Fluimucil

In this article you can read the instructions for use of the drug Fluimucil. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Fluimucil in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Fluimucil in the presence of existing structural analogues. Use for the treatment of cough and thinning of sputum in adults, children, as well as during pregnancy and breastfeeding.

Fluimucil- mucolytic drug. Liquefies mucus, increases its volume and facilitates its separation. The effect of acetylcysteine (the active ingredient of the drug Fluimucil) is associated with the ability of its sulfhydryl groups to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolarization of mucoproteins and a decrease in sputum viscosity. Remains active in the presence of purulent sputum.

It has an antioxidant effect due to the presence of an SH group that can neutralize electrophilic oxidative toxins.

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

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

Compound

Acetylcysteine + excipients.

Thiamphenicol glycinate acetylcysteinate + excipients (Fluimucil antibiotic IT).

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. Penetrates into the intercellular space, predominantly distributed in the liver, kidneys, lungs, and bronchial secretions. Penetrates through the placental barrier. Rapidly deacetylated to cysteine in the liver. In plasma, a mobile equilibrium of free acetylcysteine and its metabolites (cysteine, cystine, diacetylcystine) is observed, free and bound to plasma proteins. It is excreted in the urine in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestines.

Indications

respiratory diseases accompanied by impaired sputum discharge (including bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, pulmonary emphysema, laryngotracheitis, interstitial lung diseases, pulmonary atelectasis (due to blockage of the bronchi by mucus plug));
catarrhal and purulent otitis, sinusitis, incl. sinusitis (to facilitate the passage of secretions);
to remove viscous secretions from the respiratory tract in post-traumatic and postoperative conditions;
preparation for bronchoscopy, bronchography, aspiration drainage;
for washing abscesses, nasal passages, maxillary sinuses, middle ear, treatment of fistulas, surgical field during operations on the nasal cavity and mastoid process;
with concomitant nonspecific forms of respiratory infections to improve drainage, including cavernous lesions, with mycobacterial infections.

Release forms

Solution for injection and inhalation (sometimes mistakenly called syrup).

Effervescent tablets 600 mg.

Granules for the preparation of a solution for oral administration 200 mg (sometimes mistakenly called powder).

Lyophilisate for the preparation of solution for injection and inhalation in ampoules (Fluimucil antibiotic IT).

Instructions for use and method of use

Solution

Inhalation

For aerosol therapy, 3-9 ml of a 10% solution is sprayed in ultrasound devices, and 6 ml of a 10% solution is sprayed in devices with a distribution valve. Duration of inhalation - 15-20 minutes; frequency - 2-4 times a day. When treating acute conditions, the average duration of therapy is 5-10 days; for long-term therapy of chronic conditions, the course of treatment is up to 6 months.

Due to the high safety of the drug, the frequency of administration and the relative dose can be changed by the doctor within acceptable limits, depending on the patient’s condition and the therapeutic effect. There is no need to change the adult dose when using the drug to treat children. In the case of a strong secretolytic effect, the secretion is sucked out, and the frequency of inhalations and the daily dose are reduced.

The therapeutic mixture cannot be placed in an ultrasonic nebulizer, because it quickly destroys the active substance Fluimucil. It is advisable to use a compressor device for inhalation, which provides an ideal setting for the size of the inhaled particles of the drug.

Intratracheal

To wash the bronchial tree during therapeutic bronchoscopy, use 1-2 ampoules or more per day, depending on clinical indications.

Locally

150-300 mg (1.5-3 ml) are instilled into the external auditory canal and nasal passages (into the nose) per 1 procedure.

Parenterally

Administer intravenously (preferably drip or slow stream over 5 minutes) or intramuscularly. Adults - 300 mg (3 ml) 1-2 times a day; children from 6 to 14 years old - 150 mg (1.5 ml) 1-2 times a day. The daily dose for children under 6 years of age is 10 mg/kg body weight; for children under 1 year of age, intravenous administration of acetylcysteine is possible only for health reasons in a hospital setting. The duration of treatment should be determined based on changes in the patient's condition.

It should be taken into account that oral administration of the drug is preferable for children under 6 years of age.

High local and general tolerability of the drug allows for long courses of treatment.

For intravenous administration, the solution is further diluted with 0.9% sodium chloride solution or 5% dextrose solution in a 1:1 ratio. The duration of therapy is determined individually (no more than 10 days).

