Astrace

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT AstraCe (AstraCe)

Composition:

Active substance: acetylcysteine;

One sachet contains acetylcysteine equivalent to 100% substance 200 mg;

Excipients: ascorbic acid, saccharin, sucrose, orange flavor.

Pharmaceutical form. Oral powder for solution.

Main physicochemical properties: homogeneous crystalline powder, white or almost white, without particle agglomeration, with a characteristic odor.

Pharmacotherapeutic group.

Medicinal products used for cough and colds. Mucolytic agents.

ATC code R05C B01.

Pharmacological properties.

Pharmacodynamics.

AsTaTse is a mucolytic expectorant agent used for liquefying sputum in respiratory tract diseases associated with the production of thick mucus. Acetylcysteine is a derivative of the amino acid cysteine. The mucolytic effect of the drug has a chemical nature. Due to its free sulfhydryl group, acetylcysteine breaks the disulfide bonds of acidic mucopolysaccharides, leading to depolymerization of sputum mucoproteins, reduction of mucus viscosity, and facilitating expectoration and clearance of bronchial secretions. The drug retains its activity in the presence of purulent sputum.

Acetylcysteine also possesses antioxidant pneumoprotective properties, resulting from the binding of chemical radicals by its sulfhydryl groups, thereby neutralizing them. In addition, the drug promotes increased synthesis of glutathione – an important factor in intracellular protection not only against oxidative toxins of exogenous and endogenous origin but also against certain cytotoxic substances. This characteristic of acetylcysteine allows its effective use in paracetamol overdose.

Pharmacokinetics.

After oral administration, acetylcysteine is rapidly and completely absorbed and undergoes hepatic metabolism to form cysteine, a pharmacologically active metabolite, as well as diacetylcysteine, cystine, and subsequently mixed disulfides. Bioavailability is very low – approximately 10%. Maximum plasma concentration is reached within 1–3 hours after administration. Plasma protein binding is approximately 50%. Acetylcysteine is excreted by the kidneys as inactive metabolites (inorganic sulfates, diacetylcysteine).

The elimination half-life is primarily determined by rapid biotransformation in the liver and is approximately 1 hour. In case of impaired liver function, the elimination half-life is prolonged up to 8 hours.

Clinical characteristics.

Indications.

Treatment of acute and chronic diseases of the bronchopulmonary system requiring reduction of sputum viscosity, improvement of its expectoration and clearance.

Contraindications.

Hypersensitivity to acetylcysteine or to any of the excipients. Active peptic ulcer of the stomach or duodenum, hemoptysis, pulmonary hemorrhage, severe exacerbation of bronchial asthma.

Interaction with other medicinal products and other forms of interactions.

Interaction studies have been conducted only in adults.

Concomitant use of acetylcysteine with antitussive agents may increase sputum retention due to suppression of the cough reflex.

When administered simultaneously with antibiotics such as tetracyclines (except doxycycline), ampicillin, amphotericin B, cephalosporins, and aminoglycosides, interaction with the thiol group of acetylcysteine may occur, leading to reduced activity of both agents. Therefore, the interval between administration of these drugs should be at least 2 hours. This does not apply to cefixime and loracarbef.

Activated charcoal reduces the efficacy of acetylcysteine.

It is not recommended to dissolve acetylcysteine in the same glass of water with other medicinal products.

When nitroglycerin and acetylcysteine are taken concomitantly, marked arterial hypotension and significant dilation of temporal arteries have been observed. If simultaneous use of nitroglycerin and acetylcysteine is necessary, patients should be monitored for arterial hypotension, which may be severe, and patients should also be warned about the possibility of headache.

Acetylcysteine reduces the hepatotoxic effect of paracetamol.

A synergistic effect of acetylcysteine with bronchodilators has been reported.

Acetylcysteine can act as a cysteine donor and increase glutathione levels, promoting detoxification of oxygen free radicals and certain toxic substances in the body.

Upon contact with metals or rubber, sulfides with a characteristic odor are formed; therefore, glassware should be used for dissolving the drug.

Effect on laboratory tests

Acetylcysteine may interfere with colorimetric assays for salicylates and with the determination of ketone bodies in urine.

Special precautions for use

There have been isolated reports of severe skin reactions (Stevens-Johnson syndrome and Lyell's syndrome) associated with the use of acetylcysteine. Therefore, if any changes in the skin or mucous membranes occur, the drug should be discontinued immediately and medical advice must be sought regarding further treatment.

