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

Polyneuropathy, Type 2 diabetes, Type 1 diabetes, Alcoholism

Diabetic polyneuropathy; alcoholic polyneuropathy.

Active ingredient

Thioctic acid

Composition

Active substance:

• thioctic acid (a-lipoic acid) – 600 mg;

Associates:

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

• Hyprolose (hydroxypropyl cellulose (Klucel EF)) – 32.04 mg;

• Colloidal silica (aerosil) – 24.03 mg;

• magnesium stearate – 24.03 mg;

Shell:

Opadray 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)].

How to take, the dosage

The recommended dose is 1 tablet (600 mg) once a day. The drug is administered orally, on an empty stomach, 30 minutes before breakfast, without chewing, with water. In isolated (severe) cases, treatment begins with the prescription of Octolipen® solution for intravenous injection during 2-4 weeks, then it is transferred to therapy with oral version of Octolipen® (sequential therapy). The type and duration of therapy shall be determined by the physician.

Interaction

In concomitant administration of thioctic acid and cisplatin a decrease in the effectiveness of cisplatin has been noted. Thioctic acid binds metals, therefore it should not be prescribed concomitantly with drugs containing metals (e.g., preparations of iron, magnesium, calcium).

According to the recommended route of administration, tablets of Octolipen® are taken 30 minutes before breakfast, while medications containing metals should be taken in the afternoon or evening. For the same reason during treatment it is recommended to eat dairy products only in the second half of the day.

When concurrent administration of thioctic acid and insulin or oral hypoglycemic agents may increase their effect, therefore it is recommended to monitor blood glucose level regularly, especially at the beginning of thioctic acid therapy. In individual cases it is acceptable to reduce the dose of hypoglycemic drugs in order to avoid the development of symptoms of hypoglycemia.

Ethanol and its metabolites weaken the effect of thioctic acid.

Special Instructions

Patients taking Oktoplipen^® should refrain from drinking alcohol, as drinking alcohol is a risk factor for polyneuropathy and may decrease the effectiveness of treatment.

The treatment of diabetic polyneuropathy must be accompanied by maintenance of optimal blood glucose concentrations.

Influence on the ability to drive vehicles and mechanisms

The effect on the ability to drive vehicles and mechanisms has not been specifically studied. Caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity to thioctic acid or other components of the drug.

Pregnancy, breastfeeding (there is insufficient experience in using the drug).

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

Side effects

The frequency of side effects is defined as follows:

Very often: > 1/10;

Often: < 1/10 > 1/100;

Infrequently: < 1/100 > 1/1000;

Rarely: < 1/1000> 1/10000;

Very rarely: < 1/10000.

Gastrointestinal tract: frequently – nausea; very rarely – vomiting, pain in the stomach and intestines, diarrhea, changes in taste.

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

Nervous system and sensory organs:often – dizziness.

General: very rarely, due to improved glucose utilization, blood glucose levels may decrease and symptoms of hypoglycemia (confusion, increased sweating, headache, visual disturbances) may occur.

Overdose

Symptoms: Headache, nausea, vomiting. In case of thioctic acid (alpha-lipoic acid) administration in doses of 10-40 g serious signs of intoxication may be observed (generalized convulsions; pronounced acid-base balance disorders, leading to lactoacidosis; hypoglycemia, up to hypoglycemic coma; severe blood clotting disorders, sometimes leading to death).

If there is suspicion of significant overdose of the drug (doses equal to more than 10 pills for an adult or more than 50 mg per kg of body weight for a child) the immediate hospitalization is required.

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

Pregnancy use

The use of the drug during pregnancy is contraindicated due to the lack of sufficient clinical experience in the use of thioctic acid in pregnancy. Studies of reproductive toxicity have not revealed any risks with respect to fertility, effect on fetal development and any embryotoxic properties of the drug. The use of the drug Octolipen® during lactation is contraindicated due to the lack of data on the penetration of thioctic acid into the breast milk.

Similarities

Berlithione 300, Berlithione 300 oral, Thioctacid BV, Thiogamma, Thiolepta, Berlithione, Thioctic acid