Trade name of the drug: Azit
Active ingredient (INN): azithromycin
Dosage form: 500 mg film-coated tablets
1 tablet contains:
active substance: azithromycin dihydrate (in terms of azithromycin) – 500 mg;
excipients: lactose monohydrate, corn starch, sodium lauryl sulfate, magnesium stearate, microcrystalline cellulose 101, povidone, sodium starch glycolate, purified talc, croscarmellose sodium, aerosil, Wincoat universal WT-1001 (White) coating.
Description: a tablet in the form of a capsule, covered with a white biconvex film shell, with a tear line on one side and smooth on the other. Pharmacotherapeutic group: Antibiotics (macrolide group).
ATX code : J01FA10
Broad-spectrum antibiotic. It is the first representative of a new subgroup of macrolide antibiotics – azalides. When conscious in the focus of inflammation, high concentrations have a bactericidal effect.
Gram-positive cocci are sensitive to the drug; Streptococcus pneumoniae, St. piogenes, St. agalactiae, Streptococcus groups C, F and G, St. viridans, Staphylococcus aureus; gram-negative bacteria; Hacmophilus influenzae, Moraxella catarrhalis, Bordetella perrtussis, B. parapertussis, Legionella pneumopnila, H. ducrei, Campylobacter jejuni, Neisseria gonorrhoeae, and Gardnerella vaginatis; some anaerobic microorganisms: Bacteroides bivius, Closiridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Inactive against erythromycin-resistant gram-positive bacteria.
The drug 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, the maximum concentration of azithromycin in the blood plasma is reached after 2.5-2.96 hours and is 0.4 mg / l. Bioavailability is 37%.
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. The high concentration in tissues (10-15 times higher than blood plasma) and a long half-life are due to the low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a low pH environment surrounding lysosomes. This, in turn, determines a large apparent volume of distribution (31.1 L / kg) and a high plasma clearance. The ability of azithromycin accumulates, mainly in lysosomes, it 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 inflammatory focus for 5-7 days after the last dose, which made it possible to develop short (3-day and 5-day) courses of treatment.
The elimination of azithromycin from blood plasma takes place in 2 stages: the elimination half-life 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.
Indications for use
Infectious and inflammatory diseases caused by pathogens sensitive to the drug:
– infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, otitis media);
-infection of the lower parts of the respiratory tract (bacterial and typical pneumonia, bronchitis);
– infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses).
– infections of the urogenital tract (uncomplicated urethritis and / or cervicitis);
– Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
– whitening of the stomach and duodenum associated with Helicobacter Pylori.
Method of administration and dosage
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, infections of the skin and soft tissues – appoint 500 mg / day for 3 days (course dose – 1.5 g).
In Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans), 1 g is prescribed on day 1 and 500 mg daily from days 2 to 5 (course dose – 3 g).
For uncomplicated urethritis and / or cervicitis, 1 g is prescribed once.
For diseases of the stomach and duodenum associated with Helicobacter pylori , 1 g per day is prescribed for 3 days as part of a combination therapy.
Children are prescribed the drug in doses of 10 mg / kg body weight 1 time / day for 3 days. Heading dose – 30 mg / kg body weight.
In the treatment of erythema migrans, children are prescribed at a dose of 20 mg / kg of body weight on day 1 and 10 mg / kg from 2 to 5 days.
From the digestive system : possible – nausea, vomiting, flatulence, abdominal pain, melena, cholestatic jaundice, constipation in children, gastritis, candidiasis of the oral mucosa, lack of appetite; transient increase in the activity of liver enzymes;
From the cardiovascular system: palpitations, chest pain.
From the nervous system: dizziness, headache, vertigo, drowsiness, hyperkinesia, anxiety, neurosis, sleep disturbance.
From the genitourinary system: vaginal candidomycosis, nephritis.
Allergic reactions: rash, urticaria, angioedema.
Others: hyperglycemia, arthralgia.
Hypersensitivity to antibiotics of the macrolide group, severe liver and kidney dysfunctions, children under 12 years of age and weighing less than 45 kg and children under 3 years of age, pregnancy and lactation.
The simultaneous administration of antacids and blockers of histamine H 2 -receptors does not change the absorption of the drug, but reduce C max in the blood by 30%.
With simultaneous use, the drug does not affect the concentration of carbamazepine, didanosine, rifabutin and methylprednisolone in the blood.
When terfenadine and macrolide antibiotics are taken together, they cause arrhythmia and prolongation of the QT interval.
With simultaneous use with ergot alkaloids, the risk of developing ergotism cannot be excluded.
With simultaneous use with warfarin, cases of enhancement of the effects of the latter are described.
With the simultaneous use of digoxin or digitoxin with azithromycin, a significant increase in the concentration of cardiac glycosides in the blood plasma and the risk of developing glycosidic intoxication are possible.
When used simultaneously with cyclosporine, it is recommended to control the content of cyclosporine in the blood.
With simultaneous use with lovastatin, cases of the development of rhabdomyolysis have been described.
With simultaneous use with rifabutin, the risk of developing neutropenia and leukopenia increases.
With simultaneous use, the metabolism of cyclosporine is disrupted, which increases the risk of developing side and toxic reactions caused by cyclosporine.
If one dose of the drug is missed, the missed dose should be taken as early as possible, and the subsequent ones should be taken at intervals of 24 hours.
As with any antibiotic therapy, during treatment with azithromycin, it is possible to add superinfection (including fungal).
Antacids, ethanol and food slow down and reduce the absorption of azithromycin, therefore it is recommended to observe a break of at least 2 hours between taking azithromycin and the above drugs.
If necessary, the use of the drug during pregnancy is possible only in cases where the intended benefit to the mother increases the potential risk to the fetus.
If it is necessary to use azithromycin during lactation, the question of stopping breastfeeding should be resolved.
The drug does not affect the ability to drive vehicles and other activities that require a high concentration of attention and speed of psychomotor reactions.
The drug should be stored out of the reach of children and not used after the expiration date.
Symptoms: nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: gastric lavage, the appointment of activated carbon, symptomatic therapy.
Tablets 500 mg, 3 tablets in a blister.
Store in a dry, dark place at a temperature not exceeding 25 ° C.
Conditions of dispensing from pharmacies