Composition, form of production and packaging
The tablets covered with a film membrane from light yellow to yellow color, oval, biconcave, with risk from one side; on the break from light yellow to yellow.
Thioctic (? -lipoic) acid 600 mg
Excipients: low-substituted giprolose (low-substituted hydroxypropylcellulose) - 108.88 mg, giprolose (hydroxypropylcellulose) - 28.04 mg, croscarmellose (croscarmellose sodium) - 24.03 mg, silicon colloidal dioxide 20.025 mg, magnesium stearate 20.025 mg.
Sheath composition: Opadrai yellow (OPADRY 03F220017 Yellow) - 28 mg (hypromellose (hydroxypropylmethylcellulose) - 15.8 mg, macrogol 6000 (polyethylene glycol 6000) - 4.701 mg, titanium dioxide 5.27 mg, talc 2.019 mg, quinoline yellow aluminum lacquer (E104) - 0.162 mg, ferric oxide yellow oxide (E172) - 0.048 mg).
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (6) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
Thioctic acid (О±-lipoic acid) is a coenzyme of mitochondrial multienzyme complexes participating in the oxidative decarboxylation of pyruvic acid and ОІ-keto acids. It is an endogenous antioxidant: binds free radicals, restores the intracellular level of glutathione, increases the activity of superoxide dismutase. Improves trophism of neurons and axonal conduction. By the nature of the biochemical action, thioctic acid is similar to Group B vitamins.
It plays an important role in energy exchange. Participates in the regulation of lipid and carbohydrate metabolism,
stimulates the exchange of cholesterol. Helps reduce blood glucose, increase glycogen content in the liver, reduce insulin resistance.
Has lipotropic effect, improves liver function. Has a detoxifying effect in case of poisoning with salts of heavy metals and with other intoxications.
Suction and distribution
When ingested quickly and fully absorbed into the digestive tract, taking with food simultaneously reduces the absorption of the drug. Bioavailability - 30-60% due to the effect of "first passage" through the liver. The time to reach C max is 25-60 min.
Metabolism and excretion
Metabolized in the liver by side chain oxidation and conjugation. V d = 450 ml / kg. The total plasma clearance is 10-15 ml / min.
Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T 1/2 - 25 min.
- diabetic polyneuropathy;
- alcoholic polyneuropathy.
The drug is taken orally, on an empty stomach, 30 minutes before a meal. Tablets should be swallowed whole, without chewing, squeezed with enough liquid.
The recommended dose is 1 tablet. (600 mg) 1 time / day.
It is possible to perform 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 tablets is 3 months. In some cases, therapy with Octlipen В® suggests a longer-term use. Duration of admission is determined by the attending physician.
Possible side effects with Oktalipen В® are given in the descending incidence frequency: very often (1 Г— 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10 000, <1/1000), very rarely (<1/10 000). Correlations in the incidence of side effects with the sex and age of patients are not observed.
From the side of the central nervous system: very rarely - a change or violation of taste sensations.
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); possibly the development of hypoglycemia, the symptoms of which include dizziness, increased sweating, headache, impaired vision.
From the immune system: very rarely - allergic reactions, such as skin rash, hives, itching.
- the period of lactation (breastfeeding);
- children and adolescents under 18 years of age (efficacy and safety not established);
- hypersensitivity to thioctic acid and the components of the drug.
PREGNANCY AND LACTATION
The use of the drug in pregnancy is contraindicated in connection with the lack of sufficient clinical experience with the use of thioctic acid in pregnant women.Reproductive toxicity studies did not reveal any risks with respect to fertility, effects on fetal development and any embryotoxic properties of the drug.
The use of the drug Oktalipen В® during lactation is contraindicated because there is no data on the penetration of thioctic acid into breast milk.
APPLICATION FOR CHILDREN
The use of the drug in children and adolescents under the age of 18 is contraindicated (efficacy and safety not established).
During the treatment period (especially at the initial stage), regular monitoring of blood glucose in patients with diabetes mellitus 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 the drug Oktolipen В® should refrain from drinking alcohol.
Simultaneous eating can interfere with the absorption of the drug.
When taking Oktolipen В®, the use of dairy products is not recommended (because of the calcium content in them). The interval between doses should be at least 2 hours.
Impact on the ability to drive vehicles and manage mechanisms
The effect on the ability to drive vehicles and mechanisms has not been specially studied. Required
be careful when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
Symptoms: headache, nausea, vomiting. In severe cases (when taking tioctic acid in a dose of 10-40 g or more 10 tablets at 600 mg for adults, or at a dose> 50 mg / kg of body weight in children): psychomotor agitation or confusion, generalized convulsions, severe disorders acid-base balance with lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, hemolysis, DIC-syndrome, suppression of bone marrow activity, multiple organ failure.
Treatment: when suspected of a substantial overdose of the drug, immediate hospitalization and the application of measures are recommended in accordance with the general principles adopted for accidental poisoning (calling up vomiting, washing the stomach, taking activated charcoal, etc.). Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication is symptomatic, it should be performed in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion or filtration methods with forced removal of thioctic acid from the body are not effective.
Enhances the anti-inflammatory effect of GCS.
Reduces the effectiveness of cisplatin.
Strengthens the action of insulin and oral hypoglycemic drugs (you need to adjust their dose, as well as regular monitoring of glucose in the blood to avoid hypoglycemia).
Simultaneous administration of the drug Oktalipen В® and preparations of iron, magnesium and calcium is not recommended (due to the formation of a complex with metals). The interval between the reception should be at least 2 hours.
Ethanol and its metabolites weaken the therapeutic activity of thiectic acid.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years.