of the article, right? And the essence is simple: any living organism lives as long as the processes of organization in it balance the processes of destruction. When the balance is disturbed, a slow death begins. In fact, the whole balance is kept on the balance of redox reactions, or redox balance. And this is why this balance is so fragile: oxidative reactions are easier, because they go with the release of energy, and reduction reactions, on the contrary, require energy. No wonder - break not build.
Naturopaths say: in order to defeat the disease, you should first of all increase the energy of the body. Official medicine, on the contrary, first inhibits the body's defenses with drugs and brings it to the brink of exhaustion, and then begins the process of rehabilitation. Allopathy is called, otherwise - symptomatic treatment, when the principles of emergency care are transferred to therapy.
It’s easy to increase the energy of a car: fill in the right gasoline and drive. A person also has something like a carburetor, so it seems to be easy to push our restorative reactions. But there is one catch - often the problem lies precisely in the fact that it would be necessary to calm down the oxidation processes, which literally break the chain.
And this is really a problem, since we live in an era of "oxidative stress", for which our body was not originally designed. And now, instead of normal calm burning, a fire begins in each cell, or, as firefighters put it, "uncontrolled burning." And putting out a fire means not dispersing the smoke, but flooding the hearth itself.
I started such a long introduction only to remind you that most of the diseases according to the modern classification are classified as "free radicals", that is, medicine has recognized that free radicals play the main role in fanning the fire - the same ones that remove oxidative reactions out of our control.
His antioxidant protection it just can’t cope on its own - try putting a miserable bucket of water on the fire!
In our body, many types of antioxidant substances are produced, and for certain types of free radicals, and universal, and even simply unique. That is, the quality and range of products are present, there is not enough shaft. And the whole plan goes from there to hell.
A fire is easy to extinguish before it has gained strength, which is why we focus on prevention. If the body lacks antioxidants, give it an extra amount with food! Why are fruits and vegetables so healthy? Because plants are antioxidant factories, they need them themselves. Without antioxidants, an hour after sunrise, all our vegetation would be ashes - such a huge amount of solar energy is absorbed during photosynthesis.
And if you and I consumed a sufficient amount of plant food every day, and even fresh, not industrially processed, and not grown in agricultural complexes, where plants do not see white light from pesticides and fertilizers, then everything would be "ganz" . Or "all right" if in English. In short, they would live in the village and eat from their garden. However, civilization has already taken out the village, and without urban "pickles" it is rare that a farmer sits down at the table.
It is no coincidence that the dietary supplement industry has swung so much in recent decades, because more and more people realize that it is impossible to survive in the modern world only on pasture. I say "survive" because by life I mean not just existence, but the full functioning of an individual who does not know what it is to sit in lines in clinics.
Antioxidants
is a whole trend in the modern dietary supplement industry ( , ,
, etc.), and this is also not accidental, because protection from oxidative stress is the head of everything. And you will not find a single jar of multivitamins (except junk like multitabs) that does not include at least one antioxidant complex. And not just for your protection, by no means. And also to protect the vitamins themselves, so that their radicals do not shake before they have time to get down to business.
And in the best multivitamins there are not only two or three antioxidant complexes, but also some of the strongest players, such as resveratrol, astaxanthin, rutin, quercetin and their associates (BAA). But in general, the best protection is provided by special antioxidant preparations, which either contain sufficiently high doses of individual antioxidants, or are multicomponent systems.
I wanted to write this article about a little-known representative of antioxidant substances, but along the way I changed my mind, and today will only be the beginning. I will not write about vitamins C and E, about which enough has already been written, but about those modest ones, without whom vitamins do not work at full strength, and who by themselves, like Matrosov, protect us from radicals and other Bolsheviks and Socialist-Revolutionaries with their breasts. And the first word will be about little known, but so important for our body lipoic acid .
: versatile antioxidant
The first word is why "universal". For two reasons. First, and rather unusually, it dissolves in both water and fats. And this means that lipoic acid molecules can act not only in the cells of the body, but also penetrate the blood-brain barrier into the brain, which is quite atypical for antioxidant substances. Why this is so important, we will see further.
