Thioctic acid - instructions for use, dose, side effects, contraindications

Thioktovaya (alpha-lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. As a coenzyme mitochondrial multienzyme complexes is involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids.Helps to reduce the concentration of glucose in the blood plasma and increase the concentration of glycogen in the liver, as well as overcoming insulin resistance. By the nature of the biochemical action is close to the vitamins of group B. It participates in the regulation of carbohydrate and lipid metabolism, stimulates the exchange of cholesterol. Has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic action. Improves trophic neurons.

With diabetes mellitus thioctic acid reduces the formation of final glycation products, improves endoneural blood flow, increases the glutathione content to a physiological value, which as a result leads to an improvement in the functional state of peripheral nerve fibers in diabetic polyneuropathy. Through the participation in the metabolism of fats, thioctic acid increases the biosynthesis of phospholipids, in particular, phosphoinositides, restoring the damage to cell membranes; normalizes the energy exchange and the conduct of nerve impulses. Thioctic acid eliminates the toxic effect of alcohol metabolites (acetaldehyde, pyruvic acid),reduces excessive formation of molecules of free oxygen radicals, reduces endonevralnuyu hypoxia and ischemia, weakening manifestations of polyneuropathy in the form of paresthesia, a burning sensation, pain and numbness of the extremities.

In this way, thioctic acid has an antioxidant, neurotrophic effect, improves lipid metabolism.

Pharmacokinetics:

Distribution

With intravenous administration of thioctic acid at a dose of 600 mg, the maximum plasma concentration in 30 minutes is about 20 μg / ml. The area under the concentration-time curve is about 5 μg / h / ml. Bioavailability is 30%. Thioctic acid has the effect of "first passage" through the liver. The formation of metabolites occurs as a result of oxidation of the side chain and conjugation. The volume of distribution is about 450 ml / kg.

Metabolism and excretion

Thioctic acid and its metabolites are excreted by the kidneys mainly in the form of metabolites (80-90%), in small amounts - in unchanged form. The half-life is 25 minutes. The total plasma clearance is 10-15 ml / min / kg.

Indications:

- Diabetic polyneuropathy;

- alcoholic polyneuropathy.

Contraindications:

- Hypersensitivity to tioctovirus (alpha-lipoic) acid or to other components of the drug;

- pregnancy, the period of breastfeeding (there is insufficient experience in using the drug);

- age to 18 years (efficacy and safety of the drug are not established).

Carefully:

Intravenous administration of the drug should be conducted with caution in elderly patients (over 75 years of age).

Pregnancy and lactation:

The use of thioctic acid during pregnancy is contraindicated due to the lack of sufficient experience of use.

It is not known whether the thioctic acid (α-lipoic acid) into the mother's milk. If you need to use the drug during breastfeeding, breastfeeding should be discontinued.

Dosing and Administration:

For intravenous administration.

At the beginning of treatment the drug is administered intravenously drip in a daily dose of 600 mg (2 ampoules).

Before use, the contents of 2 ampoules (20 ml) are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously drip slowly, for at least 30 minutes. Since the active substance is sensitive to light, the infusion solution is prepared immediately prior to use.The prepared solution must be protected from exposure to light, for example, using aluminum foil. The light-shielded solution can be stored for about 6 hours.

The course of treatment is 2-4 weeks. Then they switch to maintenance therapy with an oral form of thioctic acid at a dose of 600 mg per day. The duration of the course of treatment and the need for its recurrence is determined by the doctor.

Side effects:

Possible side effects when using the drug are given below on the descending frequency of occurrence: often (≥ 1/100 to <1/10); infrequently (≥ 1/1000 to <1/100); rarely (≥1 / 10000 to <1/1000); rarely (<1/10000), including individual messages. Correlations of the incidence of side effects with the sex or age of patients are not observed.

Disturbances from the hematopoiesis and lymphatic system: very rarely - petechial hemorrhages in mucous membranes, skin; hemorrhagic rash (purpura), thrombocytopathy, hypocoagulation.

Immune system disorders: very rarely - allergic reactions (skin rash, eczema, urticaria, skin itching); frequency unknown - anaphylactic shock; autoimmune insulin syndrome in patients with diabetes mellitus,which is characterized by frequent hypoglycemia in the presence of autoantibodies to insulin.

