Thioctic acid recipe in Latin. Thioctic acid: antioxidant therapy for neurological diseases. Side effects and overdose

P N015545/01

Tradename: Thioctacid ® BV

INN or group name: Thioctic acid

Dosage form:

Film-coated tablets

Compound:

1 film-coated tablet contains:

Active substance: thioctic acid ( a-lipoic acid) - 600 mg.

Excipients: low-substituted hyprolose, hyprolose, magnesium stearate. Film casing: hypromellose, macrogol 6000, titanium dioxide, talc, aluminum varnish based on quinoline yellow dye, aluminum varnish based on indigo carmine.

Description: yellow-green biconvex oblong film-coated tablets .

Pharmacotherapeutic group:

Metabolic agent.

ATX code: A05VA

Pharmacological properties

Pharmacodynamics

Thioctic (a-lipoic) acid is found in human body, where it functions as a coenzyme in the reactions of oxidative phosphorylation of pyruvic acid and alpha-keto acids. Thioctic acid is an endogenous antioxidant, according to biochemical mechanism Its action is close to that of B vitamins.

Thioctic acid helps protect cells from toxic effect free radicals arising in metabolic processes; it also neutralizes exogenous toxic compounds that have entered the body. Thioctic acid increases the concentration of the endogenous antioxidant glutathione, which leads to a decrease in the severity of symptoms of polyneuropathy. The drug has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects; improves neuronal trophism. The result of the synergistic effect of thioctic acid and insulin is an increase in glucose utilization.

Pharmacokinetics

When taken orally, it is quickly and completely absorbed from gastrointestinal tract. Taking the drug simultaneously with food may reduce the absorption of the drug. Maximum concentration in blood plasma is achieved 30 minutes after taking Thioctacid BV and is 4 mcg/ml. The drug has a “first pass” effect through the liver; the absolute bioavailability of thioctic acid is 20%. The half-life is 25 minutes. The main metabolic pathways are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%).

Indications for use

Diabetic and alcoholic polyneuropathy.

Contraindications

Hypersensitivity to thioctic acid or other components of the drug.

Pregnancy, period breastfeeding(there is no sufficient experience in using the drug).

There are no clinical data on the use of Thioctacid ® 600 BV in children and adolescents; therefore, the drug should not be prescribed to children and adolescents.

Directions for use and doses

IN severe cases treatment begins with the appointment of Thioctacid ® 600 T solution for intravenous administration for 2–4 weeks, then the patient is transferred to treatment with Thioctacid ® BV.

Side effect

Frequency of development side effects defined as follows:

Very common: > 1/10;

Often:<1/10 > 1/100;

Infrequently:<1/100 > 1/1000;

Rarely:<1/1000> 1/10000;

Very rarely:<1/10000.

From the gastrointestinal tract:

Often – nausea; very rarely - vomiting, pain in the stomach and intestines, diarrhea, changes in taste.

Allergic reactions: Very rarely - skin rash, urticaria, itching, anaphylactic shock.

From the nervous system and sensory organs: Often - dizziness.

General:

Very rarely - due to improved glucose utilization, blood glucose levels may decrease and symptoms of hypoglycemia may appear (confusion, increased sweating, headache, visual disturbances).

Overdose

Symptoms:

In the case of taking thioctic (a-lipoic) acid in doses of 10-40 g, serious signs of intoxication may be observed (generalized convulsive seizures; severe acid-base imbalance leading to lactic acidosis; hypoglycemic coma; severe blood clotting disorders, sometimes leading to a fatal outcome ).

If a significant overdose of the drug is suspected (doses equivalent to more than 10 tablets for an adult or more than 50 mg/kg body weight for a child), immediate hospitalization is necessary.

Treatment: symptomatic, if necessary - anticonvulsant therapy, measures to maintain the functions of vital organs.

Interaction with other drugs

With the simultaneous administration of thioctic acid and cisplatin, a decrease in the effectiveness of cisplatin is observed. Thioctic acid binds metals, so it should not be administered concomitantly with drugs containing metals (for example, iron, magnesium, calcium). According to the recommended route of administration, Thioctacid ® 600 BV tablets are taken 30 minutes before breakfast, while preparations containing metals should be taken at lunchtime or in the evening. For the same reason, during treatment with Thioctacid ® 600 BV, it is recommended to consume dairy products only in the afternoon.

With simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may be enhanced, therefore regular monitoring of blood glucose levels is recommended, especially at the beginning of therapy with thioctic acid. In some cases, it is permissible to reduce the dose of hypoglycemic drugs to avoid the development of symptoms of hypoglycemia.

Ethanol and its metabolites weaken the effect of thioctic acid.

special instructions

Alcohol consumption is a risk factor for the development of polyneuropathy and may reduce the effectiveness of Thioctacid ® BV, therefore patients should refrain from drinking alcoholic beverages both during treatment with the drug and during periods outside of treatment.

Treatment of diabetic polyneuropathy should be carried out while maintaining optimal blood glucose concentrations.

Release form

Film-coated tablets, 600 mg.

30, 60 or 100 tablets in a brown glass bottle with a capacity of 50.0, 75.0 or 125.0 ml, respectively, with a plastic cap with tamper evident.

1 bottle along with instructions for use in a cardboard box.

Storage conditions

At a temperature not exceeding 25° C, out of the reach of children.

List B.

Best before date

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

Conditions for dispensing from pharmacies

On prescription.

Manufacturer

MEDA Pharma GmbH & Co. KG

Benzstrasse 1, 61352 Bad Homburg, Germany.

Produced

MEDA Manufacturing GmbH,

Neurater Ring 1, 51063 Cologne, Germany.

Consumer complaints should be sent to the address of the representative office in the Russian Federation:

125167, Moscow, Naryshkinskaya alley, 5/2, office 216

Thioctic acid is a metabolic agent that regulates the metabolism of carbohydrates and fats. The instructions for use of this drug give only one indication - diabetic polyneuropathy. However, this is not a reason to downplay the importance of thioctic acid in clinical practice. This endogenous antioxidant has amazing abilities to scavenge harmful free radicals. Thioctic acid takes an active part in cellular metabolism, performing the function of a coenzyme in the chain of metabolic transformations of antitoxic substances that protect cells from free radicals. Thioctic acid potentiates the action of insulin, which is associated with the activation of the process of glucose utilization.

Diseases caused by endocrine and metabolic disorders have been in the area of ​​special attention of doctors for more than a hundred years. At the end of the 80s of the last century, the concept of “insulin resistance syndrome” was first introduced into medicine, which united, in fact, insulin resistance, impaired glucose tolerance, increased levels of “bad” cholesterol, decreased levels of “good” cholesterol, and the presence of excess body weight and arterial hypertension. Insulin resistance syndrome has a similar name: metabolic syndrome. In contrast, clinicians have developed the basics of metabolic therapy aimed at maintaining or regenerating the cell and its basic physiological functions, which is a condition for the normal functioning of the entire organism as a whole. Metabolic therapy involves hormonal therapy, maintaining normal levels of chole- and ergocalciferol (vitamins D), as well as treatment with essential fatty acids, including alpha-lipoic or thioctic acid. In this regard, it is absolutely wrong to consider antioxidant therapy with thioctic acid only in the context of the treatment of diabetic neuropathy.

As you can see, this drug is also an indispensable component of metabolic therapy. Thioctic acid was originally called “vitamin N,” hinting at its importance for the nervous system. However, due to its chemical structure, this compound is not a vitamin. Without delving into the biochemical “wilds” with mention of dehydrogenase complexes and the Krebs cycle, we should note the pronounced antioxidant properties of thioctic acid, as well as its participation in the recycling of other antioxidants, for example, vitamin E, coenzyme Q10 and glutathione. Moreover: thioctic acid is the most effective of all antioxidants, while it is regrettable to note the current underestimation of its therapeutic value and the unreasonable narrowing of indications for use, which are limited, as already mentioned, only to diabetic neuropathy. Neuropathy is a degenerative-dystrophic degeneration of nervous tissue, leading to a disorder of the central, peripheral and autonomic nervous systems and desynchronization of the work of various organs and systems. All nervous tissue is affected, incl. and receptors. The pathogenesis of neuropathy is always associated with two processes: impaired energy metabolism and oxidative stress. Considering the “tropism” of the latter for nervous tissue, the clinician’s task includes not only a scrupulous diagnosis of signs of neuropathy, but also its active treatment with thioctic acid. Since treatment (or rather, even prevention) of neuropathy is most effective even before symptoms of the disease appear, it is necessary to start taking thioctic acid as early as possible.

