Expiration date: 08/2027

Composition

One tablet of 100 mg:

Active substance: acetylcysteine - 100.00 mg.

Excipients: microcrystalline cellulose - 68.20 mg, lactose monohydrate (milk sugar) - 10.00 mg, crospovidone - 10.00 mg, povidone-K25 - 4.00 mg, lemon flavor - 2.00 mg, sodium saccharinate - 1.65 mg, aspartame - 1.35 mg, citric acid monohydrate - 0.65 mg, colloidal silicon dioxide - 1.50 mg, magnesium stearate - 0.65 mg.

One tablet of 200 mg:

Active substance: acetylcysteine - 200.00 mg.

Excipients: microcrystalline cellulose - 136.40 mg, lactose monohydrate (milk sugar) - 20.00 mg, crospovidone - 20.00 mg, povidone-K25 - 8.00 mg, lemon flavor - 4.00 mg, sodium saccharinate - 3.30 mg, aspartame - 2.70 mg, citric acid monohydrate - 1.30 mg, colloidal silicon dioxide - 3.00 mg, magnesium stearate - 1.30 mg.

One 600 mg tablet:

Active substance: acetylcysteine - 600.00 mg.

Excipients: microcrystalline cellulose - 409.20 mg, lactose monohydrate (milk sugar) - 60.00 mg, crospovidone - 60.00 mg, povidone-K25 - 24.00 mg, lemon flavor - 12.00 mg, sodium saccharinate - 9.90 mg, aspartame - 8.10 mg, citric acid monohydrate - 3.90 mg, colloidal silicon dioxide - 9.00 mg, magnesium stearate - 3.90 mg.

Dosage form

dispersible tablets

Description

The dosage is 100 mg

Round, flat-cylindrical tablets of white or beige-tinged white with slight marbling and surface roughness, with a characteristic odor, chamfered and risked.

Dosages of 200 mg and 600 mg

Oval, biconvex tablets of white or beige-tinged white with slight marbling and surface roughness, with a characteristic odor, with a risk.

Pharmacodynamics

Acetylcysteine is a mucolytic expectorant used to dilute sputum in diseases of the respiratory system. Acetylcysteine is a derivative of the natural amino acid cysteine (N-acetyl-L-cysteine). It has a pronounced mucolytic effect, belongs to the class of direct mucolytics.

The action of acetylcysteine is associated with the ability of the free sulfhydryl group to cleave intra- and intermolecular disulfide bonds of aggregates of sputum glycoproteins, which leads to depolymerization of mucoproteins, exerting a strong diluting effect and reducing the viscosity of mucus. Acetylcysteine exhibits mucolytic activity against any type of sputum - mucosal, mucopurulent, purulent. Acetylcysteine increases the secretion of less viscous sialomucins by goblet cells, reduces the adhesion of bacteria to the epithelial cells of the bronchial mucosa. It stimulates bronchial mucosal cells, the secret of which is lysed by fibrin.

Acetylcysteine dilutes sputum, increases its volume, facilitates sputum separation and significantly softens cough.

In addition to its direct mucolytic effect, acetylcysteine has powerful antioxidant pneumoprotective properties that provide effective respiratory protection from the toxic effects of negative factors: inflammatory metabolites, environmental factors, and tobacco smoke.

Acetylcysteine has a direct antioxidant effect because it includes a free thiol group (-SH) capable of interacting directly and neutralizing electrophilic oxidative toxins.

In addition, it reduces induced hyperplasia of mucoid cells, enhances the production of surfactants by stimulating type II pneumocytes, and stimulates mucociliary activity, which leads to improved mucociliary clearance.

It stimulates bronchial mucosal cells, the secret of which is lysed by fibrin. It has a similar effect on secretions formed in inflammatory diseases of the ENT organs.

Acetylcysteine protects alpha1-antitrypsin (an enzyme that inhibits elastase) from loss of activity that may occur as a result of exposure to HOCL, a powerful oxidative substance produced by the myeloperoxidase enzyme of active phagocytes.

Easily penetrating into the cell, acetylcysteine is deacetylated, releasing L-cysteine, an amino acid necessary for the synthesis of glutathione, which is the most important factor in intracellular protection against exogenous and endogenous oxidative toxins and various cytotoxic substances. This feature of acetylcysteine makes it possible to effectively use the latter in acute poisoning with paracetamol and other toxic substances (aldehydes, phenols, etc.).

The mucolytic properties of acetylcysteine begin to manifest themselves within 1-2 days of the start of therapy.

