ATS Active powder for oral use 600mg sachets, 10pcs

Composition

1 sachet contains:

Active ingredient:

acetylcysteine 600 mg;

excipients:

glyceryltrinitrate,

Polysorbate 65,

sorbitol,

xylitol,

citric acid,

sodium citrate,

magnesium citrate,

carmellose sodium,

aspartame,

flavor Black Berry “B” (natural/nature identical flavoring liquid “Forest berry”, code 5752; natural/nature identical flavoring liquid “Black Berry”, the code 5337; vanillin; maltodextrin; mannitol; gluconolactone; sorbitol; silicon dioxide colloidal anhydrous; magnesium carbonate),

magnesium stearate.

Pharmacological action

Acetylcysteine is a derivative of the amino acid cysteine. It has mucolytic and secretomotor effects in the respiratory tract, facilitates sputum discharge by directly affecting the rheological properties of sputum. The effect of the drug is due to the ability of its free sulfhydryl groups to break intra-and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolymerization of mucoproteins and a decrease in sputum viscosity.

In addition, it reduces the induced hyperplasia of mucoid cells, increases the production of surfactants by stimulating type II pneumocytes, and stimulates ciliary activity, which leads to an improvement in mucociliary clearance.

The drug remains active in the presence of purulent, mucopurulent and mucosal sputum.

Increases the secretion of less viscous sialomucins by goblet cells, reduces the adhesion of bacteria to the epithelial cells of the bronchial mucosa. It stimulates cells of the bronchial mucosa, the secret of which lyses fibrin.

It has a similar effect on the secret formed in inflammatory diseases of ENT organs.

It has an antioxidant effect due to the presence of sulfhydryl groups (SH-groups) that can neutralize electrophilic oxidative toxins. Acetylcysteine easily penetrates into the cell, where it is deacetylated to L-cysteine, from which intracellular glutathione is synthesized.

Glutathione is a highly reactive tripeptide, a powerful antioxidant, and a cytoprotector that traps endogenous and exogenous free radicals and toxins. Acetylcysteine prevents depletion and increases the synthesis of intracellular glutathione, which is involved in redox processes in cells, thus contributing to the detoxification of harmful substances. This explains the effect of acetylcysteine as an antidote for paracetamol poisoning.

Paracetamol exerts its cytotoxic effect through progressive depletion of glutathione. The main role of acetylcysteine is to maintain the proper level of glutathione concentration, which provides protection for cells.

Protects alpha-1-antitrypsin (elastase inhibitor) It depends on the inactivating effect of HOCl, an oxidant produced by myeloperoxidase of active phagocytes. It also has an anti-inflammatory effect (by suppressing the formation of free radicals and active oxygen-containing substances responsible for the development of inflammation in the lung tissue).

With prophylactic use of acetylcysteine, there is a decrease in the frequency and severity of exacerbations of bacterial infections in patients with chronic bronchitis and cystic fibrosis.

Indications

Acute and chronic respiratory diseases associated with the formation of viscous difficult-to-separate bronchial secretions (as an expectorant): bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, emphysema, laryngotracheitis, interstitial lung diseases, lung atelectasis (due to blockage of the bronchi with a mucous plug).

Inflammation of the middle ear (otitis media), acute and chronic sinusitis, rhinosinusitis (relief of secretions).

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

Recommendations for use

Inside. Powder from 1 sachet should be poured directly on the tongue. The drug stimulates salivation, so the powder is mixed with saliva and easily swallowed. The drug does not require drinking water. Oral powder should not be chewed before ingestion.

Adults:  1 sachet once a day (equivalent to 600 mg of acetylcysteine per day).

Due to the high content of acetylcysteine (600 mg) in 1 sachet, the drug should not be used in children (it is recommended to use other dosage forms of ACC® or another acetylcysteine preparation).

The duration of treatment should be evaluated individually. For short-term colds, the duration of the course is 5-7 days, for the treatment of chronic diseases-up to several months (on the recommendation of a doctor).

Contraindications

• Hypersensitivity to acetylcysteine or other components of the drug;
• hemoptysis, pulmonary bleeding;
• acute peptic ulcer of the stomach and duodenum;
• children under 18 years of age (for this dosage form);
• pregnancy and lactation;
• hereditary intolerance to fructose (contains sorbitol), phenylketonuria (contains a source of phenylalanine aspartame).

With caution

A history of gastric or duodenal ulcer, bronchial asthma, obstructive bronchitis, liver and/or kidney failure, histamine intolerance (long-term use should be avoided, as acetylcysteine affects the metabolism of histamine, which can lead to symptoms of its intolerance, such as headache, vasomotor rhinitis, pruritus), esophageal varicose veins, adrenal diseases, arterial hypertension.

Side effects

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency as follows: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (Immune system disorders

infrequently: hypersensitivity reactions;

very rarely: anaphylactic shock, anaphylactic / anaphylactoid reactions.

Nervous system disorders

infrequently: headache.

Cardiac and vascular

disorders infrequently: tachycardia, hypotension;

very rarely: bleeding*;

frequency unknown:  when taking acetylcysteine, cases of collapse have been described.

Respiratory system disorders

are rare: shortness of breath, bronchospasm (mainly in patients with hyperreactivity of the bronchi on the background of bronchial asthma).

