Octolipen tablets 600mg, no. 30

• Diabetic polyneuropathy;

• alcoholic polyneuropathy.

The drug is taken orally, on an empty stomach, 30 minutes before a meal. The tablets should be swallowed whole, without chewing, with a sufficient amount of liquid.

The recommended dose is 1 tab. (600 mg) 1 time / day.

It is possible to carry out stepwise therapy: oral administration of the drug begins after a 2-4-week course of parenteral administration of thioctic acid. The maximum course of taking pills is 3 months. In some cases, therapy with OctolipenЃ involves longer use. The duration of admission is determined by the attending physician.

Tablets, film-coated from light yellow to yellow, oval, biconvex, with a risk on one side; at the break - from light yellow to yellow.

1 tab. thioctic (alpha lipoic) acid 600 mg

Excipients: low-substituted hyprolose (low-substituted hydroxypropyl cellulose) - 108.88 mg, hyprolose (hydroxypropyl cellulose) - 28.04 mg, croscarmellose (sodium croscarmellose) - 24.03 mg, colloidal silicon dioxide - 20.025 mg, magnesium stearate - 20.025

• Pregnancy;

• lactation period (breastfeeding);

• children and adolescents under 18 years of age (efficacy and safety have not been established);

• hypersensitivity to thioctic acid and drug components.

pharmachologic effect

Thioctic acid (?-lipoic acid) is a coenzyme of mitochondrial multienzyme complexes involved in the oxidative decarboxylation of pyruvic acid and ?-keto acids. It is an endogenous antioxidant: it binds free radicals, restores the intracellular level of glutathione, increases the activity of superoxide dismutase. Improves neuronal trophism and axonal conduction. By the nature of the biochemical action, thioctic acid is similar to the B vitamins.

Plays an important role in energy metabolism. Participates in the regulation of lipid and carbohydrate metabolism,
stimulates cholesterol metabolism. Promotes a decrease in blood glucose, an increase in the content of glycogen in the liver, and a decrease in insulin resistance.

Has a lipotropic effect, improves liver function. It has a detoxifying effect in case of poisoning with salts of heavy metals and other intoxications.

Pharmacokinetics

Absorption and distribution

When taken orally, it is rapidly and completely absorbed in the gastrointestinal tract, taking it simultaneously with food reduces the absorption of the drug. Bioavailability - 30-60% due to the effect of 'first pass' through the liver. Time to reach Cmax - 25-60 minutes.

Metabolism and excretion

It is metabolized in the liver by side chain oxidation and conjugation. Vd - 450 ml / kg. The total plasma clearance is 10-15 ml / min.

Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T1 / 2 - 25 min.

Side effect

From the side of the central nervous system: very rarely - a change or violation of taste.

From the digestive system: very rarely - nausea, vomiting, heartburn, abdominal pain, diarrhea.

From the side of metabolism: very rarely - a decrease in blood glucose (due to improved absorption of glucose); hypoglycemia may develop, the symptoms of which include dizziness, increased sweating, headache, visual impairment.

From the immune system: very rarely - allergic reactions such as skin rash, hives, itching.

Application during pregnancy and lactation

The use of the drug during pregnancy is contraindicated due to the lack of sufficient clinical experience with the use of thioctic acid in pregnant women. Reproductive toxicity studies did not reveal any risks in relation to fertility, effects on fetal development and any embryotoxic properties of the drug.

The use of the drug OctolipenЃ during lactation is contraindicated due to the lack of data on the penetration of thioctic acid into breast milk.

Application in children

The use of the drug in children and adolescents under the age of 18 is contraindicated (efficacy and safety have not been established).

special instructions

During the period of treatment (especially at the initial stage), regular monitoring of blood glucose levels in patients with diabetes is necessary. In some cases, it may be necessary to reduce the dose of insulin or an oral hypoglycemic drug in order to avoid the development of hypoglycemia.

Patients taking OctolipenЃ should refrain from drinking alcohol.

Simultaneous food intake may interfere with the absorption of the drug.

When taking OctolipenЃ, the use of dairy products is not recommended (due to the calcium content in them). The interval between doses should be at least 2 hours.

Influence on the ability to drive vehicles and use mechanisms

The effect on the ability to drive vehicles and mechanisms has not been specifically studied. Care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: headache, nausea, vomiting. In severe cases (when taking thioctic acid at a dose of 10-40 g or more than 10 tablets, 600 mg each for adults, or at a dose> 50 mg / kg of body weight in children): psychomotor agitation or clouding of consciousness, generalized convulsions, severe disorders acid-base balance with lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, hemolysis, disseminated intravascular coagulation syndrome, suppression of bone marrow activity, multiple organ failure.

Treatment: if a significant overdose of the drug is suspected, immediate hospitalization is recommended and the application of measures in accordance with the general principles adopted in case of accidental poisoning (induction of vomiting, gastric lavage, intake of activated charcoal, etc.). Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication is symptomatic and should be carried out in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion, or filtration methods with forced excretion of thioctic acid from the body are not effective.

Drug interactions

Strengthens the anti-inflammatory effect of GCS.

Reduces the effectiveness of cisplatin.

Enhances the action of insulin and oral hypoglycemic drugs (correction of their dose is necessary, as well as regular monitoring of blood glucose to avoid hypoglycemia).

Simultaneous administration of OctolipenЃ and iron, magnesium and calcium preparations is not recommended (due to the formation of a complex with metals). The interval between doses should be at least 2 hours.

Ethanol and its metabolites weaken the therapeutic activity of thioctic acid.