Fluimucil, 600 mg 10 pcs

Fluimucil liquefies sputum. The presence of sulfhydryl groups in the structure of acetylcysteine helps to break disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolymerization of mucoproteins and to reduction of mucus viscosity. The drug retains activity in the presence of purulent sputum.

Acetylcysteine has an antioxidant effect due to the presence of the nucleophilic thiol SH-group, which easily gives off hydrogen, neutralizing oxidizing radicals.

Pharmacodynamics

The prophylactic use of acetylcysteine reduces the frequency and severity of exacerbations in patients with chronic bronchitis and cystic fibrosis. The protective mechanism of acetylcysteine is based on the ability of its reactive sulfhydryl groups to bind chemical radicals.

Acetylcysteine readily penetrates the cell, is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant, cytoprotector, trapping endogenous and exogenous free radicals and toxins.

Acetylcysteine prevents depletion and promotes the synthesis of intracellular glutathione, participating in the redox processes of cells, thus contributing to the detoxification of harmful substances. This explains the action of acetylcysteine as an antidote in paracetamol poisoning.

Pharmacokinetics

Fluimucil is well absorbed when taken orally. It is immediately deacetylated to cysteine in the liver. In the blood there is a dynamic equilibrium of free and bound to plasma proteins acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine). Because of the high “first pass” effect through the liver, the bioavailability of acetylcysteine is about 10%. Acetylcysteine penetrates into the intercellular space, predominantly distributed in the liver, kidneys, lungs, bronchial secretion.

After oral administration of 600 mg of acetylcysteine in healthy volunteers, Cmax in plasma is reached after approximately 1 hour and is 15 mmol/L. T1/2 from plasma is 2 hours. Acetylcysteine and its metabolites are excreted mainly by the kidneys.

Indications

Mucolytic agent for the treatment of acute and chronic respiratory diseases associated with excessive secretion of bronchial secretions: bronchitis, tracheitis, bronchiolitis, pneumonia, bronchiectasis, cystic fibrosis, lung abscess, pulmonary emphysema, laryngotracheitis, interstitial lung diseases, pulmonary atelectasis (due to blockage of the bronchi by mucus plug).

Catarrhal and purulent otitis, sinusitis, sinusitis (facilitation of secretion).

Removal of viscous secretions from the respiratory tract in post-traumatic and postoperative conditions.

Pharmacological effect

Pharmacotherapeutic group.

Expectorant mucolytic agent.

ATX code:

R05CB01.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics

A mucolytic agent that thins sputum, increases its volume, and facilitates the separation of sputum. The action is associated with the ability of free sulfhydryl groups of acetylcysteine ​​to break intra- and intermolecular disulfide bonds of acidic mucopolysaccharides of sputum, which leads to depolymerization of mucoproteins and a decrease in sputum viscosity.

In addition, it reduces induced hyperplasia of mucoid cells, enhances the production of surfactants by stimulating type II pneumocytes, and stimulates mucociliary activity, which leads to improved mucociliary clearance.

Remains active against purulent sputum, mucopurulent and mucous sputum.

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 the bronchi, the secretion of which is lysed by fibrin. It has a similar effect on the secretions formed during inflammatory diseases of the ENT organs. It has an antioxidant effect due to the presence of an SH group that can neutralize electrophilic oxidative toxins. Acetylcysteine ​​easily penetrates into the cell and is deacetylated to L-cysteine, from which intracellular glutathione is synthesized. Glutathione is a highly reactive tripeptide, a powerful antioxidant, cytoprotector that traps endogenous and exogenous free radicals and toxins. Acetylcysteine ​​prevents exhaustion and helps increase the synthesis of intracellular glutathione, which is involved in the redox processes of cells, thus promoting the detoxification of harmful substances. This explains the effect of acetylcysteine ​​as an antidote for paracetamol poisoning. Paracetamol exerts its cytotoxic effect through the progressive depletion of glutathione. The main role of acetylcysteine ​​is to maintain proper levels of glutathione concentration, thereby providing protection to cells.

Protects alpha1-antitrypsin (elastase inhibitor) from the inactivating effects of HOCl, an oxidizing agent produced by myeloperoxidase of active phagocytes. It also has an anti-inflammatory effect (by suppressing the formation of free radicals and reactive oxygen-containing substances responsible for the development of inflammation in the lung tissue).

Pharmacokinetics

Fluimucil is well absorbed when taken orally. It is immediately deacetylated to cysteine ​​in the liver. In the blood, a mobile equilibrium of free acetylcysteine ​​and its metabolites (cysteine, cystine, diacetylcysteine) is observed, free and bound to plasma proteins. Due to the high “first pass” effect through the liver, the bioavailability of acetylcysteine ​​is about 10%. Acetylcysteine ​​penetrates into the intercellular space and is predominantly distributed in the liver, kidneys, lungs, and bronchial secretions.

