Azithromycin (Sumamed): dosage form for intravenous administration. Azithromycin (Sumamed): dosage form for intravenous administration Can I give to children

Nonikov V.E., Konstantinova T.D., Makarova O.V., Evdokimova S.A.

The epidemiological situation in recent years has been characterized by an increased etiological significance of pathogens such as mycoplasma and chlamydia, widespread sensitization of the population to penicillin derivatives and sulfonamides, and a significant increase in the resistance of many microorganisms to the most commonly used antibiotics. To a large extent, the increase in resistance was the result of many years of routine use of co-trimoxazole and semi-synthetic tetracyclines in outpatient practice. In recent years, fluoroquinolones have become more widely used in polyclinics - the result was the formation of strains resistant to these drugs.

The first of the macrolides, erythromycin, was created in 1952, but drugs of this series were rarely used until the dramatic outbreak of legionella pneumonia (80s of the 20th century), accompanied by a 30% mortality rate. Quite quickly it was found that macrolides are the best drugs for the treatment of infections caused by intracellular infectious agents (legionella, mycoplasma, chlamydia), and this led to the widespread use of this group of antibiotics. A number of new drugs for oral and parenteral use have been created, differing in terms of pharmacokinetics and pharmacodynamics.

The basis of the chemical structure of macrolides is the macrocyclic lactone ring. Depending on the number of carbon atoms in the lactone ring, 14-membered (erythromycin, clarithromycin, roxithromycin), 15-membered (azithromycin) and 16-membered (josamycin, midecamycin, spiramycin) macrolides are isolated.

Azithromycin belongs to the azalide subclass because one carbon atom in its ring is replaced by a nitrogen atom. The structural features of individual drugs determine differences in pharmacokinetic characteristics, tolerability, the possibility of drug interactions, as well as some features of antimicrobial activity. Azithromycin is characterized by unique cellular kinetics, rapid and intense penetration into cells and interstitial tissues, high levels of antibiotic distribution in tissues and relatively low levels in the blood.

Azithromycin well suppresses gram-positive (pneumococci, streptococci, staphylococci) and gram-negative (moraxella, Haemophilus influenzae) microorganisms and intracellular agents (chlamydia, mycoplasma, legionella, ureaplasma). Other macrolides (except clarithromycin) are less active against Haemophilus influenzae. Given that in the etiological structure of community-acquired pneumonia, pneumococci, Haemophilus influenzae, mycoplasma, chlamydia take the leading positions, and exacerbations of chronic bronchitis (chronic obstructive pulmonary disease) are usually caused by pneumococci, Haemophilus influenzae, moraxella (less often - mycoplasma and chlamydia), it is becoming clear that azithromycin is often the antibiotic of choice for the treatment of pulmonary patients.

In the countries of Western and Southern Europe, the widespread use of macrolides has led to an increase (up to 30%) in the resistance of pneumococci to them. Corresponding indicators of resistance in our country, according to various estimates, do not exceed 4-8%. Features of azithromycin are determined not only by the spectrum of action, but also by the creation of high concentrations in the lung parenchyma and alveolar macrophages. Comparison of the concentrations created in various biological media shows that the concentration of azithromycin in the lung parenchyma is 8-10 times, and in alveolar macrophages 800 times higher than in blood serum. Thus, this drug should be highly effective in the treatment of pulmonary pathology.

Azithromycin remains in the focus of infection for 4-5 or more days, depending on the dose and tissue structure. Due to the release of the antibiotic from phagocytes during their destruction, the concentration in the focus of infection rapidly increases. High intracellular penetration and accumulation in cells and infected tissues determines the effectiveness of azithromycin, which exceeds the effect of other antibiotics, in infections caused by intracellular pathogens, including pathogens of dangerous infectious diseases (brucellosis, tularemia, etc.).

A feature of the pharmacodynamics of macrolides is a long-term post-antibiotic effect, due to which, when using an antibiotic in minimal inhibitory concentrations, the effect of the antibiotic continues after its withdrawal. With regard to azithromycin, a post-antibiotic effect lasting up to 90 hours is considered proven, and this allows to reduce the duration of antibacterial treatment.

Allergic sensitization to macrolides is relatively rare. Among the side effects, gastrointestinal manifestations predominate and, perhaps, some of them are due to the ability of macrolides to increase intestinal motility. Side effects are more frequent with erythromycin. Toxic and allergic side effects are rare with azithromycin.

Azithromycin is approved for medical use in our country in several dosage forms: capsules of 0.25 g, tablets of 0.5 g, powder for suspension 2.0 g, powder for injections of 0.5 g. Thus, the antibiotic can be used orally, intravenously and in stepwise therapy. The drug is convenient in terms of dosing regimen (administered once a day). Given the long post-antibiotic effect of azithromycin, this antibiotic has often been (and is) used in short 3-5 day courses. Dosage form - powder for the preparation of a suspension (2.0 g of azithromycin) involves treatment with a single dose of an antibiotic.

Features of pharmacokinetics allow the use of azithromycin once a day. Naturally, drugs used once or twice a day have greater compliance and are readily used by patients. There are various regimens for oral administration of azithromycin. The most common dosage in the treatment of pulmonary diseases is 500 mg on the first day of treatment and 250 mg every 24 hours for the next 4 days. With this scheme, the duration of treatment for pneumonia is 5 days. The treatment time for pneumonia caused by common bacterial agents (pneumococci, streptococci, Haemophilus influenzae, etc.) can be reduced to three days if the daily dose is 500 mg. The duration of treatment for pneumonia caused by mycoplasma and chlamydia is 14 days, and for legionella pneumonia - 21 days.

Own experience in the use of azithromycin for 15 years is based on the treatment of more than 1500 patients with pneumonia with this antibiotic, and all the described oral therapy regimens, stepwise therapy, treatment with azithromycin in combination with b-lactam antibiotics were used with high efficiency.

According to the Department of Pulmonology of the Central Clinical Hospital in 1984, macrolides (only erythromycin was used) accounted for only 9% of the antibiotics used. In 2004, the frequency of their use tripled (27.3%), second only to b-lactam antibiotics. Five oral preparations were used, of which azithromycin was used most frequently (80%). A significant frequency of prescription of macrolides is explained by the rise in the incidence of chlamydial and mycoplasmal infections, as well as the widespread use of combinations of macrolides with b-lactam antibiotics when etiological interpretation is impossible.

According to microbiological studies of sputum, pneumococcus still dominates (52.1%) as the leading etiological agent of respiratory infections. In addition to pneumococcus, cultures of viridescent streptococcus, Haemophilus influenzae were isolated from sputum. Gram-negative microorganisms and staphylococci were rarely detected. In recent years, the frequency of mycoplasma and chlamydial infections has increased significantly, and intracellular agents are often the cause of epidemic foci in families and groups.

Indications for the appointment of azithromycin are infections of the upper respiratory tract (tonsillopharyngitis, acute otitis media, sinusitis), as well as bronchitis and community-acquired pneumonia. The so-called SARS are caused by intracellular agents-viruses, mycoplasma (50% of all cases), chlamydia, legionella. Azithromycin is the best antibiotic to treat most of them. The infection is often transmitted from person to person (in recent years, several family and work outbreaks of mycoplasma and chlamydial pneumonia have been observed). An etiological diagnosis is possible by detecting specific IgM class antibodies in the blood serum or by seroconversion (in the study of paired sera).

