Acetylcysteine-astrapharm

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ACETYLCYSTEINE-ASTRAFARM

Composition:

Active substance: acetylcysteine;

One sachet contains 200 mg of acetylcysteine calculated as 100% substance;

Excipients: ascorbic acid, saccharin, sucrose, orange flavor.

Pharmaceutical form. Powder for oral solution.

Main physico-chemical properties: homogeneous crystalline powder of white or almost white color, without particle agglomeration, with a characteristic odor.

Pharmacotherapeutic group.
Mucolytic agents.
ATC code: R05CB01.

Pharmacological Properties.

Pharmacodynamics.

Acetylcysteine-AstraPharm is a mucolytic and expectorant agent used to liquefy mucus in respiratory tract diseases associated with the production of thick mucus. Acetylcysteine is a derivative of the amino acid cysteine. The mucolytic effect of the drug has a chemical nature. Due to its free sulfhydryl group, acetylcysteine breaks the disulfide bonds of acidic mucopolysaccharides, leading to depolymerization of mucus glycoproteins, reduction of mucus viscosity, and facilitation of expectoration and clearance of bronchial secretions. The drug retains its activity in the presence of purulent sputum.

Acetylcysteine also has antioxidant and pneumoprotective properties, due to the binding of chemical radicals by its sulfhydryl groups, thereby neutralizing them. In addition, the drug promotes increased synthesis of glutathione—an important factor in intracellular protection not only against oxidative toxins of exogenous and endogenous origin but also against various cytotoxic substances. This characteristic of acetylcysteine allows its effective use in paracetamol overdose.

Pharmacokinetics.

After oral administration, acetylcysteine is rapidly and completely absorbed and undergoes hepatic metabolism to form cysteine, a pharmacologically active metabolite, as well as diacetylcysteine, cystine, and subsequently mixed disulfides. Bioavailability is very low—approximately 10%. Maximum plasma concentration is reached within 1–3 hours after administration. Plasma protein binding is approximately 50%. Acetylcysteine is excreted by the kidneys as inactive metabolites (inorganic sulfates, diacetylcysteine).

The elimination half-life is primarily determined by rapid biotransformation in the liver and is approximately 1 hour. In case of impaired liver function, the elimination half-life is prolonged up to 8 hours.

Clinical characteristics.

Indications.

Treatment of acute and chronic diseases of the bronchopulmonary system that require reduction of sputum viscosity, improvement of sputum expectoration and clearance.

Contraindications.

Hypersensitivity to acetylcysteine or to other components of the drug. Active peptic ulcer of the stomach or duodenum, hemoptysis, pulmonary hemorrhage.

Interaction with other medicinal products and other types of interactions.

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

When administered simultaneously with antibiotics such as tetracyclines (except doxycycline), ampicillin, amphotericin B, cephalosporins, and aminoglycosides, interaction with the thiol group of acetylcysteine may occur, leading to reduced activity of both agents. Therefore, the interval between administration of these drugs should be at least 2 hours. This does not apply to cefixime and loracarbef.

Concomitant administration of nitroglycerin and acetylcysteine may enhance the vasodilatory effect of nitroglycerin.

If simultaneous use of nitroglycerin and acetylcysteine is necessary, patients should be monitored and warned about possible arterial hypotension, which may be severe and accompanied by headache.

Activated charcoal reduces the effectiveness of acetylcysteine.

It is not recommended to dissolve acetylcysteine together with other drugs in the same container.

Acetylcysteine reduces the hepatotoxic effect of paracetamol.

Synergism between acetylcysteine and bronchodilators has been observed.

Acetylcysteine may act as a cysteine donor and increase glutathione levels, promoting detoxification of oxygen radicals and certain toxic substances in the body.

Upon contact with metals or rubber, sulfides with a characteristic odor are formed; therefore, glassware should be used for dissolving the drug.

Special precautions.

Acetylcysteine should be prescribed with caution to patients with bronchial asthma due to the possible development of bronchospasm. When emptying the contents of the sachet into a container during solution preparation, the powder may become airborne and irritate the nasal mucosa, potentially causing reflex bronchospasm.

