Instructions for use Acetylcysteine effervescent tablets 600 mg No. 10
Composition
active ingredient: acetylcysteine;
1 effervescent tablet contains: acetylcysteine 600 mg;
excipients: anhydrous citric acid, sodium bicarbonate, adipic acid, povidone 25, micronized adipic acid, aspartame (E 951), spray-dried lemon flavor, 213°841 (flavoring agent, maltodextrin, sucrose, gum arabic (E 414), glycerol triacetate (triacetin) (E 1518), alpha-tocopherol (E 307)).
Dosage form
Effervescent tablets.
Main physicochemical properties: white or slightly yellowish, round, flat on both sides, effervescent tablets, without a break line and with a lemon odor.
Pharmacotherapeutic group
Medicines used for coughs and colds. Mucolytics. ATX code R05C B01.
Pharmacological properties
Pharmacodynamics
Acetylcysteine (AC) is a derivative of the amino acid cysteine. Acetylcysteine has secretolytic and secretomotor effects in the bronchial tract. It is believed that it breaks disulfide bonds of mucopolysaccharides and has a depolymerizing effect on DNA (in purulent mucus). This mechanism is believed to reduce mucus viscosity. An alternative mechanism of action of acetylcysteine is believed to be based on the ability of its chemically active sulfhydryl group to bind and thus detoxify chemical radicals.
In addition, acetylcysteine helps to increase the synthesis of glutathione, which is important for the detoxification of harmful substances. This explains its action as an antidote in case of paracetamol intoxication.
The protective effect of prophylactic use of acetylcysteine on the frequency and severity of bacterial exacerbations in patients with chronic bronchitis/cystic fibrosis is known.
Pharmacokinetics
After oral administration, acetylcysteine is rapidly and almost completely absorbed and metabolized in the liver to form cysteine, the pharmacologically active metabolite, as well as diacetylcysteine, cystine and other mixed disulfides. Due to the significant first-pass effect, the oral bioavailability of acetylcysteine is very low (about 10%). The maximum plasma concentration is reached 1-3 hours after administration, with the maximum plasma concentration of the cysteine metabolite being approximately 2 μmol/l. Plasma protein binding is approximately 50%.
Acetylcysteine and its metabolites occur in the body in three different forms: partly in free form, partly in a form bound to proteins via labile disulfide bridges, and partly in the form of incorporated amino acids. Excretion occurs almost exclusively via the kidneys in the form of an inactive metabolite (inorganic sulfate, diacetylcystine). The plasma half-life of acetylcysteine is approximately 1 hour and is determined mainly by rapid biotransformation in the liver. In case of reduced liver function, the plasma half-life is extended to 8 hours.
N-acetylcysteine crosses the placental barrier and is found in cord blood. Information on penetration into breast milk is not available. There is no information on the penetration of acetylcysteine through the blood-brain barrier.
Indication
Treatment of acute and chronic diseases of the bronchopulmonary system, accompanied by increased sputum production.
Contraindication
Hypersensitivity to acetylcysteine or to any of the excipients.
Gastric and duodenal ulcer in the acute stage, hemoptysis, pulmonary hemorrhage.
Due to the high content of the active substance, the drug should not be used in children under 14 years of age.
Interaction with other medicinal products and other types of interactions
Interaction studies were conducted only with adults.
The use of antitussives together with acetylcysteine may increase sputum congestion due to suppression of the cough reflex, therefore indications for such combined treatment should be established with particular caution.
Activated charcoal reduces the effectiveness of acetylcysteine.
When used simultaneously with antibiotics such as tetracyclines (except doxycycline), ampicillin, amphotericin B, cephalosporins, aminoglycosides, their interaction with the thiol group of acetylcysteine is possible, which leads to a decrease in the activity of both drugs. Reports of inactivation of antibiotics (tetracycline, aminoglycosides, penicillins) by acetylcysteine were associated exclusively with in vitro studies in which the corresponding substances were mixed directly. However, for safety reasons, oral administration of antibiotics should be separated by an interval of at least 2 hours. This does not apply to cefixime and loracarbef.
Acetylcysteine can be a cysteine donor and increase glutathione levels, which helps detoxify oxygen free radicals and certain toxic substances in the body.
Effect on laboratory tests: Acetylcysteine may interfere with the colorimetric assay of salicylates and the determination of ketone bodies in urine.
When dissolving acetylcysteine, it is necessary to use glassware and avoid contact with metal and rubber surfaces.
It is not recommended to dissolve acetylcysteine with other medications.
Application features
Patients with bronchial asthma should be closely monitored during treatment due to the possible development of bronchospasm. In the event of bronchospasm, treatment with acetylcysteine should be discontinued immediately.
