Composition
1 film-coated tablet contains the Active ingredient azithromycin 500 mg (in the form of azithromycin dihydrate); Excipients: Microcrystalline silicate cellulose — 69.00 mg, Microcrystalline cellulose-57.00 mg, Sodium Carboxymethyl starch (type A) – 46.00 mg, Povidone-24.00 mg, Magnesium stearate-10.00 mg, Talc-10.00 mg, Colloidal silicon dioxide-1.00 mg; Shell: Titanium dioxide-10.58 mg, Talc-9.57 mg, Copovidone-4.95 mg, Ethylcellulose-4.95 mg, Macrogol 6000-1.32 mg, Indigo Carmine (indigotine) E 132-1.22 mg, Dye varnish green 8% (Indigo Carmine (indigotine) E 132, Quinoline yellow E 104) – 0.41 mg
Film shell: Â
Titanium dioxide — 10.58 mg;
Talcum powder — 9.57 mg.
Copovidone — 4.95 mg;
Ethylcellulose — 4.95 mg;
Macrogol 6000 — 1.32 mg;
Indigo Carmine (indigotin) (E 132) — 1.22 mg;
Dye varnish green 8% (indigocarmin (indigotin) (E 132),
Quinoline yellow (E 104) – 0.41 mg
Pharmacological action
Broad-spectrum antibiotic. Azithromycin is a representative of a subgroup of macrolide antibiotics-azalides. In high concentrations, it has a bactericidal effect.
Hemomitsin active against aerobic gram-positive bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus spp. groups C, F and G, Streptococcus viridans, Staphylococcus aureus;
aerobic gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Helicobacter pylori, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis;
anaerobic bacteria: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.
The drug is active against intracellular microorganisms: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Borrelia burgdorferi, as well as against Treponema pallidum.
Gram-positive bacteria resistant to erythromycin are resistant to the drug.
Pharmacokinetics
Suction
Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity.
After oral use of Chemomycin at a dose of 500 mg, the Cmax of azithromycin in blood plasma is reached in 2.5-2.96 hours and is 0.4 mg/l. Bioavailability is 37%.
Distribution
Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract, into the prostate gland, into the skin and soft tissues.
The high concentration in tissues (10-50 times higher than in blood plasma) and long T1/2 are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in a low pH environment surrounding lysosomes.
This, in turn, determines the large apparent Vd (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for the elimination of intracellular pathogens.
Phagocytes have been shown to deliver azithromycin to the sites of infection, where it is released during phagocytosis.
The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema.
Despite the high concentration in phagocytes, azithromycin does not significantly affect their function.
Azithromycin remains in bactericidal concentrations in the focus of inflammation for 5-7 days after the last dose, which made it possible to develop short (3-day and 5-day) treatment courses.
Metabolism
In the liver, azithromycin is demethylated, the resulting metabolites are not active.
Deduction
Removal of azithromycin from blood plasma takes place in 2 stages: T1 / 2 is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours – in the range from 24 to 72 hours, which allows the drug to be used 1 time / day.
Active ingredients
Azithromycin
Indications
- Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
- Infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);
- Scarlet fever;
- Lower respiratory tract infections (bacterial and atypical pneumonia, bronchitis);
- Infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses);
- Urogenital tract infections (uncomplicated urethritis and / or cervicitis);
- Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
- Stomach and duodenal diseases associated with Helicobacter Pylori (as part of combination therapy).
Use during pregnancy and lactation
During pregnancy, Chemomycin is prescribed only when the expected benefit of therapy for the mother exceeds the potential risk to the fetus.
If it is necessary to use the drug during lactation, the question of stopping breastfeeding for the duration of the drug should be decided.
Contraindications
Hypersensitivity (including to other macrolides); hepatic and / or renal failure; children under 12 years of age (for this dosage form), lactation period. With caution: pregnancy, arrhythmia (possible ventricular arrhythmias and prolongation of the QT interval), children with severe liver or kidney dysfunction.
Side effects
From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less – dyspepsia, vomiting, flatulence, melena, cholestatic jaundice, increased activity of liver enzymes, constipation, anorexia, gastritis in children.
From the cardiovascular system: palpitations, chest pain (1% or less).
From the central nervous system: dizziness, headache, vertigo, drowsiness; in children-headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (1% or less).
From the genital system: vaginal candidiasis.