Thioctic acid is available in tablets. A single dose of the drug is 600 mg. Given the synergism of thioctic acid with insulin, with the simultaneous use of these two drugs, an increase in the hypoglycemic effect of insulin and tablet hypoglycemic agents may be observed.

Pharmacology

The drug is an endogenous antioxidant that binds free radicals. Thioctic (α-lipoic) acid is involved in the mitochondrial metabolism of the cell; it functions as a coenzyme in the complex for the transformation of substances that have a pronounced antitoxic effect. They protect the cell from reactive radicals arising during intermediate metabolism or during the breakdown of exogenous foreign substances, and from heavy metals. Thioctic acid exhibits synergism with insulin, which is associated with increased glucose utilization. In patients with diabetes mellitus, thioctic acid leads to a change in the concentration of pyruvic acid in the blood.

Release form

Film-coated tablets from yellow to yellow-green, round, biconvex; at the break the core is light yellow to yellow.

Excipients: microcrystalline cellulose 165 mg, lactose monohydrate 60 mg, croscarmellose sodium 24 mg, povidone K-25 21 mg, colloidal silicon dioxide 18 mg, magnesium stearate 12 mg.

Film shell composition: hypromellose 5 mg, hyprolose 3.55 mg, macrogol-4000 2.1 mg, titanium dioxide 4.25 mg, quinoline yellow dye 0.1 mg.

10 pieces. - contour cellular packaging (aluminum/PVC) (1) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (2) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (3) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (4) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (5) - cardboard packs.
10 pieces. - contour cellular packaging (aluminum/PVC) (10) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (1) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (2) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (3) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (4) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (5) - cardboard packs.
20 pcs. - contour cellular packaging (aluminum/PVC) (10) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (1) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (2) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (3) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (4) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (5) - cardboard packs.
30 pcs. - contour cellular packaging (aluminum/PVC) (10) - cardboard packs.
10 pieces. - polymer jars (1) - cardboard packs.
20 pcs. - polymer jars (1) - cardboard packs.
30 pcs. - polymer jars (1) - cardboard packs.
40 pcs. - polymer jars (1) - cardboard packs.
50 pcs. - polymer jars (1) - cardboard packs.
100 pieces. - polymer jars (1) - cardboard packs.

In this article we will look at what types of thioctic acid preparations there are.

Thioctic (α-lipoic) acid has the ability to bind free radicals. Its formation in the body occurs during the oxidative decarboxylation of α-keto acids. It participates in the oxidative process of decarboxylation of α-keto acids and pyruvic acid as an enzyme of mitochondrial multienzyme complexes. In terms of biochemical action, this substance is close to B vitamins. Thioctic acid preparations help normalize neuronal trophism, lower glucose levels, increase the amount of glycogen in the liver, reduce insulin resistance, improve liver function, and are directly involved in the regulation of lipid and carbohydrate metabolism.

Pharmacokinetics

When administered orally, thioctic acid is rapidly absorbed. In 60 minutes it reaches maximum concentrations in the body. The bioavailability of the substance is 30%. After intravenous administration of thioctic acid 600 mg, the maximum plasma level is reached within 30 minutes.

Metabolism occurs in the liver through side chain oxidation and conjugation. The medication has a first pass property to the liver. The half-life is 30-50 minutes (via the kidneys).

Release form

Thioctic acid is produced in various dosage forms, in particular in solutions for infusion. Dosages also vary significantly depending on the form of release and brand of the drug.

Indications

Indications for the use of thioctic acid preparations are described in detail in the instructions. They are prescribed for diabetic and alcoholic polyneuropathy.

