ESPA-NAC - instructions for use, dose, side effects, contraindications

Excipients: sucrose - 2744.10 mg / 2344.10 mg, flavoring orange - 50.0 mg, silicon dioxide colloid - 3.00 mg, tartaric acid - 2.00 mg, sodium chloride - 0.90 mg.

Description:ABOUTwhite powder of white or almost white color, without agglomerates and foreign particles, with a fruity odor.

Pharmacotherapeutic group:expectorant mucolytic

ATX: & nbsp

S.01.X.A.08 Acetylcysteine

R.05.C.B.01 Acetylcysteine

Pharmacodynamics:

Mucolytic agent, liquefies phlegm, increases its volume, facilitates the departure of phlegm. The effect is related to the ability of free sulfhydryl groups of acetylcysteine to rupture the intra- and intermolecular disulfide bonds of mucopolysaccharide chains, which leads to depolymerization of mucoproteins and a decrease in sputum viscosity (in some cases this leads to a significant increase in sputum volume, which requires aspiration of bronchial contents). Keeps active with purulent sputum. Does not affect immunity.

Increases the secretion of less viscous sialomucins by goblet cells, reduces the adhesion of bacteria to the epithelial cells of the bronchial mucosa.

Stimulates mucous cells of bronchi, the secret of which lyses fibrin.

A similar effect has on the secret formed by inflammatory diseases of the ENT organs.

Has an antioxidant effect due to the presence of SH-group, capable of neutralizing electrophilic oxidative toxins.

Protects alpha-1-antitrypsin (elastase inhibitor) from the inactivating effects of HOC1 - an oxidant produced by myeloperoxidase active phagocytes.

It also has some anti-inflammatory effect (by suppressing the formation of free radicals and active oxygen-containing substances responsible for the development of inflammation in the lung tissue).

It leads to an increased synthesis of glutathione, which explains the detoxification effect of paracetamol poisoning.

With the preventive use of acetylcysteine, there is a decrease in the frequency and severity of exacerbations in patients with chronic bronchitis and cystic fibrosis.

Pharmacokinetics:

Absorption after oral administration is high. Biological accessibility is low - about 10% due to the presence of a pronounced effect of "first passage" through the liver with the formation of a pharmacologically active metabolite - cysteine, as well as diacetylcystine, cystine.

The maximum concentration level (C_m_Oh) in plasma after oral administration is achieved after about 1-3 hours. Binding to plasma proteins is about 50%. It is mainly excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcystine), a small part is released unchanged with a fecal mass. The half-life (T₁_/₂) of acetylcysteine from the plasma is about 1 hour. If the liver function is violated, this value increases to 8 hours.

It penetrates the placental barrier, accumulates in the amniotic fluid.

Data on penetration through the blood-brain barrier are absent.

Indications:

Diseases of the respiratory system, accompanied by the formation of viscous hard-to-recover sputum:

- acute and chronic bronchitis, obstructive bronchitis;

- tracheitis, laryngotracheitis;

- pneumonia;

- bronchiectasis, bronchial asthma, chronic obstructive pulmonary disease (COPD), bronchiolitis;

- cystic fibrosis.

Acute and chronic sinusitis, inflammation of the middle ear (otitis media).

Contraindications:

- Hypersensitivity to acetylcysteine or other components of the drug;

- peptic ulcer of the stomach and duodenum in the stage of exacerbation;

- hemoptysis, pulmonary hemorrhage;

- deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption (the preparation contains sucrose);

- pregnancy;

- lactation period;

- children under 14 years of age (for a dosage of 600 mg), children under 2 years of age (for a dosage of 200 mg).

Carefully:

Peptic ulcer and duodenal ulcer in the anamnesis, varicose veins of the esophagus, bronchial asthma, obstructive bronchitis, adrenal diseases, hepatic and / or renal failure, arterial hypertension, histamine intolerance. acetylcysteine affects the metabolism of histamine and can lead to signs of intolerance, such as headache, vasomotor rhinitis, itching).

Pregnancy and lactation:

Data on the use of acetylcysteine during pregnancy and breastfeeding are limited, so the use of the drug in pregnancy is contraindicated.

If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be resolved.

Dosing and Administration:

In the absence of other appointments, the following recommendations should be adhered to. The powder is dissolved in 1 glass of hot water, taken orally after a meal.

ESPA-NAC® in a dosage of 200 mg:

Adults and children over 14 years of age: 2-3 times a day for 1 packet (400-600 mg).