It is recommended to use the drug with caution in patients with a history of gastric and duodenal ulcers, especially in case of concomitant use of other medications that irritate the gastric mucosa.
Acetylcysteine should be administered with caution to patients with liver or kidney disease to avoid the accumulation of nitrogenous substances in the body.
Acetylcysteine affects histamine metabolism, so caution should be exercised when used in patients with histamine intolerance. Long-term therapy should not be prescribed to such patients, as this may lead to symptoms of intolerance (headache, vasomotor rhinitis, itching).
The use of acetylcysteine, especially at the beginning of treatment, may cause liquefaction of bronchial secretions and increase their volume. If the patient is unable to cough up sputum effectively, postural drainage and bronchoaspiration are necessary.
A slight sulfuric odor is not a sign of a change in the drug, but is specific to the active ingredient.
Mucolytics may cause bronchial obstruction in children under 2 years of age. Due to the physiological characteristics of the respiratory system in children of this age group, the ability to clear respiratory secretions is limited. Therefore, mucolytics should not be used in children under 2 years of age.
1 effervescent tablet contains 150 mg sodium, which is 7.65% of the WHO recommended maximum daily intake of 2 g sodium for adults. This should be taken into account by patients on a controlled sodium (low salt) diet.
The medicine contains aspartame, a source of phenylalanine, and may be harmful for patients with phenylketonuria.
This medicinal product contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicinal product.
Use during pregnancy or breastfeeding
Pregnancy
Clinical data on the use of acetylcysteine in pregnant women are limited. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryo-fetal development, parturition or postnatal development.
Breast-feeding
There is no information on the penetration of the drug into breast milk.
The drug should be used during pregnancy or breastfeeding only after careful assessment of the benefit/risk ratio.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no evidence that acetylcysteine affects the ability to drive and use machines.
Method of administration and doses
For oral use.
The effervescent tablet should be dissolved in a glass of drinking water and the entire contents of the glass should be drunk. The medicine should be taken without delay, immediately after preparing the solution.
Adults and children aged 14 and over
1 effervescent tablet once a day (equivalent to 600 mg of acetylcysteine per day).
The duration of the course of treatment is determined by the doctor individually, depending on the nature of the disease (acute or chronic). The drug should not be used for more than 4-5 days without consulting a doctor.
Children.
Use for children over 14 years of age.
Overdose
There are no data on cases of overdose with oral administration of acetylcysteine.
Volunteers took 11.6 g of acetylcysteine per day for 3 months without experiencing serious side effects.
Acetylcysteine, when administered orally at doses of 500 mg/kg/day, was tolerated without signs of intoxication.
Symptoms: Overdose may manifest as gastrointestinal symptoms such as nausea, vomiting and diarrhoea. There is a risk of hypersecretion in infants.
Treatment. There is no specific antidote for acetylcysteine poisoning, therapy is symptomatic.
Side effects
Adverse reactions are classified according to frequency as follows: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (<1/10000); frequency unknown (cannot be estimated from the available data).
Immune system disorders: infrequently - hypersensitivity; very rarely - anaphylactic shock, anaphylactic/anaphylactoid reactions.
Blood and lymphatic system disorders: frequency unknown - anemia.
From the nervous system: infrequently - headache.
From the side of the organs of hearing and labyrinth: infrequently - tinnitus.
Cardiac: infrequently - tachycardia.
From the respiratory system: rarely - bronchospasm, dyspnea; frequency unknown - rhinorrhea.
Gastrointestinal: infrequently - vomiting, diarrhea, stomatitis, abdominal pain, nausea; rarely - dyspepsia; frequency unknown - bad breath.
Skin and subcutaneous tissue disorders: infrequently - urticaria, rash, angioedema, itching; frequency unknown - eczema.
General disorders: infrequently - hyperthermia; frequency unknown - facial edema.
Investigations: uncommon – decreased blood pressure.
In very rare cases, severe skin reactions such as Stevens-Johnson syndrome and Lyell's syndrome have been reported in association with acetylcysteine. In most cases, at least one other drug is more likely to be the cause of the mucocutaneous syndrome. Therefore, if any new changes appear on the skin or mucous membranes, you should consult a doctor and immediately discontinue acetylcysteine.
Cases of decreased platelet aggregation have been reported, but the clinical significance of this has not been determined.
Expiration date
2 years. Shelf life after first opening the tube is 12 months.
Storage conditions
Store at a temperature not exceeding 25 °C in a tightly closed tube to protect from moisture. Keep out of the reach of children.
Packaging
10 tablets in a tube; 1 tube in a cardboard box.
Vacation category
Without a prescription.
Producer
Merkle GmbH.
Address
Graf-Arko Str. 3, 89079 Ulm, Germany.
