Preparations with succinic acid

Pharmaceutical preparations containing succinic acid are used as antioxidants that normalize intracellular metabolism and promote the restoration of body functions impaired due to diseases or natural aging of human cells.

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Indications succinic acid preparations

The system name of succinic acid is 1,4-butanedioic acid, it is also called succinate (from the Latin name of amber - succinium). This is an organic compound of the class of dibasic carboxylic acids, that is, having two carboxyl groups in its molecule. This acid was first obtained by heating natural amber, and then it was discovered in living cells as an active component of organic synthesis.

Currently, succinic acid is produced from maleic anhydride, which in turn is obtained from benzene or n-butane. So, if the packaging of dietary supplements indicates that they contain succinic acid, "obtained from natural amber", this statement misleads the consumer.

Succinic acid is widely used as a food additive E363 – as a pH regulator and sequestrant (it is FDA approved).

In the body, succinic acid is synthesized in energy-producing organelles - mitochondria and is an intermediate substance in the metabolic breakdown (oxidative phosphorylation) of amino acids, carbohydrates and fats, i.e. the tricarboxylic acid cycle (Krebs cycle). This is a multi-stage sequence of repeating intracellular enzymatic reactions that provide energy resources in tissues (in the form of ATP), as well as compounds for the synthesis of substances necessary to maintain cell viability. In addition, at the stage of transformation of the coenzyme succinyl-CoA into succinic acid (succinate), its electrons are transferred to the respiratory chain of mitochondria, which ensures the supply of oxygen to the cells of the tissues of all organs.

Oxygen starvation of cells (hypoxia) causes many pathological disorders; the main regulator of the body's response to hypoxia is a special protein of cell nuclei - the hypoxia-induced transcription factor (HIF-alpha). At normal oxygen levels, the content of HIF-alpha is insignificant, but as soon as the amount of available oxygen in cells decreases, the level of HIF increases and can lead to cell apoptosis. Succinate, i.e. succinic acid, can inhibit the HIF factor and stabilize its level.

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Release form

Preparations with succinic acid are produced, which are used to activate tissue metabolism and normalize energy balance, i.e. act as metabolics. The use of succinic acid to reduce the intensity of oxidative processes is possible due to its pronounced antioxidant properties. Succinic acid compounds - succinates Na, K, Ca, Mg - improve the supply of oxygen to cells, exerting an antihypoxic effect on organ tissues during their morphological changes and dystrophy caused by a wide range of diseases and pathological conditions.

Domestic clinical practice has shown that drugs with derivatives of succinic acid, which is an endogenous metabolite, help to increase immunity and adaptive capabilities of the body after a long illness or injury, stimulate regeneration processes and restore physiological functions of all systems and organs. Also, in complex therapy, drugs with succinic acid are used to treat blood vessels, including cerebral ones. It is recommended to use drugs that use succinic acid as an inhibitor of potassium ion loss in complex therapy of strokes, heart attacks, atherosclerosis, senile memory loss and psychoneurological disorders.

Names of preparations with succinic acid:

• Succinic acid;
• Ethylmethylhydroxypyridine succinate (Mexipridol, Mexiprim, Armadin, Nikomex, etc.), Cytoflavin (tablets and injection solution), anti-shock and detoxification infusion solution Reamberin (Meglumine sodium succinate), Gelofusin (solution for plasma replacement in case of blood loss and intoxication of the body).

Preparations with succinic acid for alcoholism: Mexidol, Limontar.

Hyaluronic acid preparations with succinic acid: Hyalual Arthro – a substitute for synovial fluid in joints with osteoarthritis.

Pharmacodynamics

Although the chemical structure of exogenous succinic acid is similar to that of a metabolite of the intracellular tricarboxylic acid cycle, it is rarely included in drugs in its pure form. Even in succinic acid tablets, according to the instructions, the pharmacologically active component is acetylaminosuccinic acid. Chelate compounds - salts and chemically similar succinate esters - are used to increase intestinal absorption of drugs with succinic acid.

Thus, the pharmacodynamics of the regulatory effect on metabolism of drugs such as Mexipridol is due to 2-ethyl-6-methyl-3-oxypyridine succinate (ethylmethylhydroxypyridine succinate), which is a derivative of succinic acid.

Manufacturers claim that medicines containing this substance regulate not only oxidation processes in cells and increase the level of adenosine triphosphate, but also normalize the functioning of the brain vessels, heart muscle (primarily during hypoxia), gastrointestinal tract, endocrine glands, etc. However, the biochemical process of the entire spectrum of beneficial effects that drugs with succinic acid have is most often not explained in the instructions (for example, how they reduce cholesterol levels in the blood or eliminate vegetative-vascular symptoms and improve immunity); at best, the mechanism of the tricarboxylic acid cycle is described.

