Pharmacodynamics
Efficiency is due to the action of active metabolites. Thiol groups of metabolites cause the rupture of disulfide bridges that bind glycoprotein fibers, which leads to a decrease in the elasticity and viscosity of sputum. As a result, erdostein enhances and accelerates the release of secretions from the respiratory tract, improves the secretory function of the epithelium and increases the efficiency of mucociliary transport in the upper and lower parts of the respiratory tract.
Locally, Erdostein, through amine groups, has an antagonistic effect on oxygen free radicals and prevents the suppression of alpha-1-antitrypsin in tobacco smokers, thereby reducing the damaging effects of tobacco smoke in chronic smokers.
Erdostein increases the concentration of IgA in the mucous membrane of the respiratory tract in patients with chronic obstructive airway diseases, and also reduces the inhibitory effect of tobacco smoke on granulocyte function. When used together, erdosteine increases the concentration of amoxicillin in bronchial secretions, which allows for a faster response to therapy compared to amoxicillin monotherapy.
The effect of drug therapy develops on days 3–4 of treatment. Erdostein, as such, does not contain free SH radicals. Therefore, the drug does not have a damaging effect on the gastrointestinal tract, and side effects from the digestive system do not differ from the effects of placebo.
Pharmacological properties of the drug Erdostein
Efficiency is due to the action of active metabolites. Thiol groups of metabolites cause the rupture of disulfide bridges that bind glycoprotein fibers, which leads to a decrease in sputum viscosity. As a result, erdostein accelerates the release of secretions from the respiratory tract, improves the secretory function of the epithelium and increases the efficiency of mucociliary transport in the upper and lower parts of the respiratory tract. Locally, Erdostein, through amine groups, has an antagonistic effect on oxygen free radicals and prevents the suppression of α1-antitrypsin in tobacco smokers, thereby reducing the damaging effects of tobacco smoke in chronic smokers. Erdostein increases the concentration of IgA in the mucous membrane of the respiratory tract in patients with obstructive airway diseases, and also reduces the inhibitory effect of tobacco smoke on the functions of granulocytes. When used together, erdosteine increases the concentration of amoxicillin in bronchial secretions, which allows for a faster response to therapy compared to amoxicillin monotherapy. The effect of drug therapy develops on the 3rd–4th day of treatment. Erdostein does not contain free SH-radicals, so the drug does not have a damaging effect on the gastrointestinal tract and side effects from the digestive system do not differ from the effects of placebo. It is rapidly absorbed in the gastrointestinal tract and metabolized in the liver to 3 active metabolites, the most important of which is N-thiodiglycol-yl-homocysteine (metabolite 1 or M1). The half-life is more than 5 hours. Repeated use does not affect the pharmacokinetic parameters. The maximum concentration in blood plasma is 3.46 mcg/ml and is achieved within 1.48 hours; AUC (0-24 hours) - 12.09. 64.5% of erdosteine binds to blood plasma proteins. The drug is excreted in the form of inorganic sulfates through the kidneys and feces. In case of liver dysfunction, an increase in maximum plasma concentration and AUC is observed. The half-life may be prolonged in cases of severe liver dysfunction. In case of renal failure, accumulation of metabolites is possible.
Pharmacokinetics
It is rapidly absorbed in the gastrointestinal tract and metabolized in the liver to 3 active metabolites, the most important of which is N-thiodiglycolyl-homocysteine (metabolite 1 or M1). T1/2 - more than 5 hours. Repeated use does not affect the pharmacokinetic parameters. Cmax - 3.46 µg/ml; Tmax - 1.48 hours; AUC (0-24 hours) - 12.09. 64.5% of erdosteine binds to blood plasma proteins. The drug is excreted in the form of inorganic sulfates through the kidneys and intestines.
In case of liver dysfunction, an increase in Cmax and AUC is observed. An increase in T1/2 is possible with severe liver dysfunction. In case of renal failure, accumulation of metabolites is possible.
Indications for the drug Erdostin
The drug is indicated for the treatment of adults, adolescents and children weighing more than 15 kg in the following cases:
acute inflammatory diseases of the respiratory tract: laryngopharyngitis, acute bronchitis;
rhinitis, sinusitis;
exacerbations of chronic respiratory diseases: chronic bronchitis, COPD, hypersecretory asthma, bronchiectasis, chronic bronchitis of smokers (including seasonal exacerbations);
complex therapy (with antibiotics): exacerbation of bronchitis of bacterial etiology;
prevention of pneumonia and partial atelectasis after surgery.
Interactions of the drug Erdostein
Erdosteine may be used with antibiotics such as amoxicillin or clarithromycin. In clinical trials, the administration of erdosteine with these antibacterial drugs during exacerbation of chronic bronchitis led to an increase in the concentration of antibiotics in sputum and a more rapid disappearance of clinical symptoms compared with placebo. However, when used simultaneously with tetracyclines (except for doxycycline), ampicillin or amphotericin B, a mutual decrease in the effectiveness of the drugs due to competition for the thiol group is possible. Therefore, the interval between the administration of these drugs should be at least 2 hours. Erdosteine should not be used simultaneously with drugs that inhibit the cough reflex: due to the possibility of reducing the excretion of infected sputum. When treating BA, combination with bronchodilators is advisable.
Contraindications
hypersensitivity to ingredients contained in the drug containing free SH radicals;
liver dysfunction;
renal failure (Cl creatinine <25 ml/min);
homocystinuria (the drug is a source of homocysteine, therefore, disturbances in amino acid metabolism are possible in patients on a diet with a reduced content of free methionine);
phenylketonuria (for granules for preparing a suspension and solution, since they contain aspartame);
pregnancy (first trimester);
children's age (up to 2 years).
