Erdosteine

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Available since: 2019-09-19

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Clinical Pharmacology

The effectiveness of erdostein is due to the action of active metabolites. The thiol groups of the metabolites cause disruption of the disulfide bridges that bind glycoproteins to one another, which leads to a decrease in the elasticity and viscosity of the sputum. As a result, erdostein enhances and accelerates the release of respiratory pathways from the secret, improves the secretory function of the epithelium and increases the efficiency of mucociliary transport in the upper and lower sections of the respiratory tract.
Erdostein has an antioxidant effect and carries free radicals. In particular, erdostein protects the respiratory tract from the damaging effects of cigarette smoke against alpha-1-antitrypsin inactivation.
Erdostein increases the concentration of immunoglobulin A (IgA) in the mucous membrane of the respiratory tract in patients with chronic obstructive respiratory diseases, and also reduces the inhibitory effect of tobacco smoke on the function of granulocytes.
The effect of erdosteine therapy develops after 3-4 days of treatment. Erdostein per se does not contain free SH-radicals, therefore it does not have a damaging effect on the gastrointestinal tract, and the side effects of the digestive system do not differ from those of placebo.
Pharmacokinetics
Erdostein is rapidly absorbed from the gastrointestinal tract and is metabolized in the liver to three active metabolites, the most important of which is N-thiodiglycolyl-homocysteine (Metabolite 1 or M1). The half-life (T1 / 2) is more than 5 hours. Repeated use of erdostein or food intake does not affect the pharmacokinetic parameters. The maximum concentration (Cmax) in the blood plasma is 3.46 mcg / ml, the time to reach the maximum concentration (Tmax) is 1.48 hours, the area under the concentration-time curve (AUC0-24h) is 12.09.
Erdostein binds to plasma proteins by 64.5%. Excreted in the form of inorganic sulfates through the kidneys and intestines.
In case of abnormal liver function, an increase in indicators is observed: the maximum concentration (Cmax) and the area under the concentration-time curve (AUC).
An increase in the half-life (T1 / 2) is possible with marked impaired liver function.
In renal failure, accumulation of metabolites is possible.

Indications

Diseases of the respiratory tract with the formation of viscous sputum (in complex therapy).

Composition

Excipients: microcrystalline cellulose - 13 mg, povidone (K-30) - 8 mg, magnesium stearate - 3 mg.

Hard gelatin capsules: the body and cap of the capsule - titanium dioxide - 1.3333%, the quinoline yellow dye - 0.9197%, the sunset sunset sunflower yellow - 0.0044%, gelatin - up to 100%.

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Dosage and Administration

1 capsule (300 mg), 2 times a day.
If there is no improvement within 5 days after the start of the use of the drug or if there is a deterioration, you should contact your doctor.

Adverse reactions

The incidence of adverse reactions is according to the WHO classification: very often (≥1 / 10 cases), often (≥1 / 100 and <1/10 cases), infrequently (≥1 / 1000 and <1/100 cases), rarely (≥ 1/10000 and <1/1000 cases) and very rarely (<1/10000 cases), the frequency is unknown.
From the gastrointestinal tract: rarely - heartburn, nausea, diarrhea; very rarely, nausea, epigastric pain, loss or change in taste sensitivity at the beginning of treatment.
On the part of the skin and subcutaneous tissues: rarely - allergic reactions: redness of the skin, edema, eczema; angioedema.
Violations of the respiratory system, chest and mediastinum; very rarely - shortness of breath.

Contraindications

Hypersensitivity to the components that make up the drug.
Children's age up to 18 years.
Liver dysfunction.
Renal failure.
Homocysteinuria (the drug is a source of homocysteine, therefore, disorders of amino acid metabolism are possible in patients on a diet with a reduced content of free methionine).
Pregnancy (I trimester).
Breastfeeding period.
Carefully
The drug should be prescribed with caution to patients with marked violations of the liver; with diseases of the bronchi, accompanied by excessive accumulation of secretions.

Drug interactions

With simultaneous use of erdostein increases the concentration of amoxicillin in the bronchial secretion, which allows for a faster response to therapy compared to amoxicillin monotherapy.

Special instructions

During treatment it is necessary to take a sufficient amount of liquid, which increases the expectorant effect. In cases of impaired motility of the bronchi or with a significant amount of sputum, the use of the drug requires caution, due to the risk of delayed discharge in the respiratory tract and an increased risk of attaching infection or bronchospasm.
Influence on ability to steer vehicles, mechanisms
It does not affect the ability to drive vehicles, mechanisms and engage in other activities that require increased concentration of attention and psychomotor speed.

Overdosage

No cases of overdose have been reported. However, in cases of overdose or in case of accidental use by children, gastric lavage and symptomatic therapy are recommended.