The main component of the anti-alcohol drug Mexidol is emoxipine succinate, and Limontar contains succinic acid (200 mg in each tablet) and citric acid monohydrate (50 g), the main task of which is not only to improve metabolism, but also to increase the production of gastric juice.

The pharmacodynamics of the antioxidant vitamin remedy Cytoflavin are described in more detail. In addition to succinic acid, it contains vitamin B2 (riboflavin) and precursors of adenosine triphosphate - riboxin (inosine) and vitamin PP (niacin). That is, the effect of the drug is provided by all the ingredients in the complex.

In the Reamberin solution, used to remove toxic substances from the body, the active substance is sodium N-methylammonium succinate, which helps stabilize cell membranes, slows down the oxidation of fatty acids and activates the breakdown of glucose to compensate for energy costs in hypoxic conditions.

The pharmacodynamics of Gelofusin, a colloidal solution of succinylated medical gelatin, is based on an increase in osmotic pressure, as a result of which, after the introduction of this drug into a vein with significant blood loss, the volume of fluid in the vessels increases, ensuring the work of the heart.

Hyalual Arto is a hyaluronic acid preparation with succinic acid, used for viscosupplementation – injection into the joint capsule to replenish synovial fluid, partially or completely lost in deforming arthrosis of various joints. Succinic acid activates metabolism in bone and cartilage tissues and improves the mobility of damaged joints.

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Pharmacokinetics

After oral administration, Mexipridol (as well as Mexidol) is rapidly absorbed in the gastrointestinal tract, with maximum plasma concentrations observed after 25-30 minutes. The drug is broken down in the liver to form metabolites that are excreted by the kidneys (half-life is approximately five hours).

All components of Cytoflavin enter the bloodstream and tissues; succinic acid is metabolized most rapidly (after half an hour of oral administration, after 1.5-2 minutes of parenteral administration). Niacin reaches its maximum level in blood plasma after two hours, and inosine after five hours after a single dose. All substances, except succinic acid, are metabolized in the liver and excreted in the urine.

99% of Gelofusine is excreted from the body by the kidneys unchanged (with a half-life of about 4.5 hours).

The pharmacokinetics of the drugs Limontar and Reamberin are not presented in the instructions.

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Dosing and administration

Succinic acid – one tablet three times a day (before meals); maximum duration of use – 4 weeks.

Mexidol, Mexipridol, etc. – one tablet three times a day; duration of administration – from 14 days to 1.5 months.

Cytoflavin – two tablets twice a day (before meals); the duration of treatment is three weeks.

Reamberin and Gelofusin are administered intravenously using a dropper; the dose and duration of use are prescribed by the doctor on an individual basis.

Limontar powder is dissolved in water (0.25 g per dose) and taken orally up to four times a day.

The hyaluronic acid preparation with succinic acid Hyalual Arthro is injected directly into the joint capsule. The instructions note that three injections provide a stable therapeutic effect for 12 months.

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Use succinic acid preparations during pregnancy

The use of all drugs containing succinates during pregnancy is contraindicated.

Contraindications

The main contraindications for the use of succinic acid and its derivatives: hypersensitivity, acute liver failure, renal failure, gastric ulcer and duodenal ulcer, high blood pressure.

In addition, Cytoflavin is contraindicated for use in the treatment of patients under 18 years of age; Reamberin - for head injuries and cerebral edema; Gelofusin - for poor blood clotting and acute heart failure.

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Side effects succinic acid preparations

Succinic acid can cause allergies (skin redness and itching), diarrhea and increased drowsiness.

In addition, the use of Mexipridol, Mexidol and Limontar can cause dry mouth, nausea and increased acidity of gastric juice due to hypersecretion of hydrochloric acid. This can provoke stomach pain.

Intravenous administration may be accompanied by paresthesia of the extremities, changes in blood pressure, headache, anaphylactic shock.

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Overdose

Overdose of drugs containing succinic acid causes increased side effects.

Interactions with other drugs

Preparations containing succinic acid are incompatible with sedatives of the barbiturate group, tranquilizers and muscle relaxants.

Preparations containing ethylmethylhydroxypyridine succinate potentiate the action of drugs for the treatment of epilepsy and Parkinson's disease.

Cytoflavin is not prescribed simultaneously with antibiotics, thyroid hormones and adrenal cortex hormones.

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Storage conditions

Preparations containing succinic acid should be stored away from light, at a temperature of up to +25°C.

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Shelf life

Shelf life: Succinic acid – 12 months: Mexipridol, Cytoflavin, Gelofusin, Hyalual Arthro – 2 years; Mexidol, Reamberin, Limontar – 3 years.

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