Acetylcysteine Canon - instructions for use, dose, side effects, contraindications

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). Has a pronounced mucolytic effect, belongs to the class of direct mucolytics.

The action of acetylcysteine is related to the ability of a free sulfhydryl group to cleave intra- and intermolecular disulfide bonds of aggregates of sputum glycoproteins,which leads to the depolarization of mucoproteins, providing a strong diluting effect and reducing the viscosity of mucus. Acetylcysteine shows mucolytic activity against any kind of sputum - mucous, mucoidal, 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. Stimulates mucous cells of bronchi, the secret of which lyses fibrin.

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

In addition to direct mucolytic action, acetylcysteine possesses powerful antioxidant pneumoprotective properties, which provide effective protection of respiratory organs from toxic effects of negative factors: metabolites of inflammation, environmental factors, tobacco smoke.

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

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

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

Mucolytic properties of acetylcysteine begin to appear within 1-2 days from the start of therapy. With preventive reception, acetylcysteine reduces the frequency and severity of exacerbations of chronic bronchitis and cystic fibrosis.

Pharmacokinetics:

After oral administration acetylcysteine quickly and almost completely absorbed in the digestive tract. In the liver, it is metabolized to cysteine (pharmacologically active metabolite) and diacetylcystine, cystine and then to mixed disulfides.Bioavailability of acetylcysteine after ingestion is about 10% because of the pronounced effect of "first passage" through the liver. The maximum concentration of the drug (C_mOh) after oral administration is achieved after 1-3 hours. In organism acetylcysteine and its metabolites are determined in various forms: in part as a free substance, partly in connection with blood plasma proteins, in part as incorporated amino acids. Excreted almost completely in the form of inactive metabolites (inorganic sulfates, diacetylcystine) by the kidneys. Only a small amount of acetylcysteine is excreted unchanged through the intestine. Half-life time (T_1/2) from the blood plasma is approximately 1 hour and depends on the rate of biotransformation in the liver. With hepatic failure, it can increase to 8 hours. Acetylcysteine can penetrate through the placental barrier and accumulate in the amniotic fluid.

Indications:

Acetylcysteine is used to treat diseases of the respiratory system, accompanied by the formation of viscous hard-to-separate sputum:

- acute and chronic bronchitis;

- obstructive bronchitis;

- tracheitis;

- laryngotracheitis;

- pneumonia;

- abscess of the lung;

- bronchiolitis;

- bronchiectatic disease;

- bronchial asthma;

- cystic fibrosis;

- chronic obstructive pulmonary disease (COPD);

- acute and chronic sinusitis;

- inflammation of the middle ear (otitis media).

Contraindications:

- Hypersensitivity to acetylcysteine and other components of the drug;

- dsugar content / isomaltase, fructose intolerance, glucose-galactose malabsorption;

- phenylketonuria;

- dChildren under 6 years (for a dosage of 200 mg), children under 2 years (for a dosage of 100 mg);

- bPregnancy and the period of breastfeeding.

Carefully:

Bronchial asthma, hepatic and / or renal insufficiency, adrenal diseases, esophageal varicose veins, arterial hypertension, propensity to pulmonary hemorrhage, hemoptysis, gastric and duodenal ulcer in history, histamine intolerance. acetylcysteine affects the metabolism of histamine and can lead to signs of intolerance, such as headache, vasomotor rhinitis, itching).

Pregnancy and lactation:

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

Dosing and Administration:

Inside. Granules should be dissolved in water at room temperature and taken after meals.

DRulas for solution for oral administration 100 mg, 200 mg.

In the absence of other prescriptions, the following dosages should be adhered to:

Mucolytic therapy

Adults and adolescents older than 14 years: it is recommended to take 2 packets of the drug Acetylcysteine Canon 100 mg or 1 packet of the drug Acetylcysteine Canon 200 mg 2-3 times a day (400-600 mg per day).

Children aged 6 to 14 years: it is recommended to take 1 sachet 3 times a day or 2 sachets 2 times a day of the drug Acetylcysteine Kanon 100 mg (300-400 mg per day). Preparation Acetylcysteine Canon 200 mg should be taken 1/2 bag 3 times a day or 1 packet 2 times a day (300-400 mg per day).

Children aged 2 to 6 years: It is recommended to take 1 packet of the drug Acetylcysteine Canon 100 mg 2-3 times a day (200-300 mg per day).

Cystic Fibrosis

Children over the age of 6: It is recommended to take 2 packets of the drug Acetylcysteine Canon 100 mg or 1 packet of the drug Acetylcysteine Canon 200 mg 3 times a day (600 mg per day).

Children aged 2 to 6 years: it is recommended to take 1 packet of the drug Acetylcysteine Kanon 100 mg 4 times a day (400 mg per day).

