Description
Latin name
ACC
Release form
Granules for oral solution.
Packaging
20 sachets.
Pharmacological action of
PHARMACODYNAMICS
Acetylcysteine is a derivative of the amino acid cysteine. It has a mucolytic effect, facilitates sputum discharge due to a direct effect on the rheological properties of sputum. The action is due to the ability to break the disulfide bonds of mucopolysaccharide chains and cause depolymerization of mucoproteins of sputum, which leads to a decrease in the viscosity of sputum.
The drug remains active in the presence of purulent sputum. It has an antioxidant effect, based on the ability of its reactive sulfhydryl groups (SH-groups) to bind to oxidative radicals and, thus, neutralize them. In addition, acetylcysteine promotes the synthesis of glutathione, an important component of the antioxidant system and chemical detoxification of the body.
The antioxidant effect of acetylcysteine increases the protection of cells from the damaging effects of free radical oxidation, which is characteristic of an intense inflammatory reaction. With the prophylactic use of acetylcysteine, there is a decrease in the frequency and severity of exacerbations of bacterial etiology in patients with chronic bronchitis and cystic fibrosis.
PHARMACOKINETICS
High absorption is rapidly metabolized in the liver with the formation of a pharmacologically active metabolite – cysteine, as well as diacetylcysteine, cystine and mixed disulfides. Oral bioavailability is 10% (due to the presence of a pronounced effect of “first passage” through the liver). The time to reach maximum concentration (Cmax) in blood plasma is 1-3 hours.
Communication with plasma proteins – 50%. It is excreted mainly by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine). The half-life (T1 / 2) is about 1 hour, impaired liver function leads to an extension of T1 / 2 to 8 hours. Penetrates through the placental barrier. Data on the ability of acetylcysteine to cross the blood-brain barrier and excreted in breast milk are not available.
Indications
Respiratory diseases accompanied by the formation of viscous hard sputum:
² Ñ acute and chronic bronchitis, obstructive bronchitis
² Ñ tracheitis, laryngotracheitis
² Ñ pneumonia, bronchitis, bronchitis, bronchitis cystic fibrosis
Acute and chronic sinusitis, inflammation of the middle ear (otitis media).
Contraindications
Hypersensitivity to acetylcysteine or other components of the
preparation gastric and duodenal ulcer in the acute stage
hemoptysis, pulmonary hemorrhage
intolerance to pregnancy 6 years (for this dosage form).
Precautions: a history of gastric and duodenal ulcer, hypertension, bronchial asthma, obstructive bronchitis, liver and / or renal failure, histamine intolerance (long-term use of the drug should be avoided, since acetylcysteine affects the histamine metabolism and can lead to signs of intolerance, such as headache, vasomotor rhinitis, pruritus), varicose veins of the esophagus, diseases adrenal glands.
Use during pregnancy and lactation
Data on the use of acetylcysteine during pregnancy and breastfeeding are limited, so the use of the drug during pregnancy is contraindicated.
If you need to use the drug during lactation, you should decide on the termination of breastfeeding.
Composition
1 sachet contains: active ingredient:
acetylcysteine – 200.0 mg
excipients: sucrose – 2507.0 mg
ascorbic acid – 25.0 mg
sodium saccharin – 8.0 mg
lemon flavor – 130, 0 mg
honey flavor – 130.0 mg.
Dosage and Administration
Inside, after meals. The granules are dissolved by stirring in 1 cup of hot water. The resulting solution is drunk hot. If necessary, the prepared solution can be left for 3 hours. An additional intake of fluid enhances the mucolytic effect of the drug. For short-term colds, the duration of the course is 5 7 days. With prolonged instructions for the use of the drug for the medical use of ACC ® diseases, the course of therapy is determined by the attending physician. In chronic bronchitis and cystic fibrosis, the drug should be taken for a longer time to achieve a prophylactic effect in
infections. MUKOLITIC THERAPY
adults and adolescents over 14 years of age: 1 sachet 2? 3 times a day (400 – 600 mg)
children from 6 to 14 years: 1 sachet 2 times a day (400 mg).
cystic fibrosis
adults and children weighing? 30 kg: if necessary, the daily dose can be increased to 800 mg per day.
children over 6 years of age: 1 sachet 3 times a day (600 mg).
Side effects
According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often ( 1/10), often ( 1/100, Allergic reactions: infrequently: skin itching, rash , exanthema, urticaria, angioedema, lowering blood pressure,
tachycardia is very rare: anaphylactic reactions up to anaphylactic shock, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome)
From the respiratory Istemi: rare: shortness of breath, bronchospasm (mainly in patients with bronchial hyperreactivity in asthma).
From the gastrointestinal tract: infrequently: stomatitis, abdominal pain, nausea, vomiting, diarrhea, heartburn, dyspepsia.
From the sensory organs: infrequently: tinnitus.
Other: very rare: headache, fever, isolated reports of the development of bleeding due to the presence of a hypersensitivity reaction, decreased platelet aggregation.
Drug Interaction
When acetylcysteine and antitussives are used concurrently, sputum stasis may occur due to cough reflex suppression.
When used in conjunction with antibiotics for oral administration (penicillins, tetracyclines, cephalosporins, etc.), their interaction with the thiol group of acetylcysteine may occur, which may lead to a decrease in their antibacterial activity. Therefore, the interval between the administration of antibiotics and acetylcysteine should be at least 2 h (except cefixime and loracarb).
Concomitant administration with vasodilating agents and nitroglycerin may lead to increased vasodilator action.
Overdose
Acetylcysteine, when taken at doses of 500 mg / kg / day, does not cause signs and symptoms of overdose. In the event of an erroneous or deliberate overdose, phenomena such as diarrhea, vomiting, stomach pain, heartburn and nausea are observed. Treatment: symptomatic
Storage conditions
The drug should be stored in a dry place inaccessible to children at a temperature not exceeding 25 ° C.
Expiration
3 years.
Deystvuyuschee substances
acetylcysteine
Sandoz, Switzerland