Composition
Active ingredient: Â
acetylcysteine – 200.00 mg.
Auxiliary substances: Â cellulose microcrystalline – 136,40 mg, lactose monohydrate (milk sugar) – 20,00 mg crospovidone – 20,00 mg, povidone-To 25 – 8,00 mg, lemon flavor – 4.00 mg, sodium saccharin – 3,30 mg, aspartame – 2,70 mg, citric acid monohydrate and 1.30 mg, silicon dioxide colloid – 3,00 mg, magnesium stearate – 1,30 mg.
Pharmacological action of
Acetylcysteine – mucolytic, expectorant, used to liquefy the mucus in 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 sputum glycoprotein aggregates, 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 mucosal cells of the bronchi, the secret of which lyses fibrin.
Acetylcysteine dilutes sputum, increases its volume, facilitates sputum separation and significantly softens cough.
In addition to its direct mucolytic action, acetylcysteine has powerful antioxidant pneumoprotective properties that effectively protect the respiratory system from the toxic effects of negative factors: inflammatory metabolites, environmental factors, and tobacco smoke.
Acetylcysteine has a direct antioxidant effect, since it includes a free thiol group (-SH), which can interact directly and neutralize electrophilic oxidative toxins.
In addition, it reduces the induced hyperplasia of mucoid cells, increases the production of surfactants by stimulating type II pneumocytes, and stimulates mucociliary activity, which leads to an improvement in mucociliary clearance.
It stimulates mucosal cells of the bronchi, the secret of which lyses fibrin. It has a similar effect on the secret formed in inflammatory diseases of ENT organs.
Acetylcysteine protects alpha-1-antitrypsin (an enzyme that inhibits elastases) from the loss of activity that can occur as a result of exposure to HOCL, a powerful oxidizing 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 appear within 1-2 days after the start of therapy.
Indications
Mucolytic agent for the treatment of acute and chronic respiratory diseases associated with excessive bronchial secretion: bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, emphysema, laryngotracheitis, interstitial lung diseases, lung atelectasis (due to blockage of the bronchi by a mucous plug).
Catarrhal and purulent otitis, sinusitis, sinusitis (relief of discharge 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;Â
- peptic ulcer of stomach and duodenum in the acute stage,
- hemoptysis,
- pulmonary hemorrhage,
- hereditary lactose intolerance,
- lactase deficiency,
- glucose-galactose malabsorption,
- phenylketonuria,
- children up to age 2 years (for dispersible tablets 100 mg,200 mg),
- children up to age 14 years (for dispersible tablets 600 mg),
- pregnancy and breastfeeding.
With caution: – Bronchial asthma, – hepatic and/or renal insufficiency, – adrenal diseases, – esophageal varicose veins, – arterial hypertension, – tendency to pulmonary bleeding, hemoptysis, – history of stomach and duodenal ulcer, – histamine intolerance (long-term use of the drug should be avoided, since acetylcysteine affects the metabolism of histamine and may lead to signs of intolerance such as headache, vasomotor rhinitis, or pruritus).
Side effects
The frequency 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 (
For each frequency group, adverse events are presented in descending order of severity.
From the immune system: Â infrequently-hypersensitivity; very rarely-anaphylactic shock, anaphylactic / anaphylactoid reaction.
Nervous system disorders: Â infrequently – headache.
From the side of the organs of hearing and inner ear: Â infrequently-tinnitus.
From the heart: infrequently-tachycardia.
From the vascular system: Â very rarely – bleeding.
From the respiratory system of the thoracic aunt and mediastinum: Â rarely-bronchospasm, dyspnoea.
Gastrointestinal disorders: Â infrequently-vomiting, diarrhea, stomatitis, abdominal pain, nausea; rarely-dyspepsia.
Skin and subcutaneous tissue disorders: Â infrequently – urticaria, rash, angioedema, pruritus.
General violations and conditions in the areas of use: Â infrequently-pyrexia;Â frequency unknown-facial edema.
Analysis and research: Â infrequently – low blood pressure.
In very rare cases, serious 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 concomitant medication may have been involved in triggering the above-mentioned mucocutaneous syndromes.
For this reason, you should immediately consult a doctor if any new skin or mucosal 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 any of the side effects listed in the instructions, or they get worse, 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 simultaneously with such antibiotics as tetracyclines (excluding doxycycline), ampicillin, amphotericin B, their interaction with the thiol group of acetylcysteine is possible, which leads to a decrease in the activity of both drugs. Therefore, the interval between taking these drugs should be at least 2 hours.
Concomitant use of acetylcysteine and nitroglycerin may cause a marked decrease in blood pressure and headache.
Concomitant use of acetylcysteine and carbamazepine may result in subtherapeutic levels of carbamazepine.
Activated carbon 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 the urine.
How to take, course of use and dosage
Dispersible tablets can be taken in various ways: the tablet can be swallowed whole, washed down with water, or previously, before taking, dissolved in water. Tablets should be dissolved in at least 50 ml of water. Before taking it, the resulting suspension should be thoroughly mixed.
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 apetilcysteine 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 apetilcysteine per day).
– children from 6 to 14 years: 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).
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