The study of the clinical manifestations of mycoplasmal pneumonia showed that a prodromal period is characteristic in the form of malaise and respiratory syndrome, manifested by rhinopharyngitis, tracheobronchitis, and less often otitis media. The development of pneumonia is rapid, sometimes gradual with the onset of fever or subfebrile condition. Chills and shortness of breath are not typical. Cough, often unproductive or with mucus sputum, is the dominant symptom. In 30-50% of patients, a paroxysmal, unproductive, excruciating, whooping cough of a low timbre is typical, sometimes accompanied by difficulty in inhaling. These cough paroxysms are often caused by the development of the phenomenon of tracheobronchial dyskinesia, in which the mobility of the pars mempanacea of ​​the trachea and large bronchi increases significantly. On auscultation, dry and/or local moist rales are heard. Crepitus and signs of compaction of the lung tissue are absent. Pleural effusion rarely develops. Extrapulmonary symptoms are not uncommon: myalgia (usually pain in the muscles of the back and hips), profuse sweating, muscle weakness, arthralgia, skin and mucous lesions, gastrointestinal disorders, headaches, and sometimes insomnia.

X-ray examination reveals a typical pneumonic infiltration of the lung parenchyma (usually focal and multifocal), however, in 20-25% of patients only interstitial changes are determined, and occasionally no pathology is noted on standard radiographs (especially those performed in a hard mode). Therefore, in cases where clinically pneumonia is not in doubt, and the results of radiography are not conclusive, computed X-ray tomography can be used, which provides confirmation of the diagnosis due to viewing the image in various modes and the absence of hidden zones for the method.

The phenomenon of tracheobronchial dyskinesia is detected when performing forced expiratory lung tests. Characteristic is the appearance of additional "steps" on the spirographic curve. More precisely, the presence of this syndrome can be proved by roentgenoscopy of the trachea with a cough test.

The leukocyte formula of peripheral blood is usually not changed. Slight leukocytosis or leukopenia is possible. Occasionally, unmotivated anemia is noted. Blood cultures are sterile, and sputum is uninformative.

For mycoplasmal pneumonia, the dissociation of some clinical signs is characteristic: high fever in combination with a normal leukocyte formula and mucous sputum; low subfebrile condition with heavy sweats and severe asthenia. Thus, mycoplasmal pneumonia has certain clinical features, the comparison of which with the epidemiological situation allows you to make the right decision about choosing an antibacterial drug.

With chlamydial infection, the development of pneumonia is often preceded by a respiratory syndrome in the form of malaise and pharyngitis, which occurs with a dry cough at normal or subfebrile body temperature. The development of pneumonia is subacute with chills and fever. Cough quickly becomes productive with purulent sputum. On auscultation in early dates listen to crepitus, a more stable sign is local moist rales. With lobar pneumonia, a shortening of percussion sound, bronchial breathing, and increased bronchophony are determined. Chlamydial pneumonia can be complicated by pleurisy, which is manifested by characteristic pleural pain, pleural friction noise. With pleural effusion, dullness is determined percussion, and when listening - a sharp weakening of breathing. Some patients tolerate high fever relatively easily. In children, a pertussis-like course of chlamydial pneumonia is described, which is associated with the frequent development of tracheobronchial dyskinesia, which is hallmark and in pulmonary chlamydia in adults. Of the extrapulmonary manifestations, sinusitis is more common (5%), and myocarditis and endocarditis are much less common. Radiographic findings are extremely variable. Reveal infiltrative changes in the volume of one or more lobes, often infiltration is interstitial in nature. In typical cases, the leukocyte formula is not changed, but leukocytosis with a neutrophilic shift is often noted.

Patient H., aged 15, was hospitalized in the pulmonology department on the 7th day of illness. There is an outbreak of an acute respiratory infection at the school. In the class, 5 out of 25 students were diagnosed with pneumonia. The patient was diagnosed with pneumonia on the 2nd day of illness. Started therapy with amoxicillin/clavulanate 2.0 g/day. Treatment for 5 days without effect. All days the fever persisted up to 38-38.5°C. On admission he was in a state of moderate severity. Body temperature 38.5°C. Clinical and radiographic findings are consistent with right-sided lower lobe pneumonia. In the blood test, moderate leukocytosis without a neutrophilic shift in the leukocyte formula. Azithromycin was prescribed orally at 500 mg/day. A few hours after the first dose of the antibiotic, the body temperature returned to normal. During the examination in the blood serum, antibodies to chlamydia of the IgM class were found in high titers. Azithromycin was used for 12 days. The outcome is recovery.

In this clinical observation, the basis for a correct clinical assessment and selection of an effective antibiotic (azithromycin) was a characteristic epidemiological history and the absence of an effect from 5-day therapy with a boosted b-lactam antibiotic at an effective dose.

In addition to monotherapy with azithromycin, this antibiotic is often prescribed in combination with b-lactam drugs. If a patient is hospitalized for moderate to severe pneumonia, a de-escalation tactic is often practiced, involving the use of a combination of antibiotics for initial therapy, and usually a combination of a b-lactam drug (aminopenicillins, cephalosporins, carbapenems) with a macrolide, which is prescribed based on the possibility of legionella or chlamydia infections. Subsequently, after the diagnosis is clarified, one of the drugs is canceled.

Several years ago, on the 4th day of illness, patient N., 42 years old, was hospitalized in our department. Upon admission, the patient's condition was severe: body temperature 39.0°C, unstable hemodynamics, respiratory rate - 36 per 1 min. Clinically and radiologically - bilateral multilobar (infiltration of 3 lobes) pneumonia. Leukocytosis 22.0 with a stab shift of 30%. Antibacterial therapy was prescribed: meropenem 4.0 g/day. intravenously in combination with azithromycin 500 mg / day. orally. Pressor amines and glucocorticosteroids were used intravenously, oxygen therapy was used. Hemodynamic parameters were stabilized within 4 hours and further use of steroids and pressor amines was discontinued. Etiologically, pneumonia was deciphered as legionella (antibodies to legionella were found in the blood serum in a titer of 1:1024). Duration of treatment with azithromycin - 18 days, meropenem - 4 days (the drug was canceled after the diagnosis of legionellosis was established). Oxygen therapy was used for 7 days. The outcome is recovery.

It can reasonably be assumed that the outcome of the disease in the observed patient would be doubtful if empirical antibiotic therapy was carried out only with meropenem, and azithromycin was prescribed only after the legionella nature of pneumonia was established.

This observation prompted us to conduct de-escalation antibiotic therapy (b-lactam antibiotic + macrolide) in almost half of patients with pneumonia and in all cases of treatment of severe pneumonia.

In severe pneumonia, antibiotics are given intravenously. With intravenous use, azithromycin is dosed at 500 mg every 24 hours.

The cost of antibiotic therapy, which can be quite significant, must be reckoned with. In recent years, the so-called stepwise therapy has been successfully used. When using azithromycin according to this technique, treatment begins with intravenous antibiotic 500 mg every 24 hours. Upon reaching the clinical effect (usually after 2-3 days), when antibiotic therapy provided an improvement in the patient's condition, accompanied by a decrease or normalization of body temperature, a decrease in leukocytosis, it is possible to switch to oral administration of azithromycin (if good absorption is expected) at 0.25-0, 5/24 hours. With the high efficiency of such a technique, it is less expensive not only due to the difference in prices for parenteral and tablet preparations, but also due to a decrease in the consumption of syringes, droppers, and sterile solutions. Such therapy is more easily tolerated by patients and less often accompanied by side effects.

