A modern view on the possibilities of using alpha-lipoic acid

Alpha lipoic acid[edit | edit code]

Alpha lipoic acid

(English lipoic acid) - also known as
thioctic acid
- is a biologically active agent from the group of conditional vitamins. It is an important cofactor of pyruvate dehydrogenase and alpha-ketoglutarate dehydrogenase complexes. It has antioxidant properties and potentiates the action of insulin.

Food sources:

alpha lipoic acid is found in large quantities in kidneys (32 mg per 1 serving), heart (19 mg per 1 serving), liver (14 mg per 1 serving), spinach (5 mg per 1 serving), rice (11 mg per 1 serving). portions) and other products.

Alpha lipoic acid is conditionally essential for humans. The body is able to synthesize it only in those quantities that can prevent its deficiency. [1]

Mechanism of action of alpha lipoic acid[edit | edit code]

Alpha Lipoic Acid Content in Some Foods
Lipoic acid has several major physiological functions. [2] Alpha lipoic acid primarily acts as an antioxidant. [3] Reactive oxygen metabolites (ROM) or reactive oxygen agents (ROS) are products of oxidative metabolism that the body produces constantly. Excess free radicals lead to damage to DNA and mitochondria, inhibition of ATP production, aging and cell death. Alpha lipoic and dihydrolipoic acids serve as powerful antioxidants. Theoretically, they are able to protect cells from peroxidative damage, reducing the risk of developing diseases associated with the aggression of radicals, and also slow down the aging process. [4]

Secondly, alpha lipoic acid acts as a cofactor involved in mitochondrial metabolism. Under aerobic conditions, pyruvate enters the mitochondrion and, through a complex reaction of pyruvate dehydrogenase, is converted to acetyl-CoA for participation in the Krebs cycle. This reaction requires several coenzymes and cofactors, including alpha lipoic acid. The lack of alpha-lipoic acid is expressed in the reserving of pyruvate in the cytosol and its conversion to lactic acid. The anaerobic threshold is the limit after which lactic acid begins to accumulate in the blood. Because alpha lipoic acid serves as a cofactor in this set of reactions, its deficiency will reduce aerobic power, aerobic threshold, and available energy. Theoretically, increasing the amount of alpha-lipoic acid can increase the efficiency of converting pyruvate to acetyl-CoA, and thereby increase the amount of mediators of aerobic metabolism. For this reason, some scientists suggest that supplementation with alpha lipoic acid, B complex vitamins, and other cofactors involved in this complex reaction may raise aerobic threshold and improve aerobic metabolism.

Third, alpha lipoic acid may benefit people with diabetes. For them, there are several sources of oxidative stress, which is a precursor to a number of complications associated with diabetes (insulin resistance, neuropathy, kidney disease, etc.). Taking alpha lipoic acid as a dietary supplement has a beneficial effect on the course of the disease, reducing complications associated with radical aggression. In addition, alpha lipoic acid was found to reduce insulin resistance by improving the uptake of glucose into cells. [5]

Lipoic acid 25 mg

Lipoic acid

Registration number and date: РN 001574/01 dated 05/10/2007

Trade name of the drug: Lipoic acid

International nonproprietary name: thioctic acid Dosage form: film-coated tablets

Compound:

Active substance:

Lipoic acid (thioctic acid) -12 mg and 25 mg

Excipients: sugar (sucrose), glucose (dextrose), potato starch, calcium stearate 1-water (calcium stearate monohydrate), stearic acid, talc (magnesium hydrosilicate).

Excipients of the shell: aerosil (colloidal silicon dioxide), beeswax, titanium dioxide, basic magnesium carbonate (magnesium hydroxycarbonate), vaseline oil, low molecular weight medical polyvinylpyrrolidone (povidone), sugar (sucrose), talc (magnesium hydrosilicate), quinoline yellow dye E -104.

Description

Yellow or greenish-yellow film-coated tablets.

The cross section shows two layers.

Pharmacotherapeutic group: metabolic agent.

ATX code : [A05BA].

pharmachologic effect

Lipoic acid is a coenzyme involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids and plays an important role in the body's energy balance. By the nature of its biochemical action, thioctic acid is similar to B vitamins. It participates in the regulation of lipid and carbohydrate metabolism, has a lipotropic effect, affects cholesterol metabolism, improves liver function, and has a detoxification effect in case of poisoning with heavy metal salts and other intoxications.

