Mucoflustein (Powder) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

R05CB01 (Acetylcysteine)

Active Substance

Acetylcysteine (Rec.INN registered by WHO)

Dosage Forms

	Mucoflustein	Powder for oral solution 200 mg
		Powder for oral solution 600 mg

Dosage Form, Packaging, and Composition

Powder for oral solution

1 g – sachets (10) – cardboard packs – Over-the-Counter
1 g – sachets (12) – cardboard packs – Over-the-Counter
1 g – sachets (14) – cardboard packs – Over-the-Counter
1 g – sachets (15) – cardboard packs – Over-the-Counter
1 g – sachets (20) – cardboard packs – Over-the-Counter
1 g – sachets (3) – cardboard packs – Over-the-Counter
1 g – sachets (30) – cardboard packs – Over-the-Counter
1 g – sachets (4) – cardboard packs – Over-the-Counter
1 g – sachets (5) – cardboard packs – Over-the-Counter
1 g – sachets (6) – cardboard packs – Over-the-Counter
1 g – sachets (60) – cardboard packs – Over-the-Counter
1 g – sachets (7) – cardboard packs – Over-the-Counter
1 g – sachets (8) – cardboard packs – Over-the-Counter
1 g – sachets (9) – cardboard packs – Over-the-Counter

Powder for oral solution

3 g – sachets (10) – cardboard packs – Over-the-Counter
3 g – sachets (12) – cardboard packs – Over-the-Counter
3 g – sachets (14) – cardboard packs – Over-the-Counter
3 g – sachets (15) – cardboard packs – Over-the-Counter
3 g – sachets (20) – cardboard packs – Over-the-Counter
3 g – sachets (3) – cardboard packs – Over-the-Counter
3 g – sachets (30) – cardboard packs – Over-the-Counter
3 g – sachets (4) – cardboard packs – Over-the-Counter
3 g – sachets (5) – cardboard packs – Over-the-Counter
3 g – sachets (6) – cardboard packs – Over-the-Counter
3 g – sachets (60) – cardboard packs – Over-the-Counter
3 g – sachets (7) – cardboard packs – Over-the-Counter
3 g – sachets (8) – cardboard packs – Over-the-Counter
3 g – sachets (9) – cardboard packs – Over-the-Counter

Clinical-Pharmacological Group

Mucolytic drug

Pharmacotherapeutic Group

Drugs used for cough and colds; expectorants, excluding combinations with antitussives; mucolytic agents

Pharmacological Action

Acetylcysteine is a mucolytic agent, a derivative of the amino acid cysteine. It exerts a mucolytic effect, increases sputum volume, and facilitates its expectoration by directly affecting the rheological properties of sputum. The action of acetylcysteine is associated with the ability of its sulfhydryl groups to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides in sputum, which leads to the depolarization of mucoproteins and a decrease in sputum viscosity.

It reduces induced hyperplasia of mucoid cells, enhances the production of surface-active compounds by stimulating type II pneumocytes, and stimulates mucociliary activity, leading to improved mucociliary clearance.

It remains active in the presence of purulent, mucopurulent, and mucous sputum.

It increases the secretion of less viscous sialomucins by goblet cells and reduces bacterial adhesion to epithelial cells of the bronchial mucosa. It stimulates mucosal cells of the bronchi, the secretion of which lyses fibrin. It has a similar effect on the secretion formed in inflammatory diseases of the ENT organs.

It has an antioxidant effect due to the ability of its reactive sulfhydryl groups (SH-groups) to bind with oxidative radicals and thus neutralize them.

Acetylcysteine easily penetrates into the cell, is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant and cytoprotector, neutralizing endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and promotes an increase in the synthesis of intracellular glutathione, which is involved in the redox processes of cells, promoting the detoxification of harmful substances. This explains the action of acetylcysteine as an antidote in paracetamol poisoning.

It protects alpha1-antitrypsin (elastase inhibitor) from the inactivating effect of HOCl, an oxidant produced by myeloperoxidase of active phagocytes. It also has an anti-inflammatory effect (by suppressing the formation of free radicals and reactive oxygen species responsible for the development of inflammation in the lung tissue).

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. It is largely subject to the first-pass effect through the liver, which leads to reduced bioavailability. Plasma protein binding is up to 50% (4 hours after oral administration). It is metabolized in the liver and possibly in the intestinal wall. It is detected in the plasma unchanged, as well as in the form of metabolites – N-acetylcysteine, N,N-diacetylcysteine, and cysteine ester.

Renal clearance accounts for 30% of total clearance.

