Zitrolide®

pharmachologic effect

An antibiotic of the macrolide group, it is a representative of the azalide subgroup. Has a wide spectrum of antimicrobial action. When high concentrations are created at the site of inflammation, it has a bactericidal effect.

The drug is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Streptococcus viridans, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Helicobacter pylori, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.

Also active against: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

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

Instructions:

Clinical and pharmacological group

06.021 (Antibiotic of the macrolide group - azalide)

Release form, composition and packaging

Capsules No. 0, with a white body and an orange-yellow or yellow cap; The contents of the capsules are white to off-white powder with a creamy tint.

Excipients: magnesium stearate, microcrystalline cellulose.

Capsule shell composition: gelatin, titanium dioxide, quinoline yellow, azorubine, ponceau 4R.

6 pcs. — contour cell packaging (1) — cardboard packs. 10 pcs. — contour cell packaging (10) — cardboard packs.

pharmachologic effect

An antibiotic of the macrolide group, it is a representative of the azalide subgroup. Has a wide spectrum of antimicrobial action. When high concentrations are created at the site of inflammation, it has a bactericidal effect.

The drug is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Streptococcus viridans, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Helicobacter pylori, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.

Also active against: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

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

Pharmacokinetics

Suction

When taken orally, azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. After taking the drug orally at a dose of 500 mg, the Cmax of azithromycin in the blood plasma is reached after 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 (in particular, the prostate gland), 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 eukaryotic cells and concentrate in the low pH environment surrounding lysosomes. This, in turn, determines the large Vd (31.1 l/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to sites of infection, where it is released during the process of phagocytosis. The concentration of azithromycin in foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the severity of the inflammatory process. Despite its high concentration in phagocytes, azithromycin does not have a significant effect on their function.

Azithromycin remains in bactericidal concentrations at the site of inflammation for 5-7 days after taking the last dose, which made it possible to develop short (3-day and 5-day) courses of treatment.

Metabolism

Azithromycin is demethylated in the liver to form inactive metabolites.

Removal

The elimination of azithromycin from blood plasma occurs in 2 stages: T1/2 is 14-20 hours in the interval from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours after taking the drug, which allows it to be used once a day .

Dosage

Zitrolide and Zitrolide Forte are taken orally 1 time/day 1 hour before meals or 2 hours after meals.

Adults with infections of the upper and lower respiratory tract are prescribed 500 mg/day for 3 days; The course dose is 1.5 g.

For infections of the skin and soft tissues, 1 g is prescribed on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 g).

For acute infections of the genitourinary system (uncomplicated urethritis or cervicitis), a single dose of 1 g is prescribed.

For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 g).

For gastric and duodenal ulcers associated with Helicobacter pylori, the drug is prescribed 1 g/day for 3 days as part of combination therapy.

For children, Zitrolide and Zitrolide Forte are prescribed at the rate of 10 mg/kg body weight 1 time/day for 3 days or on the 1st day - 10 mg/kg, then for 4 days - 5-10 mg/kg/day. for 3 days (course dose - 30 mg/kg).

For Lyme disease (borreliosis), for the treatment of the initial stage of erythema migrans, children are prescribed a dose of 20 mg/kg on the 1st day and 10 mg/kg from the 2nd to the 5th day.

Overdose

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

Treatment: discontinuation of the drug, symptomatic therapy.

Drug interactions

Antacids (aluminum and magnesium containing), ethanol and food slow down and reduce the absorption of azithromycin.

With the simultaneous administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time were detected, however, given that the interaction of macrolides and warfarin may increase the anticoagulant effect, patients need careful monitoring of prothrombin time.

When used together with digoxin, the concentration of digoxin increases.

When used simultaneously with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) increases.

When used simultaneously with triazolam, clearance is reduced and the pharmacological effect of triazolam is enhanced.