Children from 6 to 14 years old: 2 times a day for 1 packet (400 mg).

Children from 2 to 6 years old: 2-3 times a day for half a packet (200-300 mg).

In cystic fibrosis:

Children from 2 to 6 years old: 2 times a day for 1 packet (400 mg).

Children over 6 years old: 3 times a day for 1 packet (600 mg).

ESPA-NAC® in a dosage of 600 mg:

Adults and children over 14 years of age: 1 time per day for 1 packet (600 mg).

In cystic fibrosis:

Children over 6 years old: 1 time per day for 1 packet (600 mg).

Additional fluid intake enhances the mucolytic effect of the drug.

With short-term catarrhal diseases, the duration of admission is 5-7 days. For chronic bronchitis and cystic fibrosis, the drug should be taken for a longer time to prevent infections. For long-term illnesses, the duration of therapy is determined by the attending physician.

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); frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

From the side of the cardiovascular system:

rarely - lowering blood pressure, increasing heart rate (tachycardia).

From the respiratory system:

rarely - development of pulmonary hemorrhage, as a manifestation of the reaction of hypersensitivity.

Allergic reactions:

rarely - bronchospasm (mainly in patients with a hyperreactive bronchial system with bronchial asthma), skin rash, itching and urticaria, exanthema, angioedevritic edema;

rarely - Anaphylactic reactions up to the development of anaphylactic shock, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the gastrointestinal tract:

rarely - stomatitis, abdominal pain, nausea, vomiting and diarrhea, heartburn, indigestion.

From the sense organs:

infrequently - noise in ears.

Other:

rarely - headache, fever, isolated reports of bleeding due to the presence of hypersensitivity reactions, decreased platelet aggregation.

Overdose:

With oral administration of acetylcysteine for three months in a daily dose of up to 11.6 g there were no life-threatening side effects. With oral administration of acetylcysteine in a dose of up to 500 mg / kg body weight, no poisoning phenomena were observed.

Symptoms: heartburn and nausea, vomiting, diarrhea, stomach pain. Newborns are at risk of developing hypersecretion.

Treatment: symptomatic.

Interaction:

With the simultaneous use of acetylcysteine and antitussives stagnation of mucus can occur due to the suppression of the cough reflex.

Concurrent administration of acetylcysteine with vasodilating agents and nitroglycerin may lead to an increase in the vasodilator effect of the latter.

Pharmaceutically incompatible with antibiotics (penicillins, cephalosporins, erythromycin, tetracycline and amphotericin B) and proteolytic enzymes.

Reduces the absorption of penicillins, cephalosporins, tetracycline (they should be taken no earlier than 2 hours after ingestion of acetylcysteine).

Special instructions:

Patients with bronchial asthma and obstructive bronchitis acetylcysteine should be administered with caution under the systematic control of bronchial patency.

When dissolving the drug, it is necessary to use glassware, avoid contact with metals, rubber (with contact formed sulfides with a characteristic odor), oxygen, easily oxidizable substances.

When treating patients with diabetes should take into account that the preparation contains sucrose (in one bag 200/600 mg contains 0.23 / 0.20 XE, respectively).

In patients with severe skin lesions - Stevens-Johnson syndrome or Lyell's syndrome - in the early phase, fever, body pain, rhinitis, cough and sore throat may appear. With symptomatic treatment, the misdirected use of mucolytic agents is possible. There are single reports (<1/10000) on the detection of Stevens-Johnson syndrome and Lyell's syndrome, coinciding with the appointment of the drug; but there is no causal relationship with taking the drug. With the development of the above syndromes (sudden appearance of rashes and spots on the face and trunk, which later can spread to other parts of the body), it is recommended to stop treatment and immediately seek medical help.

Effect on the ability to drive transp. cf. and fur:

In therapeutic doses does not affect the ability to drive vehicles and mechanisms.

Form release / dosage:

Powder for solution for oral administration, 200 mg and 600 mg.

Packaging:

By 3.0 g of powder in a bag of three-layer material (paper-aluminum-polyethylene).

20 bags with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003896

Date of registration:11.10.2016

Expiration Date:11.10.2021

The owner of the registration certificate:Esparma GmbHEsparma GmbH Germany

Manufacturer: & nbsp

LINDOPHARM, GmbH Germany

Representation: & nbspESPARMA GmbH ESPARMA GmbH Germany

Information update date: & nbsp27.10.2016

Illustrated instructions

Instructions

ESPA-NATS® (ESPA-NATS®)