INSTRUCTIONS FOR MEDICAL USE
AZIREM
Trade name of the drug: Azirem®
Active substance (INN): Azithromycin
Dosage form: suspension
Contents:
5 ml of the suspension contains:
Active substance: Azithromycin – 200 mg.
Excipients: Guar gum, Trilon B (ETDA), acrylic polymer Cugop T-135, sucralose, sodium citrate, menthol, tween 80 (polysorbate-80), propylene glycol, peppermint oil, liquid sorbitol, sodium saccharine, methyl paraben (nipagin), propyl paraben (nipazole), banana flavor, orange flavor, purified water.
Description: white or almost white suspension.
Pharmacotherapeutic group: Antibiotics (macrolide group).
ATX code: J01FA10
Pharmacological properties
It is a broad-spectrum antibiotic. It is the first representative of the new generation of bacterial antibiotics – aazilogens. It has bacteriostatic properties, and in high concentrations in the inflammation focus it has bactericidal effect. The mechanism of action of azithromycin is associated with the inhibition of microbial cell protein synthesis. It binds with 50S ribosome subunit, inhibits peptide translocation stage and inhibits protein synthesis, inhibiting bacterial growth and reproduction.
Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, Staphylococcus aureus are sensitive to the drug; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp. as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.
It is inactive against erythromycin-resistant Gram-positive bacteria.
Pharmacokinetics
The drug is quickly absorbed from gastrointestinal tract, which is due to its stability in acidic environment and lipophilicity. After oral administration with a dose of 500 mg maximum concentration (Cmax) of azithromycin in blood plasma is reached after 2-3 hours and is 0.4 mg/l. Bioavailability is 37%. Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate), skin and soft tissue. Maximal concentration (in tissues and cells 10-50 times higher than in blood plasma) and long period of semiejection (T1/2) are caused by low binding of azithromycin with blood plasma proteins as well as by its ability to penetrate into eukaryotic cells and to concentrate in low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (31.1 L/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is particularly important for the elimination of intracellular pathogens It has been shown that phagocytes deliver azithromycin to the localized sites of infection, where it is released during phagocytosis. The azithromycin concentration in the foci of infection is reliably higher than in the healthy tissues (on the average by 24-34%), and correlates with the degree of the inflammatory edema. Despite its high concentration in phagocytes, azithromycin has no significant effect on their function. Azithromycin persists in bactericidal concentrations in the spectra for 5 – 7 days after the previous dose, which allowed to develop short (3-day and 5-day) courses of treatment. It is metabolized mainly in the liver to form inactive metabolites. Excretion of azithromycin from plasma is done in 2 stages: T1/2 is 14-20 hours between 8-24 hours after taking the drug, and 41 hours between 24-72 hours, which allows using the drug once a day. It is excreted mainly with bile unchanged, a small part through the kidneys.
INDICATIONS FOR USE
Infectious-inflammatory diseases caused by pathogens sensitive to the drug:
- Infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, rhinopharyngitis, pharyngitis, tonsillitis, otitis media);
- scarlet fever;
- Lower respiratory tract infections (bacterial and typical pneumonia, bronchitis);
- skin and soft tissue infections (moderate acne (Acne vulgaris), rye, impetigo, secondary infected dermatoses);
- infections of the urogenital tract (uncomplicated urethritis and/or cervicitis);
- Lyme disease (borreliosis), for treatment of the initial stage (erythema migrans).
Dosage and administration
Orally 1 hour before or 2 hours after the meal, once a day.
In children with upper and lower respiratory tract infections, skin and soft tissue infections, the drug is prescribed at the rate of 10 mg/kg body weight once daily for 3 days (course dose – 30 mg/kg body weight) or 5 days: first day – 10 mg/kg body weight, then 5-10 mg/kg body weight once daily for 4 days.
Depending on the body weight of the child, the following dosage regimens are recommended:
Body weight | Average daily (single) dose |
10-14 kg | 2,5 ml (100 mg) |
15-24 kg | 5 ml (200 mg) |
25-34 kg | 7,5 ml (300 mg) |
35-44 kg | 10 ml (400 mg) |
>45 kg | 12,5 ml (500 mg) |
When treating Erythema migrans in children, the drug is prescribed once a day for 5 days: 20 mg/kg body weight on the first day and 10 mg/kg body weight on days 2 to 5. It is recommended to take the flacquer on the first day and 10 mg/kg of body weight on the second and fifth days. It is recommended to shake the contents of the bottle before each use.
Side effects
They occur rarely (0.7% of cases or less).
Digestive system: melena, cholestatic jaundice, nausea, vomiting, diarrhea, constipation, decreased appetite, candidomycosis of the oral mucosa, change of taste, gastritis, reversible moderate increase in liver enzymes activity.
Genitourinary system: nephritis, vaginal candidomycosis.
Cardiovascular system: palpitations, chest pain.
CNS and peripheral nervous system: dizziness, headache, somnolence, fatigue; in children – headache (in otitis media therapy), hyperkinesia, anxiety, neurosis, sleep disorders.
Allergic reactions: very rare skin rash, Quincke’s edema, skin itching, urticaria, photosensitization, conjunctivitis, Stevens-Johnson syndrome.
Laboratory parameters: in some cases – neutrophilia, eosinophilia (changed values return to normal in 2-3 weeks after discontinuation of treatment).
Other: asthenia, photosensitization.
Contraindications
- Hypersensitivity to antibiotics of macrolide group and the drug components;
- Severe liver or kidney function abnormalities;
- Children under 6 months of age (efficacy and safety has not been established);
- period of lactation.
Drug interactions
Antacids (containing aluminium, magnesium), ethanol and food considerably reduce absorption of azithromycin, therefore the drug should be taken at least 1 hour before or 2 hours after taking these drugs and food.
Unlike other macrolide antibiotics, azithromycin does not bind to cytochrome P450 isoenzymes. To date, there have been no observed interactions with te o f f l l i n g , t e r f e n d i n g , c a r ba m a z e p i n g , triazolam, digoxin. If coadministration with warfarin is necessary, careful control of prothrombin time is recommended.
Concomitant use of macrolides with ergotamine and dihydroergotamine may cause their toxic effect (vasospasm, dysesthesia). Lincosamines decrease and tetracycline and chloramphenicol increase azithromycin efficacy.
Pharmaceutically, azithromycin is incompatible with heparin. When used with bromcriptine, the blood concentration of the latter is increased.
Special indications
Caution is advised when using in patients with hepatic or renal dysfunction. It is recommended to take a break of at least 2 hours between intakes of azithromycin and antacids. If one dose of the drug is missed, the missed dose should be taken as soon as possible, and the next ones should be taken 24 hours apart.
The patient should be warned about the need to inform the doctor if any side effect occurs.
Administration of the drug in pregnancy is possible only when the proposed benefit to the mother exceeds the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (excreted with breast milk). The drug contains sorbitol; therefore, it should not be used in patients with fructose intolerance.
Overdose
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: gastric lavage, symptomatic therapy.
Form of production
200 mg/5 ml suspension in 15 ml vials, with or without measuring spoon or cup.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25°C. After the first opening of the original package, the suspension should be stored for 7 days at a temperature not exceeding 10 ° C. Keep out of the reach of children!
Shelf life
2 years. Do not use after the expiration date.
Conditions for dispensing from pharmacies
Released by a doctor’s prescription.