Тиолепта®

General characteristics. Structure:

Active agent: thioctic acid — 300 mg;
excipients: potato starch, A-300 aerosil (silicon dioxide colloid), a primelloza (sodium of a kroskarmelloz), calcium stearate, sugar milk (lactose), cellulose microcrystallic, castor oil, seleknut AQ –01812 (a gidroksipropilmetiltsellyuloz (gipromelloz), polyethyleneglycol 400 (a macrogoal 400), polyethyleneglycol 6000 (a macrogoal 6000), titanium dioxide, ferrous oxide yellow, quinolinic yellow.

Pharmacological properties:

Thioctic acid (alpha lipoic acid) — endogenous antioxidant (connects free radicals), in an organism is formed at oxidizing decarboxylation alpha ketoxylot. As a coenzyme of mitochondrial multifermental complexes participates in oxidizing decarboxylation of pyruvic acid and alpha ketonic acids. Promotes decrease in content of glucose in blood and to increase in maintenance of 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.

Pharmacokinetics. At intake it is quickly and fully soaked up from digestive tract (reception with food reduces absorption). Time of achievement of the maximum concentration — 40–60 minutes. Bioavailability — 30%.

Has effect of "the first passing" through a liver. Formation of metabolites results from oxidation of a side chain and a konjyugirovaniye.

Distribution volume — about 450 ml/kg. Thioctic 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 and alcoholic polyneuropathy.

Route of administration and doses:

Appoint inside 600 mg (2 tablets) once a day. A pill is taken on an empty stomach, approximately in 30 minutes prior to the first meal, without chewing and washing down with a small amount of liquid. Duration of a course of treatment is determined by the doctor.

Features of use:

The patients accepting the drug Tiolepta® should refrain from alcohol intake.
At patients with a diabetes mellitus constant control of concentration of glucose in blood, especially at an initial stage of therapy is necessary. In certain cases it is necessary to reduce a dose of insulin or peroral hypoglycemic drug to avoid development of a hypoglycemia.

Side effects:

Usually Tiolepta® is transferred well. Dyspepsia, including nausea, vomiting, heartburn is possible. Development of skin allergic reactions is in some cases possible (urticaria). Development of a hypoglycemia is possible (in connection with improvement of digestion of glucose).

Interaction with other medicines:

Thioctic acid reacts with ionic complexes of metals (for example, with Cisplatinum) therefore at simultaneous use of Tiolepta® can reduce effect of Cisplatinum. After administration of drug of Tiolepta® to use iron preparations, magnesium in the morning, and also it is recommended to use dairy products (because of content of calcium in them) after a lunch or in the evening.
At simultaneous use of Tiolepta® strengthens effect of insulin and peroral hypoglycemic means.
Alcohol (ethanol) reduces therapeutic activity of thioctic acid.

Contraindications:

Hypersensitivity to drug components.
Pregnancy, the breastfeeding period (there is no sufficient experience of use of drug).
Children's age (efficiency and safety of use are not established).

Overdose:

Symptoms: headache, nausea, vomiting.
Treatment: performing symptomatic therapy. There is no specific antidote.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children, the Period of validity 2 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated light yellow color, round, biconvex form.
On 10 or 15 tablets in a blister strip packaging from a film polyvinyl chloride and a foil to an aluminum printing lakirovannoynya of substance: potato starch, A-300 aerosil (silicon dioxide colloid), a primelloza (sodium of a kroskarmelloz), calcium stearate, sugar milk (lactose), cellulose microcrystallic, castor oil, seleknut AQ –01812 (a gidroksipropilmetiltsellyuloz (gipromelloz), polyethyleneglycol 400 (a macrogoal 400), polyethyleneglycol 6000 (a macrogoal 6000), titanium dioxide, ferrous oxide yellow, quinolinic yellow.