The drug should be administered with caution to patients with a history of gastric or duodenal ulcer, especially when concomitantly taking other medications that irritate the gastric mucosa.

Acetylcysteine affects histamine metabolism; therefore, prolonged therapy should not be prescribed to patients with histamine intolerance, as this may lead to symptoms of intolerance (headache, vasomotor rhinitis, itching).

Acetylcysteine should be used with caution in patients with bronchial asthma due to the risk of bronchospasm. When pouring the powder from the sachet into a container during solution preparation, the powder may become airborne and irritate the nasal mucosa, potentially causing reflex bronchospasm. If bronchospasm occurs, acetylcysteine therapy should be discontinued immediately.

Acetylcysteine should be administered with caution to patients with hepatic or renal impairment to avoid accumulation of nitrogen-containing substances in the body.

Use of acetylcysteine, particularly at the beginning of treatment, may cause liquefaction of bronchial secretions and increase their volume, especially in children under 2 years of age. If the patient is unable to effectively expectorate mucus, postural drainage and bronchoaspiration may be required.

A mild sulfurous odor is not indicative of drug deterioration but is characteristic of the active substance.

The product contains sucrose and therefore should not be administered to patients with rare hereditary forms of fructose intolerance, sucrase-isomaltase deficiency, or glucose-galactose malabsorption syndrome.

Information for diabetic patients

One sachet of powder (200 mg acetylcysteine) contains 2.5 g of sucrose (0.21 bread units).

Use during pregnancy or breastfeeding

Acetylcysteine may be used during pregnancy or breastfeeding only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.

Ability to influence reaction rate when driving or operating machinery

Does not affect.

Method of administration and dosage.

For adults and children aged 14 years and older: administer 400–600 mg of acetylcysteine per day, divided into 1–3 doses.

For children aged 6 to 14 years: administer 400–600 mg per day, divided into 2–3 doses.

For children aged 2 to 6 years: administer 200–400 mg per day, divided into 2 doses.

The medication should be taken after meals. The contents of the sachet should be dissolved in ½ glass of water, juice, or cold tea. The solution should be consumed as soon as possible after preparation. In individual cases, due to the presence of the stabilizer – ascorbic acid – in the formulation, the prepared solution may be stored for approximately 2 hours before use. Additional fluid intake enhances the mucolytic effect of the medication.

The duration of treatment for chronic diseases is determined by the physician depending on the nature and course of the disease. For acute uncomplicated conditions, acetylcysteine should be administered for 4–5 days.

Children.

The medication may be used in children aged 2 years and older.

Overdose.

There is insufficient data on cases of overdose with oral administration of acetylcysteine.

Volunteers have taken 11.6 g of acetylcysteine per day for 3 months without experiencing any serious adverse effects. Oral doses of up to 500 mg of acetylcysteine per kg of body weight per day were tolerated without any symptoms of intoxication.

Symptoms: nausea, vomiting, diarrhea. In children, there is a risk of hypersalivation.

Treatment: symptomatic therapy.

Adverse Reactions

The following classification is used to describe the frequency of adverse reactions: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10,000 to < 1/1000), very rare (< 1/10,000).

Cardiovascular system: uncommon – tachycardia, arterial hypotension.

Nervous system: uncommon – headache.

Skin: uncommon – allergic reactions (pruritus, urticaria, exanthema, eczema, rash, angioedema).

Auditory system: uncommon – tinnitus.

Respiratory system: rare – dyspnea, bronchospasm (mainly in patients with bronchial hyperreactivity associated with bronchial asthma), rhinorrhea.

Gastrointestinal tract: uncommon – heartburn, dyspepsia, stomatitis, abdominal pain, nausea, vomiting, diarrhea, unpleasant breath odor.

General disorders: uncommon – fever.

Serious skin reactions (Stevens–Johnson syndrome and Lyell’s syndrome) have been reported. With the use of acetylcysteine, hemorrhages have very rarely been reported, mostly associated with the development of hypersensitivity reactions. Cases of decreased platelet aggregation have been observed, although there is no clinical confirmation. Very rare cases of Quincke's edema (angioedema), facial swelling, anemia, hemorrhage, anaphylactic reactions, or even anaphylactic shock have been reported.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after marketing authorization is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

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

Keep out of reach of children.

Packaging.

10 sachets per cardboard box.

Supply category. Over-the-counter.

Manufacturer.

ASTRAFARM LLC.

Manufacturer's address and location of operations.

6, Kyivska Street, Vyshneve, Buchanskyi district, Kyiv region, 08132, Ukraine.