Intravenous and stepped application of azithromycin is usually used in the treatment of severe pneumonia. In the treatment of other bronchopulmonary infections, as a rule, oral therapy can be limited.

These data and our own long-term experience indicate that azithromycin currently occupies one of the main positions in the treatment of bronchopulmonary infections.

Literature
1. Practical guide on anti-infective chemotherapy (Edited by L.S. Strachunsky, Yu.B. Belousov, S.N. Kozlov) // Smolensk, IACMAH, 2007.- 464 p.
2. Nonikov V.E. Atypical pneumonia: the rebirth of macrolides // New Medical Journal.-1995.-No. 1.-p.5-7
3. Nonikov V.E. Tactics of antibacterial chemotherapy of pneumonia //RMJ.-1997.-Vol. 5.-No. 24,- p.1568-1578
4. Nonikov V.E. Macrolide antibiotics in pulmonological practice // Atmosphere: pulmonology and allergology.-2004.- No. 2 (13).- p.24-26
5. Bartlett J. Pocket Book of Infectious Diseases Therapy // Lippincott Williams & Wilkins.-2005-6.- 349p.
6. Zackom H. Pulmonary Differential Diagnosis //W.B.Saunders.- 2000.- 885 p

A popular and reliable modern antibiotic, presented in almost any pharmacy, is Azithromycin. Instructions for use of the drug indicates that the drug belongs to the category of antimicrobial compounds that are extensive in their effect. Belongs to the group of macrolides. The name of the drug was given by the active ingredient - it is azithromycin, which is part of the azalide class. The drug in pharmacies is represented by capsules, tablets and suspension. Suitable for the treatment of children and adults.

What is for sale?

Most often, patients visit a pharmacy to buy Azithromycin tablets. Instructions for use and packaging of the drug contain a mention of the amount of the active ingredient in a single dose. There are three release options: 125, 250, 500 mg. 250 mg is an option that is produced not only in tablets, but also in capsules. Distinctive features- additional components used in the manufacture of the drug. A complete list must be indicated in the instructions for use. "Azithromycin" may contain substances intolerable to a particular patient, so it is important to study the accompanying documentation.

Manufacturers most often use as auxiliary compounds:

• cellulose;
• lactose;
• povidone;
• magnesium stearate;
• aerosil.

Drug dynamics

The manufacturer in the instructions for use of "Azithromycin" indicates that the drug belongs to the class of azalides, that is, medications based on macrolides. The main effect of the application is bacteriostatic. Soon after penetration into the body, the active substance enters into strong bonds with the components of the ribosome, which means it slows down the translation of the peptide translocase. In the molecule of a pathological microorganism, the processes of formation of protein structures are inhibited, growth and reproduction are prevented, so colonies cannot develop.

The manufacturer also indicates in the instructions for use: "Azithromycin" in a high dose can have a bactericidal effect.

The effectiveness of the drug shows both against pathogens that can invade the cell, and when infected with extracellular forms. Activity has been identified in relation to certain representatives of the following species and groups:

• staphylo-, strepto-, peptrostreptococci;
• chlamydia;
• clostridia;
• Neisseria;
• legionella;
• hemophilic bacillus;
• moraxella;
• campylobacter;
• bordetella;
• urea-, mycoplasmas;
• mycobacteria;
• treponema.

Drug kinetics

According to the instructions for use, "Azithromycin" (500 mg capsules, tablets, powder for suspension) is based on an active ingredient that is absorbed into the body at a relatively high rate after oral administration. The substance is lipophilic, showing an increased level of resistance to acids. Bioavailability with a single use of 500 mg in food is estimated at 37%. The indicator is determined by the passage through the liver cells. The highest parameters in the blood of azithromycin are observed at the level of 0.4 mg/l. The time period required to achieve this indicator is from two and a half to three hours.

As follows from the instructions for use of "Azithromycin", 500 mg of the active ingredient at the initial intake is orally distributed in a volume varying about 31.1 l / kg. In the tissues, cells of the body, the substance accumulates more actively than in the blood plasma, 10-50 times.

Studies have shown that in any dosage (150, 250, 500 mg) "Azithromycin" (in the instructions for use, the manufacturer draws attention to this fact) is able to penetrate the barriers present in the body. Quite quickly, the active component enters soft tissues and organs of the respiratory system, reproductive, urinary system, prostate, skin. The cumulative effect is observed in environments that are characterized by low level acidity. "Azithromycin" is able to accumulate in lysosomes. This effect has found its application for the eradication of pathogens that invade cell cavities.

biological chemistry

In the body, the active component of the drug is carried by macrophages, phagocytes, certain categories of leukocytes. The instructions for use for "Azithromycin" (500 mg capsules and other release options) indicate the ability to penetrate cell membranes. As it was possible to reveal during specific studies, in the infected focus, the active compound accumulates in an amount that is a quarter, sometimes even a third, higher than the content in other tissues of the body. Specific indicators are determined by the intensity of the inflammatory process.

If you take tablets, syrup, capsules "Azithromycin" in a course of food according to the instructions for use (500 mg or another volume - as recommended by the doctor), after the last dose is received in the tissues and cells of the body, the active substance remains in sufficient concentrations to have a bactericidal effect, a few more days: from five to seven.

The level of binding to plasma proteins in a particular case is almost impossible to predict. In the instructions for use of Azithromycin capsules, tablets and suspensions, the manufacturer indicates that in some patients the parameter was estimated at only 7%, while in others it reached half of the entire dose used. The degree of entry into connection with plasma proteins is inversely proportional to the concentration of the components of the agent in the circulatory system.

Once in the liver cells, azithromycin enters into chemical reactions, as a result of which products are formed that do not have a pharmacological effect on the patient's body. Plasma clearance, as indicated in the instructions for use of "Azithromycin" in capsules, tablets, powder, is estimated at 630 ml / min. The withdrawal from the circulatory system occurs in two stages:

• 14-20 hours in the interval 8-24 hours after using the medication for food;
• 41 hours - in the interval 24-72 hours after administration.

Elimination of about half of the substance that enters the body is carried out through the bile ducts; the agent leaves the body without being transformed. About 6% are excreted in urine.

In the instructions for use of "Azithromycin" (500 mg and other dosage options), the manufacturer indicates a strong influence on the kinetics of the drug from food. If you use a substance during a meal, the highest rates concentrations are more than doubled. In the elderly, predominantly in men, the pharmacological kinetics remain the same as in younger patients. In women, usually the highest concentrations increase by a third, and sometimes by half, relative to typical middle-aged patients, young people.

When will it help?

The instructions for use of "Azithromycin" (500 mg, 125 and 250 mg) indicate the following diagnoses, in which the drug shows a pronounced effectiveness:

• Lyme disease (initial stage);
• cervicitis;
• tonsillitis;
• urethritis;
• erysipelas;
• dermatosis;
• bronchitis;
• pulmonary inflammation;
• impetigo;
• angina;
• otitis;
• sinusitis.

