Thiolepta, 300 mg 30 pcs

Pharmacodynamics

Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant (binds free radicals), in the body is formed during oxidative decarboxylation of alpha-keto acids. As a coenzyme of mitochondrial multienzyme complexes it participates in oxidative decarboxylation of pyruvic acid and alpha-keto acids. By the nature of its biochemical action is close to the B vitamins.

It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic action. Helps to reduce blood glucose and increase glycogen in the liver, as well as reducing insulin resistance. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function. It improves the trophism of neurons. Use of meglumine salt of thioctic acid (which has a neutral reaction) reduces the severity of adverse reactions.

Pharmacokinetics

When taken orally, it is quickly and completely absorbed from the gastrointestinal tract (ingestion with food reduces absorption). Time to reach maximum concentration – 40-60 minutes. Bioavailability – 30%.

It has the effect of “first passage” through the liver. Formation of metabolites occurs as a result of side chain oxidation and conjugation.

The volume of distribution is about 450 ml/kg. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). Half-life is 20-50 min. Total plasma clearance is 10-15 ml/min.

Indications

Diabetic and alcoholic polyneuropathy.

Pharmacological effect

Pharmacodynamics

Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of alpha-keto acids. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and alpha-keto acids. The nature of the biochemical action is close to B vitamins.

It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects. 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 cholesterol metabolism, improves liver function. Improves trophism of neurons. The use of meglumine salt of thioctic acid (which has a neutral reaction) can reduce the severity of adverse reactions.

Pharmacokinetics

When taken orally, it is quickly and completely absorbed from the gastrointestinal tract (taken with food reduces absorption). The time to reach maximum concentration is 40–60 minutes. Bioavailability – 30%.

Has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation.

Volume of distribution is about 450 ml/kg. Thioctic acid and its metabolites are excreted by the kidneys (80–90%). The half-life is 20–50 minutes. Total plasma clearance is 10–15 ml/min.

Special instructions

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

During the treatment period, patients should refrain from drinking alcohol and be careful when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of mental and motor reactions.

Active ingredient

Thioctic acid

Composition

1 film-coated tablet contains:

active ingredient:

thioctic acid – 300 mg;

excipients:

potato starch,

Aerosil A-300 (colloidal silicon dioxide),

Primellose (croscarmellose sodium),

calcium stearate,

milk sugar (lactose),

microcrystalline cellulose,

castor oil,

selectote AQ –01812 (hydroxypropyl methylcellulose (hypromellose),

polyethylene glycol 400 (macrogol 400),

polyethylene glycol 6000 (macrogol 6000),

titanium dioxide,

iron oxide yellow,

quinoline yellow.

Contraindications

Hypersensitivity to the components of the drug Thiolepta.
Pregnancy, breastfeeding (there is no sufficient experience in using the drug).
Children’s age (efficacy and safety of use have not been established).

Side Effects

Thiolepta is usually well tolerated.

Possible dyspepsia, including nausea, vomiting, heartburn.

In some cases, the development of allergic skin reactions (urticaria) is possible.

Hypoglycemia may develop (due to improved glucose absorption).

Interaction

Thioctic acid reacts with ionic metal complexes (for example, with cisplatin), therefore, when used simultaneously, Thiolept may reduce the effect of cisplatin. After taking Thiolepta in the morning, it is recommended to take iron and magnesium supplements, and also consume dairy products (due to their calcium content) in the afternoon or evening.

With simultaneous use, Thiolept enhances the effect of insulin and oral hypoglycemic agents.

Alcohol (ethanol) reduces the therapeutic activity of thioctic acid.

Overdose

Symptoms: headache, nausea, vomiting.

Treatment: symptomatic therapy. There is no specific antidote.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Manufacturer

Kanonpharma production CJSC, Russia