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

Acid, tartaric acid, citric acid anhydrous, aspartame, sodium saccharin dihydrate, lactose monohydrate, microcrystalline cellulose, crospovidone, magnesium stearate, (macrogol 4000, colloidal silicon dioxide, mint powder 00302 (peppermint oil (peppermint leaf oil) ratsementol (menthol racemic ), butylhydroxyanisole, gum arabic (acacia gum, gum arabic), dextrin) tablet weight -. 440.0 mg.

In 1 tablet 600 mg is contained:

Active substance: acetylcysteine 600 mg.

Excipients:

Acid tartaric acid, citric anhydrous, aspartame, sodium saccharinate dihydrate, lactose monohydrate, microcrystalline cellulose, crospovidone, magnesium stearate, macrogol 4000, silicon dioxide colloid, mint powder 00302 (peppermint oil (peppermint oil), racemtol (racemic acid) , butylhydroxyanisole, gum arabic (acacia gum, gum arabic), dextrin). A tablet weighing 1080.0 mg.

Description:

Tablets 200 mg: Round biconvex tablets of white color with a mint smell.

Tablets 600 mg: Oblong white tablets with a dividing notch on both sides with a mint smell.

Pharmacotherapeutic group:Expectorant mucolytic agent

ATX: & nbsp

S.01.X.A.08 Acetylcysteine

R.05.C.B.01 Acetylcysteine

Pharmacodynamics:

Acetylcysteine has a thawing effect. 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. Acetylcysteine has an antioxidant effect due to the presence of a nucleophilic thiol SH-group, which easily gives off hydrogen, neutralizing oxidative radicals.

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. The protective mechanism of acetylcysteine is based on the ability of its reactive sulfhydryl groups to bind chemical 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 that captures endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and contributes to an increase in the synthesis of intracellular glutathione involved in oxidation-reduction processes of cells, thus contributing to the detoxification of harmful substances. This explains the effect of acetylcysteine as an antidote in paracetamol poisoning.

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 diacetyl cysteine, 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-time of elimination of acetylcysteine from 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 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, pulmonary abscess, pulmonary emphysema, laryngotracheitis, chronic obstructive pulmonary disease, atelectasis of the lungs due to congestion of the bronchial mucosa).

Relief of secretion with sinusitis, sinusitis, otitis.

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

Contraindications:

Hypersensitivity to acetylcysteine. Due to its lactose content, Acce- stin® is not suitable for patients with rare hereditary galacto- zemia, congenital lactase deficiency, or glucose-galactose insufficiency syndrome.

Accein® 200 mg tablets should not be used in children younger than 6 years of age due to a high dose of active ingredient.

Acetin® 600 mg tablets should not be used in children younger than 14 years of age due to a high dose of active ingredient.

Carefully:

Peptic ulcer and duodenum 12 (in the acute stage), esophageal varices, hemoptysis, pulmonary hemorrhage, phenylketonuria, adrenal disease, hepatic and renal failure, hypotension, asthma, children under 6 years of age (the use in these cases possible only according to the doctor's prescription).

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. In pregnancy and lactation, the drug is only possible if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

Dosing and Administration:

Acestin® 200 mg tablets

Adults and adolescents over 14 years of age: 1 tablet 2-3 times a day (the equivalent of 400-600 mg per day of acetylcysteine).

Children from 6 to 14 years old: 1 tablet 2 times a day (equivalent to 400 mg per day of acetylcysteine).

In Cystic Fibrosis:

Children over 6 years old: 1 tablet 3 times a day (equivalent to 200 mg 3 times a day of acetylcysteine).

Acestin® 600 mg tablets

Tablets can be divided.

Adults and adolescents over 14 years of age: 1/2 tablet 2 times a day (equivalent to 600 mg per day of acetylcysteine) or 1 tablet 1 time per day (equivalent to 600 mg per day of acetylcysteine).

Tablets take after eating; or drink plenty of water if swallowed, or dissolve in a glass of water.

The mucolytic effect of acetylcysteine is enhanced when taken in liquid form. The attending physician should establish the duration of therapy in accordance with the type and severity of the disease.

The duration of therapy is determined individually (no more than 10 days). Patients over 65 years of age use the lowest effective doses.

Side effects:

Rarely (≥0,1% - <1%), stomatitis, headache, tinnitus, dyspnea, edema of the tissues (angioedema, allergic edema).

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

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

Very rare cases bronchospasm (<0.01%) were observed, mainly, in patients with bronchial hyperreactivity 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 the simultaneous administration of acetylcysteine with antitussive drugs because of the decrease in the cough reflex, a dangerous increase in the secretion may occur, therefore, the appointment of such a combination requires special attention.

Information about inactivation antibiotics acetylcysteine or other mucolytics are associated only with experiments in vitro, when the relevant substances are mixed directly. In vitro incompatibility has been described, mainly, 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:

With the simultaneous administration of acetylcysteine and nitroglycerin, vasodilator and disaggregant action of the latter may be enhanced.

Acetylcysteine eliminates toxic effects paracetamol.

Special instructions:

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

The presence of a light sulfuric odor is a characteristic odor of the active substance. When working with the drug should use glassware, avoid contact with metals, rubber, oxygen, easily oxidizing substances.

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

Packaging:For 10 tablets in PVC / aluminum foil blisters. 1, 2 or 5 blisters with instructions for medical use of the drug in a cardboard box.

Storage conditions:

In a dry, protected from light at a temperature of no higher than 25 ° C.

Keep out of reach of children.

Shelf life:3 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:P N010295

Date of registration:19.11.2007

Expiration Date:Unlimited

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

Manufacturer: & nbsp

STADA Arzneimittel, AG Germany

Representation: & nbspSTADA CISASTADA CISARussia

Information update date: & nbsp02.10.2017

Illustrated instructions

Instructions

Acestin® (Acestin®)