Acetal

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ACETAL

Composition:

Active substance: 1 tablet contains acetylcysteine 600 mg;

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 elongated tablets with a biconvex surface, marked with a line, having a mint odor.

Pharmacotherapeutic group. Medicinal products used for cough and colds. Mucolytic agents. Acetylcysteine. ATC code R05CB01.

Pharmacological properties.

Pharmacodynamics. Acetylcysteine is a mucolytic and expectorant agent used to liquefy sputum in respiratory 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 cleaves disulfide bonds of acidic mucopolysaccharides, leading to depolymerization of sputum mucoproteins and reduction of mucus viscosity, thus facilitating expectoration and elimination 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—a key 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 cases of impaired liver function, the elimination half-life is prolonged to 8 hours.

Clinical characteristics.

Indications. Treatment of acute and chronic diseases of the bronchopulmonary system that require 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, and 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 between acetylcysteine and bronchodilators has been observed. Contact with metals or rubber produces sulfides with a characteristic odor. Data indicate enhancement of the 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 enhance the vasodilatory effect of nitroglycerin. If simultaneous administration is necessary, careful monitoring of the patient is required to promptly detect hypotension, which may be severe and may manifest as headache.

Laboratory parameters: administration of acetylcysteine may alter results of quantitative colorimetric determination of salicylates and tests for urinary ketones.

Special precautions for use.

Acetylcysteine should not be used for the treatment of patients with impaired liver or kidney function to prevent 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, seek immediate medical advice and discontinue the drug.

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 provoke symptoms of intolerance (headache, vasomotor rhinitis, pruritus).

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 the patient has known intolerance to certain sugars, consult a physician before taking this medicinal product.

This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e., it is practically 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 speed while driving or operating machinery. Acetylcysteine does not affect the ability to drive or operate machinery.

Dosage and Administration.

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

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

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

Treatment: symptomatic treatment.

Adverse reactions.

Central and peripheral nervous system disorders: headache.

Aural and labyrinth disorders: tinnitus.

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

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

Cardiovascular disorders: tachycardia, hypotension; there have been reports of bleeding during acetylcysteine use, 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, collapse, anaphylactic reactions, or even shock. There are also reports of severe skin reactions such as Stevens-Johnson syndrome and Lyell’s syndrome occurring during acetylcysteine treatment. If any skin or mucosal changes occur, medical advice should be sought immediately 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. 600 mg tablets: № 10 (10×1), № 20 (10×2) in blisters, in a carton box.

Prescription status. Over-the-counter.

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

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