Alpha-lipoic acid

Concentrate for preparation of solution for infusions and solution for infusions

V/v, in the form of infusions, administered slowly (for 30 minutes) at a dose of 600 mg/day. The recommended course of application is 2-4 weeks. Then you can continue taking the oral form of the drug Tiogamma^® at a dose of 600 mg/day.

The vial with the infusion solution is removed from the box and immediately covered with the attached light-proof case, since thioctic acid is sensitive to light. The infusion is made directly from the bottle. The injection rate is about 1.7 ml/min.

A solution for infusions is prepared from the concentrate: the contents of 1 ampoule (contains 600 mg of thioctic acid) are mixed with 50-250 ml of 0.9% sodium chloride solution. Immediately after preparation, the bottle with the resulting solution for infusions is covered with a light-proof case. The infusion solution should be administered immediately after preparation. The maximum storage time of the prepared solution for infusions is no more than 6 hours.

Coated tablets

Inside, 1 time a day, on an empty stomach, without chewing and drinking a small amount of liquid. The duration of the course of treatment is 30-60 days, depending on the severity of the disease. It is possible to repeat the course of treatment 2-3 times a year.

Inside, on an empty stomach, 30 minutes before meals, without chewing, with a sufficient amount of liquid.

According to 1 table./2 caps. (600 mg) 1 time a day. Step-by-step therapy is possible: tablets are taken after a 2-4-week course of parenteral administration of thioctic acid. The maximum course of taking tablets is 3 months. In some cases, taking the drug involves a longer use, the timing of which is determined by the doctor.

In some (severe) cases, treatment begins with the appointment of the drug Alpha-lipoic acid^®, solution for intravenous administration, for 2-4 weeks, then transferred to treatment with an oral form of the drug Alpha-lipoic acid^® (step therapy).

The type and duration of the course of therapy are determined by the doctor.

V/v (in the form of drip infusions). The drug is pre-diluted in an isotonic solution of sodium chloride.

In severe forms of diabetic or alcoholic polyneuropathy, 300-600 mg should be administered once a day in the form of an intravenous drip infusion. The duration of the infusion is 50 minutes. The drug is recommended to be used for 2-4 weeks.

Then you can continue taking thioctic acid orally at a dose of 300-600 mg/day. The minimum duration of treatment with tablets is 3 months.

In/in, inside. In severe forms of polyneuropathy, intravenous administration of 12-24 ml (300-600 mg of alpha-lipoic acid) per day for 2-4 weeks. To do this, 1-2 ampoules of the drug are diluted in 250 ml of a physiological 0.9% sodium chloride solution and administered drip for about 30 minutes. In the future, they switch to maintenance therapy with Alpha-lipoic acid in the form of tablets at a dose of 300 mg per day.

For the treatment of polyneuropathy — 1 table 1-2 times a day (300-600 mg of alpha-lipoic acid).

In/in. Adults at a dose of 600 mg/day. Enter slowly — no more than 50 mg/min of thioctic acid (1.7 ml of solution for infusions).

The drug should be administered by infusion with 0.9% sodium chloride solution 1 time per day (600 mg of the drug is mixed with 50-250 ml of 0.9% sodium chloride solution). In severe cases, up to 1200 mg can be administered. Infusion solutions should be protected from light by covering them with light shields.

The course of treatment is from 2 to 4 weeks. After that, they switch to maintenance therapy with medicinal forms of thioctic acid for oral administration at a dose of 300-600 mg/day for 1-3 months. To consolidate the effect of treatment, the course of therapy with Alpha-lipoic acid is recommended to be carried out 2 times a year.

The efficacy and safety of the drug in children have not been established.

hypersensitivity to thioctic acid or other components of the drug,

pregnancy,

breastfeeding period,

children under 18 years of age.

Additionally, the coated tablets

hereditary galactose intolerance,

lactase deficiency,

glucose-galactose malabsorption.

Before taking the drug, you should consult your doctor.

hypersensitivity (to thioctic acid and the components of the drug),

pregnancy (there is no sufficient experience of using the drug),

the period of breastfeeding (there is no sufficient experience of using the drug),

children under 18 years of age (efficacy and safety have not been established).

hypersensitivity to the components of the drug,

children under 18 years of age (efficacy and safety of use have not been established).

Hypersensitivity, pregnancy, breast-feeding. Do not prescribe to children and adolescents (due to the lack of clinical experience with the use of this drug).

The frequency of adverse adverse reactions is given in accordance with the WHO classification: very common (more than 1/10), common (less than 1/10, but more than 1/100), on occasion (less than 1/100, but more than 1/1000), rare (less than 1/1000, but more than 1/10000), very rare (less than 1/10000, including individual cases).

