Thiolepta - instructions for use, dose, side effects, contraindications

Thioctic acid (alpha lipoic acid) - an endogenous antioxidant (binds free radicals), in the body is formed during the oxidative decarboxylation of alpha-keto acids. As a coenzyme mitochondrial multi-enzyme complexes is involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids. By the nature of the biochemical action is close to the vitamins of group B. It provides hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic action. Helps reduce blood glucose and increase glycogen content in the liver, as well as reduce insulin resistance. Participates in the regulation of lipid and carbohydrate metabolism, stimulates the exchange of cholesterol, improves liver function. Improves trophic neurons. Using

meglumine salt of thioctic acid (which has a neutral reaction) makes it possible to reduce the severity of adverse reactions.

Pharmacokinetics:

The time to reach the maximum concentration is 10-11 minutes. The area under the concentration-time curve is about 5 μg / hr / ml.

Bioavailability is 30%. Has the effect of "first pass" through the liver.Metabolized in the liver by side chain oxidation and conjugation. The volume of distribution is about 450 ml / kg. The total plasma clearance is 10-15 ml / min. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). Half-life is 20-50 minutes.

Indications:

Diabetic and alcoholic polyneuropathy.

Contraindications:

Hypersensitivity to the components of the drug.

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

Children under 18 years of age (efficacy and safety of use not established).

Dosing and Administration:

In severe forms of diabetic and alcoholic polyneuropathy, the drug is administered intravenously dropwise, 600 mg (50 ml of a solution of 12 mg / ml) once a day. At the beginning of the course, the drug is administered intravenously for 2-4 weeks. Then, it is possible to switch to the oral form of the drug (tablets) at a dose of 300 to 600 mg per day. The drug should be administered slowly, not more than 50 mg of thioctic acid per minute. Intravenous administration is possible with the help of a perfusor (duration of administration - at least 12 minutes).

When applying the drug, the vials of the infusion solution are placed in the enclosed hanging light-protective cases made of black polyethylene.

Side effects:

After intravenous administration, cramps and diplopia are possible; point hemorrhages in the mucous membranes, skin, thrombocytopenia, hemorrhagic rash (purpura), thrombophlebitis; with rapid administration may increase intracranial pressure (the emergence of a sense of heaviness in the head); difficulty breathing. The listed side effects go by themselves. 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).

Overdose:

Symptoms: until now unknown.

Treatment: symptomatic. There is no specific antidote.

Interaction:

With the simultaneous use of thioctic acid and cisplatin, there is a decrease in the effectiveness of cisplatin. Thioctic acid binds metals, so it should not be used simultaneously with preparations containing metals (for example, preparations of iron, magnesium, calcium). With the simultaneous use of thiectic acid and insulin or oral hypoglycemic drugs, their effect may be increased, so regular monitoring of blood glucose concentration is recommended, especially at the beginning

therapy with thioctic acid. In separate cases it is permissible to reduce the dose of hypoglycemic drugs in order to avoid the development of symptoms of hypoglycemia. The infusion solution of thioctic acid is incompatible with the dextrose solution, Ringer's solution and with solutions reacting with disulfide and SH groups, ethanol. Ethanol and its metabolites weaken the action of thioctic acid.

Special instructions:

Patients with diabetes require constant monitoring of blood glucose concentration, especially at the initial stage of therapy. In some cases, it is necessary to reduce the dose of insulin or an oral hypoglycemic drug in order to avoid the development of hypoglycemia.

During the treatment period, patients should refrain from drinking alcohol and take care when driving vehicles and engage in other potentially dangerous activities that require increased attention and speed of mental and motor reactions.

Form release / dosage:

Solution for infusions 12 mg / ml.

By 25 ml or 50 ml in bottles from the glass of the first hydrolytic class of brown, hermetically sealed with rubber stoppers and crimped with aluminum caps.For 1, 3, 5 or 10 bottles, along with hanging light-protecting cases, according to the number of bottles made of high-density polyethylene (HDPE) film in black, cardboard partitions and instructions for use in a pack of cardboard.

Packaging:By 25 ml or 50 ml in bottles from the glass of the first hydrolytic class of brown, hermetically sealed with rubber stoppers and crimped with aluminum caps. For 1, 3, 5 or 10 bottles, along with hanging light-protecting cases, according to the number of bottles made of high-density polyethylene (HDPE) film in black, cardboard partitions and instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009029/10

Date of registration:31.08.2010

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

FIRMA FERMENT, LLC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp07.09.2015

Illustrated instructions

Instructions

Thiolept® (Thiolepta)