In patients over 65 years of age, the minimum effective dose is used.

Effervescent tablets

The drug in the form of effervescent tablets is prescribed to adults at 600 mg (1 tablet) 1 time per day. Before use, the effervescent tablet is dissolved in 1/3 glass of water.

Granules

Granules for preparing a solution for oral administration are prescribed to adults and children over 6 years old - 200 mg 2-3 times a day; children aged 2 to 6 years - 200 mg 2 times a day or 100 mg 3 times a day; children aged 1 to 2 years - 100 mg 2 times a day.

In newborns, the drug is used only for health reasons at a dose of 10 mg/kg body weight under the strict supervision of a physician.

Before use, the required amount of granules is dissolved in 1/3 glass of water. Children of the first year of life are given the resulting solution to drink from a spoon or feeding bottle.

The duration of the course of treatment is determined individually. For acute diseases, the duration of treatment is from 5 to 10 days, for chronic diseases - up to several months.

Side effect

reflex cough;
respiratory tract irritation;
rhinorrhea;
stomatitis;
bronchospasm;
burning at the injection site;
skin rash;
hives;
impaired liver and/or kidney function (with long-term use).

Contraindications

peptic ulcer of the stomach and duodenum in the acute phase;
lactation period;
children under 2 years of age (for granules for the preparation of a solution for oral administration);
children and adolescents up to 18 years of age (for effervescent tablets);
anemia;
leukopenia;
thrombocytopenia;
hypersensitivity to acetylcysteine.

Use during pregnancy and breastfeeding

During pregnancy, the use of Fluimucil is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Special instructions

For patients with bronchial asthma and obstructive bronchitis, acetylcysteine should be prescribed with caution under systematic monitoring of bronchial patency.

With shallow intramuscular injection of the drug and in the presence of increased sensitivity, a slight and quickly passing burning sensation may occur, and therefore it is recommended to inject the drug deep into the muscle.

The Fluimucil ampoule is opened before use. An opened ampoule can be stored in the refrigerator for 24 hours, during which time the drug can only be used for inhalation.

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

Prescribed with caution for peptic ulcers of the stomach and duodenum in remission, varicose veins of the esophagus, hemoptysis, pulmonary hemorrhage, bronchial asthma (with intravenous administration the risk of developing bronchospasm increases), diseases of the adrenal glands, liver and/or kidney failure, arterial hypertension, and also for children under 6 years of age.

For children under 1 year of age, intravenous administration of acetylcysteine is possible only for health reasons in a hospital setting.

Drug interactions

The simultaneous use of Fluimucil with antitussives may increase sputum stagnation due to suppression of the cough reflex.

When used simultaneously with antibiotics, such as tetracyclines (excluding doxycycline), ampicillin, amphotericin B, they may interact with the thiol group of acetylcysteine, which leads to a decrease in the activity of both drugs, so the interval between taking acetylcysteine and antibiotics should be at least 2 hours.

The simultaneous use of Fluimucil and nitroglycerin can lead to an increase in the vasodilatory effect of the latter.

Acetylcysteine reduces the hepatotoxic effect of paracetamol.

Pharmaceutically incompatible with other drug solutions.

Analogues of the drug Fluimucil

Structural analogues of the active substance:

N-AC-ratiopharm;
N-acetylcysteine;
Acestine;
Acetylcysteine;
Acetylcysteine solution for inhalation 20%;
Acetylcysteine solution for injection 10%;
ACC 100;
ACC 200;
ACC injection;
ACC Long;
Vicks Active ExpectoMed;
Mukobene;
Mucomist;
Mukonex;
Fluimucil;
Exomyuk 200.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

effervescent tablets

Owner/Registrar

ZAMBON SWITZERLAND, Ltd.

International Classification of Diseases (ICD-10)

E84 Cystic fibrosis H66 Purulent and unspecified otitis media J01 Acute sinusitis J04 Acute laryngitis and tracheitis J15 Bacterial pneumonia, not elsewhere classified J20 Acute bronchitis J32 Chronic sinusitis J37 Chronic laryngitis and laryngotracheitis J42 Chronic bronchitis, unspecified J43 Emphysema J45 J47 Bronchiectasis J85 Lung abscess and mediastinum

Pharmacological group

Mucolytic drug with antioxidant properties

Pharmacological action

Mucolytic drug. Liquefies mucus, increases its volume and facilitates its separation. The action of acetylcysteine is associated with the ability of its sulfhydryl groups to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolarization of mucoproteins and a decrease in sputum viscosity. Remains active in the presence of purulent sputum.

