Тиолепта® solution

General characteristics. Structure:

Active agent: thioctic acid (alpha lipoic acid) of 12,00 mg;
excipients: Megluminum (N - methyl - D - glyukamin), a macrogoal (polyethyleneglycol 400), povidone (коллидон® 17 PF or пласдон S-15), water for injections.

Note:

1) active agent is the meglyuminovy salt of thioctic acid received from thioctic acid and Megluminum.
2) theoretical osmolarity 269 ¼Äß¼/l.

Description:
Transparent solution, light yellow or light yellow with greenish shade.

Pharmacological properties:

Pharmacodynamics. Thioctic acid (alpha 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. On character of a biochemical effect it is close to group B vitamins. Renders hepatoprotective, hypolipidemic, gipokholesterinemichesky, hypoglycemic action. Promotes decrease in content of glucose in blood and to increase in maintenance of a glycogen in a liver, and also to decrease in insulin resistance. Participates in regulation of lipidic and carbohydrate metabolism, stimulates cholesterol exchange, improves function of a liver. Improves a trophicity of neurons. Use of meglyuminovy salt of the thioctic acid (having neutral reaction) allows to reduce expressiveness of side reactions.

Pharmacokinetics. Time of achievement of the maximum concentration – 10-11 min. The area under a curve "concentration time" – about 5 мкг×ч/мл.
Bioavailability - 30%. Has effect of "the first passing" through a liver. It is metabolized in a liver by oxidation of a side chain and a konjyugirovaniye. Distribution volume – about 450 ml/kg. The general plasma clearance - 10-15 ml/min. Thioctic acid and its metabolites are removed by kidneys (80-90%). An elimination half-life - 20-50 min.

Indications to use:

Diabetic and alcoholic polyneuropathy.

Route of administration and doses:

At severe forms of diabetic and alcoholic polyneuropathy the drug is administered intravenously kapelno, by 600 mg (50 ml of solution 12mgml) once a day. At the beginning of a course the drug is administered intravenously within 2-4 weeks. Then transition to a peroral form of drug (tablet) in a dose of 300 - 600 mg a day is possible. It is necessary to administer the drug slowly, no more than 50 mg of thioctic acid in 1 minute. Intravenous administration is possible by means of a perfusor (introduction duration - not less than 12 minutes).

At drug use solution bottles for infusions place in the enclosed suspended light-protective cases made of polyethylene of black color.

Features of use:

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.
During treatment patients should abstain from alcohol intake and to be careful at control of vehicles and occupation other potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.

Side effects:

After intravenous administration spasms, a diplopia are possible; dot hemorrhages in mucous membranes, skin, thrombocytopenia, hemorrhagic rash (purpura), thrombophlebitis; at bystry introduction increase in intracranial pressure is possible (emergence of feeling of weight in the head); breath difficulty. The listed side effects pass independently. 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).

Interaction with other medicines:

At simultaneous use of thioctic acid and Cisplatinum decrease in efficiency of Cisplatinum is noted. Thioctic acid connects metals therefore it should not be applied along with the drugs containing metals (for example, iron preparations, magnesium, calcium). At simultaneous use of thioctic acid and insulin or peroral hypoglycemic drugs their action can amplify therefore regular control of concentration of glucose in blood, especially at the beginning of therapy is recommended by thioctic acid. Reduction of a dose of hypoglycemic drugs in order to avoid development of symptoms of a hypoglycemia is in some cases admissible.
Infusion solution of thioctic acid is incompatible with dextrose solution, Ringer's solution and with the solutions reacting with disulfide and SH groups, ethanol. Ethanol and its metabolites weaken effect of thioctic acid.

Contraindications:

Hypersensitivity to drug components.
Pregnancy, the breastfeeding period (there is no sufficient experience of use of drug).
Children's age up to 18 years (efficiency and safety of use are not established).

Overdose:

Symptoms: so far are unknown. Treatment: symptomatic. There is no specific antidote.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 12 mg/ml.
On 25 ml or 50 ml in the bottles from glass of the 1st hydrolytic class of brown color hermetically corked by rubber bungs and which are pressed out by caps aluminum.
On 1, 3, 5 or 10 bottles together with the suspended light-protective cases by quantity of bottles made of a film PHP (polyethylene of high pressure) of black color, partitions from a cardboard and the application instruction in a pack from a cardboard.