Contraindications

The list of contraindications to this drug includes:

  • lactose intolerance or deficiency;
  • galactose and glucose malabsorption;
  • lactation, pregnancy;
  • age less than 18 years;
  • high sensitivity to components.

Intravenous administration of the drug should be carried out with caution in people over 75 years of age.

Instructions for use

Thioctic acid preparations in tablet form are taken whole, 30 minutes before breakfast, with water. Recommended dosage is 600 mg once a day. Taking the tablets begins after a course of parenteral administration lasting 2-4 weeks. The maximum therapeutic course is no more than 12 weeks. Longer treatment is possible as prescribed by a doctor.

The concentrate for infusion solution is administered intravenously slowly. The solution should be prepared immediately before the infusion. The prepared product should be protected from sunlight; in this case, it can be stored for up to 6 hours. The course of using this medical form is 1-4 weeks, after which you should switch to tablet form.

Many people are interested in which thioctic acid preparation is better.

Side effects

The following pathological conditions occur as adverse reactions when using this medication:

  • vomiting, nausea, diarrhea, abdominal pain, heartburn;
  • allergic reactions (skin rashes, itching), anaphylactic shock;
  • disturbance of taste sensations;
  • hypoglycemia (excessive sweating, cephalalgia, dizziness, visual disturbances);
  • thrombocytopathy, purpura, in the mucous membranes and skin, hypocoagulation;
  • autoimmune insulin syndrome (in people with diabetes);
  • hot flashes, cramps;
  • increased activity of digestive enzymes;
  • pain in the heart area, with rapid administration of a pharmacological agent - increased heartbeat;
  • thrombophlebitis;
  • diplopia, blurred vision;
  • feeling of discomfort at the injection site, hyperemia, swelling.

With rapid administration of the drug, intracranial pressure may increase (passes on its own), difficulty breathing and weakness may occur.

Preparations containing this acid

The most common thioctic acid preparations are the following medications:

  • "Berlition".
  • "Lipothioxone".
  • "Octolipen".
  • "Tioctacid".
  • "Neurolipon".
  • "Tiogamma".
  • "Polition."
  • "Tiolepta".
  • "Espa-Lipon".

Medicine "Berlition"

The main active element of this pharmacological agent is alpha-lipoic acid, which is a vitamin-like substance that plays the role of a coenzyme in the process of oxidative decarboxylation of alpha-keto acids. It has antioxidant, hypoglycemic, and neurotrophic effects. Reduces the level of sucrose in the blood and increases the concentration of glycogen in the liver, reduces insulin resistance. In addition, this component regulates fat and carbohydrate metabolism and stimulates cholesterol metabolism.

In patients with diabetes mellitus of any type, thioctic acid changes the concentration of pyruvic acid in the blood, prevents the deposition of glucose on vascular proteins and the formation of final glycation elements. In addition, the acid promotes the production of glutathione, improves liver functionality in patients with hepatic pathologies and the function of the peripheral system in patients with diabetic sensory polyneuropathy. By participating in fat metabolism, thioctic acid is able to stimulate the production of phospholipids, as a result of which cell membranes are restored, energy metabolism and the sending of nerve impulses are stabilized.

The drug "Lipothioxone"

This thioctic acid preparation is an endogenous antioxidant that binds free radicals. Thioctic acid plays an important role in mitochondrial metabolism in cells, and functions as a coenzyme in the processes of transformation of substances that have antitoxic effects. They protect cells from radicals that arise during intermediate metabolism or during the breakdown of foreign exogenous substances, as well as from the influence of heavy metals. In addition, the main substance exhibits synergism with insulin, which is associated with an increase in glucose utilization. In diabetics, thioctic acid helps to change the level of pyruvic acid in the blood.

Medicine "Octolipen"

This is another medicine based on thioctic acid - a coenzyme of multienzyme mitochondrial groups that takes part in the process of oxidative decarboxylation of α-keto acids and pyruvic acid. This is an endogenous antioxidant: it eliminates free radicals, restores the level of glutathione inside cells, increases the functionality of superoxide dismutase, axonal conductivity and trophism of neurons. Plays an important role in energy metabolism, has lipotropic effectiveness, and improves liver function. It has a detoxification effect in cases of heavy metal poisoning and other intoxications.

