Fluimucil-antibiotic IT, lyophilizate and inhalation 500 mg 3 pcs

Pharmacotherapeutic group:

A combined antibiotic (antibiotic + mucolytic)

ATC code: [J01BA02].

Pharmacological properties

Pharmacodynamics

Thiamphenicol glycinate acetylcysteinate is a complex compound combining the antibiotic thiamphenicol and the mucolytic acetylcysteine. After absorption of thiamphenicol glycinate acetylcysteinate splits into acetylcysteine and thiamphenicol.

Thiamphenicol is a derivative of chloramphenicol, the mechanism of action is related to the inhibition of bacterial cell protein synthesis. Thiamphenicol has a wide spectrum of antibacterial activity, it is effective in vitro against the bacteria most frequently causing respiratory tract infections: Gram-positive (Streptococcus pneumoniae, Corynebacterium diphtheriae, Staphylococcus spp, Streptococcus pyogenes, Listeria spp., Clostridium spp.) and gram-negative (Haemophilus influenzae, Neisseria spp., Salmonella spp., Escherichia coli, Shigella spp., Bordetella pertussis, Yersinia pestis, Brucella spp., Bacteroides spp.)

Acetylcysteine by breaking disulfide bonds of mucoproteins quickly and effectively liquefies sputum, pus, reduces their viscosity and promotes expectoration. Acetylcysteine facilitates penetration of the antibiotic thiamphenicol into lung tissues and inhibits adhesion of bacteria on the airway epithelium.

Pharmacokinetics

Tiamphenicol is rapidly distributed in the body and accumulates in the respiratory tract tissues in therapeutic concentrations (tissue/plasma concentration ratio is about 1). Maximum plasma concentration is reached 1 hour after intramuscular administration. The elimination half-life is about 3 hours; the volume of distribution is 40 – 68 l. Binding to plasma proteins is up to 20%. It is excreted by the kidneys through glomerular filtration; 24 hours after injection the amount of unchanged thiamphenicol in the urine is 50-70% of the administered dose. It penetrates through the placental barrier.

Acetylcysteine is rapidly distributed in the body after administration, the half-life is 2 hours. In the liver it is deacetylated to cysteine. In blood there is a mobile equilibrium of free and bound to plasma proteins acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine). Acetylcysteine penetrates into the intercellular space, mainly distributed in the liver, kidneys, lungs, bronchial secretion. It is excreted by kidneys as inactive metabolites (inorganic sulfates, diacetylcysteine), a small part is excreted unchanged through the intestine. It passes through the placental barrier.

Indications

Fluimucil®-antibiotic IT is used for treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug and accompanied by mucostasis.

Diseases of the upper respiratory tract and ENT organs: exudative media otitis media, sinusitis, laryngotracheitis.

Lower respiratory diseases: acute and chronic bronchitis, lingering pneumonia, lung abscess, emphysema, bronchiectatic disease, cystic fibrosis, bronchiolitis, pertussis.

The prevention and treatment of bronchopulmonary complications after thoracic surgical interventions (bronchopneumonia, atelectasis). Prevention and treatment of obstructive and infectious complications of tracheostomy, preparation for bronchoscopy, bronchoaspiration.

In concomitant nonspecific forms of respiratory infections to improve drainage, including cavernous foci, in mycobacterial infections.

Active ingredient

Composition

How to take, the dosage

Fluimucil®-antibiotic IT is administered intramuscularly, used for inhalations, instillations, cavity washings.

Inhaled: adults – 250 mg 1-2 times daily; children – 125 mg 1-2 times daily.

The procedure of inhalation:

– remove the protective aluminum cap from the bottle;
– immediately before inhalation, open the ampoule with the solvent;
– using a syringe, inject the contents of the ampoule into the closed bottle with the drug, mix thoroughly;
– Pour the solution into the nebulizer (inhaler) reservoir;
– Use the nasal attachments or a mask to inhale for 5 – 10 minutes.
The prepared solution for inhalation can be used within 24 hours if stored at 5 0C (in the refrigerator).

Endotracheal: through bronchoscope, intubation tube, tracheostomy – 1-2 ml of solution (for adults dissolved in 4 ml of water for injection – 500 mg of dry substance, for children – 250 mg).

Topically: for injection into paranasal sinuses and for irrigation of cavities after surgical interventions in the area of the nose and the mastoid process, 1 -2 ml of the solution (for adults dissolved in 4 ml of water for injection – 500 mg of dry substance, for children – 250 mg).
In diseases of the nasopharynx and ear, 2-4 drops in each nasal passage or external auditory canal.

Intramuscularly: adults – 500 mg 2 to 3 times a day; for children under 3 years old – 125 mg 2 times a day; for children from 3 to 7 years old – 250 mg 2 times a day; for children from 7 to 12 years old – 250 mg 3 times a day; for children from 13 to 15 years old – 500 mg 2 times a day; for children from 16 to 18 years old – 500 mg 2 or 3 times a day.

For patients with creatinine clearance 20 – 50 ml/min, the dose is 500 mg 2 times a day; in creatinine clearance 5 – 19 ml/min – 500 mg once a day.

For premature and newborn infants up to 2 weeks old the average dose is 25 mg/kg per day.

If necessary, the dose can be doubled (in the first 2-3 days of treatment in particularly severe cases). The dose should not be increased in premature and newborn children, as well as in patients older than 65 years.

The course of treatment is not more than 10 days.

Interaction

Special Instructions

The peripheral blood count should be monitored during treatment. In case of decrease of leukocyte count (less than 4 thousand/μl) and granulocyte count (by more than 40%) the drug should be discontinued.

The dose of thiamphenicol should be reduced in moderate to severe renal failure. In addition, in patients with moderate to severe renal impairment it is recommended to provide separate therapy with antibacterial and mucolytic agents.

The solution of Fluimucil®-antibiotic IT should not come into contact with metal and rubber surfaces.

The use of a compressor nebulizer is recommended for inhalation and should be set up so that the nebulized particle size is 3-20 microns. A nebulizer made of glass or plastic is preferable. If the nebulizer has metal or rubber parts, they should be rinsed with water after use.

Fluimucil®-antibiotic IT does not affect the ability to drive vehicles and other mechanisms.

Contraindications

Hypersensitivity to one of the components of the drug; anemia, leukopenia, thrombocytopenia.

In hepatic failure and chronic renal failure. In children of the first two years of life due to age-related features of renal function.

Side effects

For systemic and local routes of administration – allergic reactions.

In intramuscular administration mild burning at the injection site, reticulocytopenia, anemia, leukopenia, neutropenia, thrombocytopenia, nausea, vomiting, diarrhea are possible.

In long-term use, neuritis of the optic nerve and peripheral neuropathy may occur.

In case of inhalation – reflex cough, local airway irritation, stomatitis, rhinitis, nausea. Laryngeal edema and bronchospasm may occur (mainly in patients with bronchial asthma), in this case bronchodilators are prescribed.

Overdose

Pregnancy use