Indications for use

Fatty liver, liver cirrhosis, chronic hepatitis, hepatitis A, intoxication (including salts of heavy metals, toadstool), hyperlipidemia.

Contraindications

Hypersensitivity, lactation period, children's age (up to 6 years).

With caution - pregnancy

Directions for use and doses

Inside after meals. Adults - 50 mg 3-4 times a day.

Children over 6 years old - 12-24 mg 2-3 times a day.

The duration of treatment is 20-30 days. If necessary, as prescribed by a doctor, a second course of treatment is carried out after 1 month.

Side effect

Dyspepsia (including nausea, heartburn, vomiting, diarrhea, abdominal pain), allergic reactions (including urticaria, skin rash, itching and systemic allergic reactions up to anaphylactic shock), hypoglycemia.

Interaction with other drugs

Strengthens the anti-inflammatory effect of glucocorticosteroids. Reduces the effectiveness of cisplatin. Enhances the effect of insulin and oral hypoglycemic agents. Binds metals, so should not be taken simultaneously with drugs containing metal ions (iron, calcium magnesium); the interval between doses should be at least 2 hours. Ethanol and its metabolites weaken the effect of lipoic acid.

special instructions

During the treatment period, regular monitoring of glucose concentrations (especially at the beginning of therapy) in patients with diabetes mellitus is necessary; you should refrain from drinking alcohol.

Release form

Film-coated tablets 12 mg and 25 mg.

10 tablets per blister pack.

50, 100 tablets in glass jars or polymer jars.

Each jar or 5 blister packs along with instructions for use are placed in a pack.

Conditions for dispensing from pharmacies

On prescription.

Storage conditions:

In a dry place, protected from light, at a temperature not exceeding 25°C.

Best before date:

3 years. Do not use after the expiration date stated on the package.

Units:

pack

Alpha lipoic acid and bodybuilding[edit | edit code]

Alpha lipoic acid may be beneficial in bodybuilding because intense training stimulates the formation of free radicals, increasing oxidative stress in muscle fibers. Taking antioxidants such as alpha lipoic acid reduces oxidation rates. [6] Thus, the effect of exercise on the formation of free radicals is weakened, and the destruction of proteins and cells is inhibited. In theory, this could allow athletes to train harder with less damage to muscle and other fibers, and to recover faster after training.

In addition, alpha lipoic acid has insulin-like properties, improving glucose uptake into muscles. [7] Thus, glycogen storage processes are stimulated, the amount of glucose in the muscles increases during exercise, and stable blood glucose levels are maintained. In addition, it is very interesting whether consuming alpha-lipoic acid with other nutrients (for example, creatine) can speed up insulin-related absorption processes in muscles. And third, there is evidence that alpha lipoic acid can promote breakdown in mitochondria. This means that the electronic transport system becomes less efficient as a result of increased heat production. This scenario may not be ideal for endurance athletes, but may be an effective way to enhance thermogenesis and increase energy expenditure in a similar manner to decoupled polymers such as UCP-1. In other words, alpha lipoic acid can serve as a powerful fat burner.

Benefit

The beneficial properties of lipoic acid are still being studied. To date, it has been found that this is a powerful antioxidant that slows down the aging process in the body and suppresses the formation of free radicals. It is able to penetrate every cell of the body and protect them from radical damage and, as a result, from various pathologies. The substance enhances the antioxidant effect of vitamin C, E and coenzyme Q10. Thanks to this property, lipoate has a beneficial effect on the body:

Preparations with lipoic acid are prescribed to people with diabetes. It has been proven that the substance reduces the need of body cells for glucose and increases their susceptibility to it. It also helps maintain normal blood glucose levels.

Athletes and people who frequently exercise take this drug as it improves metabolism and helps build muscle mass. When combined with intense training, lipoate helps you burn fat faster and release more energy, thereby helping you achieve your desired shape.

If you don’t want to build up muscles, but want to reduce volume and lose weight, then you should take the drug according to a certain regimen, which should be prescribed by your doctor. Due to the fact that lipoate improves metabolism, it is able to increase the digestibility of carbohydrates and prevent them from being deposited in excess fat on the body.

