Fluimucil^®-Antibiotic IT (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Zambon, S.p.A. (Italy)

ATC Code

J01BA02 (Thiamfenicol)

Active Substance

Thiamphenicol, glycinate acetylcysteinate (Rec.INN Mod. registered by WHO, modified name)

Dosage Form

Fluimucil®-Antibiotic IT

Lyophilizate for preparation of solution for injections and inhalations 810 mg: vial 3 pcs. in a set with solvent

Dosage Form, Packaging, and Composition

Excipients: disodium edetate.

Solvent: water for injections (4 ml).

810 mg – vials (3) in a set with solvent (amp. 3 pcs.) – plastic trays (1) – cardboard packs.

Clinical-Pharmacological Group

Antibiotic in combination with a mucolytic and an antioxidant

Pharmacotherapeutic Group

Combined antibiotic (antibiotic + mucolytic)

Pharmacological Action

Thiamphenicol glycinate acetylcysteinate is a complex compound combining the antibiotic thiamphenicol and the mucolytic agent acetylcysteine. After absorption, thiamphenicol glycinate acetylcysteinate is broken down into acetylcysteine and thiamphenicol.

Thiamphenicol is a derivative of chloramphenicol; its mechanism of action is associated with the inhibition of bacterial cell protein synthesis. Thiamphenicol has a broad spectrum of antibacterial action and is effective in vitro against bacteria most commonly 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 the disulfide bonds of mucoproteins, rapidly and effectively thins sputum and pus, reduces their viscosity, and promotes expectoration. Acetylcysteine facilitates the penetration of the antibiotic thiamphenicol into lung tissues and inhibits bacterial adhesion to the respiratory epithelium.

Pharmacokinetics

Thiamphenicol is rapidly distributed in the body, accumulating in respiratory tract tissues at therapeutic concentrations (the tissue/plasma concentration ratio is about 1). C_max in plasma is reached 1 hour after IM administration. T_1/2 is about 3 hours, V_d is 40-68 L. Plasma protein binding is up to 20%. It is excreted by the kidneys via glomerular filtration; 24 hours after administration, the amount of unchanged thiamphenicol in urine is 50-70% of the administered dose. It crosses the placental barrier.

Acetylcysteine after administration is rapidly distributed in the body; T_1/2 is 2 hours. It is deacetylated in the liver to cysteine. A dynamic equilibrium of free and plasma protein-bound acetylcysteine and its metabolites (cysteine, cystine, diacetylcysteine) is observed in the blood. Acetylcysteine penetrates into the intercellular space, being predominantly distributed in the liver, kidneys, lungs, and bronchial secretions. It is excreted by the kidneys as inactive metabolites (inorganic sulfates, diacetylcysteine); a small portion is excreted unchanged through the intestines. It crosses the placental barrier.

Indications

• Diseases of the upper respiratory tract and ENT organs: exudative otitis media, sinusitis, laryngotracheitis;
• Diseases of the lower respiratory tract: acute and chronic bronchitis, prolonged pneumonia, lung abscess, emphysema, bronchiectasis, cystic fibrosis, bronchiolitis, whooping cough;
• 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;
• For concomitant nonspecific forms of respiratory infections to improve drainage, including cavernous foci, in mycobacterial infections.

ICD codes

Dosage Regimen

It is administered intramuscularly, used for inhalations, applications, and cavity lavage.

By inhalationfor adults – 250 mg 1-2 times/day; for children – 125 mg 1-2 times/day.

Endotracheally via bronchoscope, intubation tube, tracheostomy – 1-2 ml of solution (for adults, dissolved in 4 ml of water for injections – 500 mg of dry substance, for children – 250 mg).

Locally for introduction into the paranasal sinuses, as well as for lavage of cavities after surgical interventions in the area of the nose and mastoid process, 1-2 ml of solution ( for adults dissolved in 4 ml of water for injections – 500 mg of dry substance, for children – 250 mg).

For diseases of the nasopharynx and ear, instill 2-4 drops into each nasal passage or external auditory canal.

Intramuscularlyfor adults – 500 mg 2-3 times/day; for children under 3 years – 125 mg 2 times/day; 3-7 years – 250 mg 2 times/day; 7-12 years – 250 mg 3 times/day.

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

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

The course of treatment should not exceed 10 days.

Adverse Reactions

Possible allergic reactions.

With IM administration, mild burning at the injection site is possible; rarely – reticulocytopenia, anemia, leukopenia, neutropenia, thrombocytopenia.

With inhalation administration – reflex cough, local irritation of the respiratory tract, stomatitis, rhinitis, nausea. Bronchospasm is possible, in which case bronchodilators are prescribed.

Contraindications

• Anemia;
• Leukopenia;
• Thrombocytopenia;
• Hypersensitivity to any component of the drug.

With caution in hepatic insufficiency and chronic renal failure; in children during the first two years of life due to age-related features of renal function.

Use in Pregnancy and Lactation

During pregnancy, the drug is prescribed only when the potential benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued for the duration of treatment.

Use in Hepatic Impairment

Use with caution in hepatic insufficiency.

Use in Renal Impairment

Use with caution in chronic renal failure.

Pediatric Use

Use with caution in children during the first two years of life due to age-related features of renal function.

Geriatric Use

The dose should not be increased in patients over 65 years of age.

Special Precautions

During treatment, the peripheral blood picture should be monitored. If the number of leukocytes (less than 4 thousand/µl) and granulocytes (by more than 40%) decreases, the drug should be discontinued.

The solution should not come into contact with metal and rubber surfaces.

Drug Interactions

Concomitant use of antitussive agents may increase sputum stasis due to suppression of the cough reflex.

It is not recommended to mix with other drugs in an aerosol.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.