During treatment with drugs based on thioctic acid, you should refrain from drinking alcoholic beverages. Patients with diabetes need regular monitoring of blood sugar levels, especially during the initial period of using a particular medication. To avoid the development of hypoglycemia, dosage adjustment of insulin or oral hypoglycemic medication may be necessary. If symptoms of hypoglycemia occur, the use of thioctic acid should be discontinued immediately. This is also advisable in cases of hypersensitivity reactions, such as skin itching and malaise.

Use of medications during pregnancy, lactation and children

According to the instructions for the use of drugs containing thioctic acid, these drugs are contraindicated during pregnancy and lactation. The use of these drugs in childhood is also contraindicated.

Drug interactions

It is necessary to maintain an interval of at least 2 hours when using thioctic acid with medications that contain metals, as well as with dairy products. Significant drug interactions of this acid are observed with the following substances:

  • cisplatin: its effectiveness decreases;
  • glucocorticosteroids: enhancing their anti-inflammatory effect;
  • ethanol and its metabolites: reducing the effects of thioctic acid;
  • oral hypoglycemic medications and insulin: their effects are enhanced.

These drugs in the form of concentrates for the preparation of infusion solution are incompatible with solutions of dextrose, fructose, Ringer's solution, as well as with solutions that react with SH- and disulfide groups.

Price of these drugs

The cost of medications containing thioctic acid varies significantly. Approximate price of tablets 30 pcs. at a dose of 300 mg is equal to - 290 rubles, 30 pcs. at a dose of 600 mg - 650-690 rubles.

Your doctor will help you choose the best thioctic acid preparation.

Thioctacid 600 T is a metabolic drug that regulates lipid and carbohydrate metabolism and has an antioxidant effect. Indications for treatment with Thioctacid are clinical manifestations of peripheral polyneuropathy in patients with diabetes mellitus. Thioctic acid protects the cell from the toxic “creeps” of free radicals formed during metabolic processes.

The drug is produced in the form of a solution for injection of a transparent yellowish color. You can also purchase Thioctacid in the form of tablets, film-coated, yellowish-greenish in color. Thioctic acid, which is part of it, is produced by the body. But with alcohol abuse, diabetes and a number of other diseases, the amount synthesized by the body is not enough for the normal functioning of nerve cells.

Active ingredient: thioctic acid (thioctic (-lipoic) acid). Thioic acid is a powerful endogenous antioxidant; its mechanism of action is very similar to vitamin B.

1 ampoule contains the active substance - trometamol thioctate - 952.3 mg, which is equivalent to the content of 600 mg of thioctic (-lipoic) acid.
1 film-coated tablet contains 600 mg of thioctic (-lipoic) acid.

People suffering from alcoholism, diabetes mellitus and a number of other serious diseases caused by metabolic disorders often experience a deficiency of adenosine triphosphoric (ATP) acid. An additional portion of the active metabolite restores the structure of nerve fibers and increases their functionality.

Short-acting tablets are simply called Thioctacid, and long-acting tablets are called Thioctacid BV. The concentrate for preparing a solution for intravenous infusion is correctly called Thioctacid 600.

The main component of the drug is an endogenous antioxidant, the presence of which in the body ensures:

  • normalization of neuronal trophism;
  • enhanced glucose removal;
  • protecting cells from the effects of toxins and free radicals;
  • reduction of symptoms of pathology.

Thus, Thioctacid 600, according to the official instructions for use, has hypolipidemic, hepatoprotective, hypoglycemic and hypocholesterolemic effects. The drug is successfully used for the treatment and prevention of neuropathy and sensitivity disorders caused by this pathology in alcoholism and diabetes. Reviews from doctors and patients about Thioctacid 600 confirm the high effectiveness of the drug.

Indications for use Thioctacid 600

Indications for use of Thioctacid 600 are:

  • diabetic and alcoholic polyneuropathy,
  • hyperlipidemia,
  • fatty liver degeneration,
  • liver cirrhosis and hepatitis,
  • intoxication (including salts of heavy metals, toadstool),
  • treatment and prevention of coronary atherosclerosis.

