Espa-Lipon

General characteristics. Structure:

Active ingredient: 25 mg of thioctic (alpha and lipoic) acid.

Excipients: water for injections.

Pharmacological properties:

Pharmacodynamics. Thioctic (alpha and lipoic) acid – endogenous antioxidant (connects free radicals), in an organism is formed at oxidizing decarboxylation of alpha ketonic acids. As a coenzyme of mitochondrial multifermental complexes participates in oxidizing decarboxylation of pyruvic acid and alpha ketonic acids. Promotes decrease in concentration of glucose in blood and to increase in a glycogen in a liver, and also to overcoming insulin resistance. On character of a biochemical effect it is close to group B vitamins. Participates in regulation of lipidic and carbohydrate metabolism, stimulates cholesterol exchange, improves function of a liver. Renders hepatoprotective, hypolipidemic, gipokholesterinemichesky, hypoglycemic action. Improves a trophicity of neurons.

Pharmacokinetics. At intake it is quickly and completely soaked up from digestive tract (reception with food reduces absorption). Time of achievement of the maximum concentration - 40-60 minutes.

At intravenous administration time of achievement of the maximum concentration – 10-11 min., the maximum concentration – 25-38 mkg/ml, the area under a curve concentration time – about 5 mkg of h/ml.

Thioctic (alpha and lipoic) acid has effect of "the first passing" through a liver. Formation of metabolites results from oxidation of a side chain and a konjyugirovaniye. Bioavailability - 30%.

Distribution volume – about 450 ml/kg. Thioctic (alpha and lipoic) acid and its metabolites are removed by kidneys (80-90%). An elimination half-life - 20-50 min. The general plasma clearance - 10-15 ml/min.

Indications to use:

• diabetic polyneuropathy;
• alcoholic polyneuropathy.

Route of administration and doses:

Drug is intended for preparation of solution for infusions after preliminary cultivation in isotonic solution of sodium chloride.

Severe forms of diabetic or alcoholic polyneuropathy. Once a day in the form of intravenous drop infusions of 24 ml of solution in 250 ml of isotonic solution of sodium chloride (that corresponds to 600 mg of alpha lipoic acid a day). Drug is recommended to be used within 2-4 weeks. Solutions for infusions should be entered within 50 minutes. The prepared solutions need to be stored in the place protected from light and to use as much as possible within 6 hours after preparation.

Further it is necessary to pass to a maintenance therapy in the form of tablets in a dose 400-600 mg a day. The minimum term of treatment by tablets – 3 months.

Features of use:

At patients with a diabetes mellitus, especially in an initiation of treatment, frequent control of concentration of glucose in blood is necessary. In some cases the dose decline of hypoglycemic means is required.

During treatment it is necessary to abstain from alcohol intake as the therapeutic effect of thioctic (alpha and lipoic) acid is weakened at alcohol influence strictly.

Drug is light-sensitive therefore ampoules should be got from packaging only just before use.

Side effects:

Allergic reactions are possible: a small tortoiseshell, system allergic reactions (up to development of an acute anaphylaxis). Development of a hypoglycemia is possible (in connection with improvement of digestion of glucose). At intake the dispepsichesky phenomena, including nausea, heartburn, vomiting are possible.

At intravenous administration spasms are very seldom possible; diplopia; dot hemorrhages in mucous membranes, skin; trombotsitopatiya; hemorrhagic rash (purpura), thrombophlebitis.

At bystry introduction increase in intracranial pressure is possible (emergence of feeling of weight in the head); breath difficulty.

Interaction with other medicines:

At simultaneous use with insulin and peroral hypoglycemic means strengthening of hypoglycemic effect is observed.

Thioctic (alpha and lipoic) acid forms with sugar molecules (for example, levuloza solution) difficult soluble complex compounds, therefore, is incompatible with glucose solution, Ringer's solution, and also with the connections (including their solutions) interacting with disulfide and SH groups.

Thioctic (alpha and lipoic) acid (in the form of solution for infusions) leads to decrease in effect of Cisplatinum.

Contraindications:

• hypersensitivity to drug components;
• children's age (efficiency and safety of use are not established);
• pregnancy, the breastfeeding period (there is no sufficient experience of use of drug.

Overdose:

Symptoms: headache, nausea, vomiting.

Treatment: symptomatic. There is no specific antidote.

Storage conditions:

List B. To store at a temperature not above 25 °C. To store in the place protected from light! To store in the place, unavailable to children! A concentrate period of validity for preparation of solution for infusions: 3 years. The period of validity of the solution prepared for use after cultivation in isotonic solution of sodium of chloride makes at most 6 hours at storage it in the place protected from light. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 12 ml (300 mg / 12 ml) or 24 ml (600 mg / 24 ml) in ampoules of dark glass. On 10 ampoules (300 mg / 12 ml) or on 5 ampoules (600 mg / 24 ml) in the plastic pallet together with the application instruction place in a cardboard pack.