Carefully:
irrational use with antitussive therapy (possible accumulation of liquid secretions in the bronchi and increased risk of developing superinfection or bronchospasm);
renal failure (accumulation of metabolites is possible);
severe liver dysfunction (possible increase in T1/2).
Special instructions for the use of the drug Erdostein
If used irrationally with antitussive therapy, liquid secretions may accumulate in the bronchi and increase the risk of superinfection or bronchospasm. If the symptoms of the disease do not decrease within 5 days from the start of taking the drug or if the patient becomes worse, you should consult your doctor for advice on the advisability of further treatment. During pregnancy and breastfeeding. Experimental studies did not reveal embryotoxic effects. However, experience with the use of the drug during pregnancy and breastfeeding is limited, so the use of the drug during pregnancy (especially in the first trimester) and breastfeeding should be carried out only according to strict indications. The drug does not have any effect on the ability to drive vehicles or use other machinery.
Directions for use and doses
Inside.
For adults.
Capsules - 1 capsule. (300 mg) 2-3 times a day.
Granules for the preparation of a suspension for oral administration - 8.5 ml (300 mg) 2 times a day. Dosage per body weight: 10 mg/kg body weight 2 times a day.
Granules for preparing a solution for oral administration - 1 sachet (225 mg) 2-3 times a day.
For children.
The recommended form is granules for the preparation of a suspension for oral administration. The dosage regimen is determined based on body weight and age as follows:
15–20 kg (from 3 to 6 years) - 2.5 ml 2 times a day;
21–30 kg (from 7 to 12 years) - 5 ml 2 times a day;
over 30 kg (over 12 years) - 5 ml 3 times a day.
Cooking method
Granules for preparing the suspension:
Fill the contents of the bottle (dry granulate) with water up to the special mark. Shake thoroughly until a homogeneous suspension is formed. Check the level of contents in the bottle and (if necessary) add water and shake the bottle again. The prepared suspension can be used for a maximum of 10 days if stored in the refrigerator at a temperature of 2–8 °C.
Shake before each use.
Granules for the preparation of solution for oral administration:
The contents of the sachet are dissolved in a glass of water or tea and taken orally.
Erdomed, 300 mg, capsules, 10 pcs.
Directions for use and dosage regimen
Capsules, granules for suspension and granules for oral solution are taken orally.
Adults
Capsules: 1 capsule (300 mg) 2 – 3 times a day;
Granules for oral suspension: 8.5 ml (300 mg) twice a day. Dosage per body weight: 10 mg/kg body weight twice daily;
Granules for preparing a solution for oral administration: 1 sachet (225 mg) 2 – 3 times a day.
Children
The recommended dosage form for children is granules for oral suspension: the dosage regimen is determined based on body weight and age as follows:
15 – 20 kg (ages 3 to 6 years): 2.5 ml twice a day;
21 – 30 kg (ages 7 to 12 years): 5 ml twice a day;
over 30 kg (age over 12 years): 5 ml three times a day.
Precautionary measures
If your symptoms do not improve within 5 days after starting to use the drug, or if you feel worse, contact your doctor about the advisability of further treatment.
Side effects
In rare cases, side effects from the gastrointestinal tract may occur: heartburn, nausea, and rarely, diarrhea. Very rarely, at the beginning of treatment, loss or change in taste sensitivity is possible.
In rare cases, allergic reactions are possible: redness of the skin, urticaria,
Overdose symptoms and treatment methods
No cases of drug overdose have been reported. However, in cases of overdose or accidental use by children, symptomatic therapy is recommended.
Interaction with other drugs:
When used together, Erdostein increases the concentration of ampicillin in bronchial secretions.
special instructions
Use during pregnancy and lactation: Preclinical studies did not reveal embryotoxic effects. However, experience with the use of the drug during pregnancy and breastfeeding is limited. Therefore, the use of the drug during pregnancy, especially in the first trimester, and lactation should be carried out only according to strict indications.
Impact on the ability to drive a car or use other machinery:
The drug does not have any effect on the ability to drive a car or use other machinery.
Release form:
Capsules: 10 capsules in a blister made of PVC/PVDC film and aluminum foil; 1 blister with instructions in a cardboard box.
Granules for the preparation of a suspension for oral administration: bottles of 100 and 200 ml of brown transparent glass with an aluminum cap with protection and a measuring cup; 1 bottle with instructions in a cardboard box.
Granules for the preparation of solution for oral administration: 4.425 mg in a sachet (paper/aluminum/polyethylene). 20 sachets along with instructions in a cardboard box.
Storage conditions:
Store at temperatures below 25?C.
Keep out of the reach of children!
The finished suspension should be stored in the refrigerator at a temperature of 2-8°C.
Best before date:
— Capsules — 4 years;
— Granules for the preparation of suspension for oral administration — 3 years,
the finished suspension can be used for 10 days,
— Granules for the preparation of a solution for oral administration — 3 years.
Do not use after the expiration date indicated on the pack.
Conditions for dispensing from pharmacies:
On prescription.
Produced
Medicom International s.r.o., Czech Republic, produced by Edmond Pharma S.r.l., Italy
“Medicom International sro”, Czech Republic, manufactured by
Edmond Pharma Srl, Italy
Address: Paterni 7, 635 00 Brno, Czech Republic/Czech Republic, 635 00 Brno, st. Paterzhni 7.
Address of the representative office in Moscow: 115478, Kashirskoe shosse, 24, House of Scientists of the Russian Academy of Medical Sciences, 2nd floor, room A.
Tel., 324 96 40
Fax, 324 55 08
And about. Director of IDKELS A.N. Vasiliev
Company representative: L.A. Makhotina