Instructions for use Thioctacid 600, dosage

Standard dosages

Thioctacid 600 injections are administered intravenously (stream, drip). Tablets Thioctacid 600 - dosage 600 mg/day for 1 dose (in the morning on an empty stomach 30-40 minutes before breakfast), prescription 200 mg 3 times a day is less effective.

Special

In severe forms of polyneuropathies - slowly (50 mg/min), 600 mg or IV drip, 0.9% NaCl solution once a day (in severe cases, up to 1200 mg is administered) for 2-4 weeks. Subsequently, they switch to oral therapy (adults – 600-1200 mg/day, adolescents – 200-600 mg/day) for 3 months. IV administration is possible using a perfuser (duration of administration is at least 12 minutes).

The method of treating patients suffering from diabetic polyneuropathy with thioctacid is well established and has a solid scientific and practical basis. Therapy begins with the administration of thioctacid intravenously at a dose of 600 mg for two weeks.

When treating with potent medications and Thioctacid simultaneously, you should strictly follow the recommendations of your doctor.

Features of application

Many patients complain about the long time it takes to administer the drug Thioctacid 600 T in the form of a solution for intravenous infusion. Despite this, doctors recommend this particular form of the drug at the beginning of treatment for the disease. It is completely absorbed and allows you to titrate the effective dosage as accurately as possible.

When using the drug, you should refrain from driving vehicles and working with potentially dangerous mechanisms.

If there is a need to take these drugs simultaneously, then you need to maintain an interval of five to six hours between taking them.

The drug in ampoules is not exposed to light until direct use. The prepared solution is used within six hours and protected from light.

Drinking alcohol may reduce the effectiveness of the drug. Therefore, it is recommended to refrain from drinking any liquids containing alcohol during treatment with the drug.

Combine with caution with metal-containing drugs, cisplatin, insulin, and medications for diabetes.

At the initial stages of treatment, it is possible that the discomfort of neuropathy may increase, which is associated with the process of restoring the structure of the nerve fiber.

Side effects and contraindications Thioctacid 600

With rapid intravenous administration of Thioctacid 600 T, intracranial pressure can sometimes increase and breathing may be delayed. As a rule, these disorders go away on their own.

During the use of Thioctacid, in some cases the level of glucose in the blood may decrease (due to improved utilization). In this case, hypoglycemia may occur, the main symptoms of which are: dizziness, headache, increased sweating (hyperhidrosis) and visual disturbances.

Thioctic acid INN

International name: Thioctic acid

1.Dosage form: concentrate for the preparation of solution for infusion, solution for intramuscular administration, solution for infusion

Chemical name:

1, 2 - dithiolane - 3 - pentanoic acid (as amide or trometamol or sodium salt)

Pharmachologic effect:

Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of alpha-ketoxylots. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and alpha-keto acids. Helps reduce blood glucose concentrations and increase glycogen in the liver, as well as overcome insulin resistance. By the nature of its biochemical action it is close to B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function. It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects. Improves trophism of neurons. The use of trometamol salt of thioctic acid in solutions for intravenous administration (which has a neutral reaction) can reduce the severity of adverse reactions.

Pharmacokinetics:

Bioavailability - 30%. Has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Volume of distribution is about 450 ml/kg. The main metabolic pathways are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T1/2 - 20-50 min. Total plasma clearance is 10-15 ml/min.

Indications:

Diabetic and alcoholic polyneuropathy.

Contraindications:

Hypersensitivity, children's age (efficacy and safety of use have not been established). Caution. Pregnancy, lactation period.

Dosage regimen:

IV (stream, drip), IM. In severe forms of polyneuropathy - slowly (50 mg/min), 600 mg or IV drip, 0.9% NaCl solution once a day (in severe cases, up to 1200 mg is administered) for 2-4 weeks. IV administration is possible using a perfuser (duration of administration is at least 12 minutes). When administered intramuscularly to the same place, the dose of the drug should not exceed 50 mg. Subsequently, they switch to oral therapy for 3 months.

