Thiolipone - instructions for use, dose, side effects, contraindications

Thioctic acid (alpha lipoic acid) - an endogenous antioxidant (binds free radicals), in the body is formed during the oxidative decarboxylation of alpha-keto acids. As a coenzyme mitochondrial multienzyme complexes is involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids.Helps reduce blood glucose and glycogen in the liver, as well as overcome 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, improves liver function. Has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic action. Improves trophic neurons.

Pharmacokinetics:

With intravenous administration, the time to reach the maximum concentration is 10-11 minutes, the maximum concentration is 25-38 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. Thioktovaya. acid and its metabolites are excreted by the kidneys (80-90%). Half-life is 20-50 minutes. The total plasma clearance is 10-15 ml / min.

Indications:diabetic polyneuropathy; alcoholic polyneuropathy

Contraindications:

hypersensitivity to the components of the drug;

children under 18 years of age (efficacy and safety of use not established);

pregnancy and the period of breastfeeding.

Dosing and Administration:

The drug is intended for the preparation of a solution for intravenous administration after preliminary dilution in an isotonic solution of sodium chloride.

When severe forms of diabetic or alcoholic polyneuropathy should be administered 300-600 mg once a day in the form of intravenous drip infusion. Intravenous infusion should be administered within 50 minutes. The drug is recommended for 2-4 weeks.

Then you can continue taking the drug inside at a dose of 300-600 mg per day. The minimum duration of treatment with pills is 3 months.

Side effects:

With intravenous administration, convulsions are rarely possible; diplopia; point bleeding in mucous membranes, skin; thrombocytopathy; hemorrhagic rash (purpura), thrombophlebitis.

With rapid administration, it is possible to increase intracranial pressure (the appearance of a feeling of heaviness in the head); difficulty breathing. The listed side effects go by themselves.

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

Possible the development of hypoglycemia (in connection with improving the absorption of glucose).

Overdose:

Symptoms: headache, nausea, vomiting.

Treatment ', symptomatic. There is no specific antidote.

Interaction:

Alpha-lipoic acid (in the form of a solution for intravenous administration) leads to a decrease in the effect of cisplatin.

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

Alpha-lipoic acid forms hardly soluble complex compounds with sugar molecules (for example, a solution of levulose), therefore, it is incompatible with glucose solution, Ringer's solution, and also with compounds (including their solutions), reacting with disulfide and SH-groups .

Special instructions:

In patients with diabetes, especially at the beginning of treatment, frequent monitoring of the concentration of glucose in the blood. In some cases, a reduction in the dose of hypoglycemic agents is required.

During treatment, it is necessary to strictly refrain from drinking alcohol, because when the effect of alcohol therapeutic effect of thioctic acid is weakened.The preparation possesses photosensitivity, therefore it is necessary to take ampoules from the package just before use. It is advisable to protect the bottle with solution from light during the infusion (light-protective bags, aluminum foil can be used). The prepared solution should be stored in a dark place and used for a maximum of 6 hours after cooking.

Form release / dosage:

Concentrate for the preparation of a solution for intravenous administration

30 mg / ml of 10 ml in ampoules from the light-protective glass.

Packaging:

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

1, 2 contour packs together with the ampoule knife or Scarifier and instructions for use are placed in a pack of cardboard ..

10 ampoules with instructions for the use of the drug and the ampoule or scarifier are placed in a cardboard box.

When using ampoules with notches, a ring of fracture, a scarifier or an ampoule knife is not inserted.

Storage conditions:

In a place protected from light and inaccessible to children, at a temperature of no higher than 25 ° C.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005118/08

Date of registration:01.07.2008

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia

Information update date: & nbsp09.09.2015

Illustrated instructions

Instructions

Thiolipon (Thiolipon)