Acetal

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ACETAL

Composition:

Active substance: 1 tablet contains 200 mg of acetylcysteine;

Excipients: tartaric acid, citric acid, aspartame (E 951), sodium saccharin, lactose monohydrate, microcrystalline cellulose, crospovidone, magnesium stearate, polyethylene glycol, colloidal anhydrous silicon dioxide, peppermint oil.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or almost white tablets, round, biconvex, with a mint odor.

Pharmacotherapeutic group. Agents used in cough and colds. Mucolytic agents. Acetylcysteine. ATC code R05C B01.

Pharmacological properties.

Pharmacodynamics. Acetylcysteine is a mucolytic and expectorant agent used to liquefy 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 the presence of a free sulfhydryl group, acetylcysteine breaks the disulfide bonds of acidic mucopolysaccharides, leading to depolymerization of sputum mucoproteins and reduction of mucus viscosity, thus facilitating expectoration and clearance of bronchial secretions. The drug retains its activity in the presence of purulent sputum.

Acetylcysteine also possesses antioxidant and pneumoprotective properties, which are due to 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 chemical detoxification. 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 dithioacetylcysteine, 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, dithioacetylcysteine).

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 sputum expectoration and clearance.

Contraindications. Hypersensitivity to acetylcysteine or to any other components of this drug; gastric and duodenal peptic ulcer in the stage of exacerbation, hemoptysis, pulmonary hemorrhage, diseases of the liver, kidneys, adrenal glands.

Interaction with other medicinal products and other types of interactions. Combination of Acetal with antitussive agents may reduce the cough reflex, promoting dangerous accumulation of sputum; therefore, these drugs should not be used simultaneously.

Acetal is pharmacologically incompatible with antibiotics and proteolytic enzymes. It reduces the absorption of penicillins, cephalosporins, tetracyclines, and aminoglycosides. The interval between their administration should be at least 2 hours. This does not apply to cefixime and loracarbef.

Synergism of acetylcysteine with bronchodilators has been reported. Contact with metals or rubber leads to the formation of sulfides with a characteristic odor. There are data on the enhancement of vasodilatory and antithrombotic effects of nitroglycerin when used concomitantly with acetylcysteine.

Activated charcoal reduces the effectiveness of acetylcysteine.

Concomitant use of nitroglycerin and acetylcysteine may lead to enhanced vasodilating effect of nitroglycerin. If simultaneous administration is necessary, careful monitoring of the patient is required to detect hypotension promptly, which may be severe and may manifest as headache.

Laboratory parameters: administration of acetylcysteine may alter the results of quantitative colorimetric determination of salicylates and urine ketone tests.

Special precautions.

Acetylcysteine should not be used for the treatment of patients with impaired liver or kidney function due to the risk of increased absorption of nitrogenous substances.

Isolated cases of skin reactions, such as Stevens-Johnson syndrome and Lyell's syndrome, have been observed during short-term exposure to acetylcysteine. In the event of other skin or mucous membrane reactions, immediate medical advice must be sought and administration of the drug discontinued.

The drug should be used with caution in patients with bronchial asthma or a history of peptic ulcer disease.

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

Acetylcysteine causes liquefaction of bronchial secretions. If the patient is unable to effectively expectorate sputum, postural drainage and bronchoaspiration are required.

The product contains aspartame, a phenylalanine derivative, which may be dangerous for patients with phenylketonuria.

If a patient has known intolerance to certain sugars, medical advice must be sought before taking this medicinal product.

This medicinal product contains less than 1 mmol (23 mg) of sodium per dose, i.e. essentially "sodium-free".

Use during pregnancy or breastfeeding. Clinical data on the effects of acetylcysteine in pregnant women are limited. There are no data regarding its passage into breast milk. The drug may be prescribed during pregnancy and breastfeeding only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.

Ability to influence reaction rate while driving or operating machinery. Acetylcysteine does not affect the ability to drive or operate machinery.

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 of acetylcysteine per day, divided into 2–3 doses.

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

The medication should be taken after meals. The tablet should be dissolved in a glass of water and consumed as quickly as possible. Additional fluid intake enhances the mucolytic effect of the drug.

The duration of treatment for chronic conditions is determined by the physician depending on the nature and course of the disease. For acute uncomplicated conditions, acetylcysteine should be used for 5–7 days.

Children. The medication is indicated for children aged 2 years and older.

Overdose. There are no data on cases of overdose with oral administration of acetylcysteine.

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

Treatment: symptomatic therapy.

Adverse reactions.

Central nervous system: headache.

Ear and labyrinth disorders: tinnitus.

Respiratory, thoracic and mediastinal disorders: dyspnea, bronchospasm – predominantly in patients with hyperreactive bronchial systems, especially in bronchial asthma.

Gastrointestinal disorders: stomatitis, abdominal pain, nausea, vomiting, diarrhea, heartburn, dyspepsia.

Cardiovascular system: tachycardia, hypotension; cases of bleeding during acetylcysteine use have been reported, sometimes due to hypersensitivity reactions. Various studies have demonstrated reduced platelet aggregation in the presence of acetylcysteine. The clinical significance of these findings has not yet been established.

General disorders: allergic reactions, including pruritus, urticaria, exanthema, bronchospasm, angioneurotic edema, tachycardia, hypotension, flushing, anaphylactic reactions, or even shock. There have also been reports of severe skin reactions such as Stevens-Johnson syndrome and Lyell's syndrome occurring during acetylcysteine treatment. In case of skin or mucous membrane changes, immediate medical advice should be sought and acetylcysteine discontinued.

Shelf life. 2 years.

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

Keep out of reach of children.

Packaging. 200 mg tablets: No. 10 (10×1), No. 20 (10×2) in blisters, packed in a box.

Pharmaceutical category. Over-the-counter.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's address and place of business. Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenka Street, 22.