Pharmacokinetics

Absorption

Acetylcysteine is well absorbed by oral administration. It is immediately deacetylated to cysteine in the liver. A mobile balance of free acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine) is observed in the blood. Due to the high effect of the first passage through the liver, the bioavailability of acetylcysteine is about 10%.

Distribution

Acetylcysteine is distributed both unchanged (20%) and as active metabolites (80%), penetrates into the intercellular space, and is mainly distributed in the liver, kidneys, lungs, and bronchial secretions. The volume of distribution of acetylcysteine varies from 0.33 to 0.47 l / kg, the maximum plasma concentration is reached 1-3 hours after oral administration and is 15 mmol / l, the binding to plasma proteins is 50% 4 hours after administration and decreases to 20% after 12 hours. Penetrates through the placental barrier.

Metabolism

After oral administration, acetylcysteine is rapidly and extensively metabolized in the intestinal walls to form a pharmacologically active metabolite, cysteine, as well as cystine and diacetylcysteine.

Withdrawal

It is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestine. The half-life is about 1 hour, with impaired liver function it increases to 8 hours.

Indications for use

Mucolytic agent for the treatment of acute and chronic respiratory diseases associated with excessive secretion of bronchial secretions: bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, pulmonary emphysema, laryngotracheitis, interstitial lung diseases, lung atelectasis (due to blockage of the bronchi with a mucous plug).

Catarrhal and purulent otitis media, sinusitis, sinusitis (relief of secretions).

Removal of viscous secretions from the respiratory tract in post-traumatic and postoperative conditions.

Contraindications

Hypersensitivity to acetylcysteine and other components of the drug, peptic ulcer of the stomach and duodenum in the acute stage, hemoptysis, pulmonary bleeding, hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption, phenylketonuria, children under 2 years of age (for 100 mg, 200 mg dispersible tablets), children under 14 years of age (for 600 mg dispersible tablets), pregnancy and lactation.

Use during pregnancy and lactation

The use of the drug during pregnancy and lactation is contraindicated.

Side effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very common (1/10), common (1/100, <,1/10), infrequent (1/1000, <, 1/100), rare (1/10 000, <, 1/1000), very rare (<,1/10 000), frequency unknown: the frequency cannot be evaluated based on the available data.

For each frequency group, the adverse events are presented in descending order of severity.

From the immune system: infrequently - hypersensitivity, very rarely - anaphylactic shock, anaphylactic / anaphylactoid reaction.

From the nervous system: infrequently - headache.

From the organs of hearing and the inner ear: infrequently - tinnitus.

From the side of the heart: infrequently - tachycardia.

From the vascular system: very rarely - bleeding.

Respiratory system disorders of the thoracic cavity and mediastinum: rarely - bronchospasm, dyspnea.

Gastrointestinal disorders: infrequently - vomiting, diarrhea, stomatitis, abdominal pain, nausea, rarely - dyspepsia.

From the skin and subcutaneous tissues: infrequently - urticaria, rash, angioedema, itching.

Common disorders and conditions at the site of application: infrequently - pyrexia, frequency unknown - facial edema.

Tests and studies: infrequently - low blood pressure.

In very rare cases, severe skin reactions such as Stevens-Johnson syndrome and Lyell's syndrome have been reported, depending chronologically on the use of acetylcysteine. In most cases, at least one drug taken at the same time could be involved in triggering the above-mentioned mucocutaneous syndromes. For this reason, you should immediately consult a doctor if any new skin or mucous membrane changes occur, and immediately stop taking acetylcysteine.

A decrease in platelet aggregation in the presence of acetylcysteine has been confirmed by various studies. The clinical significance has not yet been established.

If you experience side effects listed in the instructions, or they worsen, or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction

The combined use of acetylcysteine with antitussive agents may increase sputum congestion due to suppression of the cough reflex.

When used concomitantly with antibiotics such as tetracyclines (excluding doxycycline), ampicillin, and amphotericin B, they may interact with the thiol group of acetylcysteine, which leads to a decrease in the activity of both drugs. Therefore, the interval between taking these drugs should be at least 2 hours.

Simultaneous administration of acetylcysteine and nitroglycerin can cause a marked decrease in blood pressure and headache.

The simultaneous use of acetylcysteine and carbamazepine may result in subtherapeutic carbamazepine levels.

Activated charcoal can reduce the effect of acetylcysteine.

Acetylcysteine eliminates the toxic effects of paracetamol.

Acetylcysteine may affect the results of colorimetric determination of salicylates. Acetylcysteine may affect the analysis of ketones in urine.

