Azithromycin 250mg – 30 capsules (5 packs of 6 capsules)
Antibiotic macrolides, is representative of azalidov. It has a wide range of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of microbial cell protein synthesis. Binding to 50S ribosome subunit, inhibits peptidtranslokazu on the stage of the translation, inhibits protein synthesis and slows the growth and reproduction of bacteria. Acts bacteriostatically. In high concentrations has a bactericidal effect.
It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.
Gram-positive cocci are sensitive to azithromycin: Streptococcus pneumoniae (penicillin-sensitive strains), Streptococcus pyogenes, Staphylococcus aureus (methicillin-sensitive strains); aerobic gram-negative bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhal, Pasteurella multocida, Neisseria gonorrhoeae; some anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.; and also Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.
Microorganisms with acquired azithromycin resistance: aerobic gram-positive microorganisms-Streptococcus pneumoniae (penicillin-resistant strains and strains with average penicillin sensitivity).
Microorganisms with natural resistance: aerobic gram-positive microorganisms-Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis (methicillin-resistant strains), anaerobic microorganisms – Bacteroides fragilis.
Cases of cross-resistance between Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic Streptococcus group a), Enterococcus faecalis and Staphylococcus aureus (methicillin-resistant strains) to erythromycin, azithromycin, other macrolides and lincosamides are described.
Azithromycin has not been used to treat infectious diseases caused by Salmonella typhi (MIC < 16 mg/l) and Shigella spp.
After oral azithromycin is well absorbed and quickly distributed in the body. After a single dose of 500 mg bioavailability is 37% due to the effect of “first pass” through the liver. Cmax in blood plasma is achieved after 2-3 h and is 0.4 mg / l.
Protein binding is inversely proportional to the concentration in the plasma of the blood and is 7-50%. The apparent Vd is 31.1 l / kg. Penetrates cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily permeates through gistogematicalkie barriers and enters the tissue. The concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection – 24-34% more than in healthy tissues.
The drug is metabolized in the liver. Metabolites do not have antimicrobial activity.
T1/2 is very long – 35-50 h. T1/2 from the tissues much more. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mainly unchanged-50% through the intestine, 6% by the kidneys.
Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin: infections of the upper respiratory tract and ENT organs (angina, sinusitis, tonsillitis, pharyngitis, otitis media); infections of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis, pneumonia, including those caused by atypical pathogens); infections of the skin and soft tissues (acne ordinary moderate severity, erysipelas, impetigo, secondary infected dermatoses); uncomplicated urinary tract infections caused by chlamydia trachomatis (urethritis and/or cervicitis); the initial stage of Lyme disease (borreliosis) – erythema migrans (erythema migrans).
For oral administration
The drug is taken orally 1 time / day for 1 hour before or 2 hours after eating, without chewing.
Adults and children over 12 years and weighing more than 45 kg
In infections of the upper and lower respiratory tract, ENT organs, infections of the skin and soft tissues (except for chronic erythema migrans)-500 mg/day for 1 reception for 3 days (course dose – 1.5 g).
With acne of ordinary moderate severity-500 mg 1 time / day for 3 days, then 500 mg 1 time per week for 9 weeks; course dose-6 g. the First weekly dose should be taken 7 days after taking the first
daily dose (8th day from the beginning of treatment), the next 8 weekly doses-at intervals of 7 days.
In acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) – 1 g once.
In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) – 1 g on the 1st day and from the 2nd to the 5th day-500 mg daily (course dose-3 g).
For the treatment of elderly patients over 65 years of age, the same doses are used as for adults. Since this category of patients may have proarrhythmogenic factors, it is necessary to pay special attention to the possibility of developing their arrhythmia and ventricular tachycardia of the “pirouette”type.
In violation of renal function (QC more than 40 ml/min) dose adjustment is not required.
With moderate impairment of liver function dose adjustment is not required.