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Azithromycin is a popular antibacterial agent that is used to treat diseases of the upper and lower respiratory tract and bacterial lesions of the genitourinary system, including in children. It has a low level of toxic effects on the child’s body and a long-lasting effect. Therefore, the drug can be taken only once a day.

The antibiotic Azithromycin is sold in any pharmacy in the form of tablets, capsules and powder for preparing a suspension.

There is also a number of its complete analogues: Azitrus, Azivok, Sumametsin, Zitrolide, Zitrocin, Ecomed, ZI-factor, etc.

The listed drugs are prepared on the basis of one active substance - 9-Deoxo-9a-aza-9a-methyl-9a-homoerythromycin A, and they all have an identical effect.

Azithromycin is well tolerated by children under one year of age.

How does the medicine work?

Azithromycin belongs to a group of drugs called macrolides due to their special structure (if you go deeper into chemistry, they are based on a 14 or 16-membered lactone ring with attached carbohydrate residues).

The most famous representative of macrolides is Erythromycin, which was used to treat the fathers and mothers, grandfathers and grandmothers of today's children.

Azithromycin is a new generation medicine, which means it has fewer side effects.

It is effective against a whole range of pathological microorganisms that are resistant to other antibiotics. Among them, many types are the plague of the twentieth century, as experts call it. Moreover, this the only drug that can fight Haemophilus influenzae, which, together with staphylococcus, takes an active part in the development of pneumonia and meningitis.

The drug has the ability to easily penetrate and accumulate in sputum located in the bronchi, as well as in the tissues of the bronchi and lungs, organs of the genitourinary system and skin. This allows the medicine to act directly on the site of inflammation. The mechanism of action of the antibiotic is based on the fact that it prevents microbial cells from synthesizing protein. And without this basic “building material” no cell can exist. Azithromycin reaches its highest concentration in the child’s blood plasma within 2-3 hours after administration. From there it penetrates into foci of inflammation, accumulates in the tissues of the affected organs and immediately begins its work.

The antibiotic is taken once a day. It would be enough.

In addition to its speed of action, the drug is characterized by slow elimination from the body, which prolongs the therapeutic effect. The antibiotic is usually cleared from the child’s body in 35-55 hours. It is this property of Azithromycin that makes it possible to take it only once a day.

One of the main advantages of the antibiotic is the absence of any interaction with antiallergic drugs. This allows it to be taken by children suffering from allergic diseases and, in particular, bronchial asthma.

In what cases is it prescribed?

Children Azithromycin is usually treated for respiratory diseases:

• bronchitis, pneumonia caused by chlamydia and mycoplasma;
• complicated pneumonia with an identified pathogen that is sensitive to the drug;
• with exacerbations of chronic bronchitis;
• in the absence of effect from treatment with antibiotics related to cephalosporins and penicillins, as well as intolerance to these drugs;
• if the child has allergies or bronchial asthma.

If pneumonia is suspected, pediatricians usually prescribe Azithromycin.

In addition to the diseases listed, Azithromycin is used to treat:

• , sore throat;
• scarlet fever;
• skin diseases - erysipelas, impetigo, pustular lesions;
• inflammation of the urethra;
• Lyme disease.

How to navigate the variety of analogues and release forms?

Azithromycin has several release forms, from which you can choose the most suitable one:

1. Powder for preparing a suspension or ready-made suspension 100 mg/5 ml, equipped with a dispenser syringe for children from six months to three years.
2. Powder for preparing a suspension or ready-made suspension 200 mg/5 ml - from three to 14 years.
3. Tablets 125 mg.
4. Tablets with a dosage of 250 mg are rarely used to treat children.

When we talk about dosage, we mean that it is the same for all Azithromycins, marketed under the different names discussed above. Some drugs, for example, Sumamed, are presented in all dosage forms - in the form of tablets, powder for suspension and capsules, but Azimed, Azitrus, Azitrox are intended only for preparing a suspension. Ecomed is a ready-to-use mixture.

A more expensive analogue of Azithromycin with the same main active ingredient is Sumamed.

Dosage and regimen

Before you start using the drug, be sure to read the instructions for use (). The dosage of Azithromycin depends on the child’s body weight.

Thus, the total dose required for the course is 30-50 mg per kilogram of weight.