Method of administration and dosage

Dispersible tablets can be taken in various ways: the tablet can be swallowed whole, washed down with water, or dissolved in water before taking it. Tablets should be dissolved in at least 50 ml of water. The resulting suspension should be thoroughly mixed before use.

Mucolytic therapy

Adults: 600 mg (in terms of the required number of dispersible tablets) 1 time per day or 300 mg (in terms of the required number of dispersible tablets) 2 times a day or 200 mg (in terms of the required number of dispersible tablets) 3 times a day.

The maximum daily dose of apethylcysteine is 600 mg/day.

Children:

• children from 2 to 6 years: 100 mg (in terms of the required number of dispersible tablets) 2-3 times a day (corresponds to 200-300 mg of apethylcysteine per day).
• children from 6 to 14 years of age: 100 mg (in terms of the required number of dispersible tablets) 3-4 times a day or 200 mg (in terms of the required number of dispersible tablets) 2 times a day (corresponds to 300-400 mg of acetylcysteine per day).
• children over 14 years of age: 300 mg (in terms of the required number of dispersible tablets) 2 times a day or 200 mg (in terms of the required number of dispersible tablets) 2-3 times a day (corresponds to 400-600 mg of acetylcysteine per day).

Cystic fibrosis

• children from 2 to 6 years: 100 mg (in terms of the required number of dispersible tablets) 3-4 times a day (corresponds to 300-400 mg of acetylcysteine per day),
• children from 6 to 14 years of age: 100 mg (in terms of the required number of dispersible tablets) 4 times a day or 200 mg (in terms of the required number of dispersible tablets) 2-3 times a day (corresponds to 400-600 mg of acetylcysteine per day),
• children over 14 years of age and adults: 200 mg (based on the required number of dispersible tablets) 3 times a day or 300 mg (based on the required number of dispersible tablets) 2 times a day (corresponds to 600 mg of acetylcysteine per day).

The duration of treatment should be assessed individually. In acute diseases, the duration of the course of treatment is from 5 to 10 days, in the treatment of chronic diseases - up to several months (on the recommendation of a doctor).

If there is no improvement after treatment, or if the symptoms worsen or new symptoms appear, you should consult your doctor. Use the drug only according to the method of application and in the doses specified in the instructions.

Overdose

Acetylcysteine when taken at a dose of 500 mg / kg / day does not cause signs and symptoms of overdose.

Symptoms

The following symptoms may occur: nausea, vomiting, and diarrhea.

Treatment

There is no specific antidote, and the treatment is symptomatic.

Special instructions

The drug contains aspartame, its use in patients with phenylketonuria is contraindicated.

When acetylcysteine is dissolved, it is necessary to use glassware, avoid contact with metal, rubber surfaces, oxygen and easily oxidizing substances.

Cases of severe allergic reactions, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), have been reported very rarely with the use of acetylcysteine. If changes in the skin and mucous membranes occur, you should immediately consult a doctor, and the drug should be discontinued.

Acetylcysteine should be prescribed with caution to patients with bronchial asthma and obstructive bronchitis under systematic monitoring of bronchial patency.

Do not take the drug immediately before bedtime (it is recommended to take the drug before 18:00).

Acetylcysteine may have a minor effect on histamine metabolism, so caution should be exercised when using the drug for the long-term treatment of patients suffering from histamine intolerance, with symptoms of intolerance (headache, vasomotor rhinitis, pruritus).

Influence on the ability to drive motor vehicles and manage mechanisms

In therapeutic doses, acetylcysteine does not affect the ability to drive vehicles and mechanisms.

Form of release

Dispersible tablets, 100 mg, 200 mg and 600 mg.

Packaging

10, 25 or 30 tablets each in a contoured cell package made of polyvinyl chloride film and aluminum foil printed varnished.

By 10, 20, 25, 30, 50, 60 or 100 tablets in cans made of polyethylene terephthalate for medicines or polypropylene for medicines, capped with lids made of high-pressure polyethylene with first-opening control or polypropylene lids with a push-turn system or lids made of low-pressure polyethylene with first-opening control.

One jar or 1, 2, 3, 4, 5, 6 or 10 contour cell packages together with the instructions for use are placed in a cardboard package (pack).

It is allowed to pack 2 or 3 cardboard packages (bundles) into a group package (shipping container) made of cardboard for consumer packaging.

Conditions of release from pharmacies

Without a prescription

Storage conditions

At a temperature not exceeding 25 C.

Keep out of reach of children.

Expiration date

3 years. Do not use after the expiration date.