Disorders from the metabolism and nutrition: very rarely - hypoglycemia (due to improved glucose uptake), the symptoms of which include dizziness, increased sweating, headache and visual impairment.

Disturbances from the nervous system: very rarely - a change or violation of taste, "hot flashes", cramps.

Disorders from the gastrointestinal tract: often - nausea, vomiting; rarely - pain in the abdomen, diarrhea.

Disturbances from the liver and bile ducts: rarely - Increased activity of "liver" enzymes.

Heart Disease: frequency unknown - pain in the heart, tachycardia with rapid administration of the drug.

Vascular disorders: rarely - Thrombophlebitis.

Disturbances on the part of the organ of sight: rarely - Diplopia, blurred vision.

General disorders and disorders at the site of administration: very rarely - a burning sensation at the injection site, the frequency is unknown - allergic reactions at the injection site - irritation, flushing or swelling.

Other: very rarely - with rapid intravenous injection, there were self-reported increases in intracranial pressure (a feeling of heaviness in the head) and difficulty in breathing, weakness.

Overdose:

Symptoms: headache, nausea, vomiting.

In severe cases (with the use of thioctic acid in a dose of 10-40 g): psychomotor agitation or impaired consciousness, generalized convulsions, severe acid-base balance with lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, DIC syndrome , hemolysis, bone marrow suppression, multi-organ failure.

Treatment: when an overdose of thioctic acid is suspected, emergency hospitalization is recommended. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of overdose should be conducted in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion or filtration methods with forced excretion of thioctic acid are ineffective.

Interaction:

Due to thioctic acid is capable of forming chelate complexes with metals, joint use with preparations of iron, magnesium, and calcium should be avoided.

The simultaneous use of thioctic acid with cisplatin reduces the effectiveness of the latter.

With sugar molecules thioctic acid forms poorly soluble complex compounds. Thioctic acid It is incompatible with solutions of dextrose (glucose), fructose, Ringer, and also with solutions reacting with disulfide or SHgroups.

Thioctic acid enhances the hypoglycemic action of insulin and hypoglycemic drugs for oral administration when combined.

Thioctic acid enhances the anti-inflammatory effect of glucocorticosteroids.

Ethanol and its metabolites reduce the therapeutic efficacy of thioctic acid.

Special instructions:

Patients with diabetes require constant monitoring of the concentration of glucose in the blood plasma, especially at the initial stage of therapy with the drug Thioctic acid. In some cases, it may be necessary to reduce the dose of insulin or hypoglycemic drugs for oral use in order to avoid the development of hypoglycemia.If symptoms of hypoglycemia occur (dizziness, increased sweating, headache, visual disturbance, nausea), stop the injection immediately.

With parenteral application, hypersensitivity reactions may occur. When symptoms appear, such as itching, malaise, drug treatment Thioctic acid should be stopped immediately.

Alcohol intake reduces the effectiveness of drug treatment, so patients during drug therapy Thioctic acid should refrain from drinking alcohol throughout the course of treatment, and, if possible, in the intervals between courses. The use of alcohol during treatment with thioctic acid is also a risk factor for the development and progression of neuropathy.

Prepared solution of the drug should be protected from exposure to light.

Several cases of autoimmune insulin syndrome development in patients with diabetes mellitus have been described against thioctic acid therapy, which was characterized by frequent hypoglycemia in the presence of autoantibodies to insulin. The possibility of developing an autoimmune insulin syndrome is determined by the presence in patients of haplotypes HLA-DRB1 * 0406 and IILA-DRB1 *0403.

Effect on the ability to drive transp. cf. and fur:

The effect of the drug on the ability to drive vehicles and control mechanisms is not specifically studied, so during the period of drug treatment Thioctic acid caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Concentrate for solution for infusion, 30 mg / ml.

Packaging:

For 10 ml in ampoules of light-protective neutral glass type I with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch. One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding can additionally be applied to the ampoules.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film or without foil and without film. Or 5 ampoules are placed in a prefabricated form (tray) made of cardboard with cells for laying ampoules.

1 or 2 contour squares or cardboard trays, together with the instruction for use and the ampoule ampoule or ampoule scarifier, or without the ampoule ampoule ampoule scraper and ampoule ampoule are placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003918

Date of registration:21.10.2016

Expiration Date:21.10.2021

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp11.11.2016

Illustrated instructions

Instructions

Thioctic acid (Thioctic acid)