AzitRus, powder for suspension 50mg sachets 4,2g 3pcs

Composition

Active ingredient: azithromycin dihydrate in terms of azithromycin – 50 mg. Auxiliary substances: sodium citrate (three-substituted sodium citric acid), food grade orange flavor, sodium saccharinate (soluble saccharin), collidone CL-M (crospovidone), sugar (sucrose).

Pharmacological action

Broad-spectrum antibiotic of the macrolide group, azalide. It acts bacteriostatically. Binding to the 50S subunit of the ribosome, it suppresses protein synthesis and slows down the growth and reproduction of bacteria. In high concentrations, it has a bactericidal effect. It acts on extracellular and intracellular pathogens.

Active against gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except for erythromycin resistant), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; 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 intracellular pathogens: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

Azithromycin is not active against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics

Suction

After oral use, azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. After oral use at a dose of 500 mg_{, cmax} in plasma is reached in 2.5-2.9 hours and is 0.4 mg/l. Bioavailability – 37.5%.

Distribution

Azithromycin is rapidly distributed throughout the body, and high concentrations of the antibiotic are achieved in the tissues. It 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 long T_1/2 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

Azithromycin is metabolized in the liver by demethylation to form inactive metabolites.

Deduction

Removal of azithromycin from blood plasma takes place in 2 stages: T_1/2 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.

It is mainly excreted in the bile in unchanged form, a small part is excreted by the kidneys.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

— infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);

— the scarlet fever;

— infections of the lower respiratory tract (bacterial, including caused by atypical pathogens of pneumonia, exacerbation of chronic pneumonia, bronchitis);

infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

— urinary tract infection (gonococcal urethritis and degeneracy);

infections of the female genital organs (cervicitis);

Lyme disease (borreliosis) in the initial stage (erythema migrans);

— diseases of the stomach and duodenum, associated with Helicobacter pylori (in combination therapy).

Contraindications

— renal failure;

hepatic failure;

— lactation (breastfeeding);

— children’s age up to 6 months (for suspension);

— children’s age up to 3 years of age and/or weighing less than 25 kg (caps);

— children’s age up to 12 years of age and/or weighing less than 50 kg (for tablets, film-coated);

— hypersensitivity to the components of the drug, as well as to other macrolides.

With caution, the drug is prescribed to patients with cardiac arrhythmias (possible ventricular arrhythmias, prolongation of the QT interval), children with severe renal or hepatic dysfunction, during pregnancy.

Side effects

Nervous system and sensory disorders: dizziness, vertigo, headache, paresthesia, agitation, increased fatigue, drowsiness; rarely-tinnitus, reversible hearing impairment up to deafness (when taken in high doses for a long time); in children — headache (in the treatment of otitis media), hyperkinesia, nervousness, anxiety, sleep disorders, conjunctivitis.

Cardiovascular and blood disorders (hematopoiesis, hemostasis): chest pain, palpitations.

Gastrointestinal disorders: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased ALT and AST activity, bilirubin levels, cholestasis, jaundice; rarely — constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, liver failure (possibly fatal); in children — decreased appetite, gastritis, candidiasis of the oral mucosa.

From the genitourinary system: vaginal candidiasis, nephritis.

Allergic reactions: rash, pruritus, urticaria; rarely-angioedema, anaphylactic shock.

Other: photosensitivity, eosinophilia, transient neutrophilia; with intravenous use (optional) – bronchospasm, pain and inflammation at the injection site.

Interaction

When used concomitantly, antacids (aluminum – and magnesium-containing), ethanol, and food slow down and reduce the absorption of azithromycin.

When azithromycin was co-administered in therapeutic doses with warfarin, no changes in prothrombin time were observed, however, given that the interaction of macrolides with warfarin may increase the anticoagulant effect, when prescribing this combination to patients, careful monitoring of prothrombin time is necessary.

With simultaneous use, the concentration of digoxin in the blood plasma increases.

When used simultaneously, the toxic effect (vasospasm, dysesthesia) of ergotamine and dihydroergotamine increases.

When used concomitantly, the clearance decreases and the pharmacological effect of triazolam increases.

Azithromycin inhibits microsomal oxidation in hepatocytes, which leads to a slowing of excretion and an increase in plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline).

Lincosamines reduce the effectiveness of azithromycin.

Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

Special instructions

The drug is not taken during meals.

If a missed 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 at least 2 hours between taking AzitRus® and antacids.

After discontinuation of the drug, hypersensitivity reactions may persist in some patients; in such cases, it is recommended to prescribe specific therapy under the supervision of a doctor.

How to take it, course of use and dosage

The drug is taken orally 1 time / day for 1 hour before or 2 hours after meals.

Adults

For infections of the upper and lower respiratory tract,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 is prescribed on the 1st day, then 500 mg 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 peptic ulcer of the stomach and duodenum associated with Helicobacter pylori,1 g/day is prescribed for 3 days as part of combined anti-helicobacter therapy.

Children

The drug is in capsule form are prescribed to children over 3 years of age and/or weighing more than 25 kg with infections of the upper and lower respiratory tract, skin and soft tissue at the rate of 10 mg/kg of body weight 1 time/day for 3 days (course dose – 30 mg/kg), or the 1st day of 10 mg/kg, then 4 days 5 to 10 mg/kg/day.

When treating the initial stage (erythema migrans) of Lyme disease (borreliosis), the drug is prescribed at a dose of 20 mg / kg on day 1, then 10 mg / kg from day 2 to day 5.

The drug is in the form of a suspension for oral use are prescribed for children older than 6 months with infections of the upper and lower respiratory tract, skin and soft tissue at the rate of 10 mg/kg of body weight 1 time/day for 3 days (course dose – 30 mg/kg), or within 5 days within 1 day – 10 mg/kg, then 4 days 5 to 10 mg/kg/day.

Recommended doses of the drug depending on the child’s body weight are shown in the table.

When treating the initial stage (erythema migrans) of Lyme disease (borreliosis), the drug is prescribed at a dose of 20 mg / kg on day 1, then 10 mg / kg from day 2 to day 5.

Overdose

Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: gastric lavage, symptomatic therapy.

Form of production

Powder for the preparation of a suspension for oral use,50 mg of azithromycin. 4.2 g (50 mg of azithromycin) in heat-sealed single-dose bags made of combined multilayer material based on foil, polyethylene or polyethylene-coated packaging paper. Packaging: 3 bags with instructions for use are placed in a pack of cardboard.

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-25 °C.

Shelf life

2 years

Active ingredient

Azithromycin

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Children older than 6 months, Children as prescribed by a doctor

Indications

Skin Infections, Tonsillitis, Respiratory Tract Infections, Pharyngitis, Pneumonia, Infectious Diseases, Sore Throat, Sinusitis, Bronchitis, Urethritis, Otitis