Azitral (Azithromycin) tablets

Release form and composition: 

Hard gelatin capsules, size No. 0, with case and cap, white contents of capsules – white powder.

1 capsule contains:

azithromycin dihydrate (in terms of azithromycin) 250 mg

Auxiliary substances: lactose anhydrous, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methyl paraben, propyl paraben, gelatin.

6 PCs. – blisters (1) – packs cardboard.

6 PCs. – blisters (2) – packs cardboard.

6 PCs. – blisters (3) – packs cardboard.

6 PCs. – blisters (4) – packs cardboard.

Hard gelatin capsules, size No. 0, with case and cap, white contents of capsules – white powder.

1 capsule contains:

azithromycin dihydrate (in terms of azithromycin) 500 mg

Auxiliary substances: lactose anhydrous, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methyl paraben, propyl paraben, gelatin.

3 PCs. – blisters (1) – packs cardboard.

3 PCs. – blisters (2) – packs cardboard.

3 PCs. – blisters (3) – packs cardboard.

3 PCs. – blisters (4) – packs cardboard.

Pharmacological action:

Broad-spectrum antibiotic from the group of macrolides, a derivative of azalide. When creating in the focus of inflammation of high concentrations has a bactericidal effect.

Active against gram-positive cocci: Streptcccus pneumniae, Streptcccus pygenes, Streptcccus agaactiae, streptococci groups C, F, and G viridans Staphycccus, Staphycccus aureus gram negative bacteria: Haemphius infuenae, Mraxea catarrhais, Brdetea pertussis, parapertussis Brdetea, Leginea pneumphia, Haemphius ducreyi, Campybacter jejuni, Heicbacter pyri, Neisseria gnrrheae, Gardnerea vaginais some anaerobic microorganisms: Bacterides bivius, Cstridium perfringens, Peptstreptcccus spp. it is also active against other microorganisms: Chamydia trachmatis, Mycpasma pneumniae, Ureapasma ureayticum, Trepnema Minify, Brreia burgdferi.

Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics:

Suction

Azithromycin is rapidly absorbed from the digestive tract, due to its resistance to acidic medium and lipophilicity. After receiving Azithral oral dose of 500 mg C max azithromycin in plasma achieved through 2.5-2.96 h 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), into the skin and soft tissues. High concentrations in tissues (10-50 times higher than in blood plasma) and prolonged 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 a low pH environment surrounding lysosomes. This in turn determines the large Vd=31.1 l / kg and the high plasma clearance.

The ability of azithromycin to accumulate mainly in lysosomes is especially important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the sites of infection localization, where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin has no significant effect on their function.

Azithromycin remains in bactericidal concentrations in inflammation within 5-7 days after the last dose, which allowed to develop a short (3-day and 5-day) courses of treatment.

Metabolism

Demetiliruetsa in the liver with formation of inactive metabolites.

Breeding

Removal of azithromycin from blood plasma occurs in 2 stages: T1/2 is 14-20 h in the range from 8 h to 24 h after administration of the drug and 41 h – in the range from 24 h to 72 h, which allows the drug 1 time / day.

Indications:

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

• infections of the upper respiratory tract and ENT organs (angina, sinusitis, tonsillitis, pharyngitis, otitis media)
• infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis)
• scarlatina
• infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses)
• infections of the urogenital tract (gonorrhoeal urethritis and/or cervicitis)
• Lyme disease (borreliosis) – for the treatment of the initial stage (erythema migrans)
• gastric and duodenal ulcer associated with Heicbacter pyri (as part of combination therapy).

Dosage regimen:

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

In infections of the upper and lower respiratory tract, adults are prescribed 500 mg / day in 1 reception for 3 days, the course dose is 1.5 g.

In infections of the skin and soft tissues, adults are prescribed 1 g in the 1st day in 1 reception further-500 mg in 1 reception daily from the 2nd to the 5th days, the course dose is 3 g.

In uncomplicated urethritis and/or cervicitis appoint one 1 g in 1 reception.

In Lyme disease (borreliosis) for the treatment of the initial stage (erythema migrans) appoint 1 g in the 1st day and 500 mg in 1 reception daily from the 2nd to the 5th days (course dose-3 g).

In gastric ulcer and duodenal ulcer associated with Heicbacter pyri, the drug is prescribed 1 g/day for 3 days as part of combination antihelicobacter therapy.

The drug is prescribed for children 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 3 days – 5-10 mg/kg/day (course dose is determined at the rate of 30 mg/kg). In the treatment of erythema migrans dose is 20 mg/kg in the 1st day and 10 mg / kg from the 2nd to the 5th days.

Side effect:

From the digestive system: nausea (3%), diarrhea (5%), abdominal pain (3%) dyspepsia, vomiting, flatulence, melena, cholestatic jaundice, increased activity of hepatic transaminases (1% or less). Children have constipation, anorexia, gastritis.

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

From the Central nervous system: headache, dizziness, drowsiness in children – headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (1% or less).

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

Allergic reactions: rash, photosensitivity, angioedema.

Other: fatigue, candidomycosis of the oral cavity in children-conjunctivitis, itching, urticaria.

Contraindications:

• renal failure
• liver failure
• lactation period (breastfeeding)
• children under 12 months of age
• hypersensitivity to azithromycin and other antibiotics of the macrolide group.

With caution prescribed for arrhythmia (possible ventricular arrhythmia and prolongation of THE Qt interval), pregnancy, as well as children with severe impaired liver or kidney function.

Pregnancy and lactation:

In pregnancy, Azitral can be used when the intended benefit of such therapy significantly exceeds the risk existing in the application of drugs during pregnancy.

When prescribing the drug during lactation breastfeeding should be suspended for the duration of treatment.

Special instruction:

In the case of pass reception, the missed dose should be taken as early as possible and then every 24 h

It should be borne in mind that after discontinuation of the drug allergic reactions in some patients may persist, which requires appropriate therapy and medical supervision.

Between taking Azitral and antacid drugs, it is recommended to observe a break of at least 2 hours.

Overdose:

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

Treatment: symptomatic therapy.

Drug interaction:

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

In the joint application of warfarin and Azitral in the recommended doses, changes in prothrombin time have not been revealed, however, given that the interaction of macrolides and warfarin may increase anticoagulant effect requires control of prothrombin time.

When used together, azithromycin increases the concentration of digoxin.

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

When used together, azithromycin slows down the excretion and enhances the pharmacological effects of triazolam.

When used together, azithromycin slows down the excretion, increases the concentration in blood plasma and increases the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine.

Azithromycin inhibits microsomal oxidation in hepatocytes, slows excretion, increases concentration in the blood serum and enhances the toxicity of carbamazepine, terfenadine, cyclosporine, gexobarbitala, ergot alkaloids, valproic acid, phenytoin, dizopiramid, bromocriptine, theophylline (and other xanthine derivatives), oral hypoglycemic agents.

In a joint application lincosamine weaken the effectiveness of azithromycin, tetracycline and chloramphenicol enhance.

Storage conditions and terms:

List B. the Drug should be stored out of reach of children, in a dry place at a temperature not exceeding 25°C. shelf life – 3 years.