From the hematopoietic system and the lymphatic system: spot hemorrhages in the mucous membranes, skin, thrombocytopenia, thrombophlebitis-very rare (for r-ra d / inf.), thrombopathy-very rare (for conc. for r-ra d / inf.), hemorrhagic rash (purpura) - very rarely (for conc. for r-ra d/inf. and r-ra d/inf.).

On the part of the immune system: systemic allergic reactions (up to the development of anaphylactic shock) - very rarely (for the table), in some cases (for the end. for r-ra d/inf. and r-ra d/inf.).

From the central nervous system: change or violation of taste sensations-very rare (for all forms), epileptic seizure-very rare (for conc. for r-ra d/inf.), convulsions-very rarely (for r-ra d/inf.).

On the part of the visual organ: diplopia-very rare (for conc. for r-ra d/inf. and r-ra d/inf.).

From the skin and subcutaneous tissue: allergic skin reactions (urticaria, itching, eczema, rash) - very rarely (for the table), in some cases (for the end. for r-ra d/inf. and r-ra d/inf.).

From the gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea — very rarely (for Table).

Other adverse reactions: allergic reactions at the injection site (irritation, redness or swelling) — very rare (for the end. for r-ra d/inf.), in some cases (for r-ra d/inf.), in the case of rapid administration of the drug, an increase in ICP is possible (there is a feeling of heaviness in the head), difficulty breathing (these reactions pass independently) - often (for conts. for r-ra d/inf.), very rarely (for r-ra d/inf.), due to improved glucose uptake, a decrease in blood glucose concentration may occur, while symptoms of hypoglycemia may occur (dizziness, increased sweating, headache, vision disorders) — very rare (for the end. for r-ra d/inf. and table.), in some cases (for r-ra d/inf.)

If any of these side effects have worsened or there are any other side effects that are not specified in the instructions, you should inform your doctor.

Possible side effects when using Alpha-lipoic acid^® given by descending frequency of occurrence: very often (>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 sensations.

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

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

General character: very rarely-due to improved glucose utilization, blood glucose levels may decrease and symptoms of hypoglycemia may appear (confusion, increased sweating, headache, vision disorders).

With intravenous administration, seizures, diplopia, spot hemorrhages in the mucous membranes, skin, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis are very rare.

With rapid administration, it is possible to increase ICP (the appearance of a feeling of heaviness in the head), difficulty breathing. The listed side effects go away on their own.

Possible allergic reactions: urticaria, systemic allergic reactions (up to the development of anaphylactic shock).

Perhaps the development of hypoglycemia (in connection with the improvement of glucose uptake).

Solution for injection: sometimes a feeling of heaviness in the head and difficulty breathing (with rapid intravenous administration). There may be allergic reactions at the injection site with the appearance of urticaria or a burning sensation. In some cases — convulsions, diplopia, spot hemorrhages in the skin and mucous membranes.
Coated tablets: in some cases — skin allergic reactions.

It is possible to reduce the level of sugar in the blood.

Symptoms: nausea, vomiting, headache.

In the case of taking doses of 10 to 40 g of thioctic acid in combination with alcohol, cases of intoxication were observed, up to a fatal outcome.

Symptoms of acute overdose: psychomotor agitation or confusion, usually followed by the development of generalized seizures and lactic acidosis. Cases of hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation, bone marrow depression, and multi-organ failure are also described.

Treatment: symptomatic. There is no specific antidote.

Symptoms: headache, nausea, vomiting.

In the case of taking thioctic (alpha-lipoic) acid in doses of 10-40 g, serious signs of intoxication may be noted (generalized convulsions, severe acid-base balance disorders leading to lactate acidosis, hypoglycemia, up to hypoglycemic coma, severe blood clotting disorders, sometimes leading to death). If a significant overdose of the drug is suspected (more than 10 tablets for an adult or more than 50 mg/kg for a child), immediate hospitalization is required.

Treatment: there is no specific antidote. Treatment is symptomatic, if necessary — anticonvulsant therapy, measures to maintain the function of vital organs.

Symptoms: headache, nausea, vomiting.

Treatment: symptomatic. There is no specific antidote.

Symptoms: headache, nausea, vomiting.
Treatment: symptomatic therapy. There is no specific antidote.

Thioctic acid is an endogenous antioxidant (binds free radicals). The body is formed in the oxidative decarboxylation of alpha-ketoximes. As a coenzyme of mitochondrial multi-enzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and alpha-keto acids.

It helps to reduce the concentration of glucose in the blood and increase glycogen in the liver, as well as reduce insulin resistance. Participates in the regulation of lipid and carbohydrate metabolism, affects the metabolism of cholesterol, improves liver function, has a detoxifying effect in poisoning with heavy metal salts and other intoxications. It has a hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect. Improves the trophism of neurons.