Example: if Alyosha weighs 14 kg, then he will need 140 mg of Azithromycin per day at one time. A 280-milligram tablet may be split in half or given as a suspension. The boy will need 5 ml of suspension obtained from a 100 mg bottle of powder (according to the table below). If Alyosha’s weight were, for example, 15 kg, it would be impossible to accurately divide the tablet. In this case, it is advisable to use a suspension. Here is a table (from the instructions for use) that will help calculate the required amount of suspension based on the child’s weight:

The drug should not be given simultaneously with food - either one hour before a meal or two hours after it.

Take the drug strictly on an empty stomach!

In some cases, during the treatment process, it becomes necessary to adjust the dosage or replace the drug, and this can only be done by a doctor. Therefore, taking an antibiotic should only be done under the supervision of a pediatrician and on his recommendation.

How to prepare a suspension from powder

The suspension is prepared immediately before the first use. To a bottle with 100 mg of the drug you need to add 11 ml of boiled cooled water using a syringe dispenser and shake well until a homogeneous liquid is obtained. Vials with 200 mg of the drug are diluted with 14.5 ml of water - here the concentration of the drug is higher.

The resulting suspension is given to the child using a double-sided dosing spoon or syringe dispenser. The diluted medicine is stored in the refrigerator for no more than 5 days.

A dispenser syringe is a great helper for mothers!

It is more convenient for very young children to give the suspension using a dosing syringe. To do this, you need to position the child as if for feeding, carefully insert the tip of the syringe into his mouth and slowly squeeze out the medicine so that he has time to swallow.

Contraindications and side effects

After antibiotics, children often experience digestive disorders, stool disturbances, and the child cannot eat foods that were easily tolerated before. Therefore, it is necessary to restore children's immunity. But how to do it right?

Azithromycin

International nonproprietary name

Azithromycin

Dosage form

Capsules 250 mg

Compound

One capsule contains

active substance- azithromycin (in terms of 100%) - 250 mg

Excipients: microcrystalline cellulose, potato starch, calcium stearate, lactose monohydrate.

capsule composition: gelatin, glycerin, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium lauryl sulfate, titanium dioxide (E 171), purified water.

Description

Hard gelatin capsules, size No. 0, cylindrical in shape with hemispherical ends, white.

The contents of the capsules are white powder with varying particle sizes.

Pharmacotherapeutic group

Antibacterial drugs for systemic use. Macrolides, lincosamides and streptogramins. Macrolides. Azithromycin.

ATX code J01FA10

Pharmacological properties

Pharmacokinetics

Rapidly absorbed from the gastrointestinal tract. Acid resistant. After oral administration at a dose of 500 mg, the maximum concentration in the blood is reached after 2.5-3 hours and is 0.4 mg/l. Bioavailability - 37%.

Penetrates well into the respiratory tract, organs and tissues of the urogenital tract, skin and soft tissues. High concentration in tissues (10-50 times higher than in blood plasma) and long half-life are due to the ability of the drug to concentrate in cell lysosomes and destroy intracellular microorganisms. This determines the large apparent volume of distribution (31.1 l/kg) and high plasma clearance. Phagocytes deliver azithromycin to sites of infection, where it is released through the process of phagocytosis. The concentration of azithromycin in foci of infection is higher than in healthy tissues (on average by 24-34%). Despite its high concentration in phagocytes, azithromycin does not have a significant effect on their function.

Azithromycin remains in bactericidal concentrations at the site of inflammation for 5-7 days after taking the last dose.

In the liver it is demethylated to form inactive metabolites.

It is released in 2 stages: the time for reducing the concentration in the blood of the first phase is 14-20 hours, the second phase is 41 hours, which allows you to take the drug once a day.

Pharmacodynamics

Azithromycin is a broad-spectrum antibacterial agent, an azalide. By binding to the 50S ribosomal subunit, it inhibits peptidyl translocase, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and in high concentrations has a bactericidal effect. Acts on extra- and intracellular pathogens.

Active against gram-positive microorganisms: Streptococcus spp.(groups C, F and G, except those resistant to erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms : Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; and Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi.

Inactive against gram-positive bacteria resistant to erythromycin.

