Pharmacological properties

Pharmacodynamics. Acetylcysteinum (azz) — mucolytic, the expectorant applied to depression of a phlegm at the diseases of a respiratory system which are followed by formation of dense slime. Acetylcysteinum is derivative amino acids cysteine. the mucolytic effect of medicine has the chemical nature. due to presence of free sulfhydryl group Acetylcysteinum breaks disulfide bridges of acid mucopolysaccharides that leads to a depolymerization of mukoproteid of a phlegm and reduction of viscosity of slime and promotes expectoration and an otkhozhdeniye of a bronchial secret. medicine keeps activity in the presence of a purulent phlegm.

Acetylcysteinum has also antioxidant pneumotyre-tread properties caused by binding by its sulfhydryl groups of chemical radicals and, thus, their neutralization. Besides, medicine promotes increase in synthesis of glutathione — an important factor of intracellular protection not only against the oxidized toxins of exogenous and enedogenny origin, but also from a number of cytotoxic substances. This feature of Acetylcysteinum gives the chance to effectively apply the last at paracetamol overdose.

Pharmacokinetics. After oral administration Acetylcysteinum quickly and completely is soaked up and exposed to metabolism in a liver with formation of cysteine, pharmacological an active metabolite and also diacetylcysteinum, cystine and further — the mixed disulfides. Bioavailability very low — about 10%. With _max in blood plasma it is reached in 1–3 h after reception. Linking with proteins of blood plasma — about 50%. Acetylcysteinum is emitted with kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteinum). is defined

T _½ by p, mainly, fast biotransformation in a liver and makes about 1 h. In case of depression of function of a liver of T _½

Indication

Treatment of the sharp and chronic diseases of a bronchopulmonary system demanding reduction of viscosity of a phlegm, improvement of its otkhozhdeniye and expectoration increases to 8 h

.

Use

to Adults and children is aged more senior than 14 years appoint 400–600 mg of Acetylcysteinum a day distributed on 1–3 receptions.

to Children at the age of 6–14 years: 400–600 mg/days distributed on 2–3 receptions.

to Children aged from 2 up to 6 years: on 200–400 mg/days divided into 2 receptions.

is recommended to take the Drug after a meal. To dissolve contents of a bag when stirring in ½ glasses of hot water and to drink, whenever possible, hotter. Additional intake of liquid enhances mucolytic effect of medicine.

Term of treatment of chronic diseases is defined by the doctor depending on character and a course of the disease. In sharp uncomplicated diseases it is necessary to apply Acetylcysteinum 5–7 days.

Contraindication

Hypersensitivity to Acetylcysteinum or other components of medicine.

Peptic ulcer of a stomach and duodenum in an aggravation stage, a pneumorrhagia, pulmonary bleeding.

Side effects

from a cardiovascular system: tachycardia, arterial hypotension.

from nervous system: headache.

from skin: allergic reactions (itch, urticaria, dieback, eczema, rash, Quincke's disease).

from an organ of hearing: a ring in ears.

from a respiratory system: short wind, a bronchospasm (mainly at patients with hyperreactivity of a bronchial system which is associated with OH), a rhinorrhea.

from a digestive tract: heartburn, dyspepsia, stomatitis, an abdominal pain, nausea, vomiting, diarrhea, an unpleasant smell from a mouth.

General violations: fever.

to

It was reported about separate heavy reactions from skin (Stephens's syndrome — Johnson and Layell). At use of Acetylcysteinum it was very seldom reported about developing of bleedings which were most often connected with development of reactions of hypersensitivity. Cases of decrease in aggregation of platelets were noted, however it does not have clinical confirmation. It was very seldom reported about a Quincke's edema, a face edema, cases of anemia, a hemorrhage, anaphylactic reactions or even shock.

Special instructions

Is recommended to be taken with caution 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.

and to consult with the doctor of rather further reception.

Should appoint

with care Acetylcysteinum sick OH because of possible development of a bronchospasm. In a bag contents rash in ware in preparation time of solution powder can get to air and irritate a mucous membrane of a nose therefore there can be a reflex bronchospasm.

to Patients with diseases of a liver or kidneys should appoint Acetylcysteinum by

with care in order to avoid accumulation of nitrogen-containing substances in an organism.

Use of Acetylcysteinum causes fluidifying of a bronchial secret. If the patient is not capable to cough up effectively a phlegm, the postural drainage and a bronkhoaspiration are necessary.

Acetylcysteinum influences metabolism of a histamine therefore patients should not appoint long therapy with intolerance of a histamine as it can lead to emergence of symptoms of intolerance (a headache, vasomotorial rhinitis, an itch).

Drug contains sucrose therefore it patients should not appoint with rare hereditary forms of intolerance of fructose, deficiency sucrose-isomaltase or a syndrome of glyukozo-galaktozny malabsorption.

Information for patients with diabetes. 1 bag of powder (200 mg of Acetylcysteinum) contains 2.5 g of sucrose (0.21 XE).

1 bag of powder (600 mg of Acetylcysteinum) contains 2 g of sucrose (0.17 XE).

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

Ability to influence speed of response at control of vehicles or work with other mechanisms. Does not influence.

Children. Powder on 200 mg: to apply at children 2 years aged are more senior.

Powder on 600 mg: to apply at children 14 years aged are more senior.

Interaction

Simultaneous use of Acetylcysteinum with antibechics can increase stagnation of a phlegm because of reduction of expressiveness of a tussive reflex.

At simultaneous application with such antibiotics as tetracycline (except for doxycycline), ampicillin, Amphotericinum B, cephalosporins, aminoglycosides, 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. It does not concern a tsefiksim and a lorakarbef.

Activated carbon reduces efficiency of Acetylcysteinum.

does not recommend to dissolve

in one glass Acetylcysteinum with other medicines.

Acetylcysteinum reduces expressiveness of hepatotoxic action of paracetamol.

by

notes synergism of Acetylcysteinum with bronchial spasmolytics.

Atsetiltsistein can be the donor of cysteine and increase glutathione level that promotes a detoxication of free radicals of oxygen and certain toxics in an organism.

Concomitant use of nitroglycerine and Acetylcysteinum can lead

to strengthening of vazodilatatorny effect of nitroglycerine.

by

At contact with metals or rubber form sulfides with a characteristic smell therefore for dissolution of medicine it is necessary to use glasswares.

Overdose

Is not present data on overdose cases at oral administration of Acetylcysteinum.

Symptoms: nausea, vomiting, diarrhea. Children have a risk of development of hypersecretion.

Therapy symptomatic.

Storage conditions

At a temperature not above 25 °C. to store out of children's reach.