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

Type 1 diabetes, Type 2 diabetes, Alcoholism, PolyneuropathyDiabetic and alcoholic polyneuropathy.

Active ingredient

Thioctic acid

Composition

active ingredient: thioctic acid (α-lipoic acid), in terms of 100% substance – 300 mg; accessory substances: calcium hydrophosphate (calcium phosphate displaced) – 23.7 mg, pregelatinized starch – 21.0 mg, colloidal silica (aerosil) – 1.8 mg, magnesium stearate – 3.5 mg, Solid 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%].

How to take, the dosage

The drug is taken orally, on an empty stomach, 30 minutes before breakfast, without chewing, with water.

The recommended dose is 600 mg (2 capsules) once a day.

In some (severe) cases the treatment is started with parenteral form of Octolipen^® (infusion solution) for 2-4 weeks and then switched to therapy with oral form of Octolipen®, (stepwise therapy).

The type and duration of treatment is determined by the doctor.

Interaction

When concomitant administration of thioctic acid and cisplatin a decrease in the effectiveness of cisplatin is noted. Thioctic acid binds metals, so it should not be prescribed simultaneously with drugs containing metals (e.g., preparations of iron, magnesium, calcium). According to the recommended method of administration, the drug Oktoplipen® is taken 30 minutes before breakfast, while the drugs 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 afternoon. When concomitant use of thioctic acid and insulin or oral hypoglycemic agents may increase their effect, so it is recommended to monitor blood glucose levels, especially at the beginning of thioctic acid therapy. In some 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

When taking Octolipen® , alcohol should be avoided because alcohol consumption 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 and operate vehicles

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

Perhaps caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Solid opaque gelatin capsules #0 of yellow color. The contents of the capsules – powder of light yellow or yellow. Admissible inclusions of white color.

Contraindications

Hypersensitivity to thioctic acid or other components of the drug. Pregnancy and breastfeeding (there is insufficient experience in using the drug). Childhood under 18 years of age (efficacy and safety of use have not been 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, pruritus, anaphylactic

shock.

Nervous system and sensory organs: often – dizziness.

General nature: 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:

In case of thioctic acid (α-lipoic acid) administration at doses of 10-40 g, serious signs of intoxication (generalized convulsions; pronounced acid-base balance disorders leading to lactoacidosis; hypoglycemia, up to hypoglycemic coma; severe clotting disorders, leading sometimes to fatal outcome) may be observed. In case of suspected severe overdose of medicine (doses equal to more than 20 capsules for adults, or more than 50 mg of thioctic acid per kg of body weight for children) the patient should be immediately hospitalized.

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

Pregnancy use

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

Similarities

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