Thioktacid BV, 600 mg 30 pcs

Pharmacodynamics

Thioctic acid (a-lipoic acid) is found in the human body, where it acts as a coenzyme in the reactions of oxidative phosphorylation of pyruvic acid and alpha-keto acids. Thioctic acid is an endogenous antioxidant, by the biochemical mechanism of action it is similar to the B vitamins.

Tiokoctic acid protects cells from the toxic effects of free radicals produced during metabolic processes; it also neutralizes exogenous toxic compounds released into the body. Thioctic acid increases the concentration of endogenous antioxidant glutathione, which reduces the severity of symptoms of polyneuropathy. The drug has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect, improves trophic neurons. Synergistic action of thioctic acid and insulin results in increased glucose utilization.

Tioktacid® BV (rapid release) is an optimized dosage form for oral administration that avoids the high variability of plasma concentrations of thioctic acid.

Pharmacokinetics

Thioctic acid is quickly and completely absorbed from the gastrointestinal tract when the drug is taken orally. Taking the drug Tioktacid® BV simultaneously with meals may decrease absorption of thioctic acid.

The administration of the drug according to the recommendations 30 min before a meal helps to avoid undesirable interaction with food, because absorption of thioctic acid at the time of eating is already complete. Maximal concentration of thioctic acid in blood plasma is reached 30 minutes after taking the preparation and is 4 mcg/ml.

Tioctic acid has a “first pass” effect through the liver. Absolute bioavailability of thioctic acid is 20%. The main pathways of metabolism are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). The elimination half-life is 25 minutes.

Indications

Diabetic and alcoholic polyneuropathy.

Pharmacological effect

Thioctic (a-lipoic) acid is found in the human body, where it functions as a coenzyme in the oxidative phosphorylation reactions of pyruvic acid and alpha-keto acids. Thioctic acid is an endogenous antioxidant; according to its biochemical mechanism of action, it is close to B vitamins.
Thioctic acid helps protect cells from the toxic effects of free radicals arising in metabolic processes; it also neutralizes exogenous toxic compounds that have entered the body. Thioctic acid increases the concentration of the endogenous antioxidant glutathione, which leads to a decrease in the severity of symptoms of polyneuropathy. The drug has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects; improves neuronal trophism. The result of the synergistic effect of thioctic acid and insulin is an increase in glucose utilization.
Thioctacid® BV (immediate release) is an optimized oral dosage form that avoids the high variability of plasma thioctic acid concentrations.

When taking the drug orally, thioctic acid is quickly and completely absorbed from the gastrointestinal tract. Taking Thioctacid® BV simultaneously with food may reduce the absorption of thioctic acid. Taking the drug as recommended 30 minutes before meals allows you to avoid unwanted interactions with food, since the absorption of thioctic acid is already complete at the time of eating. The maximum concentration of thioctic acid in the blood plasma is reached 30 minutes after taking the drug and is 4 mcg/ml. Thioctic acid has a first-pass effect through the liver. The absolute bioavailability of thioctic acid is 20%.
The main metabolic pathways are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). The half-life is 25 minutes.

Special instructions

Alcohol consumption is a risk factor for the development of polyneuropathy and can reduce the effectiveness of Thioctacid® BV, therefore patients should refrain from drinking alcoholic beverages both during treatment with the drug and during periods outside of treatment. Treatment of diabetic polyneuropathy should be carried out while maintaining optimal blood glucose concentrations.

Active ingredient

Thioctic acid

Composition

1 film-coated tablet contains:

Active substance: thioctic acid (α-lipoic acid) – 600 mg.

Excipients: low-substituted hyprolose 157.00 mg, hyprolose 20.00 mg, magnesium stearate 24.00 mg.

Film coating: hypromellose 15.80 mg, macrogol 6000 4.70 mg, titanium dioxide 4.00 mg, talc 2.02 mg, aluminum varnish based on quinoline yellow dye 1.32 mg, aluminum varnish based on indigo carmine 0.16 mg.

Contraindications

Hypersensitivity to thioctic acid or other components of the drug.
Pregnancy, breastfeeding period (there is no sufficient experience in using the drug).
There are no clinical data on the use of Thioctacid® 600 BV in children and adolescents; therefore, the drug should not be prescribed to children and adolescents.

Side Effects

The incidence of side effects is determined as follows: Very common: > 1/10;

Often: 1/100; Uncommon: 1/1000; Rarely: 1/10000;

Very rare: <1/10000.

From the gastrointestinal tract:

Often – nausea; very rarely – vomiting, pain in the stomach and intestines, diarrhea, changes in taste.

Allergic reactions: Very rarely – skin rash, urticaria, itching, anaphylactic shock.

From the nervous system and sensory organs: Often – dizziness.

General:

Very rarely – due to improved glucose utilization, blood glucose levels may decrease and symptoms of hypoglycemia may appear (confusion, increased sweating, headache, visual disturbances).

Interaction

With the simultaneous administration of thioctic acid and cisplatin, a decrease in the effectiveness of cisplatin is observed. Thioctic acid binds metals, so it should not be administered concomitantly with drugs containing metals (for example, iron, magnesium, calcium). According to the recommended route of administration, Thioctacid® 600 BV tablets are taken 30 minutes before breakfast, while preparations containing metals should be taken at lunchtime or in the evening. For the same reason, during treatment with Thioctacid® 600 BV, it is recommended to consume dairy products only in the afternoon.
With simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may be enhanced, therefore regular monitoring of blood glucose levels is recommended, especially at the beginning of therapy with thioctic acid. In some cases, it is permissible to reduce the dose of hypoglycemic drugs to avoid the development of symptoms of hypoglycemia.
Ethanol and its metabolites weaken the effect of thioctic acid.

Overdose

Symptoms:
In the case of taking thioctic (a-lipoic) acid in doses of 10-40 g, serious signs of intoxication may be observed (generalized convulsive seizures; severe acid-base imbalance leading to lactic acidosis; hypoglycemic coma; severe blood clotting disorders, sometimes leading to a fatal outcome).
If a significant overdose of the drug is suspected (doses equivalent to more than 10 tablets for an adult or more than 50 mg/kg body weight for a child), immediate hospitalization is required.
Treatment: symptomatic, if necessary – anticonvulsant therapy, measures to maintain the functions of vital organs.

Short product description

Thioctic acid. Metabolic agent.

ATX code: A05BA

Storage conditions

At a temperature not exceeding 25° C, out of the reach of children.

List B.

Shelf life

5 years.

Do not use after the expiration date stated on the package.

Manufacturer

Rottapharm Ltd, Ireland