It has an antioxidant effect due to the presence of an SH group that can neutralize electrophilic oxidative toxins.

Pharmacokinetics

Suction

When taken orally, it is well absorbed from the gastrointestinal tract. After oral administration, Cmax in plasma is reached within 1-3 hours and is 15 mmol/l. Bioavailability is 10% due to the pronounced “first pass” effect through the liver.

Distribution

Penetrates into the intercellular space, predominantly distributed in the liver, kidneys, lungs, and bronchial secretions. Penetrates through the placental barrier. Binding to blood plasma proteins - 50%.

Metabolism

Rapidly deacetylated to cysteine in the liver. In plasma, a mobile equilibrium of free acetylcysteine and its metabolites (cysteine, cystine, diacetylcystine) is observed, free and bound to plasma proteins.

Removal

T1/2 when taken orally is 1 hour, with cirrhosis of the liver it increases to 8 hours. It is excreted in the urine in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestines.

Respiratory diseases accompanied by impaired sputum discharge (including bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, pulmonary emphysema, laryngotracheitis, interstitial lung diseases, pulmonary atelectasis /due to blockage of the bronchi by mucus plug/);

Catarrhal and purulent otitis, sinusitis, incl. sinusitis (to facilitate the passage of secretions);

To remove viscous secretions from the respiratory tract in post-traumatic and postoperative conditions.

Peptic ulcer of the stomach and duodenum in the acute phase;

Lactation period;

Children under 2 years of age (for granules for the preparation of a solution for oral administration);

Children and adolescents up to 18 years of age (for effervescent tablets);

Hypersensitivity to acetylcysteine.

The use of the drug in the form of granules for the preparation of a solution for oral administration in children under 2 years of age is possible only if there are vital indications and under strict medical supervision.

WITH caution prescribed for peptic ulcers of the stomach and duodenum, varicose veins of the esophagus, hemoptysis, pulmonary hemorrhage, phenylketonuria, bronchial asthma, diseases of the adrenal glands, liver and/or kidney failure, arterial hypertension.

From the digestive system: rarely - heartburn, nausea, feeling of fullness in the stomach, vomiting, diarrhea; Cases of the development of stomatitis have been described.

Allergic reactions: rarely - skin rash, itching, urticaria; Cases of bronchospasm have been described.

Others: rarely - nosebleeds, tinnitus; Cases of collapse and decreased platelet aggregation have been described.

Overdose

Fluimucil ® when taken at a dose of 500 mg/kg/day does not cause signs and symptoms of overdose.

Special instructions

For patients with bronchial asthma and obstructive bronchitis, Fluimucil ® can be prescribed with caution under systematic monitoring of bronchial conduction.

When dissolving the drug, you must use glass containers and avoid contact with metal and rubber surfaces. When opening a bag of granules, there may be a smell of sulfur, which is the smell of the active substance.

For renal failure

The drug should be prescribed with caution to patients with kidney disease.

In case of liver dysfunction

The drug should be prescribed with caution to patients with liver disease.

Use during pregnancy and breastfeeding

During pregnancy, the use of Fluimucil is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Drug interactions

The simultaneous use of Fluimucil with antitussives may increase sputum stagnation due to suppression of the cough reflex.

The simultaneous use of Fluimucil and nitroglycerin can lead to an increase in the vasodilatory and antiplatelet effects of the latter.

Acetylcysteine reduces the hepatotoxic effect of paracetamol.

The drug is in the form effervescent tablets appoint adults 600 mg (1 tablet) 1 time/day. Before use, the effervescent tablet is dissolved in 1/3 glass of water.

Granules for the preparation of solution for oral administration appoint adults and children over 6 years old- 200 mg 2-3 times/day; children aged 2 to 6 years- 200 mg 2 times/day or 100 mg 3 times/day; children aged 1 to 2 years- 100 mg 2 times/day.

U newborn children the drug is used only for health reasons at a dose of 10 mg/kg body weight under the strict supervision of a physician.

Before use, the required amount of granules is dissolved in 1/3 glass of water. Children of the first year of life Give the resulting solution to drink from a spoon or feeding bottle.

The duration of the course of treatment is determined individually. For acute diseases, the duration of treatment is from 5 to 10 days, for chronic diseases - up to several months.