In diabetes mellitus, thioctic acid reduces the formation of glycation end products, improves endoneural blood flow, increases the content of glutathione to a physiological value, which as a result leads to an improvement in the functional state of peripheral nerve fibers in diabetic polyneuropathy.

Thioctic acid (alpha-lipoic acid) is found in the human body, where it acts as a coenzyme in the oxidative phosphorylation reactions of pyruvic acid and alpha-keto acids. Thioctic acid is an endogenous antioxidant. Thioctic acid helps to protect the cell from the toxic effects of free radicals that occur in the metabolic processes, it also neutralizes exogenous toxic compounds. 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 a hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect, improves the trophism of neurons. The result of the synergistic action of thioctic acid and insulin is an increase in glucose utilization.

Thioctic acid (α-lipoic acid) is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of α-keto acids. As a coenzyme of mitochondrial multi-enzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and α-keto acids. It helps to reduce the concentration of glucose in the blood and increase glycogen in the liver, as well as to 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, improves liver function. It has a hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect. Improves neuron trophism

When taken orally, it is quickly and completely absorbed into the gastrointestinal tract, while taking it with food reduces absorption. Bioavailability-30-60% due to the effect of the first passage through the liver. T_maxabout 30 min., C_max — 4 mcg/ml.

With the I / V introduction of T_max — 10-11 min, C_max it is about 20 mcg/ml.

It has the effect of first passing through the liver. It is metabolized in the liver by side chain oxidation and conjugation. The total plasma clearance is 10-15 ml / min. Thioctic acid and its metabolites are excreted by the kidneys (80-90%), in a small amount — in unchanged form. T_1/2 — 25 min.

When taken orally, it is quickly and completely absorbed into the gastrointestinal tract, taking simultaneously with food can reduce the absorption of the drug.

Taking the drug, according to the recommendations, 30 minutes before meals allows you to avoid unwanted interaction with food, because the absorption of thioctic acid at the time of eating is already completed. C_max thioctic acid in the blood plasma is reached 30 minutes after taking the drug and is 4 mcg/ml. Thioctic acid has the effect of first passing through the liver. The absolute bioavailability of thioctic acid is 20%.

The main metabolic pathways are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T_1/2 — 25 min.

At the I / V introduction of C_max it is 25-38 mcg / ml, T_max10-11 min, AUC-about 5 mcg h / ml. Bioavailability of 30%.

Thioctic acid has the effect of first passing through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. V_d - about 450 ml / kg — Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T_1/2 — 20-50 min. The total plasma clearance is 10-15 ml / min.

When taken orally, it is quickly and completely absorbed from the gastrointestinal tract (ingestion with food lowers absorption). Time to reach C_max — 40-60 min. Bioavailability of 30%. It has the effect of "first pass" through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. The 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%). T_1/2 — 20-50 min. Total plasma Cl — 10-15 ml / min.

With the simultaneous administration of thioctic acid and cisplatin, there is a decrease in the effectiveness of cisplatin.

Thioctic acid binds metals, so it should not be prescribed simultaneously with preparations containing metal ions (for example, preparations of iron, magnesium, calcium). The interval between the reception should be at least 2 hours.

Increases the anti-inflammatory effect of GCS.

With the simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may increase.

Ethanol and its metabolites weaken the effect of thioctic acid.

Additionally for concentrate for preparation of infusion solution and infusion solution

Thioctic acid reacts with sugar molecules to form hardly soluble complexes, for example, with a solution of levulose (fructose). Infusion solutions of thioctic acid are incompatible with a solution of dextrose, Ringer and solutions that react with disulfide and SH-groups.

With the simultaneous administration of thioctic acid and cisplatin, there is a decrease in the effectiveness of cisplatin.

Thioctic acid binds metals, so it should not be prescribed simultaneously with preparations containing metals (for example, preparations of iron, magnesium, calcium). According to the recommended method of use, tablets of the drug Alpha-lipoic acid^® take 30 minutes before breakfast, while preparations containing metals should be taken at lunch or in the evening. For this reason, during the period of treatment it is recommended that the consumption of dairy products in the second half of the day.

With the simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may increase, so 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 in order to avoid the development of symptoms of hypoglycemia.

Ethanol and its metabolites weaken the effect of thioctic acid.

alpha-lipoic acid (in the form of an infusion solution) reduces the effect of cisplatin.

When used simultaneously with insulin and other oral hypoglycemic agents, an increase in the hypoglycemic effect is observed.

α-Lipoic acid forms complex compounds with sugar molecules (for example, levulose solution) that are difficult to dissolve, and therefore it is incompatible with glucose solution, Ringer's solution, as well as with compounds (including their solutions) that react with disulfide and SH groups.

Weakens the effect of cisplatin, increases the effect of hypoglycemic drugs.