Patients with cystic fibrosis and a body weight of more than 30 kg, if necessary, may increase the dose to 800 mg of acetylcysteine per day.

Additional fluid intake enhances the mucolytic effect of the drug.

With short-term catarrhal diseases, the duration of admission is 5-7 days.

For long-term illnesses, the duration of therapy is determined by the attending physician. In chronic bronchitis and cystic fibrosis, the drug should be taken for a longer time to achieve a preventive effect in infections.

Caveats:

Granules for solution for oral administration 200 mg

Due to the high content of active ingredient (200 mg of acetylcysteine in the bag), it is not necessary to take the drug to children under the age of 6 years. In this case, it is recommended to use the drug Acetylcysteine Canon in other dosage forms with a lower content of acetylcysteine.

Granules for solution for oral administration 600 mg

In the absence of other prescriptions, the following dosages are recommended.

1 packet of the drug Acetylcysteine Canon 600 mg once a day (600 mg of acetylcysteine per day).

Caveats:

Due to the high content of active ingredient (600 mg of acetylcysteine in a bag), do not take the drug to children under the age of 14 years. In this case, it is recommended to use the drug Acetylcysteine Canon in other dosage forms with a lower content of acetylcysteine.

With short-term catarrhal diseases, the duration of admission is 5-7 days.

In chronic bronchitis and cystic fibrosis, the drug should be taken for a longer time to achieve a preventive effect in infections.

Side effects:

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (≥1 / 10); often (≥1 / 100 and <1/10); infrequently (≥1 / 1000 and <1/100); rarely (≥1 / 10000 and <1/1000); very rarely (<1/10000); frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

Allergic reactions: infrequently - skin itching, rashes, exanthema, urticaria, angioedema, lowering of blood pressure,tachycardia; very rarely - anaphylactic reactions up to anaphylactic shock, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

From the nervous system: very rarely - a headache.

From the side of the cardiovascular system: very rarely - lowering blood pressure, increasing heart rate (tachycardia).

From the respiratory system: rarely shortness of breath, bronchospasm (mainly in patients with bronchial hyperreactivity in bronchial asthma).

From the gastrointestinal tract: infrequently - stomatitis, abdominal pain, nausea, vomiting, diarrhea, heartburn, indigestion.

From the sense organs: infrequently, noise in the ears.

Other: very rarely - fever, isolated reports of bleeding due to the presence of hypersensitivity reactions, reduced platelet aggregation.

Overdose:

Symptoms: with erroneous or deliberate overdosage, such phenomena as diarrhea, vomiting, stomach pain, heartburn and nausea are observed. To date, no serious and life-threatening side effects have been observed.

Treatment: symptomatic.

Interaction:

With the simultaneous use of acetyl cysteine and antitussive agents, mucus congestion may occur due to suppression of the cough reflex. Therefore, such combinations should be selected with caution.

Pharmaceutically incompatible with antibiotics (penicillins, cephalosporins, erythromycin, tetracycline and amphotericin B) and proteolytic enzymes.

Reduces the absorption of penicillins, cephalosporins, tetracycline (they should be taken no earlier than 2 hours after ingestion of acetylcysteine).

Simultaneous intake of acetylcysteine and nitroglycerin may lead to an increase in the vasodilator effect of the latter.

Upon contact with metals, rubber, sulphides with a characteristic odor are formed.

Special instructions:

In the treatment of patients with diabetes it is necessary to take into account that the preparation contains sucrose (1 packet of Acetylcysteine Canon 600 mg corresponds to 0.19 XE, 200 mg to 0.23 XE, 100 mg to 0.24 XE).

When working with the drug should use glassware, avoid contact with metals, rubber, oxygen, easily oxidizable substances.

With the use of acetylcysteine, very rarely reported cases of severe allergic reactions, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).If skin and mucous membrane changes occur, the doctor should be consulted immediately, and the drug should be discontinued.

Do not take the drug immediately before bedtime (it is recommended to take the drug before 6pm).

Effect on the ability to drive transp. cf. and fur:

In therapeutic doses, the drug Acetylcysteine Canon does not affect the ability to drive vehicles and mechanisms.

Form release / dosage:

Granules for the preparation of oral solution, 100 mg, 200 mg and 600 mg.

Packaging:

3 grams per pack of combined material (paper / foil / polyethylene).

Dosages of 100 mg and 200 mg: 20 packs along with instructions for use are placed in a pack of cardboard.

Dosage 600 mg: for 6 or 10 packs, along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003938

Date of registration:07.11.2016

Expiration Date:07.11.2021

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acetylcysteine ​​Canon (Acetylcysteine ​​Canon)

Acetylcysteine Canon (Acetylcysteine Canon)