Pharmacological properties

Pharmacodynamics

N-Acetylcysteinum has mucolytic effect. Existence in structure of Acetylcysteinum of sulfhydryl groups promotes a rupture of disulfide bridges of acid mucopolysaccharides of a phlegm that leads to depolarization of mucoproteins and reduction of viscosity of slime. Drug keeps activity in the presence of a purulent phlegm.

Moreover, Acetylcysteinum has the direct antioxidant effect caused by existence free thiol (-SH) nucleophilic group which easily interacts with electrophilic groups of oxidizing radicals, neutralizing them. In particular, modern data that Acetylcysteinum protects α-antitrypsin — the protein inhibiting elastase from the destruction under the influence of perchloric acid expressed the oxidizing agent who is produced by protein myeloperoxidase of the activated phagocytes are of interest.

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At preventive use of Acetylcysteinum notes decrease in frequency and weight of aggravations at patients with chronic bronchitis and a mucoviscidosis. The protective mechanism of Acetylcysteinum is based on ability of its reactive sulfhydryl groups to connect free radicals.

Therefore Fluimucil can be applied to treatment of the sharp and chronic diseases of a respiratory system which are followed by dense and viscous secretion.

Thanks to the molecular structure Acetylcysteinum can easily get through cellular membranes. In a cell Acetylcysteinum is deacetylated to L-cysteine — amino acid from which intracellular glutathione is synthesized.

Glutathione — high-reactive tripeptide, powerful antioxidant, a cytoprotector, is the expressed factor of intracellular protection not only against oxidizing toxins of both exogenous, and endogenous origin, but also from a number of cytotoxic substances.

Acetylcysteinum prevents exhaustion and promotes increase in synthesis of the intracellular glutathione which is taking part in oxidation-reduction processes of cages, promoting thus a detoxication of hazardous substances. Effect of Acetylcysteinum as antidote is explained by it at poisoning with paracetamol.

Pharmacokinetics

Acetylcysteinum is completely absorbed by

at oral administration. After oral administration, medicine is quickly metabolized in walls of intestines and liver. Owing to metabolism in walls of intestines and effect of the first passing bioavailability of Acetylcysteinum at oral administration very low (about 10%). With _max in blood plasma it is reached in 1–3 h after reception and remains high for 24 h

Acetylcysteinum spreads as in not changed look (20%), and in the form of metabolites (80%), is mainly distributed in a liver, kidneys, lungs and a bronchial secret.

Acetylcysteinum distribution Volume — 0.33-0.47 l/kg of body weight. Communication with proteins makes about 50% in 4 h after reception and decreases up to 20% in 12 h. About 30% are allocated with kidneys. T _1/2 makes 6.25 h

Solution for injections.

At in in introduction of 600 mg of Acetylcysteinum With _max in blood plasma is made by 300 mmol/l, T _1/2 blood plasma — 2 h. The general clearance is equal to 0.21 l/h/kg, and distribution volume at achievement of an equilibrium state is equal to 0.34 l/kg. Drug gets into intercellular space, is mainly distributed in a liver, kidneys, lungs, a bronchial secret. Acetylcysteinum and its metabolites are removed generally by kidneys.

Indication

a disease of respiratory organs, followed by formation of a phlegm of the increased viscosity: acute and chronic bronchitis, pneumonia, bronkhoektatichnesky disease, Mucoviscidosis.

Use

Tablet sparkling to preparation of solution for oral administration is applied at adults and children 14 years are aged more senior.
Tablet of sparkling 600 mg is dissolved in ¹ / ₃ a glass of water and accepted 1 time a day. The doctor determines duration of a course of treatment individually, depending on the nature of a disease (sharp or chronic).
Granules for preparation of solution for oral administration:
Adults: 400–600 mg/days distributed on 1–3 receptions depending on clinical conditions.
Children: at the age of 2–6 years: 200–400 mg/days distributed on 1–3 receptions; 6–12 years: 400–600 mg/days; 12 years — doses as for adults are more senior.

Granule is dissolved in ¹ / ₃ a glass of water.

Duration of a course of treatment the doctor defines

individually, depending on the nature of a disease (sharp or chronic).

needs to use

At dissolution of Acetylcysteinum of sparkling tablets or granules glasswares, to avoid contact with metal and rubber surfaces. Not to administer other medicaments in this solution.

Solution for injections:
Parenteral administration.

Adult 1 ampoule of 300 mg are entered deeply in oil or in/in by drop infusion or slowly bolyusno by 1–2 times a day. To children at the age of 6–14 years 2 times a day enter 150 mg, the dose for children is aged younger than 6 years — 10 mg/kg of body weight each 12 h. The course of treatment makes 5–10 days.

Inhalation: on 1 ampoule 1–2 times a day on doctor's orders for 5–10 days or more long courses. There is no need of change of a dose for adults in case of use of medicine for treatment of children.
Endobronchial introduction:

to adults and children to enter

on 1 ampoule (if necessary — 2) 1–2 times a day, according to the chosen device for introduction (a constant catheter, the bronchoscope, etc.).

Contraindication

hypersensitivity to Acetylcysteinum and components of medicine. A round ulcer of a stomach and duodenum in an aggravation stage, a pneumorrhagia, pulmonary bleeding, OH without condensation of a phlegm.

