Octolipen, 600 mg 30 pcs.

Pharmacotherapeutic group: metabolic agent.

ATX code: A16AX01

Pharmacological properties

Pharmacodynamics:

Thioctic acid (alpha-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 protect the cell from the toxic effects of free radicals that occur during metabolic processes; it also detoxifies exogenous toxic compounds. Thioctic acid increases the concentration of endogenous antioxidant glutathione, which leads to a decrease in 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:

When taken orally it is quickly and completely absorbed in the gastrointestinal tract, taking it simultaneously with food may reduce absorption of the drug. Administration of the drug, according to the recommendations, 30 min before meals avoids unnecessary interaction with food, because absorption of thioctic acid at the time of eating is already complete.

The maximum concentration of thioctic acid in 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 elimination half-life (T 1/2) is 25 min.

Indications

Diabetic polyneuropathy; alcoholic polyneuropathy.

Pharmacological effect

Pharmacotherapeutic group: metabolic agent.

ATX code: A16AX01

Pharmacological properties

Pharmacodynamics:

Thioctic acid (alpha-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; it also 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, it is quickly and completely absorbed from the gastrointestinal tract; taking it simultaneously with food may reduce the absorption of the drug. Taking the drug, according to the recommendations, 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 (T 1/2) is 25 minutes.

Special instructions

Patients taking Octolipen® 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 (a-lipoic acid) – 600 mg;

Excipients:

low-substituted hyprolose (low-substituted hydroxypropyl cellulose L-HPC LH-B1) – 120.90 mg;

hyprolose (hydroxypropylcellulose (Klucel EF)) – 32.04 mg;

colloidal silicon dioxide (Aerosil) – 24.03 mg;

magnesium stearate – 24.03 mg;

Shell:

Opadry yellow (OPADRY 03F220017 Yellow) – 28.00 mg [hypromellose (hydroxypropyl methylcellulose), macrogol-6000 (polyethylene glycol 6000), titanium dioxide, talc, quinoline yellow aluminum varnish (E104), iron oxide yellow dye (E172)].

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. Reproductive toxicity studies did not reveal any risks to fertility, effects on fetal development or any embryotoxic properties of the drug.
The use of Octolipen® during lactation 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, breastfeeding period (there is no sufficient experience in using the drug).

Children under 18 years of age (efficacy and safety 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, the level of glucose in the blood 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® tablets are taken 30 minutes before breakfast, while medications 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: Headache, nausea, vomiting. In the case of taking thioctic (alpha-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 death).

If a significant overdose of the drug is suspected (doses equivalent to more than 10 tablets for an adult or more than 50 mg per kg of body weight for a child), immediate hospitalization is necessary.

Treatment: There is no specific antidote. Treatment is symptomatic, if necessary – anticonvulsant therapy, measures to maintain the function 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