Secondly, lipoic acid has a unique property - it not only acts as an antioxidant itself, but is also able to "raise from the dead" other antioxidants that died on the barricades. It resuscitates glutathione, vitamins C and E, and coenzyme Q10. No other nutrient can do this.
“Lipoic acid, alpha-lipoic acid or thioctic acid, whatever it is called, does not change the fact that until recently no one had ever heard of it. However, today progressive health advocates recognize it as a universal antioxidant and the main treatment for diabetic neuropathy.If the findings of the early studies prove correct, lipoic acid will be one of the most precious nutrients for preventing many of the consequences of high blood sugar, and perhaps even slowing down the aging process itself."
I took this quote from Robert Atkins' book "Bio Supplements" because it confused me a little in the context of Atkins' article on lipoic acid. How is it, he writes, that lipoic acid has been used in Europe for thirty years, but in America no one has heard of it yet? Truly, the pharmaceutical mafia has no boundaries!
But be that as it may, I will tell you what I learned about lipoic acid.
What can acid do for you?
1. Reduce insulin resistance and improve glucose metabolism.
Every person who is overweight or who prefers a carbohydrate diet is at risk of impaired insulin metabolism. Therefore, lipoic acid is potentially beneficial for most of us.
As a result of animal experiments, it was found that lipoic acid protects pancreatic cells that produce insulin. The destruction of these cells leads to diabetes I and subsequent dependence on insulin injections. Lipoic acid should help in the very early stages of type 1 diabetes, when not all insulin-producing cells in the pancreas have died yet.
2. Help in the treatment of diabetic neuropathy.
While the ability of lipoic acid to protect the pancreas has not yet been sufficiently studied, its role in the treatment of diabetic neuropathy has been clinically confirmed, and it is primarily for this purpose that it is used in Europe.
Excess blood sugar triggers glycolysis, which causes fat molecules to stick together, and this is one of the main types of cell damage that scientists associate with aging. Glycolysis causes damage to nerve cells, resulting in diabetic neuropathy, and if this process affects the optic nerves, then we are dealing with diabetic retinopathy.
Studies have shown that alpha-lipoic acid can prevent nerve damage if taken before permanent damage occurs. Apparently, its action is associated with an improvement in blood flow to nerve cells and cell metabolism.
Studies conducted at the Mayo Clinic confirmed a significant reduction in the symptoms of diabetic neuropathy in 71% of patients who took alpha-lipoic acid. And since lipoic acid can also enter brain cells, it can also help with damage to the optic nerves.
3. Help get rid of excess weight.
Alpha-lipoic acid works as a coenzyme in carbohydrate-to-energy reactions, so in addition to lowering glucose levels, it can also speed up the conversion of carbohydrates into energy, and therefore reduce fat storage. In addition, it promotes the oxidation of fatty acids, so it can help the body burn fat stores.
The fact that lipoic acid is a "friend" in the brain is also of no small importance: due to its affinity for glucose receptors in the hypothalamus, it blocks the protein kinase enzyme, which gives signals of hunger, and therefore suppresses appetite.
4. Protect your liver.
Lipoic acid is also a reliable protector of the liver. In people who regularly drink wine, it protects the liver from the toxic effects of alcohol.
But not only drinkers can benefit from taking lipoic acid. Recently, steatosis has become more and more common - non-alcoholic fatty liver due to excess weight (abdominal type of obesity) and poor nutrition.
Alpha lipoic acid helps to reduce the deposition of fats in the liver. This reduces the risk of developing fatty liver, even if your diet is too high in fat.
5. Protect blood vessels and heart.
Although the role of alpha-lipoic acid in preventing cardiovascular disease is not yet fully understood, scientists suggest that taking lipoic acid may be a promising approach to reduce cardiovascular risk.
In any case, in studies in mice, lipoic acid supplements showed a 55% reduction in atherosclerotic lesions - the formation of fatty layers that cause clogging of the arteries. Lipoic acid also caused a decrease in triglycerides, which are a risk factor for cardiovascular disease.