Drug in the form of sparkling tablets and granules contains aspartame therefore its application for patients with phenylketonuria is not recommended.

For medicine in the form of solution for injections: serious illness of a liver and kidneys; OH without condensation of a phlegm.

Side effects

At oral administration:

Co of the party of the immune system: reactions of hypersensitivity, anaphylactoid reactions, acute anaphylaxis, Quincke's edema.

from central nervous system: headache.

from an organ of hearing: a ring in ears.

from a cardiovascular system: tachycardia.

Vascular disorders: hemorrhages.

from a respiratory system: bronchospasm, dispnoe.

from a GIT: stomatitis, abdominal pain, nausea, vomiting, diarrhea, dyspepsia.

from skin and its appendages: urticaria, skin rash, Quincke's disease, itch.

General violations: hyperthermia, face edema.

Results of researches: decrease in the ABP.

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it was Very seldom reported about anemia cases. In extremely exceptional cases heavy skin reactions, such as Stephens's syndrome — Johnson, a Lyell's disease are possible.

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noted cases of decrease in aggregation of platelets, but the clinical value of it is not defined.
At parenteral administration of Fluimucil perhaps easy burning in the injection site, skin rash, a small tortoiseshell, nausea, vomiting, sonitus.

At inhalation introduction — reflex cough, local irritation of airways, stomatitis, rhinitis, in isolated cases — a bronchospasm (in that case appoint bronchodilators).

Special instructions

Patients with OH have to be under stringent control during treatment in connection with possible development of a bronchospasm. In case of a bronchospasm the treatment by Acetylcysteinum should be stopped immediately.

Is recommended to take with care the medicament at patients with a round ulcer of a stomach and duodenum in the anamnesis, especially in case of the accompanying intake of other medicines irritating a mucous membrane of a stomach.

Acetylcysteinum Use, generally in an initiation of treatment, can cause fluidifying of a bronchial secret and increase its volume. If the patient cannot effectively cough up a phlegm, the postural drainage and a bronkhoaspiration are necessary.

Light sulfuric smell is not sign of change of medicine, and is specific to active ingredient of medicine.

Single dose of Fluimucil of tablets of sparkling 600 mg contains 6.82 mmol (156.74 mg) of sodium. The patients keeping to a diet with sodium consumption control need to consider it.

Medicine in the form of granules for preparation of solution for oral administration contains sorbite therefore patients with hereditary intolerance of fructose should not take the medicament in this form.

Fluimucil needs to be applied to parenteral administration with care at persons with diseases of a liver, kidneys, violation of functions of adrenal glands.

Sick with OH and obstructive bronchitis can appoint Fluimucil by

with restriction at systematic control of bronchial passability. In case of a bronchospasm the treatment is required to be stopped immediately.

Drug contains aspartame therefore its application is not recommended at patients with phenylketonuria.

Solution of Fluimucil should not contact to rubber and metal surfaces.

is forbidden to Use medicine from earlier opened ampoule for injections.

Use during pregnancy and feeding by a breast

during pregnancy and feeding by a breast use of Acetylcysteinum is only possible

if the expected advantage for mother exceeds potential risk for a fruit or the child.

Children. Drug in the form of sparkling tablets is appointed to children aged 14 years are more senior.

Granule for preparation of solution for oral administration is appointed to children aged 2 years are more senior.

Ability to influence speed of response at control of vehicles or work with other mechanisms

is not present

Data.

Interaction

Use together with Acetylcysteinum of antibechics can cause stagnation of a phlegm in connection with suppression of a tussive reflex.

At simultaneous application with such antibiotics as tetracyclines (excepting doxycycline), ampicillin, Amphotericinum B, their interaction with thiol group of Acetylcysteinum is possible

that leads to decrease of the activity of both medicines. Therefore the interval between use of these medicines has to make not less than 2 h

Concomitant use of Acetylcysteinum and nitroglycerine can lead to strengthening of vasodilating and dezagregantny action of the last.

Activated carbon reduces efficiency of Acetylcysteinum.

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does not recommend dissolution in one glass of Acetylcysteinum with other medicines.

Acetylcysteinum eliminates with

toxic effects of paracetamol.

Influence on laboratory researches. Acetylcysteinum can affect results of a colorimetric research of salicylates and definition of urates and ketone ph.

Overdose

there is no

data on cases of overdose of any dosage forms of Acetylcysteinum intended for intake.
Use of medicine in the specified doses does not cause overdose symptoms Acetylcysteinum. Acetylcysteinum at reception in a dose of 500 mg/kg/days does not cause signs and symptoms of overdose. High doses of medicine can initiate massive discharge of a bronchopulmonary secret that will lead to obstruction of airways. It can make necessary mechanical removal of slime of a tracheobronchial tree.
Symptoms: it can be shown by gastrointestinal symptoms, such as nausea, vomiting and diarrhea.
Treatment: does not have specific antidote at poisoning with Acetylcysteinum, therapy symptomatic.

Storage conditions

Tablet sparkling — do not need special storage conditions.

— to keep

Granule at a temperature not above 30 °C.

— to store

Ampoule at the room temperature (15–25 °C). The opened ampoule can be stored in the fridge for 24 h