Lipoic acid is important in the treatment of liver diseases. It is prescribed for viral hepatitis B and C, cirrhosis and fatty liver, liver failure, non-alcoholic steatohepatitis. The drug improves the functioning of the organ, inhibits the development of fibrosis and malignant tumors, thanks to its antioxidant properties, normalizes fat metabolism in liver cells and stops inflammatory processes.

Lipoate improves body tone and prevents the development of many aging diseases, including Parkinson's, Alzheimer's, dementia, etc. The drug is prescribed for chronic fatigue, stress, decreased memory and attention. The drug is also able to prevent glaucoma and cataracts, which develop mainly in old age.

The substance is able to bind heavy metal salts and remove them from the body. Therefore, its use is prescribed for severe intoxication of the body, including alcohol and drugs.

Lipoic acid is similar in effect and structure to vitamin B, so it is often prescribed for diseases of the nervous system and cardiovascular pathologies. It helps normalize blood pressure, improve vascular permeability, and eliminate numbness in the limbs.

Harm

There is no need to think that this antioxidant will not cause any harm to the body. If you take the drug incorrectly or use it excessively, the following side effects are possible:

Heartburn, stomach or intestinal upsets, nausea, skin rash, itchy skin; in severe cases, anaphylactic shock is possible.

A sharp drop in blood glucose levels. Therefore, persons suffering from diabetes should under no circumstances violate the drug dosage regimen and take it only under the supervision of a doctor.

Lipoate reduces the effectiveness of chemotherapy, so it is not recommended to combine them.

If you have problems with the thyroid gland and hormonal imbalance, you should use the substance with caution, as it can negatively affect hormonal levels.

Long-term use of the drug for peptic ulcers and gastritis can aggravate the problem. Also, for any other chronic diseases, long-term use is agreed with the doctor.

Alpha lipoic acid and training[edit | edit code]

A number of studies have examined the effects of alpha lipoic acid supplementation on markers of oxidative stress and muscle damage. In most cases, oxidative stress was alleviated. However, there is much less data on the effects of alpha lipoic acid on the training itself. Several studies have recently been published on the effects of alpha-lipoic acid on markers of oxidative stress in rats. [8] For example, Saengsirisuwan and colleagues reported that the use of alpha-lipoic acid in combination with exercise improved insulin levels in insulin-resistant obese rats. However, in the same experiment, but with lean, insulin-sensitive rodents, similar results were not obtained.

Although most research on the properties of alpha-lipoic acid has been carried out on animals, an experiment has also been conducted on humans, during which a mixture of antioxidants (including alpha-lipoic acid) was used. Schmidt et al[9] studied the effects of a mixture of antioxidants on a group of sailors who trained in cold weather for 24 days. The mixture included vitamin E, beta-carotene, ascorbic acid, selenium, alpha-lipoic acid, N-acetyl l-cysteine, catechin, lutein and lycopene. Indicators of oxidative stress were assessed. Both the experimental and control groups (placebo) showed high levels of oxidative stress after 24 days of training. There were no significant differences in oxidative stress levels between both groups.

However, an independent study conducted by Petersen Shay in 2008 confirmed that alpha lipoic acid has an antioxidant effect in humans and also inhibits aging due to the modulation and transduction of gene transcription signals, and therefore improves the antioxidant status of the cell. [10]

Summary[edit | edit code]

Alpha lipoic acid has antioxidant properties, inhibits the aging of the body and increases insulin consumption by tissues. Theoretically, athletes and bodybuilders may benefit from consuming alpha lipoic acid as a dietary supplement by reducing oxidative stress and regulating glucose metabolism. However, we can say with confidence that alpha-lipoic acid does not have a pronounced anabolic effect, that is, it does not contribute to muscle growth.

Biological role of ALA

The main effect of alpha lipoic acid is to inhibit oxidative stress in cells. This is extremely important for preventing the negative effects of free radicals, maintaining health and maintaining a youthful body. The main benefits of alpha lipoic acid in the body:

• Improving the functioning of the cardiovascular, endocrine and other systems;
• Protecting nerve tissue from stress;
• Improved elimination of toxins and metabolic by-products from the body;
• Improving the utilization of fat cells;
• Improves liver function.

In general, alpha-lipoic acid has many indications for use; the substance has a positive effect on almost all tissues, organs and systems. The range of uses of vitamin N ranges from simply increasing energy to supporting the body in diabetes or liver damage. The substance is also used in cosmetology; it is included in many creams for skin rejuvenation, eliminating age spots, and smoothing wrinkles. Although topical use of alpha lipoic acid has minimal effect compared to obtaining the compound from food or supplements.

