Description
Release form
effervescent tablets.
Packing
6 pcs 600 mg
Pharmacological action
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
Absorption is high. It is rapidly metabolized in the liver with the formation of a pharmacologically active metabolite – cysteine, as well as diacetylcysteine, cystine and mixed disulfides. The bioavailability of the oral route of administration is 10% (due to the presence of a pronounced effect of “first passage” through the liver).
Time to reach maximum concentration (Cmax) in blood plasma is 1-3 hours. Communication with plasma proteins is 50%. It is excreted 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.
Crosses 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: acute and chronic bronchitis, obstructive bronchitis
tracheitis, laryngotracheitis
pneumonia
lung abscess bronchitis bronchitis, bronchitis obstructive disease 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 14 years (for this dosage form).
Caution: history of gastric and duodenal ulcer, history of arterial hypertension, bronchial asthma, obstructive bronchitis, liver and / or renal failure, histamine intolerance (long-term use of the drug should be avoided, since acetylcysteine affects histamine metabolism and can lead to signs of intolerance such as headache, vasomotor rhinitis, pruritus), varicose veins of the esophagus, adrenal disease.
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 it is necessary to use the drug during breastfeeding, the issue of its discontinuation should be resolved.
Composition
1 sachet contains: active ingredient:
acetylcysteine – 600.0 mg
excipients:
sucrose – 2045.0 mg
ascorbic acid – 75.0 mg
sodium saccharin – 20.0 mg
flavor lemon , 0 mg
honey flavor – 130.0 mg.
Dosage and Administration
Inside, after meals.
The powder is dissolved in 1 cup (150-200 ml) of hot, but not boiling, water. The resulting solution was stirred and drunk hot. The temperature should be acceptable for drinking. The prepared solution must be consumed immediately after preparation. 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 long-term illnesses, 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 preventive effect in infections.
Unless otherwise prescribed, the following dosages are recommended:
Mucolytic therapy:
adults and adolescents over 14 years of age: 1 sachet (600 mg) 1 time per day.
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, <1/10), infrequently ( 1/1000, <1/100), rarely ( 1/10000, <1/1000) and very rarely (<1/10000) the frequency is unknown (the frequency of occurrence of phenomena cannot be determined based on available data). Immune system disorders infrequent: hypersensitivity reactions are very rare: anaphylactic / anaphylactoid reactions up to shock. Disorders of the skin and subcutaneous tissue infrequently: skin itching, rash, exanthema, urticaria, angioedema is very rare: Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). Disorders of the heart and blood vessels infrequently: lowering blood pressure, tachycardia is very rare: bleeding. From the respiratory system, chest and mediastinal organs rarely: shortness of breath, bronchospasm (mainly in patients with bronchial hyperreactivity in asthma). Disorders of the gastrointestinal tract infrequently: abdominal pain, nausea, vomiting, diarrhea rarely: dyspepsia. Hearing impairment and labyrinthine disorders infrequently: tinnitus. Common disorders infrequently: headache, fever frequency unknown: swelling of the face, decreased platelet aggregation. Drug Interaction When acetylcysteine and antitussives are used at the same time, phlegm stagnation 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 There are no cases of toxic overdose with acetylcysteine. There were no symptoms of intoxication when administered acetylcysteine at a dose of 500 mg / kg body weight. There were no severe adverse events when taken by healthy volunteers of acetylcysteine at a dose of 11.6 g per day for 3 months. 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 out of the reach of children, in a dry, dark place at a temperature not exceeding 30 ° C. After taking the pill, close the tube tightly. Expiration 3 years. Deystvuyuschee substances acetylcysteine pharmacies over-the-counter conditions form Dosage form oral solution sandoz, switzerland
