Acetylcysteine-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ACETYLCYSTEINE-ZDOROVYE (ACETYLCYSTEINE-ZDOROVYE)

Composition:

Active substance: acetylcysteine;

1 ml of the preparation contains 100 mg of acetylcysteine;

Excipients: sodium hydroxide, edetate disodium, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: a clear, colorless solution with a slight sulfurous odor. After opening the ampoule, a faint pinkish-violet tint may appear upon prolonged exposure to air.

Pharmacotherapeutic group. Mucolytic agent. ATC code R05C B01.

Pharmacological properties.

Pharmacodynamics.

Acetylcysteine liquefies sputum. The presence of sulfhydryl groups in the acetylcysteine structure promotes cleavage of disulfide bonds in acidic mucopolysaccharides of sputum, resulting in depolymerization of mucoproteins and reduction of mucus viscosity. The drug retains activity in the presence of purulent sputum.

Acetylcysteine exerts an antioxidant effect due to the presence of a nucleophilic thiol (SH) group, which readily donates hydrogen, thereby neutralizing oxidative radicals.

The protective mechanism of acetylcysteine is based on the ability of its reactive sulfhydryl groups to bind free radicals.

Acetylcysteine easily penetrates into the cell, where it is deacetylated to L-cysteine, which is used for the synthesis of intracellular glutathione.

Glutathione is a highly reactive tripeptide, a potent antioxidant and cytoprotective agent that captures endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and promotes increased synthesis of intracellular glutathione, which participates in cellular redox processes, thereby supporting detoxification of harmful substances.

Pharmacokinetics.

After intravenous administration of 600 mg of acetylcysteine, the maximum plasma concentration reaches 300 mmol/L, and the plasma half-life is 2 hours. Total clearance is 0.21 L/h/kg, and the volume of distribution at steady state is 0.34 L/kg. Acetylcysteine penetrates into the interstitial space and is distributed predominantly in the liver, kidneys, lungs, and bronchial secretions. Acetylcysteine and its metabolites are primarily excreted by the kidneys.

Clinical characteristics.

Indications.

Acute and chronic respiratory tract diseases associated with increased mucus production.

Contraindications.

Hypersensitivity to acetylcysteine or to any of the excipients, active gastric or duodenal ulcer, haemoptysis, pulmonary haemorrhage.

Interaction with other medicinal products and other forms of interaction.

Studies on interactions with other medicinal products have been conducted in adults only.

Concomitant administration of nitroglycerin and acetylcysteine may lead to pronounced arterial hypotension and dilatation of cerebral arteries. If concomitant use of nitroglycerin and acetylcysteine is necessary, the patient must be under medical supervision for the development of arterial hypotension, which may be severe. The patient should be warned about the possibility of developing headache.

Acetylcysteine should not be administered concomitantly with antitussive agents, as suppression of the cough reflex may enhance bronchial secretions retention.

The drug may be used concomitantly with common bronchodilators and vasoconstrictors.

Available information on the interaction between antibiotics and acetylcysteine comes from in vitro studies and indicates reduced antibiotic activity after mixing the two substances. Therefore, mixing antibiotics with acetylcysteine solution is not recommended.

Laboratory parameters

Acetylcysteine may interfere with the quantitative determination of salicylates by colorimetric methods and with urinary ketone testing.

Special precautions for use

The drug should be used with particular caution in patients with a history of peptic ulcer, especially when other medications that irritate the gastric mucosa are taken concomitantly.

Administration of acetylcysteine, mainly at the beginning of therapy, may liquefy bronchial gland secretions and increase their volume. If the patient cannot effectively expectorate sputum, postural drainage or bronchoaspiration should be performed to prevent sputum accumulation.

The intravenous formulation must be administered under strict medical supervision. Adverse effects following intravenous administration of acetylcysteine may occur more frequently if the drug is administered too rapidly or in high doses. Therefore, it is recommended to strictly follow the instructions provided in the section "Method of administration and dosage".

Bronchial asthma

There is evidence that patients with a history of atopy and asthma may have an increased risk of developing anaphylactoid reactions.

Patients with bronchial asthma should be under medical supervision during treatment with this drug. If bronchospasm develops, administration of acetylcysteine should be discontinued immediately and appropriate treatment initiated.