Indications

As a 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; pulmonary emphysema; laryngotracheitis; interstitial lung diseases; lung atelectasis (due to bronchial obstruction by a mucous plug); in catarrhal and purulent otitis, sinusitis (to facilitate secretion discharge); to remove viscous secretion from the airways in post-traumatic and postoperative conditions.

Preparation for bronchoscopy, bronchography, aspiration drainage.

For washing abscesses, nasal passages, maxillary sinuses, middle ear, treating fistulas, and the surgical field during operations on the nasal cavity and mastoid process.

As an antidote in adults and children for the treatment of paracetamol overdose.

ICD codes

Dosage Regimen

It is taken orally, in the form of inhalations, intratracheally, and also topically. It is administered intravenously.

The dose depends on the patient’s age. The frequency and duration of the course are set individually.

Topically – instilled into the external auditory canal and nasal passages.

Intravenous therapy is intended for use in ICU patients and only when oral administration of acetylcysteine is not possible.

Adverse Reactions

Blood and lymphatic system disorders very rarely – decreased platelet aggregation.

Immune system disorders uncommon – hypersensitivity reactions, angioedema; very rarely – anaphylactic reactions up to anaphylactic shock, bleeding (isolated reports in connection with the presence of a hypersensitivity reaction).

Nervous system disorders rare – headache.

Ear and labyrinth disorders uncommon – tinnitus.

Cardiac disorders uncommon – tachycardia, decreased blood pressure; cases of collapse have been described with acetylcysteine use.

Respiratory, thoracic and mediastinal disorders rare – dyspnea, bronchospasm (mainly in patients with bronchial hyperreactivity in bronchial asthma).

Gastrointestinal disorders uncommon – stomatitis, abdominal pain, diarrhea, nausea, vomiting; rare – heartburn, dyspepsia.

Skin and subcutaneous tissue disorders uncommon – skin itching, skin rash, exanthema, urticaria; very rarely – Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

General disorders and administration site conditions very rarely – fever; frequency unknown – facial edema.

Contraindications

Hypersensitivity to acetylcysteine; peptic ulcer of the stomach and duodenum in the acute phase, breastfeeding period, children under 2 years of age (except for use as an antidote).

Contraindications for use in children under 18 years of age depend on the dosage form and are indicated in the instructions for use of the specific drug.

With caution

Hemoptysis, pulmonary hemorrhage; history of peptic ulcer of the stomach and duodenum; esophageal varices; bronchial asthma; obstructive bronchitis; hepatic and/or renal failure; adrenal gland diseases; arterial hypertension; histamine intolerance.

Use in Pregnancy and Lactation

Use is contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Acetylcysteine should be used with caution in patients with liver diseases.

Use in Renal Impairment

Acetylcysteine should be used with caution in patients with kidney diseases.

Pediatric Use

Use is contraindicated in children under 2 years of age.

Contraindications for use in children under 18 years of age depend on the dosage form and are indicated in the instructions for use of the specific drug.

Special Precautions

In patients with bronchial asthma and obstructive bronchitis, Acetylcysteine should be used with caution and under systematic control of bronchial patency.

Acetylcysteine may slightly affect histamine metabolism, so caution should be exercised when using this agent for long-term treatment of patients suffering from histamine intolerance, if symptoms of intolerance appear (headache, vasomotor rhinitis, itching).

If changes in the skin and mucous membranes occur, you should immediately consult a doctor and stop taking acetylcysteine.

Use in patients with renal and/or hepatic insufficiency should be avoided to prevent additional formation of nitrogenous compounds.

If the patient is unable to cough effectively, drainage or aspiration of the secretion should be performed.

Acetylcysteine should not be taken immediately before bedtime (it is recommended to take it 4 hours before bedtime).

Strict adherence to the correspondence between the route of administration and the dosage form used must be observed.

Drug Interactions

Concomitant use of acetylcysteine with antitussive agents may increase sputum stasis due to suppression of the cough reflex.

When used concomitantly with antibiotics (including tetracycline, ampicillin, amphotericin B), their interaction with the thiol group of acetylcysteine is possible.

Concomitant administration of acetylcysteine and nitroglycerin may cause a pronounced decrease in blood pressure and headache.

Concomitant use of acetylcysteine and carbamazepine may be accompanied by a decrease in carbamazepine concentration to a subtherapeutic level.

Acetylcysteine eliminates the toxic effects of paracetamol.

Acetylcysteine may affect the results of the colorimetric determination of salicylates.

Acetylcysteine may affect the results of urine ketone analysis.

Upon contact of acetylcysteine with metals and rubber, sulfides with a characteristic odor are formed.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.