Acetin - instructions for use, dose, side effects, contraindications

Acetin® effervescent tablets contain as active ingredient - acetylcysteine 200 mg or 600 mg; Excipients: citric acid anhydrous, sodium bicarbonate, lemon flavor, adipic acid, povidone (polyvinylpyrrolidone soluble), adipic acid micronized, aspartame.

Description:

Round flat tablets from white to white with a slightly yellowish shade of color with a risk on one side, with the smell of lemon.

Pharmacotherapeutic group:Expectorant mucolytic agent

ATX: & nbsp

S.01.X.A.08 Acetylcysteine

R.05.C.B.01 Acetylcysteine

Pharmacodynamics:

Acetylcysteine dilutes and facilitates sputum evacuation, increases its volume. The presence of sulfhydryl groups in the structure of acetylcysteine promotes the rupture of disulfide bonds of acid mucopolysaccharides of sputum, which leads to depolarization of mucoproteins and a decrease in mucus viscosity. The drug remains active in the presence of purulent sputum. Does not affect immunity.

Acetylcysteine has an antioxidant effect due to the presence of a nucleophilic thiol SH-group, which easily gives off hydrogen, neutralizing oxidative radicals. Acetylcysteine easily penetrates the cell, deacetylates to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant, a cytoprotector, detoxifying endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and promotes an increase in the synthesis of intracellular glutathione involved in redox processes of cells, thus contributing to the detoxification of harmful substances.

With the preventive use of acetylcysteine, there is a decrease in the frequency and severity of exacerbations in patients with chronic bronchitis and cystic fibrosis. Protective the mechanism of acetylcysteine is based on the ability of its reactive sulfhydryl groups to bind chemical radicals.

Pharmacokinetics:

Ingestion acetylcysteine quickly and almost completely absorbed. In the liver, it is metabolized with the formation of cysteine, a pharmacologically active metabolite, and also with the formation of diacetylcysteine, cystine and other disulfides.

When administered, the bioavailability of acetylcysteine is very low (about 10%) because of the pronounced "first pass" effect through the liver.The maximum concentration in the plasma occurs in 1-3 hours, the maximum concentration in the plasma of the cysteine metabolite is 2 μmol / l. Binding to plasma proteins of acetylcysteine is about 50%.

Acetylcysteine and its metabolites are present in the body in three different forms: a free drug; metabolite associated with the protein via unstable disulfide bonds; bound amino acid. It is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine). The half-life of acetylcysteine from the plasma is about 1 hour due to rapid biotransformation in the liver. With reduced liver function, the half-life of plasma can increase up to 8 hours.

Acetylcysteine penetrates the placental barrier in rats and is determined in the amniotic fluid. After 0.5, 1, 2 and 8 hours after ingestion of 100 mg / kg of acetylcysteine, the concentration of the metabolite L-cysteine in the placenta and in the fetus is higher than the concentration in the mother's plasma.

Indications:

Diseases of the respiratory system, accompanied by the formation of sputum of increased viscosity: acute and chronic bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, bronchial asthma with difficulty in sputum discharge, chronic obstructive pulmonary disease (COPD), atelectasis of the lung (due to congestion of the bronchial mucosa), pulmonary abscess, pulmonary emphysema, laryngotracheitis.

Relieving mucus from sinusitis, sinusitis, otitis.

Removal of a viscous secretion from the respiratory tract in post-traumatic and postoperative conditions.

Preparation for bronchoscopy, bronchography, aspiration drainage.

Contraindications:

Hypersensitivity to acetylcysteine, pregnancy, breast-feeding.

Acetin® tablets effervescent 200 mg should not be used in children younger than 2 years of age.

Acetin® tablets effervescent 600 mg should not be used in children younger than 14 years of age.

Carefully:

Peptic ulcer of the stomach and duodenum (at the stage of exacerbation), varicose veins of the esophagus, hemoptysis, pulmonary hemorrhage, adrenal diseases, hepatic and renal insufficiency, arterial hypotension, bronchial asthma, obstructive bronchitis, phenylketonuria.

Pregnancy and lactation:

Passage through the placenta and breast milk, as well as effects on the fetus or babies in humans have not been studied, so the use of the drug during pregnancy and lactation is contraindicated.

Dosing and Administration:

Inside. The effervescent tablets should be dissolved in 1/2 a glass of water and taken immediately after dissolution, the tablets can be divided.