Administration of acetylcysteine results in the liquefaction of bronchial secretions. If the patient is unable to effectively expectorate mucus, postural drainage and bronchoaspiration may be required.

Acetylcysteine should be administered with caution in patients with liver or kidney disease to avoid accumulation of nitrogen-containing substances in the body.

Patients with a history of gastric or duodenal ulcer should take the medication cautiously, especially when concurrently using other medicinal agents that irritate the gastric mucosa.

Acetylcysteine affects histamine metabolism; therefore, prolonged therapy should not be prescribed to patients with histamine intolerance, as it may lead to symptoms of intolerance (headache, vasomotor rhinitis, pruritus).

There have been isolated reports of severe skin reactions (Stevens-Johnson syndrome and Lyell’s syndrome) associated with acetylcysteine use. Therefore, if skin or mucosal changes occur, the drug should be discontinued immediately and medical advice should be sought regarding further treatment.

The product contains sucrose and therefore should not be administered to patients with rare hereditary forms of fructose intolerance, sucrase-isomaltase deficiency, or glucose-galactose malabsorption syndrome.

One sachet of Acetylcysteine-Astrafarm contains 2.7 g of sucrose (approximately 0.23 bread units). This should be taken into account when administering the drug to patients with diabetes mellitus.

Use during pregnancy or breastfeeding.

During pregnancy or breastfeeding, acetylcysteine may be used only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.

Ability to influence reaction rate when driving or operating machinery.

Does not affect.

Method of Administration and Dosage.

For adults and children aged 14 years and older: 400–600 mg of acetylcysteine per day, divided into 1–3 doses.

For children aged 6 to 14 years: 400–600 mg per day, divided into 2–3 doses.

For children aged 2 to 6 years: 200–400 mg per day, divided into 2 doses.

The medication should be taken after meals. The contents of the sachet should be dissolved in ½ glass of water, juice, or cold tea. The prepared solution should be consumed as soon as possible. In individual cases, due to the presence of the stabilizer – ascorbic acid – in the formulation, the prepared solution may be stored for approximately 2 hours before use. Additional fluid intake enhances the mucolytic effect of the medication.

The duration of treatment for chronic diseases is determined by the physician depending on the nature and course of the disease. For acute uncomplicated conditions, acetylcysteine is administered for 5–7 days.

Children.

The medication may be used in children aged 2 years and older.

Overdose.

There are no reported cases of overdose with oral administration of acetylcysteine.

Symptoms: nausea, vomiting, diarrhea. In children, there is a risk of hypersecretion.

Treatment: symptomatic therapy.

Side effects.

The following classification is used to describe the frequency of adverse reactions: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10,000, < 1/1000), very rare (< 1/10,000).

Cardiovascular system: uncommon – tachycardia, arterial hypotension.

Nervous system: uncommon – headache.

Skin: uncommon – allergic reactions (itching, urticaria, exanthema, eczema, rash, angioneurotic edema).

Auditory system: uncommon – tinnitus.

Respiratory system: rare – dyspnea, bronchospasm (mainly in patients with bronchial hyperreactivity associated with bronchial asthma), rhinorrhea.

Gastrointestinal tract: uncommon – heartburn, dyspepsia, stomatitis, abdominal pain, nausea, vomiting, diarrhea, unpleasant breath odor.

General disorders: uncommon – fever.

Serious skin reactions (Stevens-Johnson syndrome and Lyell's syndrome) have been reported in isolated cases.

With the use of acetylcysteine, very rare cases of bleeding have been reported, mostly associated with the development of hypersensitivity reactions. Cases of reduced platelet aggregation have been observed, although there is no clinical confirmation. Very rare cases of Quincke's edema (angioedema), facial swelling, anemia, hemorrhage, anaphylactic reactions, or even shock have been reported.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

10 sachets per cardboard box.

Prescription status. Over-the-counter.

Manufacturer.

LLC "ASTRAFARM".

Manufacturer's address and location of its business activities.

6, Kyivska Street, Vyshneve, Kyiv-Sviatoshyn District, Kyiv Oblast, 08132, Ukraine.