Broad-spectrum antibiotic. He is the first representative of a new subgroup of macrolide antibiotics – azalide. When creating in inflammation in high concentrations has a bactericidal effect.

For drug sensitive Gram positive cocci; Streptococcus pneumoniae, St.pyogenes, St.agalactiae, streptococci groups C, F and G, St.viridans, Staphylococcus aureus; Gram-negative bacteria; Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B.parapertussis, Legionella pneumonila, H.ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginatis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp .; and Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Activity against Gram-positive bacteria resistant to erythromycin.

Pharmacokinetics

The drug is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic medium and lipophilicity. After oral administration of 500 mg of the maximum concentration (Cmax) of azithromycin in plasma achieved through 2.5-2.96 h and is 0.4 mg / l. Bioavailability is 37%.

The drug was well into the respiratory tract, genitourinary organs and tissues (in particular in the prostate gland), the skin and soft tissue. The high concentration in tissues (10-15 times higher than the blood plasma) and a long half-life (T1 / 2) of azithromycin due to low binding to plasma proteins, and its ability to penetrate into eukaryotic cells and concentrated in a low pH environment, environmental lysosomes. This, in turn, defines a large apparent volume of distribution (Vd) – 31,1 l / kg and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important to eliminate intracellular pathogens. It proved that phagocytes deliver azithromycin localization of infection sites where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissue (on average 24-34%) and correlated 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 of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.

The drug is metabolized in the liver by demethylation.

Excretion of azithromycin from plasma passes in 2 stages: T1 / 2 of 14-20 hours, in the range of 8 to 24 hours after drug administration and 41 hours – in the range from 24 to 72 hours, which allows for preparation 1 time / day. It writes mainly as unchanged – 50% through the gut and 6% – kidneys.

– lower respiratory tract infections – bacterial and typical pneumonia, bronchitis;

– upper respiratory tract infections and upper respiratory tract – tonsillitis, sinusitis, tonsillitis, otitis media;

– urogenital infections – uncomplicated urethritis and / or cervicitis,

– skin and soft tissue infections – folliculitis, boils, carbuncles, acne (Acne vulgaris) impetigo, pyoderma, infected ulcer, infected dermatitis, cellulitis and erysipelas.

– Lyme disease (borreliosis), for the treatment of early stage (erythema migrans);

– gastric and duodenal ulcer disease associated with Helicobacter pylori.

Dosing and Administration
The drug is taken 1 hour before meals or 2 hours after meals, 1 time / day.

Adults with infections of the upper and lower respiratory tract, skin and soft tissue infections – administered with 500 mg / day for 3 days (course dose – 1.5 g).

When Lyme disease (borreliosis), for the treatment of early stage (erythema migrans) appoint 1 g (2 tablets of 500 mg) in 1-day and 500 mg daily from 2 to 5 days (course dose – 3 g) .

In uncomplicated urethritis and / or cervicitis designate single 1 g (2 tablets of 500 mg).

In stomach and duodenum diseases associated with Helicobacter pylori appoint 1 g (2 tablets of 500 mg) daily for 3 days in a combination therapy.

Babies at doses of drug administered at 10 mg / kg body weight one time / day for 3 days. Heading dose – 30 mg / kg body weight.

When treating children erythema migrans administered in a dose of 20 mg / kg body weight in 1 day and 10 mg / kg – from 2 to 5 days.

From the digestive system: – nausea, vomiting, flatulence, abdominal pain, melena, cholestatic jaundice in children constipation, gastritis, candidiasis oral mucosa, lack of appetite; transient increase in liver enzymes;

Cardio-vascular system: palpitation, chest pain.

From the nervous system: dizziness, headache, vertigo, drowsiness, hyperkinesia, anxiety, neurosis, sleep disturbance.

With the genitourinary system: vaginal candidiasis, jade.

Allergic reactions: rash, urticaria, angioedema.

Other: hyperglycemia, arthralgia.

Simultaneous administration of antacids and H2-histamine receptors do not alter the absorption of the drug, but reduce Cmax in the blood of 30%.

With simultaneous use of the drug does not affect the concentration of carbamazepine is not, didanosine, rifabutin and methylprednisolone in the blood.

When co-administered terfenadine and macrolide antibiotics cause arrhythmias and prolongation of QT interval.

While the use of ergot alkaloids can not exclude the risk of ergotism.

In an application with warfarin described cases enhance the effects last.

With simultaneous use of digoxin or digitoxin with azithromycin may be a significant increase in the concentration of cardiac glycosides in plasma and the risk of glycoside intoxication.

At simultaneous application with cyclosporine is recommended to control the content of cyclosporine in the blood.

In an application with lovastatin cases of rhabdomyolysis reported.

While the use of rifabutin increased risk of neutropenia and leucopenia.

With simultaneous use of disturbed metabolism of cyclosporine, which increases the risk of side effects and toxicity caused by cyclosporin.

Special instructions
When you miss a single dose of the drug – the missed dose should be taken as soon as possible, and the next – with breaks in 24 hours.

As with any antibiotic therapy during the treatment with azithromycin, perhaps joining superinfection (including fungal).

Antacids, ethanol and food slow and reduce the absorption of azithromycin therefore recommend that a break of at least 2 hours between azithromycin and the aforementioned reception medicaments.

If necessary, use of the drug during pregnancy is possible only when the intended benefits to the mother increases the potential risk to the fetus.

If necessary, the use of azithromycin in the period of lactation should decide the issue of termination of breastfeeding.

The drug does not affect the ability to drive vehicles and other activities that require high concentration and speed of psychomotor reactions.

Keep out of the reach of children, and it should not be used after the expiration date.

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

Treatment: gastric lavage, symptomatic therapy

Contraindications
Hypersensitivity to macrolide antibiotics, heavy human liver and kidneys, children under 12 years of age and weighing less than 45 kg (for 500 mg tablet) and children up to 3 years (for tablets 125 mg) during pregnancy and lactation