Storage conditions and shelf life

The drug should be stored in a dry place, out of reach of children, at a temperature not exceeding 25°C. Shelf life - 3 years.

Release from pharmacies

The drug is approved for use as an over-the-counter product.

Fluimucil

International nonproprietary name

Acetylcysteine

Dosage form

Granules for the preparation of solution for oral administration

Compound

1 gram of granules contains

active substance - acetylcysteine 200 mg,

excipients: aspartame, beta-carotene 1% (E 160), orange flavor, sorbitol.

Description

Granules are whitish-yellow in color with orange inclusions with a characteristic orange, slightly sulfuric odor

Pharmacotherapeutic group

Medicines to relieve symptoms of colds and coughs. Expectorants. Mucolytics. Acetylcysteine.

ATX code R05СB01

Pharmacological properties

Pharmacokinetics

Acetylcysteine is well absorbed when taken orally. It is immediately deacetylated to cysteine in the liver. In the blood, a mobile equilibrium of free acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine) is observed, free and bound to plasma proteins. Due to the high “first pass” effect through the liver, the bioavailability of acetylcysteine is about 10%. Acetylcysteine penetrates into the intercellular space and is predominantly distributed in the liver, kidneys, lungs, and bronchial secretions. The maximum concentration in plasma is reached 1-3 hours after oral administration and is 15 mmol/l, binding to plasma proteins is 50%. T1/2 is about 1 hour, with liver cirrhosis it increases to 8 hours. It is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestines. Penetrates through the placental barrier.

Pharmacodynamics

A mucolytic agent that thins sputum, increases its volume, and facilitates the removal of sputum. The action is associated with the ability of the free sulfhydryl groups of the drug Fluimucil to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolymerization of mucoproteins and a decrease in sputum viscosity. Remains active against purulent sputum. Increases the secretion of less viscous sialomucins by goblet cells, reduces the adhesion of bacteria to the epithelial cells of the bronchial mucosa. Stimulates mucous cells of the bronchi, the secretion of which is lysed by fibrin. It has an antioxidant effect due to the presence of the SH group and is able to directly interact with electrophilic groups of oxidative radicals. Fluimucil easily penetrates into the cell and is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, antioxidant, cytoprotector that traps endogenous and exogenous free radicals and toxins. Fluimucil prevents exhaustion and helps increase the synthesis of intracellular glutathione, which is involved in the redox processes of cells, thus promoting the detoxification of harmful substances. This explains the effect of Fluimucil as an antidote for paracetamol poisoning. Additional properties: weakening of induced hyperplasia of epithelial cells, increasing surfactant production by stimulating type 2 pneumocytes, stimulating the activity of the mucociliary apparatus, leading to improved mucociliary clearance. Protects alpha1-antitrypsin (elastase inhibitor) from the inactivating effects of HOCl, an oxidizing agent produced by myeloperoxidase of active phagocytes. It also has an anti-inflammatory effect (by suppressing the formation of free radicals and reactive oxygen-containing substances responsible for the development of inflammation in the lung tissue).

Indications for use

Mucolytic agent for the treatment of acute and chronic respiratory diseases accompanied by excessive sputum production (as part of complex therapy):

acute and chronic bronchitis

laryngitis

bronchial asthma
cystic fibrosis (as additional therapy)

Directions for use and doses

To prepare a solution for oral administration, the contents of 1 packet are dissolved in a glass of water. Fluimucil must be taken without delay immediately after preparing the solution.

Standard dosage for acute diseases

Children from 2 to 12 years: 100 mg 3 times a day or 200 mg 2 times a day.

Children over 12 years of age and adults: 200 mg 3 times a day or 600 mg 1 time a day.

Special dosing regimens

Long-term treatment (only if prescribed by a doctor): 400-600 mg per day, divided into one or more doses, maximum duration of treatment from 3 to 6 months.

If there is excessive secretion production and, as a consequence, continued cough after 2 weeks of treatment, the diagnosis should be reconsidered, in order to exclude, for example, a possible malignant disease of the respiratory tract.

Cystic fibrosis: Despite the above, for children over 6 years old, 200 mg 3 times a day or 600 mg 1 time a day.

