Espa-Lipon - instructions for use, dose, side effects, contraindications

Thioktovaya (alpha-lipoic) acid - an endogenous antioxidant (binds free radicals) in the body is formed by 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:

When ingested quickly and completely absorbed from the gastrointestinal tract (intake with food reduces absorption). The time to reach the maximum concentration is 40-60 minutes.

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.

Thioktovaya (alpha-lipoic) 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. Bioavailability is 30%.

The volume of distribution is about 450 ml / kg. Thioktovaya (alpha-lipoic) 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's age (efficacy and safety of use not established);

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

Dosing and Administration:

Concentrate for solution for infusion:

The preparation is intended for the preparation of a solution for infusions after preliminary dilution in isotonic sodium chloride solution.

Severe forms of diabetic or alcoholic polyneuropathy Once a day in the form of intravenous drip infusions 24 ml of solution in 250 ml of isotonic sodium chloride solution (corresponding to 600 mg of alpha-lipoic acid per day). The drug is recommended for 2-4 weeks. Infusion solutions should be administered within 50 minutes. Prepared solutions should be stored in a dark place and used for a maximum of 6 hours after cooking.

Next, you should switch to maintenance therapy in the form of tablets at a dose of 400-600 mg per day.The minimum duration of treatment with pills is 3 months.

Side effects:

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). With oral administration, dyspepsia may occur, including nausea, heartburn, and vomiting.

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.

Overdose:

Symptoms: headache, nausea, vomiting.

Treatment: symptomatic. There is no specific antidote.

Interaction:

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

Thioktovaya (alpha-lipoic) acid forms difficultly 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 (incl.their solutions) interacting with disulfide and SH-groups. Thioktovaya (alpha-lipoic) acid (in the form of a solution for infusions) leads to a decrease in the effect of cisplatin.

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, since the therapeutic effect of thioctic (alpha-lipoic) acid is weakened by exposure to alcohol.

The drug is light-sensitive, so the ampoules should be removed from the package only immediately before use.

Form release / dosage:

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

Packaging:

For 12 ml (300 mg / 12 ml) or 24 ml (600 mg / 24 ml) in the ampoules of dark glass.

Two plastic pallets of 5 ampoules (300 mg / 12 ml) or 1 plastic tray of 5 ampoules (600 mg / 24 ml), together with instructions for use, are placed in a cardboard box.

Storage conditions:

List B. Store at a temperature of no higher than 25 ° C.

Keep in a dark place! Keep out of the reach of children!

Shelf life:

3 years.

Shelf life of the solution prepared for use after dilution in an isotonic solution of sodium chloride is a maximum of 6 hours when stored in a place protected from light.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:П N012834 / 02

Date of registration:30.07.2007

The owner of the registration certificate:Esparma GmbHEsparma GmbH Germany

Manufacturer: & nbsp

ESPARMA, GmbH Germany

Representation: & nbspESPARMA GmbH ESPARMA GmbH Germany

Information update date: & nbsp09.09.2015

Illustrated instructions

Instructions

Espa Lipon (Espa-lipon)