Gastrointestinal disorders

infrequently: abdominal pain, nausea, vomiting, diarrhea, stomatitis;

rarely: dyspepsia;

frequency unknown: heartburn.

Skin and subcutaneous tissue disorders

infrequently: urticaria, exanthema, rash, angioedema, pruritus;

very rarely: Stevens-Johnson syndrome, Lyell’s syndrome (see section “Special instructions”).

Hearing disorders and labyrinth disorders

infrequently: tinnitus.

General disorders

uncommon: fever;

frequency unknown: facial edema.

* There have been isolated reports of bleeding associated with the use of acetylcysteine, sometimes with hypersensitivity reactions. A decrease in platelet aggregation during the use of acetylcysteine has been confirmed in some studies, but the clinical significance of this phenomenon has not yet been clarified.

Interaction

When acetylcysteine is used simultaneously with antitussive medications, sputum congestion in the bronchi may occur due to suppression of the cough reflex. Before prescribing such combination therapy, a thorough assessment of the patient’s condition is necessary.

Current reports of acetylcysteine inactivation of antibacterial drugs such as tetracyclines (excluding doxycycline), aminoglycosides, cephalosporins, penicillins (ampicillin), and antifungal drugs (amphotericin B) refer exclusively to in vitro studies (pharmaceutical incompatibility). However, oral antibacterial agents and ADC®are not recommended. The active agent should be applied at intervals of at least 2 hours (not applicable to cefixime and loracarbef).

Concomitant use with acetylcysteine may increase the vasodilating and antiplatelet effects of nitroglycerin. If the combined use of nitroglycerin and acetylcysteine is required, the patient’s condition should be monitored for the potential development of arterial hypotension (sometimes severe, may manifest as headache).

Concomitant use of acetylcysteine and carbamazepine may result in a decrease in the concentration of carbamazepine to a subtherapeutic level.

Simultaneous use of activated carbon may reduce the effect of acetylcysteine.

Acetylcysteine eliminates the toxic effects of paracetamol.

Overdose

Cases of toxic overdose when taking acetylcysteine orally are not described. Acetylcysteine at doses up to 500 mg / kg / day did not cause symptoms of overdose. Healthy volunteers received acetylcysteine at a dose of 11.6 g per day for 3 months without developing any severe adverse reactions.

Symptoms:  gastrointestinal symptoms may include nausea, vomiting, and diarrhea.

Treatment: symptomatic therapy if necessary.

Description

White to yellowish-white powder with easily disintegrating agglomerates, with a blackberry smell. There may be a faint sulfur smell.

Functional features

Absorption

Acetylcysteine is rapidly and almost completely absorbed when taken orally. Due to the high presystemic metabolism (the effect of “primary passage” through the liver), the bioavailability of oral forms of acetylcysteine is about 10%. The maximum concentration (Cmax) of acetylcysteine in blood plasma after oral use is reached in 1-3 hours and is 15 mmol/l, the Cmax of the cysteine metabolite is approximately 2 mmol/l.

Distribution

The binding to plasma proteins is about 50% after 4 hours and decreases to 20% after 12 hours

. Acetylcysteine is distributed both unchanged (20%) and in the form of active metabolites (80%), penetrates the intercellular space, and is distributed mainly in the liver, kidneys, lungs, and bronchial secretions. Acetylcysteine penetrates the placental barrier and is detected in the umbilical cord blood. There is no information on excretion in breast milk. There are no data on the ability of acetylcysteine to cross the blood-brain barrier.

Metabolism

Acetylcysteine is metabolized in the liver to cysteine, a pharmacologically active metabolite, as well as to diacetylcysteine, cystine, and other mixed disulfides. In the body, acetylcysteine and its metabolites can be detected in various forms: in free form, bound to plasma proteins by labile disulfide bonds, or as linked amino acids.

Elimination

Acetylcysteine is excreted almost exclusively in the form of inactive metabolites (inorganic sulfates, diacetylcysteine) by the kidneys, a small part is excreted unchanged through the intestine. The plasma half-life of the drug (T1/2) is approximately 1 h and depends on the rate of biotransformation in the liver. With impaired liver function, T1 / 2 of acetylcysteine can increase up to 8 hours.

Special instructions

In patients with asthma and obstructive bronchitis, acetylcysteine should be administered with caution under systemic monitoring of bronchial patency. If the patient is unable to clear his throat effectively, drainage or aspiration of the secretions should be performed.

Severe allergic reactions, such as Stevens-Johnson syndrome and Lyell’s syndrome, have been reported very rarely with acetylcysteine. If you experience changes in the skin and mucous membranes, you should immediately consult a doctor, stop taking the drug.

Do not take the drug immediately before bedtime (it is recommended to take the drug before 18.00).

Influence on laboratory data. Acetylcysteine may affect the results of colorimetric determination of salicylate concentration in blood plasma. In a urine test, acetylcysteine can affect the results of determining ketone bodies.

 Influence on the ability to drive vehicles, mechanisms

Acetylcysteine does not affect the ability to drive vehicles and work with mechanisms.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 2 years.

Do not use after the expiration date indicated on the package.

Active ingredient

Acetylcysteine

Dosage form

solution for oral use

Purpose

Children over 14 years old, For adults

Indications

Sinusitis, Sinusitis, Cough, Tracheitis, Pneumonia, Chronic Obstructive Pulmonary Disease, Bronchitis, Otitis