Before taking it is reasonable to conduct a test to establish the sensitivity of pathological microorganisms to azithromycin. Efficiency (special attention is paid to this in the instructions for use of "Azithromycin" - capsules of 250, 125 and 500 mg, tablets, suspensions) is expressed only if the disease is caused by strains sensitive to the antimicrobial drug.

Restrictions

The manufacturer indicates that Azithromycin is not intended for use by persons suffering from hypersensitivity to drugs from the macrolide category.

Particular attention should be paid to patients who have established insufficiency of the functioning of the kidneys and liver. Such health problems are not absolute contraindications to use, but improper use can provoke adverse reactions.

Rules and volumes

The choice of dosage, format must be subordinated to:

• diagnosis;
• sensitivity of pathological forms of life to an antibiotic;
• individual characteristics of the patient (weight, age).

As a rule, the doctor sends for tests to establish the specifics of the pathological microflora. Based on the information received, the doctor prescribes the drug, writes out a prescription for it (in any form, the drug is not dispensed from pharmacies without it, as indicated in the instructions for use). Adults "Azithromycin" is often recommended in the form of tablets, capsules. The manufacturer advises to use the medicine in this form one hour before a meal or 120 minutes after it. "Azithromycin" is used once a day.

If infection of the skin, soft tissues, organs of the respiratory system is established, for adult patients the optimal course format is:

• 0.5 g on the first day;
• 0.25 g for another 2-5 days.

How is borreliosis treated at the initial stage? According to the instructions for use, "Azithromycin": 250 mg (four capsules) or 500 mg (two capsules) on the first day, then the dosage is halved.

When compiling a regimen for minors, it is necessary to focus not only on age, but also on body weight. The optimal format is a suspension for children. The instructions for use of "Azithromycin" indicate that with a weight of more than 10 kg on the first day, the agent is used in an amount of 10 mg per kilogram of weight, then the dosage is halved and maintained at this level until the end of the program. An alternative option is a three-day course, each day the dose is calculated as 10 mg per kilogram of body weight.

Features of use

The manufacturer draws attention to the fact that if a dose is missed, it is necessary to replenish this amount as soon as possible. The next dose should be a day after the use of the missed amount.

As tests have shown - and this is recorded in the instructions for use - "Azithromycin" (250 mg, 500, 125 mg) is characterized by increased resistance to acid influence. The agent is quickly and effectively absorbed when passing through the gastrointestinal tract, penetrates into the skin, other organs and tissues.

An increase in the concentration of azithromycin in the inflammatory focus allows you to achieve a bactericidal effect, the duration of which is up to a week after the last dose is ingested. Therefore, you can use the tool for a very short course, following the instructions for use. Reviews for "Azithromycin" contain information about the effectiveness of the composition, even if they are treated for only three days. Sometimes a five-day intake is necessary, it is almost always enough to achieve a pronounced result.

Patients using an antimicrobial drug in combination with antacids deserve special attention. Between taking these groups of drugs, at least two hours must pass, otherwise the effectiveness of the antibacterial composition will be too low.

Negative effects: what to prepare for?

In general, the drug is well tolerated, so its use is practiced even for the treatment of children. And yet, as can be seen from the responses to the drug (as well as from the text of the instructions for use), "Azithromycin" (suspension, tablets, capsules) can cause:

• vomiting;
• nausea;
• increased gas formation;
• activation of liver enzymes.

In a small percentage of patients, skin rashes were observed during the use of the composition.

If you feel sick and vomit very much, the stool is disturbed, your hearing worsens, the patient probably took too much Azithromycin. To alleviate the condition, urgent gastric lavage is required. Therapy is carried out, focusing on the disturbing symptoms. There is no specific antidote for the antimicrobial drug.

Needs attention!

As stated for different options dosages (125, 500, 250) in the instructions for use, "Azithromycin" for children in the womb can cause some harm, so the use of the drug by pregnant women is allowed only in extremely rare cases. The doctor evaluates the obvious benefits of the medication, possible dangers, informs the woman, only after that they decide on the use of the medication.

Since studies have shown that active ingredients can penetrate into mother's milk, in order to avoid the effect of "Azithromycin" on children, the instructions for use contain an indication of the need to stop breastfeeding for the duration of treatment until the composition is completely removed from the mother's body.

In rare cases, the antimicrobial composition can cause side effects on vision, the nervous system. This forces you to be especially careful during the period of using tablets, when driving vehicles and other units, devices that require increased care. At the same time, there are no strict restrictions on such activities, since the risk of developing negative side effects is assessed as low.

Mutual influence

Digoxin and azithromycin in combination can cause an increase in serum P-glycoprotein. In some cases, the amount of cardiac glycosides in the blood plasma increases significantly, which means that the likelihood of glycoside poisoning increases.

The combination of zidovudine and azithromycin can cause a low efficiency of the first compound, since it is possible to change the kinetics with a single use of one gram of azithromycin in food or multiple doses of 0.6-1.2 g. It is known that the combination of azithromycin and zidovudine can cause an increase in mononuclear cells in the peripheral circulatory system of the active product of zidovudine processing. At the moment, it was not possible to establish the clinical significance of this phenomenon.

To a low degree, azithromycin reacts with cytochrome isoenzymes. The simultaneous use of an antimicrobial composition and ergot alkaloids is accompanied by a risk of ergotism, so the combination of these groups of drugs should be avoided.

Daily use of 0.5 g of azithromycin and 10 mg of atorvastatin does not cause changes in the concentration of the second substance in the circulatory system during the course, but it is known that some patients have recorded rhabdomyolysis when combined with an antimicrobial composition and some statins.

Terfenadine and azithromycin in combination can lead to heart rhythm disturbances, an increase in the QT interval. Ventricular fibrillation is possible against the background of a combination of an antibiotic and disopyramide. Rhabdomyolysis is possible when combined with lovastatin, and in combination with rifabutin, the risk of neutro-, leukopenia increases.

Simultaneous intake of cyclosporine and the drug in question leads to improper processing of the first compound, which means that the risk of poisoning, side effects inherent in cyclosporine, increases.

Antacids, which contain aluminum, magnesium, ethanol, food can reduce the absorption of the antimicrobial substance.

What else to pay attention to?

In the instructions, the manufacturer mentions that the combination of the drug with warfarin can provoke an adjustment in the prothrombin time if the formulations are used at doses higher than those recommended by the manufacturers. At the moment, such cases have not been recorded, but the experience of the combined use of warfarin, macrolides shows that patients require special monitoring and periodic checks of the quality of the circulatory system.

The combination of the drug in question and dihydroergotamine, ergotamine can cause poisoning by the latter. The condition manifests itself as vasospasm, dysesthesia. When combined with triazolam, the clearance weakens, which means that the pharmacological effect becomes more pronounced.

"Azithromycin" can cause slow elimination, an increase in the number of substances in the plasma, as well as toxicity above normal for the following drugs:

• cycloserine;
• coagulants that have an indirect effect on the body;
• methylprednisolone;
• felodipine;
• substances that are oxidized at the microsomal level.

Azithromycin acts more pronounced if the antibiotic is combined with tetracycline, chloramphenicol. A decrease in the effectiveness of the intake is observed with the simultaneous ingestion of the drug in question and lincosamides.