Indications for use

Infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, otitis media)

Lower respiratory tract infections (bacterial and atypical pneumonia, bronchitis)

Infections of the skin and soft tissues (erysipelas, impetigo, secondary infected dermatoses, Lyme disease (borreliosis) in the initial stage (erythema migrans))

Infections of the urogenital tract (uncomplicated urethritis, cervicitis)

Diseases of the stomach and duodenum associated with Helicobacter pylori(as part of combination therapy).

Directions for use and doses

Orally, 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 is prescribed for 3 days (course dose - 1.5 g).

For uncomplicated urethritis and/or cervicitis, a single dose of 1 g (4 capsules of 250 mg) is prescribed.

With Lyme disease (borreliosis) in the initial stage ( erythema migrans) are prescribed 1 g (4 capsules of 250 mg each) on the 1st day and 500 mg daily from the 2nd to the 5th day (course dose - 3 g). In children over 12 years of age, the dose is 20 mg/kg on the first day and 10 mg/kg from the 2nd to the 5th day.

For diseases of the stomach and duodenum associated with Helicobacter pylori, 1 g (4 capsules of 250 mg) per day is prescribed for 3 days as part of combination therapy.

Children over 12 years of age are prescribed at a 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. x days (course dose - 30 mg/kg).

Side effects

Often

Nausea, vomiting, diarrhea, abdominal pain

Rarely

Thromocytopenia

Aggression, agitation, anxiety, nervousness, insomnia, development of suicidal thoughts, suicidal behavior

Paresthesia, asthenia

Hearing impairment, deafness and tinnitus

Tachycardia, arrhythmia with ventricular tachycardia, prolongation of the QT interval

Loss of appetite, flatulence, constipation, pseudomembranous colitis

Transient increase in the level of liver aminotransferases, bilirubin, cholestatic jaundice, hepatitis

Hypersensitivity reactions (redness, skin rash, itching,

angioedema, photosensitivity), erythema multiforme, Steven-Johnson syndrome and toxic epidermal necrolysis, anaphylactic shock including edema (in rare cases leading to death)

Interstitial nephritis, acute renal failure

Very rarely

Fatigue, headache, dizziness, convulsions

Changes in taste and smell

Arthralgia

Vaginitis, candidiasis, superinfections

Contraindications

Hypersensitivity to azithromycin and macrolide antibiotics

Severe liver dysfunction

Severe renal impairment

Children and teenagers up to 12 years old

Pregnancy and lactation

Drug interactions

Antacids (aluminum and magnesium containing), ethanol and food slow down and reduce absorption.

When warfarin and azithromycin were co-administered (in usual doses), no changes in prothrombin time were detected, however, patients need careful monitoring of prothrombin time.

Increases the concentration of digoxin by reducing its inactivation by intestinal flora.

When azithromycin is taken simultaneously with ergotamine and dihydroergotamine, their toxic effects (vasospasm, dysesthesia) may occur.

Reduces clearance and enhances the pharmacological effect of triazolam.

Slows down the elimination, increases the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs subject to microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, theophylline and other xanthine derivatives) - due to inhibition of their oxidation in hepatocytes.

Lincosamines weaken the effectiveness of azithromycin, tetracycline and chloramphenicol enhance them.

Pharmaceutically incompatible with heparin.

special instructions

If a dose is missed, the missed dose should be taken as soon as possible and subsequent doses should be taken 24 hours apart.

It is necessary to observe a 2-hour break when using antacids simultaneously.

If any side effect occurs, you should notify your doctor.

The following side effects have been reported when taking macrolide antibiotics: ventricular arrhythmia, including ventricular tachycardia and torsades de pointes (ventricular fibrillation), in patients with a prolonged QT interval.

It is extremely rare that during treatment with azithromycin there may be flutter-fibrillation (ventricular fibrillation) and subsequent myocardial infarction in persons with a history of arrhythmia.

Prolonged cardiac repolarization and QT interval, which increased the risk of developing cardiac arrhythmia and ventricular flutter/fibrillation, were observed during treatment with other macrolide antibiotics. A similar effect of azithromycin cannot be completely excluded in patients with an increased risk of prolonged cardiac repolarization.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

During treatment with the drug, you must refrain from driving vehicles and engaging in potentially hazardous activities.

Overdose

Active ingredient of the drug: azithromycin dihydrate (in terms of azithromycin) 0.500 g and 0.250 g.

pharmachologic effect

Azithromycin is an antibacterial drug from the group of macrolides-azalides, with a wide bacteriostatic spectrum of action.

