Espa-Lipon

General characteristics. Structure:

Active ingredient: 200 mg or 600 mg of thioctic (alpha and lipoic) acid.

Excipients: lactoses monohydrate, povidone, cellulose microcrystallic, cellulose powder, silicon dioxide colloid, silicon dioxide, sodium carboxymethylstarch, magnesium stearate.

Cover: gipromelloza, macrogoal 6000, talc, titanium dioxide (Е 171), quinolinic yellow (Е 104).

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:

It is recommended to appoint tablets inside as the supporting treatment after 2-4 weeks infusional and drop therapy. The minimum course of reception of tablets – 3 months.

In the absence of other appointments about 1 tablet is recommended to accept on 600 mg, or on 2-3 tablets on 200 mg that corresponds to 400-600 mg of thioctic (alpha and lipoic) acid a day.

It is necessary to accept in 30 minutes prior to meal, without chewing and washing down with a small amount of liquid. In certain cases administration of drug assumes more prolonged use which terms are defined by the attending physician.

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! Tablet period of validity coated 200 mg: 2 years. Tablets coated 600 mg: 3 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets coated 200 mg. On 25 or 30 tablets in the blister from foil PVC/A½. 1 blister on 30 tablets or 4 blisters on 25 tablets with the application instruction in a cardboard box.

Tablets coated 600 mg. On 10 tablets in the blister from foil PVC/A½. On 3, 6 or 10 blisters with the application instruction in a cardboard box.