Histamine intolerance

Acetylcysteine may moderately affect histamine metabolism. Therefore, caution should be exercised when prescribing the drug for long-term therapy in patients with histamine intolerance, considering the possible occurrence of intolerance symptoms.

Anaphylactoid reactions

Anaphylactoid reactions/hypersensitivity reactions may occur during acetylcysteine administration. During this period, patients should be closely monitored for signs of anaphylactoid reactions.

Children and adolescents

The same warnings and precautions indicated for adults apply to children and adolescents.

Information on excipients

This medicinal product contains 1.86 mmol (or 42.75 mg) of sodium per dose (1 ampoule). Caution is advised when administering to patients on a sodium-restricted diet.

The sulfurous odor that appears upon opening the ampoule is a characteristic smell of the active substance and does not affect the possibility of using the drug.

The acetylcysteine solution, when stored in opened ampoules or transferred into nebulization equipment, may rarely develop a slight violet coloration; this does not affect the efficacy or tolerability of the drug.

Use during pregnancy or breastfeeding

Pregnancy

Clinical data on the use of acetylcysteine in pregnant women are limited.

Animal studies do not indicate a direct or indirect harmful effect on reproductive function.

Before administering the drug during pregnancy, the potential risk to the fetus should be weighed against the expected benefit to the mother.

Breastfeeding period

There is no information available on the excretion of the drug and its metabolites in human breast milk.

A risk to the infant cannot be excluded. A decision should be made whether to discontinue breastfeeding or to discontinue/abruptly stop treatment with the drug, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.

Fertility

There are no data on the effect of acetylcysteine on human fertility. Animal studies do not indicate a harmful effect on human fertility when administered at recommended doses.

Ability to influence reaction speed while driving or operating machinery

There are no data confirming an effect on reaction speed.

Method of Administration and Dosage

Local administration

Inhalation administration: for adults – 1 ampoule 1–2 times daily as prescribed by a physician for 5–10 days; for children aged 6 years and older – up to 1 ampoule 1–2 times daily as prescribed by a physician for 5–10 days.

Endobronchial administration: for adults and children aged 6 years and older – up to 1 ampoule 1–2 times daily.

Systemic administration

Intramuscular administration: for adults – 1 ampoule of 300 mg 1–2 times daily administered deep intramuscularly.

Intravenous administration: the medicinal product should be administered slowly by infusion in 0.9% sodium chloride solution or 5% glucose solution. For adults – 1 ampoule of 300 mg 1–2 times daily.

Children.

The drug is not administered intramuscularly or intravenously to children. For local administration, the medicinal product may be prescribed to children aged 6 years and older.

Overdose

Intravenous administration

Symptoms

Symptoms of overdose are similar to those of adverse reactions but of greater severity.

Treatment

Treatment requires immediate discontinuation of the drug and initiation of symptomatic therapy and resuscitation measures. There is no specific antidote. Dialysis is effective.

Local administration

Symptoms

Cases of overdose have not been reported. High doses of the drug may stimulate excessive production of bronchopulmonary secretions, potentially leading to airway obstruction.

Treatment

Perform bronchoaspiration.

Adverse reactions.

The following adverse reactions have been reported during post-marketing use; their frequency is unknown (cannot be estimated from the available data):

Inhalation use

Parenteral administration

In very rare cases, serious skin reactions such as Stevens–Johnson syndrome and Lyell’s syndrome have been observed during the use of acetylcysteine.

In most cases, it was suspected that the above-mentioned skin and mucous membrane syndromes could be caused by concomitant use of at least one other medicinal product. If skin or mucous membrane changes occur, medical advice must be sought and acetylcysteine should be discontinued immediately.

Some studies have confirmed a reduction in platelet aggregation during acetylcysteine treatment. The clinical significance of these findings is currently not established.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after the medicine has been authorized is important. It allows continuous monitoring of the benefit-risk balance of the medicine. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy through the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions.

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

Keep out of reach of children.

An opened ampoule intended for topical use may be stored in the refrigerator for up to 24 hours.

Incompatibilities.

The solution of the medicinal product must not come into contact with rubber or metal surfaces.

It is recommended to use glass or plastic equipment for inhalations. After use, the equipment should be rinsed with water.

Packaging. 3 ml in an ampoule № 10 (5x2) in a blister pack in a carton.

Prescription status. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer’s address and location of its business activity. 22 Shevchenka Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.