Analogues

The instructions for use of "Azithromycin" indicate that the active component of this drug is called the same as the medication itself - azithromycin. Medicines are based on it:

• "Hemomycin";
• "Azimycin";
• "Sumamed".

It is possible to replace the medication in question with Ecomed or Zitrocin.

Based on the diagnosis, the patient's condition, the individual characteristics of the body, the doctor may advise drugs as an alternative:

• "Fromilid";
• "Lecoclair";
• "Rovamycin".

Antibiotics "Macropen" and "Spiramycin" have a good reputation. Recently, Clarithromycin and Erythromycin have been widely used. The drugs "Arvicin" and "Oleandomycin" have a pronounced effect and a wide spectrum of action.

The choice of replacement is best left to the doctor. Incorrect selection of the drug can cause ineffectiveness of therapy, negative side reactions, unpredictable acquisition of immunity to drugs by pathological life forms.

Will it help?

As can be seen from the responses, most often "Azithromycin" is used due to chlamydia, tonsillitis and sinusitis. Attracts the attention of many instructions for the use of "Azithromycin" for children, since the drug is one of those few antimicrobials that can be used before reaching the age of majority. The list of microorganisms sensitive to the active ingredient is quite wide, which means that the agent shows a pronounced effect with a variety of diagnoses.

It is noted that the drug often provokes side effects if used without a doctor's recommendation, at one's own discretion. Children are especially susceptible to them. In the instructions for use of "Azithromycin" (250 mg and other dosage options), the manufacturer draws attention to the need to sell the drug strictly according to the doctor's prescription, but in reality this rule is often not followed. Having decided to use the medicine at your discretion, you need to understand that negative reactions can be very different, often unpredictable, but no one can guarantee the effectiveness of the course. In order not to risk it, it is better to seek help from a doctor.

Usually "Azithromycin" shows a pronounced effect, since the antibacterial agent is strong, effective against different strains. All adverse reactions that appear during the course disappear soon after the completion of the therapeutic program. As can be seen from the responses, few face them: more often "Azithromycin" does not provoke side effects.

Sexually transmitted infections are the scourge of our time. Almost 50% of adults are carriers of dangerous infections. Azithromycin - effective remedy for their destruction.

Azithromycin is a broad-spectrum antibiotic that belongs to the group of macrolides. The main active ingredient is the substance of the same name - a semi-synthetic antibiotic, the first of the azalide subclass.

Azithromycin is actively used to treat various infectious diseases, since the agent has a pronounced bactericidal effect. The main directions of therapy: colds, skin and genital infections. The advantage of the drug is a short list of possible side effects.

Usually, the drug is prescribed in a short course and in small doses, which allows it to be classified as a new generation of antibiotics.

pharmachologic effect

Azithromycin is able to destroy colonies of streptococci (G, CF), gram-positive cocci, anaerobic microbes and gram-negative microorganisms. The bactericidal properties of the drug are well revealed in the treatment of diseases caused by pale treponema, chlamydia, mycoplasmas, ureaplasmas and Borrelia spirochete.

You can prescribe the drug only after laboratory tests. In cases where the disease is caused by different bacteria, it is often necessary to combine Azithromycin with antibiotics of other groups.

The active substances of the drug are rapidly absorbed into the blood, and in full, since azithromycin is resistant to the acidic environment of the stomach. The maximum concentration of components in the plasma is reached 2-3 hours after ingestion.

The drug is able to penetrate into any tissues and fluids, so it continues to fight pathogens for a long time (about a week). This property of the drug makes it possible to treat many diseases with Azithromycin, excluding relapses. Active substances do not violate the natural microflora, which makes the drug safe for different categories of patients.

Advantages

The antibiotic has the most pronounced cumulative ability among all antibacterial drugs. With microbial inflammation, the active substances are deposited in the organs of the reproductive system, the mucosa of the gastrointestinal tract and lungs, the prostate gland and the urethra.

Macrolides persistently accumulate in the cytoplasm and phagolysosomes - the habitat of chlamydia, mycoplasmas and legionella. Namely, these microorganisms have recently increasingly become the cause of urethritis and prostatitis.

The great advantage of Azithromycin is its ability to suppress the reproduction of atypical and intracellular pathogens that are insensitive to most antibiotics. Also, the drug is widely used in the treatment of sexually transmitted infections.

Among all macrolides, Azithromycin has the highest degree of penetration into leukocytes, which increases anti-infective protection. Anti-inflammatory, immunomodulatory and mucoregulatory abilities of drugs have been proven clinically and experimentally.

Due to the unique ability to accumulate in tissues, short courses of Azithromycin are most often prescribed for sexually transmitted infections.

Indications

Azithromycin is one of the few antibiotics approved for children and pregnant women (due to low toxicity). It is widely used for the prevention of inflammation of the pelvic organs.

Often prescribed for such diseases:

• inflammatory processes in the upper and lower respiratory tract, as well as diseases of the ENT organs (sinusitis, tonsillitis, sinusitis, tonsillitis, pneumonia, bronchitis);
• infections of soft tissues and skin (erysipelas, dermatosis, impetigo);
• acute infections that most often occur in children (measles, scarlet fever);
• inflammatory diseases of the genitourinary system;
• Lyme disease.

Sometimes this antibiotic is prescribed for chancroid, non-gonococcal urethritis and inguinal granuloma. In severe forms of infections, intravenous administration of the drug is possible.

Standard reception pattern

The drug should be taken once a day. You need to choose a time one hour before or after a meal. The drug does not cause side effects from the digestive system, but the doctor should be warned about the presence of gastrointestinal diseases.

The standard regimen for taking Azithromycin for infection:

1. One tablet (500 mg) or two tablets (250 mg) once on the first day.
2. 250 mg daily from the second to the fifth/seventh day.
3. Individual pathologies are treated with a single dose of 500 mg of antibiotic ().
4. Three days, 500 mg per day for intestinal infections.

You can not take Azithromycin uncontrollably for sexually transmitted infections and colds.

In recent years, complications (prostatitis, urethritis, epididymitis) are treated with a course of 1-7-14, 1 g per day. Usually the cause of urogenital infection is chlamydia, combined with other microorganisms. This treatment regimen (pulse therapy) reduces the number of relapses to 1.2% in men and 2.5% in women. A similar effect is not feasible with any other macrolides or tetracyclines.

Only laboratory diagnostics allows you to determine the correct dosage, otherwise the treatment will be ineffective or even fatal. Incorrect self-treatment leads to the fact that the symptoms are “blurred” and complicate the diagnosis of the true cause of the disease.

Azithromycin for chlamydia

Therapy for chlamydia may include various drugs. The main ones are macrolides, fluoroquinolones and tetracyclines. Azithromycin is a leader in the treatment of chlamydial infection.

In the treatment of chlamydia, monotherapy is assumed. This is due to the fact that, accumulating in the affected tissues, the active substances do not always adequately interact with other drugs (antimicrobial agents are acceptable). However, it should be remembered that taking Azithromycin exclusively is permissible only at the initial stage of the development of chlamydia.

Even the standard regimen and dosages indicated in the instructions can be dangerous. With improper treatment of chlamydia, the disease becomes chronic. Often self-treatment of infections with antibiotics leads to the development of complications.

