Instructions for ACC Long lemon effervescent tablets 600 mg in sachet No. 6
Composition
active ingredient: acetylcysteine;
1 effervescent tablet contains 600 mg of acetylcysteine;
excipients: anhydrous citric acid (E 330), sodium bicarbonate, anhydrous sodium carbonate, mannitol (E 421), anhydrous lactose, ascorbic acid (E 300), sodium cyclamate (E 952), sodium saccharin (E 954), sodium citrate dihydrate (E 331), zinc sulfate monohydrate, lemon flavoring "BB".
Dosage form
Effervescent tablets.
Main physicochemical properties: white round tablets with a dividing line, surface without defects, lemon smell, specific odor.
Pharmacotherapeutic group
Medicines used for coughs and colds. Mucolytics.
ATX code R05C B01.
Pharmacological properties
Pharmacodynamics.
N-acetyl-L-cysteine (acetylcysteine) is a mucolytic, expectorant agent used to thin sputum in diseases of the respiratory system, accompanied by the formation of thick mucus. Acetylcysteine is a derivative of the amino acid cysteine. Acetylcysteine has a pronounced mucolytic effect on mucous and mucopurulent secretions due to the depolymerization of mucoprotein complexes and nucleic acids, which impart viscosity to the hyaline and purulent components of sputum and other secretions. Additional properties: reduction of induced hyperplasia of mucocytes, increased production of surfactant due to stimulation of type II pneumocytes, stimulation of the activity of the mucociliary apparatus, which contributes to improving mucociliary clearance. As a result, sputum becomes less viscous.
N-acetyl-L-cysteine also exerts a direct antioxidant pneumoprotective effect due to the presence of a nucleophilic free thiol group (SH), which is able to directly interact with electrophilic groups of oxidative radicals. Of particular interest is the fact that acetylcysteine prevents the inactivation of a-1-antitrypsin, an enzyme that inhibits elastase, by hypochlorous acid (HOCl), a strong oxidant produced by myeloperoxidase of active phagocytes.
In addition, the molecular structure of acetylcysteine enables it to easily penetrate cell membranes. Inside the cell, acetylcysteine is deacetylated to form L-cysteine, an essential amino acid for the synthesis of glutathione. In addition, acetylcysteine, which is a precursor of glutathione, exerts an indirect antioxidant effect. Glutathione is a highly active tripeptide, widespread in various animal tissues and indispensable for maintaining the functional capacity of the cell and its morphological integrity. In fact, it is part of the most important intracellular defense mechanism against oxidative radicals, both exo- and endogenous, and some cytotoxic substances, including paracetamol.
Paracetamol exerts its cytotoxic effect by progressively reducing glutathione levels. Acetylcysteine plays a primary role in maintaining adequate glutathione levels, thus enhancing cellular defense. As a result, acetylcysteine is a specific antidote for poisoning with paracetamol and other toxic substances (aldehydes, phenols).
In patients with COPD (chronic obstructive pulmonary disease), taking 1200 mg of acetylcysteine per day for 6 weeks resulted in a significant increase in inspiratory volume and FVC (forced vital capacity), possibly due to a decrease in air trapping.
In patients with IPF (idiopathic pulmonary fibrosis), the use of acetylcysteine orally at a dose of 600 mg 3 times a day for one year in combination with standard IPF therapy (prednisolone and azathioprine) contributed to the preservation of vital capacity (VC) and lung diffusion capacity, measured by the single inhalation method of carbon monoxide.
In the form of inhalation therapy for one year, acetylcysteine helped reduce the intensity of disease progression in patients with IPL.
When used in very high doses (up to 3000 mg daily for 4 weeks) in patients with cystic fibrosis, acetylcysteine did not have a significant toxic effect.
The antioxidant efficacy of acetylcysteine is associated with a marked reduction in sputum elastase activity, the most important indicator of lung function in patients with cystic fibrosis. In addition, treatment was associated with a reduction in the number of neutrophils in the respiratory tract, as well as the number of neutrophils actively secreting elastase-rich granules.
Pharmacokinetics.