Side effects

Uncommon

hypersensitivity

headache, ringing, tinnitus

tachycardia

stomatitis

abdominal pain

nausea, vomiting

urticaria, skin rash, itching, angioedema
Quincke's edema
hyperthermia
lower blood pressure

Rarely

bronchospasm

dyspepsia

Very rarely

anaphylactic shock

allergic reactions

anaphylactic/anaphylactoid reactions ( Johnson-Stevens syndrome, Lyell's syndrome)

bleeding

Frequency unknown

fever, facial swelling

Contraindications

hypersensitivity to any component of the drug

peptic ulcer of the stomach and duodenum in the acute stage

lactation period

children under 2 years old

phenylketonuria

hereditary fructose intolerance

Drug interactions

The combined use of Fluimucils with antitussives may increase sputum stagnation due to suppression of the cough reflex. When used simultaneously with antibiotics such as tetracyclines (excluding doxycycline), ampicillin, amphotericin B, they may interact with the thiol group of Fluimucil, which leads to a decrease in the activity of both drugs. Therefore, the interval between doses of these drugs should be at least 2 hours. Concomitant use of Fluimucil and nitroglycerin can lead to an increase in the vasodilator and antiplatelet effect of the latter. Fluimucil eliminates the toxic effects of paracetamol. Activated carbon may reduce the effectiveness of acetylcysteine. Acetylcysteine is incompatible with most metals and is inactivated by oxidizing agents.

Special instructions

Particular caution is required in patients at risk of developing gastrointestinal bleeding (for example, with inactive peptic ulcers or esophageal varices), since there is evidence that acetylcysteine when taken orally can cause vomiting.

Caution should also be taken into account by patients suffering from bronchial asthma and a hyperreactive bronchial system due to the risk of developing bronchospasm. The use of Fluimucil, especially at the beginning of treatment, thins and therefore increases the volume of bronchial secretions. If the patient is unable to cough on his own, the doctor should take appropriate measures. Allergic reactions affecting the skin and respiratory tract may occur in susceptible patients; bronchospasm may also develop in patients suffering from bronchial asthma or hyperresponsiveness of the bronchial system. In the event of allergic reactions or bronchospasm, use of the drug should be stopped immediately and, if necessary, appropriate therapeutic measures should be taken.

In very rare cases, the onset of serious skin reactions, such as Stevens-Johnson syndrome or Lyell's syndrome, is temporarily associated with acetylcysteine. If manifestations occur on the skin or mucous membrane, you should immediately consult a doctor and stop using acetylcysteine. In the majority of reported cases, there was concomitant use of at least one other drug, which may have caused increased mucocutaneous manifestations. If rashes or breathing problems occur during previous use of another drug with the same active substance as Fluimucil, you must inform your doctor before starting treatment.

Concomitant use with certain other drugs may lead to their interaction. The effectiveness of some medicines for the treatment of coronary artery disease (for example, nitroglycerin, used to treat angina) may be increased, and concomitant use of antitussives may affect the effect of Fluimucil. The concomitant use of antitussives that suppress the cough reflex and the physiological mechanism of self-cleaning of the respiratory tract can cause mucus stagnation with a possible risk of developing bronchospasm and respiratory tract infection. The concomitant use of antitussives is not clinically justified.

Mucolytic agents may cause bronchial obstruction in children under 2 years of age. In fact, due to the physiological characteristics of the respiratory system of children in this age group, the ability to clear airway secretions is limited. Therefore, mucolytic agents should not be used in children under 2 years of age.

Patients with arterial hypertension who are on a strict salt-free diet should note that each effervescent tablet of acetylcysteine 200 mg and 600 mg contains approximately 140 mg of sodium (corresponding to approximately 350 mg of sodium chloride). In these cases, it is recommended to use Fluimucil granules, film-coated tablets, or other salt-free acetylcysteine preparations.

Various studies confirm a decrease in platelet aggregation with the use of acetylcysteine. The clinical significance of this finding is uncertain.

The patient's breath may temporarily have an unpleasant sulfurous odor, characteristic of the active substance.

Acetylcysteine may interfere with the determination of salicylates by colorimetric assays.

Acetylcysteine may interfere with the determination of ketones in urine.

Pregnancy and lactation

Clinical data on the use of acetylcysteine by women during pregnancy are limited. The drug is prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus. There is no information on penetration into breast milk.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

Mucolytic drug with antioxidant properties

Active ingredient

Release form, composition and packaging

◊ Effervescent tablets white, round, with a rough surface; with a lemony, slightly sulfuric odor; the solution prepared by reconstituting the tablets in water should be slightly opalescent, with a characteristic odor and taste of lemon flavor.