1. In the early stage, take one tablet (1 g) daily, two hours before meals.
2. With mild symptoms, drink one tablet on the first day, then 0.5 g for another two to three days. From the fourth to the seventh days appoint 0.25 g.

The patient should receive approximately 3 g of Azithromycin per week. Often this is enough to adequately affect chlamydia. The scheme is acceptable for both women and men, but you should also consult a doctor on this issue. When treating chlamydia with Azithromycin, some side effects may occur: diarrhea, allergic rash, drowsiness, tinnitus, rarely chest pain.

Treatment of ureaplasmosis

It starts only after the analysis for Trichomonas. The causative agent of the disease - ureaplasma - is able to live inside these microorganisms, using them as protection against antibiotics. The results of the analysis help to choose the right treatment regimen.

Possible dosages of Azithromycin for ureaplasmosis:

1. Before treatment with antibiotics, an injection course of immunomodulators should be started. Cycloferon is usually prescribed (once every two days intramuscularly). Injections should be continued during antibiotic therapy.
2. The second stage is bactericidal antibiotics. For these purposes, Oflox is prescribed (400 mg each in the first two days in the morning and evening, the rest of the days, 200 mg each).
3. After a course of bactericidal agents, Azithromycin is prescribed (in the first six days, an hour and a half before breakfast, 1 g of the drug, a break of five days, again 1 g, a break, the third dose of 1 g).

Therapy of ureaplasmosis with Azithromycin takes 15-16 days. Often, along with an antibiotic, antifungal agents are prescribed at 150-400 mg two to three times a day. After a course of antibiotics, restorative therapy should be carried out, the work of the gastrointestinal tract and liver should be normalized. It usually lasts two weeks, includes one drug per tablet per day. Means for strengthening the liver are prescribed for three doses a day before meals.

Treatment of urethritis with antibiotics

With inflammation urethra antibiotics are the most effective. Azithromycin is considered one of the best in therapy.

Benefits of this antibiotic:

• the ability to cross cell membranes;
• rapid absorption and accumulation in tissues;
• prolonged effect (long);
• acid resistance.

With urethritis, this antibiotic is effective due to its ability to inhibit protein synthesis in pathogenic microorganisms. Small doses of the antibiotic can slow down the growth and reproduction of bacteria, and high doses can destroy the colonies and prevent the recurrence of inflammation of the urethra.

Azithromycin is the best choice with urethritis, which is caused by microplasmas, chlamydia, spirochetes, treponemas and ureaplasmas. If the cause is streptococcus, staphylococcus, or enterococcus, Erythromycin should be taken.

With urethritis, the drug is usually prescribed at an early stage. The standard course includes taking one tablet of 0.5 g daily for three days. A course is possible, including taking two tablets of 0.5 g once a day, maintaining an interval.

The antibiotic is best taken before meals, preferably one hour or two hours after. However, with disorders of the gastrointestinal tract, the drug can be drunk with meals. This reduces the absorption rate, which, however, does not affect the effectiveness.

When treating with Azithromycin, all citrus fruits are excluded from the diet: their components, in combination with the active substances of the drug, can disrupt the work of the heart muscle.

Azithromycin for inflammation of the ovaries

- inflammation of the fallopian tubes and ovaries, which is of an infectious nature. It is most common among women 20-30 years old, and poses a serious danger to reproductive function.

With adnexitis, Azithromycin is indicated at the initial stage of the development of the disease, with a subsequent transition to other antibacterial agents (Amoxiclav). To save reproductive function, treatment of adnexitis should be started in a timely manner.

The high effectiveness of the agent against various infections allows for the treatment of acute adnexitis without test results. The efficiency of the drug makes it possible to avoid tubal infertility.

The scheme of treatment of adnexitis with Azithromycin:

1. 500 mg once a week, combined with Amoxiclav.
2. Combination of different drugs: Azithromycin, Metronidazole, Ceftriaxone.

Acute inflammation involves a short course of antibiotics. The drug is well combined with antimicrobial drugs, it is ineffective only for certain types of microbes.

Azithromycin after abortion

After termination of pregnancy, restorative therapy is prescribed.

Recovery after an abortion includes:

• antibiotics that prevent inflammation;
• combined oral contraceptives that restore hormonal levels;
• vitamin supplements that strengthen the immune system.

Antibiotics should be taken anyway. They protect the body from infections, so doctors prescribe strong drugs (, Metronidazole). Azithromycin is indicated on the day of abortion (1 g). Thus, the risk of infectious post-abortion complications is reduced by 88%.

Is it possible to give to children

Children over 3 years of age should take Azithromycin on an individual basis, which is based on the weight of the baby. For children less than 10 kg, the drug is prescribed extremely rarely (in case of danger to life), it is replaced with gentle analogues.

The safety of the drug for adult patients does not guarantee an adequate response of the child's body. Only the attending physician, based on the results of the tests, can prescribe Azithromycin to the child.

Complications, contraindications and side effects

There is an opinion that Azithromycin can become an indirect cause of infertility, like many other strong antibiotics. Improper use of such drugs leads to the fact that the patient relieves the symptoms, but does not cure the sexually transmitted disease.

The drug is not prescribed to patients who are allergic to antibiotics from the macrolide group. At risk are people with kidney failure, pregnant and lactating women. When carrying a child, the drug is prescribed only as a last resort, therefore, with symptoms of an infection, it is imperative to consult a doctor.

Side effects in the treatment of Azithromycin are very rare. Sometimes patients complain of dizziness, headaches, nervousness and symptoms of indigestion, fatigue, vaginitis and nephritis.

Side effects are observed only in 1% of cases, 64% of which are mild. When Azithromycin is included in therapy for pregnant women, there is no risk of damage to the fetus. The drug does not have a toxic effect on the unborn child.

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Azithromycin: respiratory specificity and uniqueness

Authors: D.B. UTESHEV, Department of Hospital Therapy, Moscow Faculty of the Russian State Medical University, I.A. KRYLOV, O.V. BUYUKLINSKAYA, Northern State Medical University, Arkhangelsk

Azithromycin is a representative of azalides, a subclass of macrolide antibiotics. Chemically, it differs from macrolides by the presence of a 15-membered lactone ring containing a nitrogen atom. In the arsenal of antibacterial agents intended for the treatment of respiratory infections, azithromycin invariably retains its leading position: depending on the nosological form, it is used as a first-line drug, an alternative agent, or in combination with other antibiotics. This is due to a number of exceptional features of azithromycin, which favorably distinguish it from other antibacterial agents.

Spectrum of antibacterial activity

Azithromycin has a broad spectrum of antibacterial activity that covers most types of bacteria that cause infections of the respiratory tract. The drug is effective against gram-positive microorganisms, including those producing β-lactamase (streptococci, staphylococci), as well as gram-negative bacteria (enterococci, E. coli, Haemophilus influenzae, shigella, salmonella), atypical pathogens (Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae), anaerobes and spirochetes. Azithromycin is 2-4 times less active against staphylococci and streptococci than erythromycin, but surpasses it in its effect on haemophilus influenzae and Gram-negative cocci. A positive feature of azithromycin is the low level of resistance of microorganisms to it.