Azithromycin slows down the excretion and increases the concentration of plasma and the toxicity of cycloserin, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs subjected to microsomal oxidation (carbamazepine, terphenin, cyclosporine, hexobarbital, alkaloids of knorbus, valproic acid, dysopyramid, dysopyramid, dysopyramida, dysopyramida bromocriptine, phenytoin, oral hypoglycemic agents , xanthine derivatives, including theophylline) due to the inhibition of microsomal oxidation in hepatocytes by azithromycin.

Lincosamines weaken the effectiveness of azithromycin.

Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

Use during pregnancy and lactation

During pregnancy, Zitrolide and Zitrolide Forte should be used with caution and in cases where the expected benefit of therapy for the mother significantly exceeds the potential risk to the fetus.

The drug is contraindicated for use during lactation (breastfeeding). If it is necessary to use Zitrolide and Zitrolide Forte during lactation, it is recommended to suspend breastfeeding during treatment.

Side effects

From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); ≤1% - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of liver transaminases; in children - constipation, anorexia, gastritis, change in taste (≤1%).

From the cardiovascular system: palpitations, chest pain (≤1%).

From the central nervous system: dizziness, headache, drowsiness; in children - headache (during treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance (≤1%).

From the genitourinary system: vaginal candidiasis, nephritis (≤1%).

Allergic reactions: rash, photosensitivity, Quincke's edema; in children (≤1%) - conjunctivitis, itching, urticaria.

Storage conditions and periods

List B. The drug should be stored out of the reach of children, in a dry place, protected from light at a temperature not exceeding 25°C. The shelf life of Zitrolide is 3 years, Zitrolide forte is 2 years.

Indications

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

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

— infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);

- scarlet fever;

— infections of the skin and soft tissues (including erysipelas, impetigo, secondary infected dermatoses);

— infections of the genitourinary system (including uncomplicated urethritis and/or cervicitis);

- Lyme disease (borreliosis) - for the treatment of the initial stage (erythema migrans);

- diseases of the stomach and duodenum associated with Helicobacter pylori (as part of combination therapy).

Contraindications

- severe liver failure;

- severe renal failure;

- lactation period (breastfeeding);

- children under 3 years of age;

- hypersensitivity to azithromycin or other macrolides.

The drug should be used with caution during pregnancy, arrhythmias (possible development of ventricular arrhythmias and prolongation of the QT interval), and in children with severe impairment of liver or kidney function.

special instructions

It is necessary to observe a break of 2 hours while using antacids.

After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.

Use for renal impairment

The drug should be used with caution in children with severe renal impairment.

The drug is contraindicated in severe renal failure.

Use for liver dysfunction

The drug should be used with caution in children with severe liver dysfunction.

The drug is contraindicated in severe liver failure.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Indications for use

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

• infections of the upper respiratory tract and ENT organs (including tonsillitis, pharyngitis, sinusitis, tonsillitis, otitis media);
• infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
• scarlet fever;
• infections of the skin and soft tissues (including erysipelas, impetigo, secondary infected dermatoses);
• infections of the genitourinary system (including uncomplicated urethritis and/or cervicitis);
• Lyme disease (borreliosis) - for the treatment of the initial stage (erythema migrans);
• diseases of the stomach and duodenum associated with Helicobacter pylori (as part of combination therapy).

Directions for use and doses

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

• For adults with 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 is prescribed on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 g).
• For acute infections of the genitourinary system (uncomplicated urethritis or cervicitis), a single dose of 1 g is prescribed.
• For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 g).
• For gastric and duodenal ulcers associated with Helicobacter pylori, the drug is prescribed 1 g/day for 3 days as part of combination therapy.
• For children, the drug is prescribed at the rate of 10 mg/kg body weight 1 time/day for 3 days or on the 1st day - 10 mg/kg, then for 4 days - 5-10 mg/kg/day (course dose - 30 mg/kg).
• For Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), children are prescribed a dose of 20 mg/kg on the 1st day and 10 mg/kg from the 2nd to the 5th day.

Zitrolide

Active substance:

Azithromycin*

Pharmgroup:

Macrolides and azalides

Average price in pharmacies