Azitrox capsules 250mg, No. 6

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

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

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

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

• infections of the urogenital tract (including urethritis and / or cervicitis);

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

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

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

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

For infections of the skin and soft tissues, it is prescribed in a dose of 1 g / day for 1 dose on the first day, then - 500 mg / day daily from 2 to 5 days. Heading dose - 3 g.

For uncomplicated urethritis and / or cervicitis, 1 g is prescribed once.

With complicated, long-term urethritis / cervicitis caused by Chlamydia trachomatis, 1 g 3 times with an interval of 7 days (taking the drug on days 1-7-14 of treatment). Heading dose - 3 g.

In 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 days. Heading dose - 3 g.

For gastric ulcer and duodenal ulcer associated with Helicobacter pylori, 1 g / day is prescribed for 3 days as part of a combined anti-Helicobacter pylori therapy.

For children weighing more than 45 kg with infections of the upper and lower respiratory tract, skin and soft tissues, scarlet fever, the drug is prescribed at 500 mg / day (1 capsule) for 1 dose for 3 days.

For children over 12 years old, the drug (250 mg capsules) is prescribed at the rate of 10 mg / kg 1 time / day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day within 3 days. Heading dose - 30 mg / kg.

In the treatment of erythema migrans in children, the dose of the drug (caps. 500 mg) is 1 g on the 1st day and 500 mg daily from the 2nd to the 5th days. Heading dose - 3 g. AzitroxЃ should be used in the form of 250 mg capsules at a dose of 20 mg / kg on the 1st day and 10 mg / kg from the 2nd to the 5th day.

White capsules, No. 0; the contents of the capsules are white or white with a yellowish tinge powder.

1 caps.

azithromycin dihydrate 262.03 mg,?

which corresponds to the content of azithromycin 250 mg

Excipients: mannitol (mannitol) - 42.55 mg, corn starch - 13.1 mg, magnesium stearate - 2 mg, sodium lauryl sulfate - 0.32 mg.

• Liver failure;

• renal failure;

• children weighing less than 45 kg (for capsules 500 mg);

• children under 12 years of age;

• hypersensitivity to antibiotics of the macrolide group.

• The drug should be used with caution in case of arrhythmias (ventricular arrhythmias, prolongation of the QT interval are possible), in children with severe impaired liver or kidney function.

pharmachologic effect

A broad-spectrum antibiotic, a representative of the subgroup of macrolide antibiotics - azalides. By binding to the 50S ribosome subunit, it inhibits peptide translocase at the translation stage, inhibits protein synthesis, and slows down the growth and reproduction of bacteria. It acts bacteriostatically, in high concentrations it has a bactericidal effect. Acts on extra- and intracellular pathogens.

Active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, 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 Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

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

Pharmacokinetics

Suction

After taking the drug inside, azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. After oral administration of 500 mg of azithromycin, Cmax in plasma is reached after 2.5-3 hours and is 0.4 mg / l. Bioavailability - 37%.

Taking the drug simultaneously with food slows down and reduces the absorption of azithromycin.

Distribution

Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), into the skin and soft tissues. A high concentration in tissues (10-50 times higher than in blood plasma) and a long T1 / 2 are due to the low binding of azithromycin to blood 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 a large apparent Vd (31.1 L / kg) and a 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 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 its high concentration in phagocytes, azithromycin does not significantly affect their function.

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

Metabolism

In the liver, azithromycin is demethylated, the resulting metabolites are inactive.

Withdrawal

The elimination of azithromycin from blood plasma takes place 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 interval from 24 to 72 hours, which allows the drug to be used 1 time / day.

Side effect

From the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases; in children - constipation, anorexia, gastritis. Candidomycosis of the oral mucosa is possible.

From the side of the cardiovascular system: palpitations, chest pain (? 1%).

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

From the reproductive system:? 1% - vaginal candidiasis.

From the urinary system:? 1% - nephritis.

Dermatological reactions: in some cases - rash, photosensitivity.

Allergic reactions: rash, itching, Quincke's edema, urticaria, conjunctivitis.

Others: increased fatigue.

Application during pregnancy and lactation

The use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be resolved.

Application for violations of liver function

The drug is contraindicated in severe liver dysfunction.

Application for impaired renal function

The drug is contraindicated in severe renal impairment.

Application in children

Contraindicated: children under 12 years of age.

special instructions

AzitroxЃ should not be taken with food.

If the next dose is missed, the missed dose should be taken as soon as possible, and the next dose should be taken with an interval of 24 hours.

It is necessary to observe a break of at least 2 hours between taking Azitrox and antacids.

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

Overdose

Symptoms: when using the drug in high doses, side effects may increase - severe nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: gastric lavage, the appointment of activated carbon, symptomatic therapy.

Drug interactions

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

Azithromycin does not bind to cytochrome P450 isoenzymes. Unlike most macrolides, there is currently no interaction of azithromycin with theophylline, terfenadine, carbamazepine, triazolam, digoxin.

Macrolides (with the exception of azalides) slow down the excretion and increase the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs that undergo microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, alkaloids, dysyroxyaloic acid, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline), due to inhibition of microsomal oxidation in hepatocytes, while with the use of azalides, such interaction has not been observed to date.

With the simultaneous use of azithromycin with digoxin, an increase in the concentration of the latter is observed.

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

With the simultaneous use of azithromycin with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) increases.

With the simultaneous use of azithromycin with triazolam, clearance decreases and the pharmacological effect of triazolam increases.

Lincosamines reduce the effectiveness of azithromycin.

Tetracycline and chloramphenicol increase the effectiveness of azithromycin.

Pharmaceutical incompatibility

Azithromycin is pharmaceutically incompatible with heparin.