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 mukoproteid and to reduction of viscosity of slime. medicine 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. In particular, modern data that Acetylcysteinum protects a α-antitripsin-belok which inhibits elastase, from the destruction under the influence of perchloric acid expressed the oxidizing agent which is produced by protein of myeloperoxidase of the activated phagocytes are of interest.

Therefore Acetylcysteinum can be applied to treatment of patients with the acute 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 which is necessary for glutathione synthesis.

Glutathione is a high-reactive tripeptide which 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.

Pharmacokinetics. Acetylcysteinum is completely absorbed at oral administration. Because of metabolism in walls of intestines and effect of the first passing bioavailability of Acetylcysteinum at oral administration very low (≈10%). The C _max in blood plasma is reached in 1–3 h after reception and remains high during 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 — from 0.33 to 0.47 l/kg of body weight. Communication with proteins makes ≈50% in 4 h after reception and decreases up to 20% — in 12 h

Acetylcysteinum after oral administration is quickly metabolized by

in walls of intestines and liver.

About 30% are allocated to

with kidneys. The t _½ Acetylcysteinum makes 6.25 h

Indication

Mucolytic cure for treatment for the sharp and chronic diseases of a bronchopulmonary system which are followed by the increased formation of a phlegm.

Use

Tablet on 200 mg

Adult:

400-600 mg/days in 2–3 receptions depending on clinical conditions.

to Children aged:

2-6 years — 200–400 mg/days in 1–2 receptions;

6-12 years — 400–600 mg/days in 2–3 receptions depending on clinical conditions.

12 years — doses as for adults.

Duration of a course of treatment the doctor defines

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

Caution for the patients adhering to a diet with the limited content of sodium: each sparkling tablet contains 191 mg of sodium.

Tablet on 600 mg

Adults and children are aged more senior than 14 years — on 1 sparkling tablet of 1 times a day (600 mg of Acetylcysteinum a day are equivalent).

Caution for the patients adhering to a diet with the limited content of sodium: each sparkling tablet contains 150 mg of sodium.

In sharp uncomplicated diseases medicament is used by no more than 4-5 days without observation of the doctor.

Period of treatment of chronic diseases is defined by the doctor. The medicament is recommended to be taken after a meal. Sparkling tablets dissolve in ½ glasses of water, juice or cold tea. At dissolution of Acetylcysteinum it is necessary to use glasswares, to avoid contact with metal and rubber surfaces. Not to mix this solution with other medicines. For strengthening of mucolytic effect of Acetylcysteinum the additional intake of liquid is recommended.

Contraindication

Hypersensitivity to active agent or to any of excipients. ulcer of stomach and duodenum in an aggravation stage, a pneumorrhagia, pulmonary bleeding.

Side effects

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

from 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, short wind.

from digestive system: stomatitis, abdominal pain, nausea, vomiting, diarrhea, dyspepsia.

from skin and its appendages: urticaria, 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. Skin reactions, such as Stephens's syndrome — Johnson, a Lyell's disease are in rare instances possible.

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noted cases of decrease in aggregation of platelets, but the clinical value of it is not defined.

Special instructions

Patients with oh demand stringent control during treatment because of possible development of a bronchospasm. in case of a bronchospasm the treatment by Acetylcysteinum should be stopped immediately. it is recommended to use with care medicament to patients with ulcer of stomach and duodenum in the anamnesis, especially in case of the accompanying intake of other medicines which irritate a mucous membrane of a stomach.

Acetylcysteinum Use, mainly in an initiation of treatment, can cause fluidifying of a bronchial secret and increase its volume. If the patient is not capable to cough up effectively a phlegm, the postural drainage and a bronkhoaspiration are necessary. The light sulfuric smell is not sign of change of medicine, and is specific to active ingredient. It is necessary to consider sodium content to patients who adhere to a diet with sodium consumption control.

Medicine contains sorbite. If at the patient the intolerance of some sugars is established, consultation of the doctor is necessary before taking this drug.

Use during pregnancy and feeding by a breast. During pregnancy and feeding by a breast use of Acetylcysteinum is possible only if the expected advantage for mother exceeds potential risk for the fruit/child.

Children. Tablets on 200 mg apply at children aged from 2 years. Tablets on 600 mg apply at children aged from 14 years.

Ability to influence speed of response at control of vehicles or work with other mechanisms. There are no data.

Interaction

Use along with Acetylcysteinum of antibechics can increase stagnation of a phlegm because of suppression of a tussive reflex.

At simultaneous application with such antibiotics as tetracyclines (except for 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

Simultaneous 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 reduces expressiveness of toxic effect of paracetamol.

Influence on laboratory researches. Acetylcysteinum can influence colorimetric researches of salicylates and on definition of urates and ketone ph.

Overdose

Is not present data on cases of overdose of the dosage forms of Acetylcysteinum intended for intake.

Acetylcysteinum at reception in a dose of 500 mg/kg/days does not cause signs and symptoms of overdose.

Symptoms. The overdose can be shown by gastrointestinal symptoms, such as nausea, vomiting and diarrhea.

Treatment. There is no specific antidote at poisoning with Acetylcysteinum, therapy symptomatic.

Storage conditions

B protected from light at a temperature not above 25 °C.