Excipients: citric acid, aspartame, lemon flavor.

2 pcs. - blisters (5) - cardboard packs.
2 pcs. - blisters (10) - cardboard packs.
10 pcs. - blisters (1) - cardboard packs.
10 pcs. - blisters (2) - cardboard packs.

◊ white-yellow in color, with orange inclusions, with a characteristic orange, slightly sulfurous odor.

Excipients: aspartame, betacarotene, orange flavor, sorbitol.

Multilayer bags (20) - cardboard packs.
Multilayer bags (60) - cardboard packs.

Pharmacological action

It has an antioxidant effect due to the presence of an SH group that can neutralize electrophilic oxidative toxins.

Acetylcysteine easily penetrates into the cell and is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant and cytoprotector that neutralizes endogenous and exogenous free radicals and toxins. Acetylcysteine prevents exhaustion and helps increase 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 for poisoning.

Protects alpha1-antitrypsin (elastase inhibitor) from the inactivating effects of HOCI, an oxidizing agent produced by myeloperoxidase of active phagocytes. It also has an anti-inflammatory effect (by suppressing the formation of free radicals and reactive oxygen-containing substances responsible for the development of inflammation in the lung tissue).

Pharmacokinetics

Suction

When taken orally, it is well absorbed from the gastrointestinal tract. After oral administration, Cmax is reached within 1-3 hours and is 15 mmol/l. Bioavailability is 10% due to the pronounced “first pass” effect through the liver.

Distribution

Metabolism

Removal

Indications

- diseases of the respiratory system, accompanied by impaired sputum discharge (including bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, pulmonary emphysema, laryngotracheitis, interstitial lung diseases, pulmonary atelectasis /due to blockage of the bronchi by mucus plug/) ;

- catarrhal and purulent otitis media, sinusitis, incl. sinusitis (to facilitate the passage of secretions);

- to remove viscous secretions from the respiratory tract in post-traumatic and postoperative conditions.

Contraindications

- peptic ulcer of the stomach and duodenum in the acute phase;

- lactation period;

- children under 2 years of age (for granules for the preparation of a solution for oral administration);

- children and adolescents up to 18 years of age (for effervescent tablets);

- hypersensitivity to acetylcysteine.

Dosage

The drug is in the form effervescent tablets appoint adults 600 mg (1 tablet) 1 time/day. Before use, the effervescent tablet is dissolved in 1/3 glass of water.

U newborn children the drug is used only for health reasons at a dose of 10 mg/kg body weight under the strict supervision of a physician.

Before use, the required amount of granules is dissolved in 1/3 glass of water. Children of the first year of life Give the resulting solution to drink from a spoon or feeding bottle.

The duration of the course of treatment is determined individually. For acute diseases, the duration of treatment is from 5 to 10 days, for chronic diseases - up to several months.

Side effects

From the digestive system: rarely - heartburn, nausea, feeling of fullness in the stomach, vomiting, diarrhea; Cases of the development of stomatitis have been described.

Allergic reactions: rarely - skin rash, itching, urticaria; Cases of bronchospasm have been described.

Others: rarely - nosebleeds, tinnitus; Cases of collapse and decreased platelet aggregation have been described.

Overdose

Fluimucil, when taken at a dose of 500 mg/kg/day, does not cause signs and symptoms of overdose.

Drug interactions

The simultaneous use of Fluimucil with antitussives may increase sputum stagnation due to suppression of the cough reflex.

When used simultaneously with antibiotics, such as tetracyclines (excluding doxycycline), ampicillin, they may interact with the thiol group of acetylcysteine, which leads to a decrease in the activity of both drugs, therefore the interval between taking acetylcysteine and antibiotics should be at least 2 hours.

Simultaneous administration of Fluimucil can lead to an increase in the vasodilatory and antiplatelet effects of the latter.

Instructions for medical use

medicine

Trade name

Fluimucil

International nonproprietary name

Acetylcysteine

Dosage form

Solution for injection and inhalation, 100 mg/ml, 3 ml

Compound

One ampoule contains

active substance- acetylcysteine 300 mg,

excipients: disodium edetate, sodium hydroxide, water for injection.

Description

Transparent colorless solution with a faint sulfuric odor

Pharmacotherapeutic group

Expectorants. Mucolytics.