Acetin® tablets effervescent 200 mg:

- adults and adolescents over 14 years - 1 effervescent tablet 2-3 times a day (200 mg of acetylcysteine 2-3 times a day),

- children 6-14 years - 1 effervescent tablet 2 times a day (200 mg of acetylcysteine 2 times a day),

- children 2-6 years - ½ effervescent tablets 2-3 times a day (100 mg of acetylcysteine 2-3 times a day.

In cystic fibrosis:

- children over 6 years: 1 effervescent tablet 3 times a day (200 mg of acetylcysteine 3 times a day day),

- children 2-6 years old: ½ effervescent tablets 4 times a day (100 mg of acetylcysteine 4 times a day).

Acetin® tablets effervescent 600 mg:

- adults and adolescents over 14 years of age: ½ effervescent tablets 2 times a day (300 mg of acetylcysteine 2 times a day) or 1 effervescent tablet once a day (600 mg of acetylcysteine once a day).

Additional fluid intake enhances the mucolytic effect of the drug.

Acetin® tablets effervescent should be taken after meals.

With short-term catarrhal diseases, the duration of admission is 5-7 days.In chronic diseases, the duration of therapy is determined by the attending physician.

Side effects:

Rarely (≥0,1% - <1%) there was stomatitis, headache and tinnitus.

In some cases (≥0,01% - <0,1%), heartburn, nausea, vomiting and diarrhea can be observed.

Rarely (<0.01%) reported allergic reactions caused by admission acetylcysteine, for example, itching, urticaria, exanthema, rash. Cases of development are described nasal bleeding, reduced platelet aggregation, collapse, tachycardia, or lowering blood pressure.

Very rare cases bronchospasm (<0.01%) were observed, mainly, in patients with hyperreactivity of bronchi in bronchial asthma.

Overdose:

Acetylcysteine at a dose of 500 mg / kg / day does not cause signs and symptoms of an overdose. Symptoms: diarrhea, heartburn, nausea, vomiting, pain in the stomach. Treatment: symptomatic.

Interaction:

With concomitant administration of acetylcysteine with antitussive drugs, a dangerous increase in secretion may occur due to a decrease in the cough reflex, so this combination requires special attention.

Information on the inactivation of antibiotics by acetylcysteine or other mucolytics are only related to experiments in vitro, when the relevant substances were mixed directly. Incompatibility in vitro was mainly described for semisynthetic penicillins, tetracyclines, cephalosporins and aminoglycosides. For safety reasons, these antibiotics should be taken separately from acetylcysteine at intervals of at least 2 hours. Absence of incompatibility was noted for such antibiotics as amoxicillin, doxycycline, erythromycin, thiamphenicol and cefuroxime.

There was also an increase in vasodilator and antithrombotic effects nitroglycerin with simultaneous admission with acetylcysteine. The clinical validity of these phenomena is still unclear.

Acetylcysteine eliminates the toxic effects of paracetamol.

Special instructions:

Patients with bronchial asthma and obstructive bronchitis acetylcysteine should be administered with caution under the systematic control of bronchial patency.

The presence of a light sulfuric odor is a characteristic property of the active substance.

When working with the drug should use glassware, avoid contact with metals, rubber, oxygen, easy-oxidizing substances.

When treating patients with phenylketonuria, it should be noted that the composition of the drug is aspartame - source phenylalanine.

When observing a low-salt or salt-free diet, it should be borne in mind that a 200 mg tablet contains 191 mg of sodium, a tablet of 600 mg to 150 mg of sodium.

Form release / dosage: Acetin® tablets are effervescent 200, 600 mg.

Packaging:

Acetin® tablets effervescent 200 mg. For 20 effervescent tablets in a polypropylene tube with polyethylene stopper. 1 tube together with instructions for medical use of the drug in a cardboard box.

Acetin® tablets effervescent 600 mg. For 10 effervescent tablets in a polypropylene tube with polyethylene stopper. 1 tube with instructions for medical use of the drug in a cardboard box.

Storage conditions:

Store in a place protected from moisture and light at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-005200/09

Date of registration:29.06.2009

Expiration Date:Unlimited

Date of cancellation:2017-09-18

The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany

Manufacturer: & nbsp

STADA Arzneimittel, AG Germany

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acestin® (Acestin®)