It has an effect on both bacteria located inside cells and bacteria located outside them.

The active substance interacts with the 50S subunit of ribosomes, inhibits the activity of the peptide translocase enzyme at the translation stage, as a result of which protein synthesis is inhibited, the growth and reproduction of bacteria slows down. High concentrations of Azithromycin kill bacteria, that is, they have a bactericidal effect.

Bacterial resistance to the drug may be initial or develop during antibiotic therapy.

Scale of sensitivity of microorganisms to azithromycin (minimum inhibitory concentration (MIC), mg/l):

Sensitive to Azithromycin:

• Aerobic gram-positive microorganisms: Staphylococcus aureus (methylcillin-sensitive), Streptococcus pneumoniae penicillin-sensitive), Streptococcus pyogenes;
• Aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;
• Anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.;
• Other: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdoferi.

Moderately sensitive or insensitive:

Aerobic gram-positive microorganisms: Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).

Resistant to the action of Azithromycin:

• Aerobic gram-positive microorganisms: Enterococcus faecalis, Staphylococci spp. (methicillin-resistant), Staphylococcus aureus (including methicillin-sensitive strains), Staphylococus pneumoniae, Staphylococcus spp. Group A (beta-hemolytic).
• Azithromycin is inactive against strains of gram-positive bacteria resistant to erythromycin.
• Anaerobes: Bacteroides fragilis group.

Azithromycin is well absorbed from the gastrointestinal tract and quickly distributed throughout the tissues of the body. After a single dose of 0.5 g, bioavailability is 37% (the “first pass” effect through the liver). The maximum concentration after oral administration (0.5 g - 0.4 mg/l) is achieved after 2-3 hours. The intracellular and tissue concentration of the antibiotic is 10-50 times higher than the serum concentration.

Azithromycin is acid-resistant and lipophilic. Passes through histohematic barriers without hindrance. Easily penetrates the genitourinary organs and tissues, including the prostate gland, respiratory organs, skin and soft tissues. Some drugs are also transported to the infectious focus by phagocytes (macrophages and polymorphonuclear leukocytes), where they are released in the presence of bacteria.

Penetrating through cell membranes, it creates high intracellular concentrations, due to which it acts against pathogenic bacteria located inside cells. In places where the infectious process is localized, antibiotic concentrations are 24-34% higher than in healthy tissues, and the more intense the inflammation, the higher the concentrations. After taking the last dose of Azithromycin, its effective concentrations remain for 5-7 days.

More than half of azithromycin is excreted unchanged by the intestines, 6% is excreted by the kidneys.

Pharmacokinetics are greatly influenced by food intake, namely, the maximum concentration increases by 31%.

In elderly men (65-85 years old), the pharmacokinetic parameters do not change; in elderly women, the maximum concentration increases by 30-50%.

Indications for use

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• infections of the upper respiratory tract and ENT organs: pharyngitis, tonsillitis, sinusitis, otitis media;
• lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, including those caused by atypical pathogens;
• infections of the skin and soft tissues: acne vulgaris of moderate severity, erysipelas, impetigo, secondary infected dermatoses;
• the initial stage of Lyme disease (borreliosis) - erythema migrans;
• urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications

• Increased individual sensitivity to macrolide antibiotics;
• Severe liver or kidney failure;
• Children under 12 years of age with body weight less than 45 kg (for this dosage form);
• Breast-feeding;
• Simultaneous use with ergotamine and dihydroergotamine.

Carefully :

• With moderate impairment of liver and kidney function;
• For arrhythmias or predisposition to arrhythmias and prolongation of the QT interval;
• When used together with terfenadine, warfarin, digoxin.

Instructions for use and dosage

Azithromycin capsules are taken orally, 500 mg once a day, regardless of meals. For adults (including the elderly) and children over 12 years of age weighing more than 45 kg, the drug dosage regimen is as follows:

• For the treatment of infectious diseases of the ENT organs, respiratory tract, skin and soft tissues, 500 mg is prescribed once a day for 3 days (course dose -1.5 g).
• For moderate treatment: 2 capsules of 250 mg once a day for 3 days, then 250 mg twice a week for 9 days. Course dose 6.0 g.
• For the treatment of borreliosis (erythema migrans): on the first day, a single dose of 1 gram of the drug (2 capsules of 500 mg each), then from the 2nd to the 5th day, 500 mg daily. Course dose 3.0 g.
• For genitourinary infections caused by Chlamydia trachomatis (urethritis, cervicitis): 2 capsules of 500 mg at a time.

