Oktolipen, capsules 300 mg 30 pcs

Pharmacotherapeutic group:metabolic agent

ATX code: A16AX01

Pharmacological properties.

Pharmacodynamics

Thioctic acid (α-lipoic acid) is found in the human body, where it serves as a coenzyme in the oxidative phosphorylation reactions of pyruvic acid and alpha-keto acids. Thioctic acid is an endogenous antioxidant. Thioctic acid helps to protect the cell from the toxic effects of free radicals arising from metabolic processes, neutralizes exogenous toxic compounds. 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; it improves the trophism of neurons. Synergistic action of thioctic acid and insulin results in increased glucose utilization.

Pharmacokinetics

The drug is quickly and completely absorbed from the gastrointestinal tract when taken orally, simultaneous administration with food may decrease absorption of the drug. Administration of the drug, according to the recommendations, 30 min before a meal, allows to avoid undesirable interaction with food, because absorption of thioctic acid at the time of eating is completed. The maximum concentration of thioctic acid in blood plasma is reached 30 min after taking the drug and is 4 mcg/ml. Thioctic 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 half-life (T_1/2) is 25 minutes.

Indications

Diabetic and alcoholic polyneuropathy.

Pharmacological effect

Pharmacotherapeutic group: metabolic agent

ATX code: A16AX01

Pharmacological properties

Pharmacodynamics

Thioctic (α-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. Thioctic acid helps protect cells from the toxic effects of free radicals arising in metabolic processes and neutralizes exogenous toxic compounds. 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.

Pharmacokinetics

When taken orally, the drug is quickly and completely absorbed from the gastrointestinal tract; simultaneous administration with food may reduce the absorption of the drug. Taking the drug, according to the recommendations, 30 minutes before meals, avoids 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%). Half-life (T1/2) – 25 minutes.

Special instructions

When taking Octolipen®, you should refrain from drinking alcoholic beverages, since alcohol consumption is a risk factor for the development of polyneuropathy and may reduce the effectiveness of treatment.

Treatment of diabetic polyneuropathy should be carried out while maintaining optimal blood glucose concentrations.

Impact on the ability to drive vehicles and machinery

The effect on the ability to drive vehicles and machinery has not been specifically studied.

Care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Thioctic acid

Composition

active ingredient: thioctic acid (α-lipoic acid), calculated as 100% substance – 300 mg; excipients: calcium hydrogen phosphate (dibasic calcium phosphate) – 23.7 mg, pregelatinized starch – 21.0 mg, colloidal silicon dioxide (Aerosil) – 1.8 mg, magnesium stearate – 3.5 mg, hard gelatin capsules – 97.0 mg [titanium dioxide (E 171) – 2.667%, quinoline yellow (E 104) – 1.839%, sunset yellow dye (E 110) – 0.0088%, medical gelatin – up to 100%].

Pregnancy

The use of the drug during pregnancy is contraindicated due to the lack of sufficient clinical experience with the use of thioctic acid during pregnancy.
The use of the drug during breastfeeding is contraindicated due to the lack of data on the penetration of thioctic acid into breast milk.

Contraindications

Hypersensitivity to thioctic acid or other components of the drug.
Pregnancy and breastfeeding (there is no sufficient experience in using the drug).
Children under 18 years of age (efficacy and safety of use have not been established).

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 rare – 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, Octolipen® is taken 30 minutes before breakfast, while drugs containing metals should be taken at lunchtime or in the evening. For the same reason, during the treatment period, 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 (α-lipoic) acid in doses of 10-40 g, serious signs of intoxication may be observed (generalized convulsions; severe acid-base imbalance leading to lactic acidosis; hypoglycemia, up to 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 20 capsules for an adult or more than 50 mg of thioctic acid per kg of body weight for a child), immediate hospitalization of the patient is necessary.

Treatment: There is no specific antidote. Treatment is symptomatic, if necessary – anticonvulsant therapy, measures to maintain the functions of vital organs.

Storage conditions

Store at a temperature not exceeding 25 °C.
Keep out of the reach of children.

Shelf life

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

Manufacturer

Pharmstandard-Leksredstva, Russia