The maximum concentration in plasma is reached 1-3 hours after oral administration and is 15 mmol/l, binding to plasma proteins is 50%.

T1/2 is about 1 hour, with liver cirrhosis it increases to 8 hours. It is excreted by the kidneys in the form of inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestines. Penetrates through the placental barrier.

Special instructions

For patients with bronchial asthma and obstructive bronchitis, acetylcysteine ​​should be prescribed with caution under systematic monitoring of bronchial patency.

The drug contains aspartame, its use is contraindicated in patients with phenylketonuria.
There are no restrictions for use in diabetes mellitus, impaired glucose tolerance, metabolic syndrome,
obesity.

The presence of a slight sulfuric odor is the characteristic odor of the active substance.

When dissolving acetylcysteine, you must use glass containers and avoid contact with metal and rubber surfaces.

Acetylcysteine ​​may have a slight effect on histamine metabolism, so caution must be exercised when using the drug for long-term treatment of patients suffering from histamine intolerance when symptoms of intolerance occur (headache, vasomotor rhinitis, itching).

Active ingredient

Acetylcysteine

Composition

One tablet contains:

Active substance:

Acetylcysteine ​​600 mg;

Excipients:

Citric acid 680 mg,

sodium bicarbonate 500 mg,

aspartame 20 mg,

lemon flavor 100 mg.

Pregnancy

The drug is prescribed during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Contraindications

Hypersensitivity to acetylcysteine, peptic ulcer of the stomach and duodenum in the acute stage, phenylketonuria, children under 18 years of age, lactation period.

With caution – Peptic ulcer of the stomach and duodenum, varicose veins of the esophagus, hemoptysis, pulmonary hemorrhage, bronchial asthma, diseases of the adrenal glands, liver and/or kidney failure, arterial hypertension.

Side Effects

The table below lists adverse reactions by organ system class and frequency of occurrence (very common (>1/10), common (>1/100 to 1/1000 to 1/10000 to <1/1000), very rare (<1/10000) and unknown (not estimable based on available data).
For each frequency group, adverse events are presented in order of decreasing severity.

System-organ class

Adverse reactions

Uncommon

(>1/1000 – <1/100)

Rarely

(< 1/ 10000 - < 1/ 1000)

Very rare (< 1/10000)

Not known

Immune system disorders

Hypersensitivity

Anaphylactic shock,

anaphylactic/anaphylactoid reaction

Nervous system disorders

Headache

Hearing and inner ear disorders

Tinnitus

Heart disorders

Tachycardia

Vascular disorders

Bleeding

Respiratory, thoracic and mediastinal disorders

Bronchospasmdyspnea

Gastrointestinal disorders

Vomit,

diarrhea, stomatitis, abdominal pain, nausea

Dyspepsia

Violations concerning

skin and subcutaneous tissues

Hives,

rash, angioedema, itching

General disorders and conditions at the site of application

Pyrexia

Facial swelling

Analyzes and research

Low blood pressure

In very rare cases, serious skin reactions such as Stevens-Johnson syndrome and Lyell’s syndrome have been reported in a chronological relationship with the use of acetylcysteine. In most cases, at least one concomitantly taken drug could be involved in triggering the above mucocutaneous syndromes. For this reason, you should immediately consult a doctor if any new changes to the skin or mucous membrane occur, and immediately stop taking acetylcysteine.

A decrease in platelet aggregation in the presence of acetylcysteine ​​has been confirmed by various studies. Clinical significance has not yet been established.

Interaction

The combined use of acetylcysteine ​​with antitussives may increase sputum stagnation due to suppression of the cough reflex.

When used simultaneously with antibiotics such as tetracyclines (excluding doxycycline), ampicillin, amphotericin B, they may interact with the thiol group of acetylcysteine, which leads to a decrease in the activity of both drugs. Therefore, the interval between doses of these drugs should be at least 2 hours.

The simultaneous use of acetylcysteine ​​and nitroglycerin can cause a pronounced decrease in blood pressure and headache.

Concomitant use of acetylcysteine ​​and carbamazepine may result in subtherapeutic levels of carbamazepine.

Activated carbon can reduce the effect of acetylcysteine.

Acetylcysteine ​​eliminates the toxic effects of paracetamol.

Acetylcysteine ​​may interfere with the colorimetric determination of salicylates.

Acetylcysteine ​​may interfere with urinary ketone analysis.

Overdose

Acetylcysteine ​​when taken at a dose of 500 mg/kg/day does not cause signs and symptoms of overdose.

Symptoms

The following symptoms may occur: nausea, vomiting and diarrhea.

Treatment

There is no specific antidote; treatment is symptomatic.

Storage conditions

Store at a temperature not exceeding 25 oC.
Keep out of the reach of children.

Shelf life

3 years. Do not use after the expiration date stated on the package.

Manufacturer

Zambon S.p.A., Italy