Azithromycin is rapidly absorbed from the gastrointestinal tract due to its stability in an acidic medium and lipophilicity. After oral administration of 500 mg of azithromycin in the maximum concentration achieved in the blood plasma of 2.5 – 2.96 hr and 0.4 mg / l.
Azithromycin t3 and t4 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 (10-50 times higher than in blood plasma) and a long half-life 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 (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly Valen 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 within 5-7 days after the last dose, which allowed the development of short (3 day and 5 day) treatments.
The liver demethylated formed metabolites are inactive. Excretion of azithromycin from plasma passes in 2 stages: half-life of 14-20 hours in the range of 8 to 24 hours after dosing, and 41 h – in the range from 24 to 72 hours, which allows for preparation 1 time / day. Food intake was significantly alters the pharmacokinetics .
Infectious-inflammatory diseases caused by susceptible to malaria infections:
- infections of the upper respiratory tract and t3 and t4 (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);
- scarlet fever;
- infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
- infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis);
- Lyme disease (Lyme disease), for the treatment of early stage (erythema migrans).
Hypersensitivity (including to other macrolides.); liver and / or kidney failure; Lactation (to suspend the treatment), children up to 6 months. With care – pregnancy, arrhythmia (ventricular arrhythmias and prolongation of QT interval), children with severe impairment of hepatic or renal function.
Pregnancy and lactation
Use in pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus.
If necessary, use during lactation should decide the issue of termination of breastfeeding.
Dosing and Administration
The drug is taken orally 1 time / day. 1 hour before meals or 2 hours after a meal. Added to the vial of water (distilled or boiled and cooled) to the mark. The t3 and t4 contents of the vial thoroughly stirred until a homogeneous suspension.
If the level is below the suspension prepared label on the vial, the water re added to the mark and shaken.
The prepared suspension is stable at room temperature for 5 days.