Features of pharmacokinetics

Azithromycin has unique pharmacokinetic characteristics: first of all, a high degree of accumulation in tissues and inside cells, where its levels are 10-100 times higher than in blood plasma. This property is due to the high lipophilicity of the drug. The maximum concentration of azithromycin is determined in the lung tissue (compared to erythromycin, which has no differences in plasma and lung levels). Due to the accumulation of azithromycin in phagocytes, the drug is distributed to the foci of infectious inflammation. The concentration of azithromycin in the focus of infection is significantly higher than in unaffected tissues.

Azithromycin is metabolically stable. It acts for a long time (half-life 2-4 days), with a post-antibiotic effect (maintaining effective concentrations in the focus of infection for 3-5 days after discontinuation of the drug) against S.pyogenes, S.pneumoniae, H.influenzae, L.pneumophila. The duration of the post-antibiotic effect in relation to H.influenzae And L.pneumophila azithromycin more than clarithromycin. This determines the exceptional feature of the use of azithromycin in the treatment of respiratory tract infections - the effectiveness of 3-5-day courses of treatment.

The drug does not penetrate the blood-brain barrier. Elimination occurs in the urine unchanged and in the bile. In renal and hepatic insufficiency, the half-life does not change. The drug does not affect the microsomal system of the liver, therefore, there is no risk of undesirable effects inherent in this interaction.

In the United States, a new oral dosage form of azithromycin, sustained-release microspheres (SR) has been developed and introduced into clinical practice. Food and Drug Administration medicines The United States (FDA) approved the use of azithromycin ER for the treatment of community-acquired pneumonia and mild/moderate sinusitis in a single dose per course. Compared with the conventional dosage form, azithromycin ER is absorbed more slowly in the intestine, the maximum plasma concentration is reached after 2.5 hours, and the bioavailability is 82.8%. The use of azithromycin pollutants is characterized by a lower incidence of dyspeptic disorders. The combined use of antacids does not significantly affect the pharmacokinetic parameters of azithromycin ER (maximum plasma concentration, area under the pharmacokinetic curve). The introduction of azithromycin ZV allowed not only to achieve high efficiency of antibiotic therapy, but also to increase compliance: the drug is prescribed once, has a favorable safety and tolerability profile.

Clinical Application

Azithromycin has received justifiably widespread use in the treatment of pathologies of the respiratory system. This is due to the favorable spectrum of antibacterial activity, the low level of resistance of pathogens to it, the features of pharmacokinetics (high pulmonary deposition) and good tolerability.

In a comparative study of azithromycin, amoxicillin / clavulanate and the combination of cefuroxime with erythromycin in community-acquired pneumonia, the same clinical efficacy of the compared regimens was established, however, azithromycin was characterized by better tolerability and a lower incidence of adverse effects (12%). In the group of patients treated with cefuroxime in combination with erythromycin, the frequency of adverse effects was 48% (mainly dyspeptic symptoms). The pharmacoeconomic comparison of empiric therapy with azithromycin or the combination of cefuroxime with erythromycin in stepped therapy regimens established the equivalent cost of these regimens (however, the cost reduction in the azithromycin group due to the lower frequency of adverse effects, the simplification of the treatment process and the reduction in staff labor costs was not taken into account).

Azithromycin, along with other macrolide antibiotics, is the drug of choice for the treatment of atypical (mycoplasmal, legionella, chlamydial) pneumonia. According to some data, these intracellular pathogens account for more than 30% of all cases of community-acquired pneumonia, and the verification of these pathogens requires the use of expensive techniques. In this regard, the empirical use of azithromycin in the treatment of community-acquired pneumonia seems reasonable. In severe pneumonia, the empirical appointment of a combination of azithromycin with ceftriaxone is justified.

A new form of azithromycin (sustained-release microspheres) has been used in a single dose of 2 g per course for the empirical treatment of community-acquired pneumonia and mild to moderate bacterial sinusitis. A single dose of azithromycin was comparable in efficacy to the use of levofloxacin or clarithromycin for 7 days for community-acquired pneumonia or levofloxacin for 10 days for sinusitis. The use of a new form of azithromycin showed high compliance and good tolerability.

It is justified to prescribe azithromycin as the drug of choice and for the treatment of exacerbations of chronic bronchitis, the causative agents of which, as a rule, are S.pneumoniae, M.catarrhalis, H.influenzae. The use of other macrolides is considered inappropriate due to the lack of clinically significant activity against H.influenzae.

Long-term use of low-dose azithromycin in cystic fibrosis patients with chronic infection Pseudomonas aeruginosa was accompanied by a decrease in the number of exacerbations, a positive effect on lung function, improved nutritional status and good tolerability of the drug.

Of interest are the data on the organoprotective properties of azithromycin, which may be due to the nonspecific anti-inflammatory activity and antioxidant effect of azithromycin. For example, one study demonstrated that azithromycin protects the lungs from smoking-induced damage. Azithromycin inhibits tobacco smoke-induced damage to type II alveolocytes, activation of nuclear factor k B and an increase in the concentration of tumor necrosis factor a. Such an action is undoubtedly an advantage of this antibiotic in the treatment of bronchopulmonary pathology.

Of independent interest are data on the use of azithromycin for the treatment of infectious processes of other localizations: urogenital chlamydia, syphilis, chronic bacterial prostatitis (in combination with ciprofloxacin), acne, Lyme disease, chronic periodontitis.

Conclusion

Unique pharmacokinetic characteristics (accumulation in tissues, metabolic stability, a long half-life characteristic only of azithromycin), a wide range of antibacterial activity, including atypical pathogens, the presence of a post-antibiotic effect, good tolerance, high compliance, low level of resistance of pathogens, the presence of organoprotective properties (anti-inflammatory and antioxidant activity) - all this gives grounds for wide application azithromycin for respiratory infections. The clinical efficacy of azithromycin in the empirical treatment of bronchopulmonary infections (in monotherapy and in combination with β-lactams) on an outpatient basis and in a hospital has been proven in a number of multicenter studies.

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For oral administration: infections of the upper (streptococcal pharyngitis / tonsillitis) and lower (bacterial bronchitis, interstitial and alveolar pneumonia, exacerbation of chronic bronchitis) respiratory tract, ENT organs (otitis media, laryngitis and sinusitis), genitourinary system (urethritis and cervicitis) , skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses), chronic stage of erythema migrans (Lyme disease), diseases of the stomach and duodenum associated with Helicobacter pylori. For infusions: severe infections caused by susceptible strains of microorganisms: community-acquired pneumonia, infectious and inflammatory diseases of the pelvic organs.