Absorption
In humans, acetylcysteine is completely absorbed after oral administration. Due to metabolism in the intestinal wall and the first-pass effect, the bioavailability of acetylcysteine when taken orally is very low (approximately 10%). No differences were found for different dosage forms. In patients with various respiratory and cardiac diseases, the maximum concentration of acetylcysteine in the blood plasma is reached 1-3 hours after administration and remains high for 24 hours.
Distribution
Acetylcysteine is distributed in the body both in unchanged form (20%) and in the form of metabolites (active) (80%), while it is mainly found in the liver, kidneys, lungs and bronchial secretions. The volume of distribution of acetylcysteine is from 0.33 to 0.47 l / kg. Binding to plasma proteins is about 50% 4 hours after administration and decreases to 20% after 12 hours.
After oral administration, acetylcysteine is rapidly and extensively metabolized in the intestinal wall and liver. The formed metabolite, cysteine, is considered active. Further, acetylcysteine and cysteine are metabolized by the same pathway with the formation of cysteine, a pharmacologically active metabolite, as well as diacetylcysteine, cystine and further mixed disulfides. About 30% of the dose is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine).
The half-life is determined mainly by rapid biotransformation in the liver and is approximately 1 hour.
Indication
Treatment of acute and chronic diseases of the bronchopulmonary system, accompanied by increased sputum production.
Paracetamol overdose.
Contraindication
Hypersensitivity to acetylcysteine or other components of the drug. Hepatitis, renal failure (to avoid an increase in nitrogen-containing substances in the body). Gastric and duodenal ulcer in the acute stage, hemoptysis, pulmonary hemorrhage.
Interaction with other medicinal products and other types of interactions
Interaction studies were conducted only in adults.
When using the drug simultaneously with antitussives, dangerous mucus stagnation is possible due to a decrease in the cough reflex, therefore, a careful diagnosis is necessary to prescribe combination therapy with such agents.
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. Therefore, the interval between the use of these drugs should be at least 2 hours. This does not apply to cefixime and loracarbef.
Concomitant use of nitroglycerin with ACC® Long Lemon may lead to an increase in the vasodilator effect of nitroglycerin. Significant hypotension and dilation of the temporal artery have been reported with simultaneous use of nitroglycerin and acetylcysteine. If concomitant use of nitroglycerin and acetylcysteine is necessary, patients should be monitored for hypotension, which may be severe, and they should be warned about the possibility of headaches.
Upon contact with metals or rubber, sulfides with a characteristic odor are formed, so glassware should be used to dissolve the drug.
Acetylcysteine can be a cysteine donor and increase glutathione levels, which helps detoxify oxygen free radicals and certain toxic substances in the body.
Impact on laboratory tests
Acetylcysteine may interfere with the colorimetric assay for salicylates and the determination of ketone bodies in urine.
Application features
The use of acetylcysteine early in treatment may help thin the sputum and increase the volume of bronchial secretions. If the patient is unable to cough up sputum effectively, postural drainage and bronchoaspiration are necessary.
It is recommended to drink sufficient amounts of fluids during treatment with acetylcysteine.
Special caution is required when treating patients with histamine intolerance. Long-term use of ACC® Long Lemon is not recommended for such patients due to the effect on histamine metabolism, which may cause symptoms of intolerance (e.g. headache, vasomotor rhinitis, itching).
A slight sulfuric odor is not a sign of a change in the drug, but is specific to the active ingredient.
Mucolytics can 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.
One effervescent tablet contains 6.03 mmol (138.8 mg) of sodium. This should be taken into account by patients on a controlled salt diet (low sodium or low salt diet). ACC® Long Lemon is also contraindicated in patients with certain rare hereditary disorders, in particular galactose intolerance, lactase deficiency or lactose-galactose malabsorption.
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.
Use during pregnancy or breastfeeding
Currently, there is insufficient data on the use of the drug during pregnancy and breastfeeding, so the drug can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus or child.
Acetylcysteine crosses the placenta and has been detected in cord blood. There is no data on its passage into breast milk.