ATC code R05CB01

Pharmacological properties

Pharmacokinetics

With intravenous administration of 600 mg of acetylcysteine, the maximum plasma concentration is 300 mmol/l, the plasma half-life 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.

In the liver it is deacetylated to cysteine. In the blood, a mobile equilibrium of free acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine) is observed, free and bound to plasma proteins. Acetylcysteine penetrates into the intercellular space and is predominantly distributed in the liver, kidneys, lungs, and bronchial secretions.

It is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestines.

Penetrates through the placental barrier.

Pharmacodynamics

A mucolytic agent that thins sputum, increases its volume, and facilitates the separation of sputum. The action is associated with the ability of free sulfhydryl groups of acetylcysteine to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolymerization of mucoproteins and a decrease in sputum viscosity. Remains active against purulent sputum.

Increases the secretion of less viscous sialomucins by goblet cells, reduces the adhesion of bacteria to the epithelial cells of the bronchial mucosa. Stimulates mucous cells of the bronchi, the secretion of which is lysed by fibrin. It has a similar effect on the secretions formed during inflammatory diseases of the ENT organs. It has an antioxidant effect due to the presence of an SH group that can neutralize electrophilic oxidative toxins. Acetylcysteine easily penetrates into the cell and is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant, cytoprotector that traps endogenous and exogenous free radicals and toxins. Acetylcysteine prevents exhaustion and helps increase the synthesis of intracellular glutathione, which is involved in the redox processes of cells, thus promoting the detoxification of harmful substances. This explains the effect of acetylcysteine as an antidote for paracetamol poisoning.

Indications for use

acute and chronic respiratory disorders, characterized by increased secretion of thick, difficult-to-discharge mucus.

paracetamol overdose

Directions for use and doses

Inhalation.

Adults: 300 mg (3 ml) 1-2 times a day for 5-10 days.

Children: up to 300 mg (3 ml) 1-2 times a day for 5-10 days. In the case of a strong secretolytic effect, the secretion is sucked out, and the frequency of inhalations and the daily dose are reduced. The frequency of use and relative dosage can be changed by the physician within acceptable limits, depending on the clinical manifestation and therapeutic effect, without the need to differentiate the dosage for adults and children.

Endobronchial instillation.

Adults and children: 300 mg (3 ml) 1-2 times/day or as needed, in accordance with the chosen method of administration (indwelling catheter, bronchoscope, etc.).

Instillation intranasally or endoauricularly.

Adults and children: 2-3 drops two or three times a day.

Parenterally.

The drug is administered intramuscularly (IM) deeply. The recommended dosage for adults is 300 mg (3 ml) 1-2 times a day. Children: 150 mg (1.5 ml) 1-2 times a day deep intramuscularly.

The duration of treatment should be determined on the basis of clinical analysis. Good general and local tolerability of the drug allows for long-term treatment.

Administration of Fluimucil is also possible by slow intravenous (IV) administration in a hospital setting.

Adults 300 mg (3 ml) 1-2 times a day. Children from 6 to 14 years old - 150 mg (1.5 ml) 1-2 times a day. For children under 6 years of age, oral administration of the drug is preferable. For intravenous administration, Fluimucil solution is further diluted with 0.9% sodium chloride solution or 5% dextrose solution.

The duration of therapy is determined individually (no more than 10 days). In patients over 65 years of age, the minimum effective dose is used.

Intravenous administration (as an antidote for paracetamol overdose)

Therapy must be started within the first 8 hours after taking paracetamol; further therapy is ineffective. When acetylcysteine is used within 15 hours after an overdose of paracetamol, the therapy is least effective, but there is literature evidence that treatment can be effective within 16-24 hours after taking paracetamol.

The drug is administered intravenously. The infusion should be administered slowly to reduce the risk of side effects.

For patients weighing more than 40 kg, the following treatment regimen is used:

First dose: 150 mg/kg in 200 ml solution after 60 minutes.

Second dose: 50 mg/kg in 500 ml solution after 4 hours.

Third dose: 100 mg/kg in 1000 ml solution after 16 hours.

For patients weighing more than 20 kg, the following treatment regimen is used:

First dose: 150 mg/kg in 100 ml solution after 60 minutes.

Second dose: 50 mg/kg in 250 ml solution after 4 hours.

Third dose: 100 mg/kg in 500 ml solution after 16 hours.