Azithromycin release form

substance-powder; bag (pouch) polyethylene two-layer 1 kg; substance-powder; bag (pouch) polyethylene two-layer 2 kg; substance-powder; bag (pouch) polyethylene 5 kg drum 1; substance-powder; bag (pouch) polyethylene 15 kg drum 1; substance-powder; bag (pouch) polyethylene 25 kg drum 1; substance-powder; bag (pouch) polyethylene 50 kg drum 1; substance-powder; bag (pouch) polyethylene two-layer 3 kg; substance-powder; bag (pouch) polyethylene two-layer 4 kg; substance-powder; bag (pouch) polyethylene two-layer 5 kg; substance-powder; bag (pouch) polyethylene two-layer 6 kg; substance-powder; bag (pouch) polyethylene two-layer 7 kg; substance-powder; bag (pouch) polyethylene two-layer 8 kg; substance-powder; bag (pouch) polyethylene two-layer 9 kg; substance-powder; bag (pouch) polyethylene two-layer 10 kg; substance-powder; bag (pouch) polyethylene two-layer 15 kg; substance-powder; bag (pouch) polyethylene two-layer 20 kg; substance-powder; bag (pouch) polyethylene two-layer 25 kg; substance-powder; bag (pouch) polyethylene two-layer 50 kg; substance-powder; package (bag) polyethylene two-layer 5 kg polyethylene drum 1; substance-powder; package (bag) polyethylene two-layer 10 kg polyethylene drum 1; substance-powder; package (bag) polyethylene two-layer 25 kg polyethylene drum 1;

Pharmacodynamics of the drug Azithromycin

It binds to the 50S subunit of ribosomes, inhibits the peptide translocase at the translation stage and inhibits protein biosynthesis, slowing down the growth and reproduction of bacteria; at high concentrations, a bactericidal effect is possible. The spectrum of action is wide and includes gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, streptococci of groups C, F, G, Streptococcus viridans), except for those resistant to erythromycin, and gram-negative (Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis , Bordetella parapertussis, Campylobacter jejuni, Legionella pneumophila, Neisseria gonorrhoeae, Gardnerella vaginalis) microorganisms, anaerobes (Bacteroides bivius, Peptostreptococcus spp., Peptococcus, Clostridium perfringens), chlamydia (Chlamydia trachomatis, Chlamydia pneumoniae), mycobacteria (Mycobacterium complex), avcobacteria (Mycoplasma pneumoniae), ureoplasma (Ureaplasma urealyticum), spirochetes (Treponema pallidum, Borrelia burgdorferi).

Pharmacokinetics of the drug Azithromycin

Stable in an acidic environment, lipophilic, when taken orally, it is rapidly absorbed from the gastrointestinal tract. After a single oral dose of 500 mg, bioavailability is 37% (the “first pass” effect), Cmax (0.4 mg / l) is created after 2-3 hours, the apparent volume of distribution is 31.1 l / kg, protein binding is inversely proportional concentration in the blood and is 7-50%, T1 / 2 - 68 hours. A stable plasma level is reached after 5-7 days. It easily passes histohematic barriers and enters the tissues. It is also transported by phagocytes, polymorphonuclear leukocytes and macrophages to the site of infection, where it is released in the presence of bacteria. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). Concentrations in tissues and cells are 10–50 times higher than in plasma, and in the focus of infection they are 24–34% higher than in healthy tissues. A high level (antibacterial) persists in tissues for 5–7 days after the last injection. Food intake significantly changes the pharmacokinetics (depending on the dosage form): capsules - decreases Cmax (by 52%) and AUC (by 43%); suspension - increases Cmax (by 46%) and AUC (by 14%); tablets - Cmax increases (by 31%), AUC does not change. Demethylated in the liver, losing activity. Plasma clearance - 630 ml / min. 50% is excreted in the bile unchanged, 6% - in the urine. In elderly men (65–85 years), pharmacokinetic parameters do not change, in women, Cmax increases (by 30–50%), in children aged 1–5 years, Cmax, T1 / 2, AUC decrease.

Use of the drug Azithromycin during pregnancy

During pregnancy, it is possible if the expected effect of therapy outweighs the potential risk to the fetus. Category of action on the fetus according to the FDA - B. At the time of treatment, breastfeeding should be stopped.

Contraindications to the use of the drug Azithromycin

Hypersensitivity (including to other macrolides), severe violations of the liver and / or kidneys, age up to 16 years (infusion), up to 12 years with a body weight of less than 45 kg (capsules, tablets), up to 6 months (suspension for ingestion).

Side effects of the drug Azithromycin

From the nervous system and sensory organs: dizziness, vertigo, headache, paresthesia, agitation, fatigue, drowsiness; rarely - tinnitus, reversible hearing loss up to deafness (when taken in high doses for a long time); in children - headache (in the treatment of otitis media), hyperkinesia, nervousness, anxiety, sleep disturbance, conjunctivitis. From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): chest pain, palpitations. From the digestive tract: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of ALT and AST, bilirubin levels, cholestasis, jaundice; rarely - constipation, discoloration of the tongue, pseudomembranous colitis, pancreatitis, liver necrosis, liver failure (possibly fatal); in children - loss of appetite, gastritis, candidiasis of the oral mucosa. From the genitourinary system: vaginal candidiasis, nephritis. allergic reactions: rash, itching, urticaria; rarely - angioedema, anaphylactic shock. Others: photosensitivity, eosinophilia, transient neutrophilia; with intravenous administration (optional) - bronchospasm, pain and inflammation at the injection site.

Dosing and Administration of Azithromycin

Inside, 1 hour before meals or 2 hours after meals, 1 time per day. For infections of the upper and lower respiratory tract, infections of the skin and soft tissues - 500 mg / day for 3 days (course dose - 1.5 g). With uncomplicated urethritis and / or cervicitis - once 1 g (4 caps. 250 mg each). In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans) - 1 g (4 caps. 250 mg each) on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 G). At peptic ulcer stomach and duodenum associated with Helicobacter pylori - 1 g (4 caps. 250 mg) per day for 3 days as part of combination therapy. Children are prescribed at the rate of 10 mg / kg 1 time per day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day for 3 days (course dose - 30 mg / day kg). If you miss 1 dose of the drug, the missed dose should be taken as soon as possible, and subsequent doses should be taken with a break of 24 hours.

Overdose of Azithromycin

Symptoms: nausea, vomiting, diarrhea, temporary hearing loss. Treatment: gastric lavage (when taken orally), symptomatic therapy.

Interactions of the drug Azithromycin with other drugs

Antacids, ethanol, food slow down and reduce absorption (azithromycin should be taken 1 hour before or 2 hours after taking antacids and eating). Tetracycline and chloramphenicol enhance the effectiveness of azithromycin, lincosamides - weaken. When used in therapeutic doses, azithromycin has little effect on the pharmacokinetics of atorvastatin, carbamazepine, cetirizine, didanosine, efavirenz, fluconazole, indinavir sulfate, midazolam, rifabutin, sildenafil, theophylline (in / in and inside), triazolam, co-trimoxazole, zidovudine. Efavirenz and fluconazole have little effect on the pharmacokinetics of azithromycin. Nelfinavir significantly increases the Cmax and AUC of azithromycin (when taken together, strict control is required in relation to such side effects of azithromycin as impaired liver function and hearing impairment). Careful monitoring is required when simultaneous reception azithromycin with digoxin (an increase in the concentration of digoxin in the blood is possible), with ergot alkaloids (their toxic effects are possible - vasospasm, dysesthesia), with cyclosporine and phenytoin (control of their concentration in the blood is necessary). If co-administration with warfarin is necessary, careful monitoring of PT is recommended (an increase in PT and the incidence of hemorrhages is possible). Pharmaceutically incompatible with heparin.

Precautions while taking Azithromycin

After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.

Storage conditions of the drug Azithromycin

List B.: In a dry, dark place, at a temperature not exceeding 25 ° C.

Shelf life of the drug Azithromycin

Belonging of the drug Azithromycin to the ATX-classification:

J Antimicrobials for systemic use

J01 Antimicrobials for systemic use

J01F Macrolides and lincosamides