Preparations with succinic acid

Pharmaceutical preparations with succinic acid are used as antioxidants, normalizing intracellular metabolism and contributing to the restoration of body functions, disturbed due to diseases or natural aging of human cells.

[1], [2], [3], [4]

Indications of the preparations with succinic acid

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

Now succinic acid is produced from maleic anhydride, and it, in turn, is derived from benzene or n-butane. So, if on the packaging of dietary supplements it is indicated that they contain succinic acid, "obtained from natural amber," this statement introduces the consumer into confusion.

The use of succinic acid as a food additive E363 is widely used as a pH regulator and sequestrant (it is approved by the FDA).

In the body, succinic acid is synthesized in energy-producing organelles - mitochondria and is an intermediate substance of metabolic decomposition (oxidative phosphorylation) of amino acids, carbohydrates and fats, that is, a cycle of tricarboxylic acids (Krebs cycle). This is a multistage sequence of repeated intracellular enzymatic reactions that provide energy 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 coenzyme succinyl-CoA into succinic acid (succinate), its electrons are transferred to the respiratory chain of the 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 the cell nuclei - the transcription factor of induced hypoxia (HIF-alpha). At normal oxygen levels, the content of HIF-alpha is insignificant, but as soon as the amount of available oxygen in the cells decreases, the level of HIF increases and can lead to apoptosis of the cells. Inhibit the HIF factor and stabilize its level may succinate, that is, succinic acid.

[5], [6], [7], [8], [9], [10]

Release form

There are preparations with succinic acid, which are used to activate tissue metabolism and normalize energy balance, that is, they act as metabolites. The use of succinic acid to reduce the intensity of oxidation processes is possible due to its pronounced antioxidant properties. Succinic acid compounds - succinates Na, K, Ca, Mg - improve the supply of cells with oxygen, exerting an antihypoxic effect on the tissues of organs in their morphological changes and dystrophy, caused by a wide range of diseases and pathological conditions.

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

Names of preparations with succinic acid:

• Succinic acid;
• Ethyl methyl mercaptopyridine succinate (Mexipridol, Mexiprem, Armadine, Nicomex, etc.), Cytoflavin (tablets and injection solution), anti-shock and disintoxic infusion solution Reamberin (Meglyumin sodium succinate), Gelofusin (solution for replacing plasma with blood loss and intoxication).

Preparations with succinic acid for alcoholism: Mexidol, Limonar.

Preparations of hyaluronic acid with succinic acid: Hyalual Arthro is a substitute for synovial fluid in joints with osteoarthrosis.

[11], [12], [13]

Pharmacodynamics

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

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

Producers argue that drugs containing this substance regulate not only the processes of oxidation in cells and increase the level of adenosine triphosphate, but also normalize the work of the vessels of the brain, the heart muscle (primarily in hypoxia), the gastrointestinal tract, endocrine glands etc. However, the biochemical process of the whole range of beneficial effects that drugs with succinic acid exert in the instructions is most often not explained (for example, how they reduce cholesterol in the blood or relieve vegetovascular symptoms and increase immunity); at best, the mechanism of the tricarboxylic acid cycle is described.

Mexidol is the succinate of emoxipin, and Limontar is succinic acid (in each 200 mg tablet) and citric acid monohydrate (50 g), whose main task is not only to improve metabolism, but also to increase the production of gastric juice.

The pharmacodynamics of the antioxidant vitamin Citoflavin is described in more detail. In addition to succinic acid, vitamin B2 (riboflavin) is included, and the precursors of adenosine triphosphate are riboxin (inosine) and vitamin PP (niacin). That is, the action 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 - N-methylamonium sodium succinate, which helps stabilize the cell membranes, slows the oxidation of fatty acids and activates the cleavage of glucose to compensate for energy costs under hypoxic conditions.

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

Hyalual Arto - a preparation of hyaluronic acid with succinic acid - is used for viscosupplementation - introduction into the joint bag for the replacement of synovial fluid, partially or completely lost with deforming arthrosis of various joints. Amber acid activates the metabolism in bone and cartilage tissues and improves the mobility of damaged joints.

[14], [15], [16], [17], [18], [19], [20]

Pharmacokinetics

After ingestion Mexipridol (as well as Mexidol) is rapidly absorbed in the digestive tract, the maximum concentration in the blood plasma is noted after 25-30 minutes. The drug is split in the liver with the formation of metabolites, which are excreted by the kidneys (half-life - about five hours).

All components of Cytoflavin enter the bloodstream and tissues; The fastest way to metabolism is succinic acid (with oral administration of the drug - in half an hour, with parenteral administration - after 1.5-2 minutes). The maximum level in the blood plasma niacin reaches two hours later, 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% Gelofusine is excreted from the body by the kidneys in unchanged form (with a half-life period of about 4.5 hours).

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

[21], [22], [23]

Use of the preparations with succinic acid during pregnancy

Use during pregnancy of all medicines containing succinates is contraindicated.

Contraindications

The main contraindications to the use of succinic acid and its derivatives: hypersensitivity, acute liver failure, renal insufficiency, stomach and duodenal ulcer, increased blood pressure.

In addition, Cytoflavin is contraindicated in the treatment of patients younger than 18 years; Reamberin - with trauma to the skull and edema of the brain; Gelofusin - with poor blood clotting and acute heart failure.

[24], [25], [26], [27], [28]

Side effects of the preparations with succinic acid

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

In addition, the use of Mexipridol, Mexidol and Limonar may cause dry mouth, nausea and increased acidity of gastric juice by hypersecretion of hydrochloric acid. This can provoke pain in the stomach.

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

[29], [30], [31]

Dosing and administration

Amber acid - one tablet three times a day (before meals); the maximum duration of application is 4 weeks.

Mexidol, Mexipridol, etc. - one tablet three times a day; duration of admission - 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 injected into the vein using a dropper; The dose and duration of administration is determined by the physician individually.

Powder Limontar is dissolved in water (0.25 g per one dose) and taken orally up to four times during the day.

The preparation of hyaluronic acid with succinic acid Hyalual Arthro is injected directly into the joint bag. The instruction notes that three injections provide a stable therapeutic effect for 12 months.

[32], [33], [34], [35]

Overdose

Overdosing of drugs with succinic acid causes an increase in side effects.

[36], [37]

Interactions with other drugs

In drugs with succinic acid incompatibility with sedatives of a group of barbiturates, tranquilizers and muscle relaxants.

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

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

[38], [39], [40], [41], [42], [43], [44]

Storage conditions

Preparations with succinic acid should be stored away from light, at temperatures up to + 25 ° C.

[45], [46], [47]

Shelf life

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

[48], [49]