Broad-spectrum antibiotic. It is the first representative of a new subgroup of macrolide antibiotics – azalides. When creating high concentrations of inflammation in the focus, it has a bactericidal effect.
Gram-positive cocci are sensitive to the drug; Streptococcus pneumoniae, St. pyogenes, St. agalactiae, streptococci of 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 .; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Inactive against gram-positive bacteria resistant to erythromycin.
The drug is rapidly absorbed from the gastrointestinal tract, due to its resistance to acidic environment and lipophilicity. After oral administration of 500 mg, the maximum concentration (Cmax) of azithromycin in the blood plasma reaches after 2.5-2.96 hours and is 0.4 mg / L. Bioavailability is 37%.
It penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular the prostate gland), into the skin and soft tissues. A high concentration in tissues (10-15 times higher than blood plasma) and a long half-life (T1/2) 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 distribution volume (Vd) of 31.1 l / kg and a high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to places of localization of the 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 the high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin persists in bactericidal concentrations in the focus of inflammation for 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.
The excretion of azithromycin from blood plasma takes place in 2 stages: T1/2 is 14-20 hours, in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows you to use the drug 1 time / day.
It is excreted mainly in unchanged form – 50% through the intestines, 6% – by the kidneys.
Indications for use
Infectious and inflammatory diseases caused by pathogens sensitive to the drug:
- lower respiratory tract infections – bacterial and typical pneumonia, bronchitis;
- infections of the upper respiratory tract and ENT organs – tonsillitis, sinusitis, tonsillitis, otitis media;
- infections of the urogenital tract – uncomplicated urethritis, and / or cervicitis, cervicovaginitis and salpingitis;
- infections of the skin and soft tissues – folliculitis, boils, carbuncles, acne (Acne vulgaris) impetigo, pyoderma, infected ulcers, infected dermatitis, cellulitis and erysipelas;
- Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
- diseases of the stomach and duodenum associated with Helicobacter pylori.
Dosage and administration
The drug is taken 1 hour before a meal or 2 hours after a meal, 1 time / day. Adults with infections of the upper and lower respiratory tract, infections of the skin and soft cells are prescribed 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 the 1st day and 500 mg daily from the 2nd to 5th days (course dose is 3 g).
With uncomplicated urethritis and / or cervicitis, 1 g is prescribed once.
In diseases of the stomach and duodenum, associated with Helicobacter pylori is prescribed 1 g per day for 3 days as part of combination therapy.
Children are prescribed the drug in doses of 10 mg / kg body weight 1 time / day for 3 days. The course dose is 30 mg / kg body weight.
In the treatment of erythema migrans, children are prescribed a dose of 20 mg / kg body weight on the 1st day and 10 mg / kg on the 2nd to 5th day.
From the digestive system: possible – nausea, vomiting, flatulence, abdominal pain, melena, cholestatic jaundice, in children constipation, gastritis, candidiasis of the oral mucosa, lack of appetite; transient increase in liver enzyme activity;
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.
Hypersensitivity to macrolide antibiotics, severe liver and kidney dysfunction, children under 12 years old and weighing less than 45 kg (for 500 mg capsules) and children under 3 years (for capsules), pregnancy and lactation.
The simultaneous administration of antacids and histamine H2 receptor blockers does not alter the absorption of the drug, but reduce Cmax 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 lengthening of the QT interval.
With the simultaneous use of ergot alkaloids, the risk of developing ergotism cannot be ruled out.
With simultaneous use with warfarin, cases of increased effects of the latter have been described.
With the simultaneous use of digoxin or digitoxin with azithromycin, a significant increase in the concentration of cardiac glycosides in blood plasma and a risk of developing glycoside intoxication are possible.
With simultaneous use with cyclosporine, it is recommended to control the content of cyclosporin in the blood.
With simultaneous use with lovastatin, cases of the development of rhabdomyolysis are described.
With simultaneous use with rifabutin, the risk of developing neutropenia and leukopenia increases.
With simultaneous use, cyclosporine metabolism is disrupted, which increases the risk of adverse and toxic reactions caused by cyclosporine.
If you miss one dose of the drug, the missed dose should be taken as soon as possible, and the next ones should be taken at intervals of 24 hours.
As well as during any antibiotic therapy, during treatment with azithromycin, superinfection (including fungal infection) is possible.
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 medicines.
If necessary, the use of the drug during pregnancy is possible only in cases where the intended benefits to the mother outweigh the potential risk to the fetus.
If necessary, the use of azithromycin during lactation should decide on the termination of breastfeeding.
The drug does not affect the ability to drive vehicles and other activities that require a high concentration of attention and the 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.
Capsules of 250 mg and 500 mg in a blister pack.
In a dry and dark place, at a temperature of no higher than 25°C.
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