Polythion - instructions for use, doses, side effects, contraindications

Thioctic acid (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 lipid and carbohydrate 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 the excess formation of free oxygen radical molecules, reduces endonevral hypoxia and ischemia, weakening manifestations of polyneuropathy in the form of paresthesias, burning sensations, pain and numbness of the limbs. In this way, thioctic acid has an antioxidant, neurotrophic effect, improves lipid metabolism.

Pharmacokinetics:

Absorption and distribution. With intravenous administration of thioctic acid, the maximum concentration in the blood plasma after 30 minutes is about 20 μg / ml, the area under the concentration-time curve (AUC) 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 (T ½) about 25 minutes. The total plasma clearance is 10-15 ml / min / kg.

Indications:

- diabetic polyneuropathy;

- alcoholic polyneuropathy.

Contraindications:

- hypersensitivity to thioctic acid or other components of the drug.

- pregnancy, the period of breastfeeding (there is insufficient experience of the drug).

- age to 18 years (efficacy and safety of application not established).

Pregnancy and lactation:Application during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

The drug is designed to prepare a solution for infusion for intravenous administration after preliminary dilution in a 0.9% solution of sodium chloride.

1 ampoule of the preparation in volume of 12 ml contains 300 mg of thioctic acid.

1 ampoule of the drug in the volume of 24 ml contains 600 mg of thioctic acid.

The drug should be administered in a dose of 600 mg (1 ampoule with a volume of 24 ml or 2 ampoules of 12 ml) once a day as an intravenous drip infusion.

Before use, the contents of one ampoule with a volume of 24 ml or two ampoules of 12 ml are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously drip, slowly, at a rate of no more than 2 ml / min.

The drug has photosensitivity, so the ampoule should be removed from the package immediately before use. During the infusion, the bottle with the solution is protected from light. The prepared solution should be stored in a dark place and used within 6 hours after preparation.

The drug in the form of a solution for infusions is recommended to be applied within 2-4 weeks. Then, you can continue to take thioctic acid in its oral form in a daily dose 300-600 mg. The duration of treatment and the need for its recurrence is determined by the doctor.

Side effects:

Possible side effects when using the drug are presented below in accordance with the frequency of occurrence: often (≥1/100, < 1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, < 1/1000), rarely (< 1/10000), including individual messages.

From the nervous system. Rarely: change or violation of taste sensations, diplopia, convulsions.

From the hemopoietic system and lymphatic system. Rarely: Spot hemorrhages in mucous membranes, skin; Thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis.

From the side of metabolism. Rarely: decrease in the concentration of glucose in the blood plasma (due to improved glucose uptake), hypoglycemia (dizziness, increased sweating, headache and visual impairment).

From the immune system. Rarely: allergic reactions such as skin rash, eczema, urticaria, itching, in isolated cases - anaphylactic shock.

Reactions at the site of administration. Rarely: burning sensation at the injection site. In some cases: allergic reactions at the injection site - irritation, flushing or swelling.

Other. Rarely: with rapid intravenous administration observed spontaneously passing increase in intracranial pressure (a feeling of heaviness in the head) and difficulty breathing.

Overdose:

Symptoms: headache, nausea, vomiting.

In severe cases: psychomotor agitation or confusion, generalized convulsions, severe acid-base balance disorders, lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, syndrome of disseminated intravascular coagulation (DVS-syndrome), hemolysis, suppression of bone marrow, multi-organ failure.

Treatment: when suspected of intoxication with thioctic acid (eg, the administration of more than 80 mg of thiocyte acid per 1 kg of body weight), urgent hospitalization is recommended and immediate application of the measures in accordance with the general principles adopted for accidental poisoning. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening consequences should be carried out in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion or filtering techniques with positive derivation of thioctic acid are not effective.

Interaction:

With the simultaneous use of thioctic acid and cisplatin, there is a decrease in the effectiveness of cisplatin. Thioctic acid binds metals, so it should not be used simultaneously with preparations containing metals (for example, preparations of iron, magnesium, calcium).

With simultaneous use with insulin or oral hypoglycemic agents, an increase in the hypoglycemic effect is observed.

Thioctic acid forms difficultly soluble complex compounds with sugar molecules (for example, a solution of levulose), therefore, the drug is incompatible with a solution of glucose (dextrose), Ringer's solution, and also with compounds (including their solutions) reacting with disulfide and SH - groups. Only 0,9% solution of sodium chloride can serve as a solvent for the preparation.

Enhances the anti-inflammatory effect of glucocorticosteroids.

Ethanol and its metabolites weaken the action of thioctic acid.

Special instructions:

Patients with diabetes, especially at the beginning of treatment, need constant monitoring of blood glucose. In some cases, a reduction in the dose of insulin or an oral hypoglycemic drug is required to avoid the development of hypoglycemia. If symptoms of hypoglycemia occur (dizziness, increased sweating, headache, visual disturbance, nausea), stop the injection immediately.

During treatment, it is necessary to strictly refrain from drinking alcohol, because when the effect of alcohol therapeutic effect of thioctic acid is weakened.

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

During treatment, it is advisable to use caution when driving vehicles and engaging in other potentially hazardous activities that require concentration and speed of psychomotor reactions.

Form release / dosage:

Concentrate for the preparation of a solution for infusions of 25 mg / ml.

Packaging:

For 12 or 24 ml in dark glass ampoules with a kink ring.

Five ampoules are placed in a contour mesh box made of a polyvinyl chloride film or a polyethylene terephthalate tape and aluminum foil, or paper with a polyethylene coating, or without a foil, or without paper.

For 1 or 2 contour mesh packages with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 2 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003539

Date of registration:29.03.2016

Expiration Date:29.03.2021

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp01.08.16

Illustrated instructions

Instructions

Polition (Polition)