Sports nutrition with alpha lipoic acid[edit | edit code]

• Opti-Men by Optimum Nutrition
• Cell-Tech Hardcore Pro Series by MuscleTech
• Opti-Women by Optimum Nutrition
• Cheaters Relief by BSN
• Aplodan by Muscletech
• TestostroGrow 2 HP from Ultimate Nutrition

Dosage regimen[edit | edit code]

Doses of alpha lipoic acid vary widely: from 50 to 400 mg per day.

For medicinal purposes (diabetes mellitus and its complications), alpha-lipoic acid is taken from 600 to 1800 mg per day. Take 30 minutes before meals.

Side effects[edit | edit code]

Alpha lipoic acid has virtually no side effects. In rare cases, allergic reactions, heaviness in the head, and changes in taste are possible. Much more often side effects develop after intravenous administration of the drug. In case of overdose, digestive upset, nausea, vomiting, headache, etc. may occur.

Due to the combination with metals (formation of complex compounds), it is not prescribed to patients taking cisplatin, iron-containing drugs, magnesium, calcium. It is not recommended to combine with alcohol.

Possible contraindications and side effects

Despite the huge range of positive effects, alpha lipoic acid has a number of contraindications. Therefore, you should not be negligent in taking the supplement and exceed the dosage on your own.

It is recommended to discontinue or temporarily limit intake of the supplement in the following cases:

• For peptic ulcers or inflammatory phenomena in the gastrointestinal tract;
• With iron deficiency;
• For decompensated diabetes mellitus;
• For acute bronchitis;
• While breastfeeding.

In some cases, negative effects may occur only at the beginning of the course; this is an individual reaction and increased sensitivity to the substance. In this case, doctors may temporarily lower the dosage to ease the adjustment period. The compound itself is not dangerous to the body and can cause side effects only with a severe overdose.

It is strictly forbidden to drink alpha lipoic acid in combination with any alcohol. When combined with ethanol, the risks of any side effects increase greatly.

Links[edit | edit code]

1. Bilska, A., L. Wlodek. . Postepy Hig Med Dosw 56:201-219, 2002.
2. Packer, L, K. Kraemer, G. Rimbach. Molecular aspects of lipoic acid in the prevention of diabetes complications. Nutrition 17:888-895, 2001.
3. Shapiro, K., W. C Gong. Natural products used for diabetes. J Am Pharm Assoc (Wash) 42:217–226, 2002.
4. Miquel, J. Can antioxidant diet supplementation protect against age-related mitochondrial damage? Ann NY Acad Sci 959:508-516, 2002.
5. Sytze Van Dam, P. Oxidative stress and diabetic neuropathy: pathophysiological mechanisms and treatment perspectives. Diabetes Metab Res Rev 18:176-184, 2002.
6. Sen, S. K. Update on thiol status and supplements in physical exercise. Can J Appl Physiol 26 Suppl:S4-12, 2001.
7. Greene, E.L., B.A. Nelson, K.A. Robinson, M.G. Buse. alpha-Lipoic acid prevents the development of glucose-induced insulin resistance in 3T3-L1 adipocytes and accelerates the decline in immunoreactive insulin during cell incubation. Metabolism 50:1063–1069, 2001.
8. Khanna, S., M. Atalay, D. E. Laaksonen, M. Gul, S. Roy, S. K. Sen. Alpha-lipoic acid supplementation: tissue glutathione homeostj at rest and after exercise. J Appl Physiol 86:1191–1196, 1999.
9. Schmidt, M. C, E. W. Askew, D. E. Roberts, R. L. Prior, W. Ensign, Jr., R. E. Hesslink, Jr. Oxidative stress in humans training in a cold, moderate altitude environment and their response to a phytochemical antioxidant supplement. Wilderness Environ Med 13:94-105, 2002
10. Petersen Shay K, Moreau RF, Smith EJ, Hagen TM. Is alpha-lipoic acid a scavenger of reactive oxygen species in vivo? Evidence for its initiation of stress signaling pathways that promote endogenous antioxidant capacity. IUBMB Life. 2008 Jun;60(6):362-7. Review. PMID: 18409172