Researchers have found that alpha lipoic acid causes a change in the action of genes that control cholesterol. They increase the production of enzymes that act as free radical scavengers, and this reduces the production of LDL cholesterol. However, it is still unknown how effectively this mechanism will work in humans.
6. Improve your brain function.
Alpha lipoic acid may also prevent oxidative damage to the nerves and brain. It reduces all types of free radical oxidation, whether in arteries or nerve cells. In the brain, lipoic acid may help prevent or repair cellular damage in Alzheimer's disease. Animal studies have already demonstrated that lipoic acid improves memory and cognitive function.
Animals treated with alpha-lipoic acid have been shown to have a four times higher survival rate after stroke than animals that did not receive this supplement. Alpha Lipoic Acid regenerates glutathione in the brain and thus provides protection against neurotoxins. It increases blood flow to the brain, improves glucose uptake by brain cells, and increases nerve conduction. Alpha lipoic acid is one of the few nutrients that can increase glutathione levels in brain cells. A decrease in glutathione levels is a harbinger of chronic diseases, including degenerative disorders of brain activity.
7. Help prevent cancer.
Lipoic acid is a powerful antioxidant that enhances and restores other antioxidants in the body, especially vitamin E. Biochemist Richard Passwater has shown that lipoic acid can even prevent the activation of a gene that causes cancer cells to grow.
8. Slow down aging.
Lipoic acid is produced in our body, however, with age, the natural production of this substance weakens, and decreases even more in many chronic diseases. In addition, do not forget that our body does not pull out the "plan" for antioxidants.
And what does this lead to? To reduce the level of glutathione - "amino acids of youth". That is, to accelerated aging and early death. In addition, as already mentioned, scientists consider cell damage as a result of glycosylation to be one of the main causes of aging, and lipoic acid blocks this process.
Scientists have the opinion that supplementing with lipoic acid may be able to slow, if not completely reverse, some of the effects of aging. Therefore, if you are interested in means for prolonging youth, lipoic acid should attract your attention. As a preventive measure, any amount of this antioxidant will be beneficial, but after age 50, it is better to take higher doses.
From what has been said about lipoic acid, you can conclude that there is no reliable evidence of its benefits for humans yet. However, such a speculative conclusion can be drawn in relation to almost any prophylactic agent, the same vitamin C, for example. Simply because it takes a hundred years of research to strictly statistically prove that vitamin C increases life expectancy. Therefore, laboratory studies are carried out on mice that live for 2 years.
However, lipoic acid has been used medicinally for 30 years, as I said. It is used therapeutically in the treatment of diabetic neuropathy, senile dementia, chronic fatigue syndrome, cancer, liver disease, high blood pressure, high cholesterol, and even weight loss. This is a perfect example of a natural substance that deserves - but does not receive - the status of the drug of choice in the treatment of many diseases.
Of course, therapeutic and prophylactic dosages differ like heaven and earth. Fortunately, lipoic acid has no side effects, except for one thing - diabetics may need to revise the dose of insulin in the direction of reducing it.
What about food sources? Maybe you can not fool yourself with the search for drugs, but simply click on those products that contain more lipoic acid? Yes, hardly. Unfortunately, there is very little of it in regular foods. Judge for yourself: the richest sources of lipoic acid - by-products - contain only:
- kidneys: 32 mg per serving;
- heart: 19 mg per serving;
- liver: 14 mg per serving;
- spinach: 5 mg per serving;
- rice: 11 mg per serving.
Theoretically, of course, you can have breakfast with kidneys and rice, lunch with a heart and liver, and dine with a kilo of spinach, but I personally can’t imagine such a life. Because not only lipoic acid a person lives.
Lipoic acid is similar in its action to the B vitamins, although its belonging has not yet been clearly defined, and to clear the conscience, the researchers attributed it to the conditional group of quasi-vitamins, or vitamin-like substances. However, it works best in a "family atmosphere" - along with other B vitamins, especially thiamine.
This is how it is - lipoic acid, a real workhorse of the antioxidant ambulance of our body.