From the urinary system: nephritis (1% or less).
Allergic reactions: rash, angioedema; in children-conjunctivitis, pruritus, urticaria.
Other: increased fatigue, photosensitivity.
Interaction
Simultaneous use of Chemomycin and antacids(aluminum – and magnesium-containing) slows down the absorption of azithromycin.
Ethanol and food slow and reduce the absorption of azithromycin.
When warfarin and azithromycin were co-administered (in normal doses), no changes in prothrombin time were detected, but given that the interaction of macrolides and warfarin may increase the anticoagulant effect, patients should carefully monitor prothrombin time.
The combined use of azithromycin and digoxin increases the concentration of the latter.
With the simultaneous use of azithromycin with ergotamine and dihydroergotamine, an increase in the toxic effect of the latter (vasospasm, dysesthesia) is noted.
Co-use of triazolam and azithromycin reduces clearance and enhances the pharmacological effect of triazolam.
Azithromycin slows excretion and increasing the plasma concentration and toxicity of cycloserine, anticoagulants, methylprednisolone, felodipine and drugs that undergo
microsomal oxidation (carbamazepine, terfenadine, cyclosporine, gexobarbitala, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs,
theophylline and other xanthine derivatives) due to the inhibition by azithromycin microsomal oxidation in hepatocytes.
Lincosamines weaken the effectiveness of azithromycin, while tetracycline and chloramphenicol enhance it.
Pharmaceutical interaction
Pharmacologically, azithromycin is incompatible with heparin.
How to take, course of use and dosage
Inside,1 hour before or 2 hours after meals,1 time a day.
For upper and lower respiratory tract infections,500 mg/day is prescribed for 3 days (the course dose is 1.5 g).
For infections of the skin and soft tissues — 1 g/day on the first day for 1 reception, then-0.5 g / day daily, from the 2nd to the 5th day (the course dose is 3 g).
With uncomplicated urethritis and / or cervicitis,1 g is prescribed once.
In Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans),1 g is prescribed on day 1 and 500 mg daily from day 2 to day 5 (the course dose is 3 g).
For diseases of the stomach and duodenum associated with Helicobacter pylori,1 g per day is prescribed for 3 days as part of a combination therapy.
If you miss 1 dose of the drug, the missed dose should be taken as early as possible, and the subsequent ones-with a break of 24 hours.
Overdose
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: gastric lavage, symptomatic therapy.
Purpose
Antibiotic-azalide
Description
Round, biconvex tablets, covered with a film-coated grayish-blue color.
Functional features
Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. After oral use of 500 mg, the maximum concentration of azithromycin in blood plasma is reached in 2.5-2.96 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 gland), skin and soft tissues. The high concentration in tissues (10-50 times higher than in blood plasma) and the long half-life are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding lysosomes. This, in turn, determines the large apparent volume of distribution (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for the elimination of intracellular pathogens. Phagocytes have been shown to deliver azithromycin to the sites of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatment courses. It is demethylated in the liver, and the resulting metabolites are not active. The elimination of azithromycin from blood plasma takes place in 2 stages: the half-life is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours-in the range from 24 to 72 hours, which allows the drug to be used 1 time / day. Food intake significantly changes the pharmacokinetics (depending on the dosage form): tablets — the maximum concentration (Cmax) increases (by 31%), the area under the curve (AUC) does not change.
Complete set
Film-coated tablets 500 mg. 3 tablets in an AL/PVC blister. 1 blister pack with instructions for use in a cardboard box.
Special instructions
If 1 dose is missed, the missed dose should be taken as early as possible, and subsequent doses should be taken at 24 — hour intervals.
It is necessary to observe a break of 2 hours with simultaneous use of antacids.
After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a doctor.
Form of production
Film-coated tablets
Storage conditions
Store in a dry place protected from light at a temperature of 15 to 25 °C. Keep out of reach of children.
Shelf
life is 3 years. Do not use after the expiration date indicated on the package.
Active ingredient
Azithromycin
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
Children over 12 years of age, Children prescribed by a doctor, Adults prescribed by a doctor, Pregnant women prescribed by a doctor
Indications
Otitis Media, Skin Infections, Urinary Tract Infections, Sinusitis, Tonsillitis, Urethritis, Sinusitis, Respiratory Tract Infections, Sore Throat, Pneumonia, Pharyngitis, Bronchitis, Infectious diseases
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