There is also no information on the ability of acetylcysteine to cross the blood-brain barrier.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no data on the negative impact on the ability to drive vehicles or operate complex mechanisms.
Method of administration and doses
For adults and children over 12 years of age – one effervescent tablet once a day (equivalent to a daily dose of 600 mg of acetylcysteine).
For children under 12 years of age and in cases where the daily dose should be divided into several doses, acetylcysteine is used in a different dosage form or in an appropriate dosage.
The effervescent tablet is dissolved in a glass of water and drunk after a meal. Other drugs cannot be added to this solution. After preparing the solution, it should be drunk as soon as possible. In some cases, due to the presence of a stabilizer - ascorbic acid - in the composition of the drug, the prepared solution can be left for about 2 hours before use.
Additional fluid intake enhances the mucolytic effect of the drug.
The duration of use of the drug is determined by the doctor, depending on the nature of the disease (acute or chronic). The course of treatment with the drug should not exceed 4-5 days.
Paracetamol overdose
In the first 10 hours after ingestion of a toxic substance, ACC® Long Lemon is taken as soon as possible at a rate of 140 mg/kg, then at a rate of 70 mg/kg every 4 hours for 1-3 days.
Children.
Used for children aged 12 and over.
Overdose.
No cases of severe and life-threatening side effects have been observed so far, even with significant overdose. Volunteers have taken 11.6 g of acetylcysteine per day for three months without any serious side effects. Oral doses of up to 500 mg acetylcysteine/kg body weight/day have been tolerated without any symptoms of intoxication.
Overdose may cause gastrointestinal symptoms such as nausea, vomiting, and diarrhea.
Children are at risk of hypersecretion.
There is no specific antidote for acetylcysteine poisoning; therapy is symptomatic.
Adverse reactions
The assessment of undesirable effects is based on the following classification according to the frequency of occurrence:
very common (≥ 1/10);
common (≥ 1/100, < 1/10);
uncommon (≥ 1/1000, < 1/100);
rare (≥1/10,000, <1/1,000);
rare (< 1/10,000);
frequency unknown (the available data do not allow for an estimate of the frequency).
General disorders and administration site reactions.
Uncommon: headache, fever, hyperthermia, fever, allergic reactions (itching, urticaria, exanthema, rash, bronchospasm, angioedema, Quincke's edema, tachycardia and hypotension).
Rare: anaphylactic reactions and shock.
Not known: facial edema, eczema.
From the blood and lymphatic system.
Not known: anemia.
On the part of the cardiac system, chest organs and mediastinum.
Uncommon: tachycardia, hypotension.
Rare: shortness of breath, bronchospasm - mainly in patients with bronchial hyperreactivity in bronchial asthma, dyspnea, hemorrhage.
Rare: hemorrhage.
From the gastrointestinal tract.
Uncommon: stomatitis, abdominal pain, vomiting, nausea and diarrhoea.
Uncommon: dyspepsia.
Not known: bad breath.
From the side of the organs of hearing and labyrinth.
Uncommon: ringing in the ears.
On the part of the respiratory system.
Rare: rhinorrhea.
From the nervous system.
Uncommon: headache.
From the immune system.
Uncommon: hypersensitivity reactions.
Rare: anaphylactic shock, anaphylactic/anaphylactoid reactions.
Research.
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.
Several studies have shown an attenuation of platelet aggregation in the presence of acetylcysteine. The clinical significance of this observation is unknown.
Expiration date
3 years.
Storage conditions
No special storage conditions required. Keep out of the reach of children.
Incompatibility with other medications.
In vitro incompatibility has been observed with some semisynthetic penicillins, tetracyclines, cephalosporins, and aminoglycosides. There is no evidence of incompatibility with antibiotics such as amoxicillin, erythromycin, or cefuroxime.
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 drugs in the same glass.
Packaging
1 effervescent tablet in a sachet; 6, 10 or 20 sachets in a cardboard box.
Vacation category
Without a prescription.
Producer
Salutas Pharma GmbH, Germany.
Manufacturer location
Otto-von-Guericke-Allee 1, 39179, Barleben, Germany.