Side effects:

Allergic reactions (urticaria, itching, anaphylactic shock). With intravenous administration - pinpoint hemorrhages in the mucous membranes, skin, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis, increased intracranial pressure (rapid administration), difficulty breathing, hypoglycemia (due to improved glucose absorption), convulsions, diplopia. Overdose . Symptoms: unknown to date. Treatment: symptomatic. There is no specific antidote.

Special instructions:

During treatment, you must strictly abstain from drinking ethanol. In patients with diabetes, especially at the beginning of treatment, frequent monitoring of blood glucose is necessary. The drug is photosensitive, so ampoules should be removed from the packaging only immediately before use.

Interaction:

Reduces the effectiveness of cisplatin. Strengthens the effect of insulin and oral hypoglycemic drugs. Incompatible with Ringer's and dextrose solutions, compounds (including their solutions) that react with disulfide and SH groups, ethanol. Ethanol and its metabolites weaken the effect.

2.Dosage form: film-coated tablets

Pharmachologic effect:

A coenzyme of mitochondrial multienzyme complexes, involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids, plays an important role in the energy balance of the body. By the nature of the biochemical action, thioctic (alpha-lipoic) acid is similar to B vitamins. It is an endogenous antioxidant. Participates in the regulation of lipid and carbohydrate metabolism, has a lipotropic effect, affects cholesterol metabolism, improves liver function, has a detoxification effect in case of poisoning with heavy metal salts and other intoxications. The effect on carbohydrate metabolism is expressed in a decrease in the concentration of glucose in the blood and an increase in glycogen in the liver, as well as in overcoming insulin resistance. Improves trophism of neurons.

Pharmacokinetics:

When taken orally in doses of 200-600 mg, it is quickly and completely absorbed from the gastrointestinal tract; taking it simultaneously with food reduces absorption. Bioavailability - 30-60% due to the “first pass” effect through the liver. TCmax - 25-60 min. Metabolized in the liver by side chain oxidation and conjugation. Volume of distribution - 450 ml/kg. Total clearance - 10-15 ml/min. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T1/2 - 20-50 min.

Indications:

Tablets 12 mg and 25 mg: fatty liver, cirrhosis of the liver, chronic hepatitis, hepatitis A, intoxication (including salts of heavy metals, toadstool), hyperlipidemia (including leading to the development of coronary atherosclerosis - treatment and prevention). Tablets 200 mg, 300 mg, 600 mg: diabetic and alcoholic polyneuropathy.

Contraindications:

Hypersensitivity, lactation period, children under 6 years of age (up to 18 years in the treatment of diabetic and alcoholic neuropathy). Caution. Pregnancy.

Dosage regimen:

Treatment of liver diseases and intoxications (tablets 12 mg and 25 mg): orally, adults - 50 mg 3-4 times a day. Children over 6 years old - 12-24 mg 2-3 times a day. The course of treatment is 20-30 days. If necessary, it is possible to conduct a second course after 1 month. Treatment of diabetic and alcoholic neuropathy (tablets 200 mg, 300 mg and 600 mg): orally, on an empty stomach, 30 minutes before meals (breakfast), without chewing, with water, 400-600 mg once a day. Treatment begins with parenteral administration.

Side effects:

Dyspepsia (including nausea, heartburn, vomiting, diarrhea, abdominal pain), allergic reactions (including urticaria, skin rash, itching and systemic allergic reactions up to anaphylactic shock), hypoglycemia. Overdose. Symptoms (when using 10-40 g): generalized convulsions, severe impairment of CBS with lactic acidosis, hypoglycemic coma, severe bleeding disorders, incl. with fatal outcome. Treatment: gastric lavage, induction of vomiting, activated charcoal, symptomatic therapy.

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 avoid drinking ethanol.

Interaction:

Strengthens the anti-inflammatory effect of GCS. Reduces the effectiveness of cisplatin. Strengthens the effect of insulin and oral hypoglycemic drugs (their dose adjustment is necessary to avoid hypoglycemia). Binds metals, so it should not be prescribed simultaneously with drugs containing metal ions (preparations Fe, Mg2+, Ca2+). The interval between doses should be at least 2 hours. Ethanol and its metabolites weaken the effect.

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