Acetylcysteine-Health solution for injection 100 mg/ml ampoule 3 ml No. 10

Instructions for use Acetylcysteine-Zdorovye solution for injection 100 mg/ml ampoule 3 ml No. 10

Composition

active ingredient: acetylcysteine;

1 ml of the drug contains 100 mg of acetylcysteine;

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

Dosage form

Solution for injection.

Main physicochemical properties: transparent colorless solution with a faint sulfuric odor. After opening the ampoule, a faint pink-violet hue may appear upon prolonged contact with air.

Pharmacotherapeutic group

Mucolytic agent. ATX code R05C B01.

Pharmacological properties

Pharmacodynamics.

Acetylcysteine thins sputum. The presence of sulfhydryl groups in the structure of acetylcysteine contributes to the rupture of disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolarization of mucoproteins and a decrease in mucus viscosity. The drug retains activity in the presence of purulent sputum.

Acetylcysteine has an antioxidant effect due to the presence of a nucleophilic thiol SH-group, which easily donates hydrogen, 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 the cell, is deacetylated to L-cysteine, from which intracellular glutathione is synthesized.

Glutathione is a highly reactive tripeptide, a powerful antioxidant, cytoprotector that captures endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and helps increase the synthesis of intracellular glutathione, which participates in redox processes in cells, thus contributing to the detoxification of harmful substances.

Pharmacokinetics.

With intravenous administration of 600 mg of acetylcysteine, the maximum concentration in the blood plasma is 300 mmol/l, the half-life from the blood plasma is 2 hours. The total clearance is 0.21 l/h/kg, and the volume of distribution at the plateau is 0.34 l/kg. Acetylcysteine penetrates the intercellular space, is mainly distributed in the liver, kidneys, lungs, bronchial secretions. Acetylcysteine and its metabolites are excreted mainly by the kidneys.

Indication

Acute and chronic respiratory diseases accompanied by increased sputum production.

Contraindication

Hypersensitivity to acetylcysteine or to other components of the drug, gastric and duodenal ulcer in the acute stage, hemoptysis, pulmonary hemorrhage.

Interaction with other medicinal products and other types of interactions

Drug interaction studies have only been conducted in adults.

Concomitant administration of nitroglycerin and acetylcysteine may result in marked hypotension and temporal artery dilation. If concomitant administration of nitroglycerin and acetylcysteine is necessary, the patient should be monitored for hypotension, which may be severe. The patient should be warned of the possibility of headache.

Acetylcysteine should not be administered concurrently with antitussives, as suppression of the cough reflex may increase congestion of bronchial secretions.

The drug can be used simultaneously with conventional bronchodilators and vasoconstrictors.

The available information on the interaction of antibiotics with acetylcysteine is obtained from in vitro studies and indicates a decrease in the activity of antibiotics after mixing the two substances. Therefore, it is not recommended to mix antibiotics with acetylcysteine solution.

Laboratory indicators

The use of acetylcysteine may alter the results of colorimetric salicylate quantification and urine ketone determination.

Application features

The drug should be used with extreme caution in patients with a history of peptic ulcer, especially in the case of concomitant administration of other medications that irritate the gastric mucosa.

Acetylcysteine, especially at the beginning of therapy, can dilute bronchial secretions and increase their volume. If the patient cannot cough up sputum effectively, postural drainage or bronchoaspiration should be performed to avoid sputum stagnation.

Intravenous administration of the drug should be carried out under strict medical supervision. Adverse reactions to intravenous administration of acetylcysteine may occur more frequently if the drug is administered too quickly or in large doses. Therefore, it is recommended to strictly follow the instructions given in the section "Method of administration and dosage".

Bronchial asthma

There is evidence that patients with a history of atopy and asthma may be at increased risk of developing an anaphylactoid reaction.

Patients with bronchial asthma should be under medical supervision during treatment with the drug. In the event of bronchospasm, acetylcysteine should be discontinued immediately and appropriate treatment should be initiated.

Acetylcysteine may moderately affect histamine metabolism. Therefore, caution should be exercised when prescribing the drug for long-term therapy to patients with histamine intolerance, taking into account the possibility of developing symptoms of intolerance.

Anaphylactoid reactions

Anaphylactoid/hypersensitivity reactions have been reported with acetylcysteine. During this period, the patient should be closely monitored for signs of anaphylactoid reactions.

Children and adolescents

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

Information on excipients

This medicinal product contains 1.86 mmol (or 42.75 mg) sodium per dose (1 ampoule). Caution should be exercised when administering this medicinal product to patients on a controlled sodium diet.

The sulfurous odor that appears when the ampoule of the drug is opened is a characteristic odor of the active ingredient and does not affect the possibility of using the drug in any way.

Acetylcysteine solution when stored in open ampoules or transferred to aerosol equipment may in rare cases acquire a light purple color, which does not affect the effectiveness and tolerability of the drug.

Use during pregnancy or breastfeeding.

Pregnancy

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

Animal studies do not indicate direct or indirect harmful effects with respect to reproductive function.

Before using the drug during pregnancy, the potential risk to the fetus should be compared with the expected benefit to the mother.

Breastfeeding period

There is no information on the excretion of the drug and its metabolites into breast milk.

A risk to the infant cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from the drug therapy taking into account the benefit of breast-feeding 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 used at recommended doses.

The ability to influence the reaction speed when driving vehicles or other mechanisms.

There is no data confirming the effect on reaction rate.

Method of administration and doses

Topical application

Inhalation: adults - 1 ampoule 1–2 times a day as prescribed by a doctor for 5–10 days, children from 6 years of age - up to 1 ampoule 1–2 times a day as prescribed by a doctor for 5–10 days.

Endobronchial administration: adults and children over 6 years of age – up to 1 ampoule 1–2 times a day.

Systemic application

Intramuscular administration: adults - 1 ampoule of 300 mg 1–2 times a day, administered deeply intramuscularly.

Intravenous administration: the drug should be administered slowly drip in 0.9% sodium chloride solution or 5% glucose solution. Adults - 1 ampoule of 300 mg 1-2 times a day.

Children.

The drug is not used for intramuscular and intravenous administration in children. For topical use, the drug is prescribed to children over 6 years of age.

Overdose

When administered intravenously

Symptoms Symptoms of overdose are similar to symptoms of adverse reactions of great severity.

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

When applied topically

Symptoms

Cases of overdose have not been registered. High doses of the drug may initiate the secretion of large amounts of bronchopulmonary secretions, which will lead to airway obstruction.

Treatment

Performing 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 use

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

In most cases, it was suspected that the above mucocutaneous syndromes could be caused by the simultaneous use of at least one other drug. In the event of mucocutaneous changes, it is necessary to seek medical advice and immediately discontinue acetylcysteine.

A decrease in platelet aggregation with acetylcysteine has been confirmed in some studies. The clinical significance of these results is not yet determined.

Reporting of suspected adverse reactions

Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.

Expiration date

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 for topical use only can be stored in the refrigerator for 24 hours.

Incompatibility

The drug solution should not come into contact with rubber and metal surfaces.

It is recommended to use glass or plastic equipment for inhalation; after use, the equipment should be rinsed with water.

Packaging

3 ml in ampoule No. 10 (5x2) in a blister in a box.

Vacation category

According to the recipe.

Producer

Limited Liability Company "Pharmaceutical Company "Zdorovya".

Location of the manufacturer and address of its place of business

Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenko street, building 22.