For patients weighing less than 20 kg, the following treatment regimen is used:

First dose: 150 mg/kg in 3 ml/kg solution after 60 minutes.

Second dose: 50 mg/kg in 7 ml/kg solution after 4 hours.

Third dose: 100 mg/kg in 14 ml/kg solution after 16 hours.

The solution is compatible with 5% dextrose solution, 0.45% sodium chloride solution or water for injection.

Side effects

For local use:

Reflex cough, bronchospasm, respiratory tract irritation, rhinorrhea

Stomatitis, nausea, vomiting

Hives, skin rash, itching

For parenteral use:

Anaphylactic shock, anaphylactic and anaphylactoid reactions, hypersensitivity

Tachycardia

Bronchospasm, breathing disorder

Nausea, vomiting

Angioedema, urticaria, fever, skin rash, itching

Facial swelling

Decreased blood pressure, prolongation of prothrombin time

Burning at the injection site; with long-term treatment - impaired liver and/or kidney function

In very rare cases, severe skin reactions such as Stevens-Johnson syndrome and Lyell's syndrome may develop. If such adverse reactions develop, the drug should be discontinued immediately.

Cases of decreased platelet aggregation have been described when taking acetylcysteine.

Contraindications

Hypersensitivity to acetylcysteine and auxiliary components of the drug

Peptic ulcer of the stomach and duodenum in the acute stage

Pregnancy and lactation

Hemoptysis, pulmonary hemorrhage

With caution: peptic ulcer of the stomach and duodenum in remission, varicose veins of the esophagus, bronchial asthma (with intravenous administration there is a risk of developing bronchospasm), diseases of the adrenal glands, liver and/or kidney failure, arterial hypertension, children under 6 years of age.

Drug interactions

Fluimucil can be used together with general bronchodilators, vasoconstrictors, etc.

The combined use of acetylcysteine with antitussives may increase sputum stagnation due to suppression of the cough reflex.

When used simultaneously with antibiotics such as tetracyclines (excluding doxycycline), ampicillin, amphotericin B, they may interact with the thiol group of acetylcysteine, which leads to a decrease in the activity of both drugs. Therefore, the interval between doses of these drugs should be at least 2 hours.

The simultaneous use of acetylcysteine and nitroglycerin can lead to an increase in the vasodilatory effect of the latter.

Acetylcysteine eliminates the toxic effects of paracetamol.

Special instructions

Caution should be exercised when using the drug as an antidote in patients weighing less than 40 kg, as there is a possible risk of developing fluid retention in the body with subsequent hyponatremia, seizures and death.

Taking acetylcysteine, in particular in the form of an inhaled aerosol, can lead to dilution and, at the same time, an increase in the volume of bronchial secretions at the beginning of treatment. If patients are unable to expectorate properly, the airway must be cleared using postural drainage or bronchial suctioning to avoid stagnation of secretions.

Patients suffering from bronchial asthma should be under strict supervision during the treatment period: if an attack of bronchial spasm occurs, treatment should be stopped immediately.

Use with caution in patients with peptic ulcers, including a history of peptic ulcers, especially in cases of combined use with other drugs that irritate the gastric mucosa.

Intravenous administration of the drug should be carried out under strict medical supervision.

Acetylcysteine, when used as an antidote, can prolong prothrombin time [reduce the prothrombin index, increase the international normalized ratio (INR)].

When opening the ampoule, a sulfurous odor is felt, which is a specific odor of the active substance and does not affect the quality of the drug. Acetylcysteine solution, when stored in an open ampoule or transferred to a spray device, may in exceptional cases take on a pink color, but this does not affect the effectiveness and tolerability of the drug.

The Fluimucil ampoule is opened before use. An opened ampoule can be stored in the refrigerator for 24 hours, during which time the drug can only be used for inhalation.

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

Features of the influence on the ability to drive a vehicle and potentially dangerous mechanisms

No effect.

Overdose

Symptoms: when administered intravenously, the symptoms of overdose are similar to the side effects of the drug, but more pronounced.

Local application of increased doses can lead to extensive liquefaction of secretions in the bronchi.

Treatment: Immediate cessation of drug administration and further symptomatic and supportive treatment. A specific antidote is unknown. Acetylcysteine is dialyzed. In case of difficulty in expectoration due to the formation of a large volume of mucus, mechanical suction should be performed, if necessary, to maintain the airways open.