For moderate renal impairment (creatinine clearance > 40 ml/min), no dose adjustment is required.

If for some reason the next dose of azithromycin is missed, then the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.

Side effect

From the gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea, flatulence, loose stools, digestive upset, constipation, anorexia, tongue discoloration, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory tests of liver function, liver failure, liver necrosis (possibly fatal ).

Allergic reactions: itching, skin rash, Quincke's edema, urticaria, photosensitivity, (in rare cases fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the cardiovascular system: palpitations, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia.

From the circulatory and lymphatic systems: thrombocytopenia, neutropenia, eosinophilia.

From the genitourinary system: interstitial nephritis, acute renal failure.

From the nervous system:, dizziness, drowsiness, insomnia, asthenia, anxiety, hyperactivity, aggressiveness, nervousness, convulsions, paresthesia.

From the senses: in the ears, reversible hearing loss up to deafness (if taken for a long time in high doses of the drug), impaired perception of taste and smell.

From the musculoskeletal system: arthralgia.

Others: vaginitis, candidiasis.

In some patients, after stopping treatment with azithromycin, hypersensitivity reactions may persist for a long time, and therefore specific treatment under medical supervision may be required.

In addition, given the likelihood of developing side effects from the central nervous system, caution should be exercised when driving vehicles and operating machinery.

Overdose

Symptoms of azithromycin overdose: reversible hearing loss, nausea, vomiting, diarrhea. Treatment of overdose: symptomatic.

Pregnancy and lactation

During pregnancy, Azithromycin should be prescribed only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding should be temporarily discontinued during treatment with azithromycin.

Interaction with other drugs

Analogs

Azithromycin is the active substance of the following antibacterial drugs:

• Sumamed;
• Zithrocin;
• Ecomed
• Chemomycin;
• Azimicin.

According to the mechanism of action, azithromycin analogues are:

• Lecoclair;
• Clarithromycin;
• Oleandomycin;
• Fromilid;
• Rovamycin Spiramycin-vero;
• Macropen;
• Erythromycin.

Storage and shelf life

Store in a dry, dark place, out of reach of children, at temperatures up to 25 °C. Azithromycin has a shelf life of 3 years, after which the drug cannot be used.

Antacids: Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs or eating. Cetirizine: Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not result in pharmacokinetic interactions or significant changes in the QT interval. Didinosine (dideoxyinosine): Concomitant use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal changes in the pharmacokinetic indications of didanosine compared with the placebo group. Digoxin (P-gp substrates): Concomitant use of macrolide antibiotics, including azithromycin, with P-gp substrates, such as digoxin, results in increased plasma concentrations of the P-gp substrate. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood plasma. Zidovudine: Concomitant use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has little effect on the pharmacokinetics, including renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system. Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes. Atorvastatin: Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on an HMC-CoA reductase inhibition assay). However, there have been isolated case reports of rhabdomyolysis in patients receiving concomitant azithromycin and statins. Carbamazepine: Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin. Cimetidine: in pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin were detected when cimetidine was administered 2 hours before azithromycin. Indirect anticoagulants (coumarin derivatives): In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of prothrombin time should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives). Cyclosporine: in a pharmacokinetic study involving healthy volunteers who took oral azithromycin (500 mg/day once) for three days, and then cyclosporine (10 mg/kg/day once), a significant increase in maximum plasma concentration (Cmax) was detected. and area under the concentration-time curve (AUCo-5) of cyclosporine. Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly. Efavirenz: Concomitant use of azithromycin (600 mg/day as a single dose) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction. Fluconazole: Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and half-life of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance. Indinavir: simultaneous use of azithromycin (1200 mg once) did not cause a statistically significant effect on the pharmacokinetics of indinavir (800 mg three times a day for 5 days). Methylprednisolone: ​​Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone. Nelfinavir: simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg three times a day) causes an increase in the equilibrium concentration of azithromycin in the blood plasma. No clinically significant side effects were observed. No dose adjustment of azithromycin is required when used concomitantly with nelfinavir. Rifabutin: simultaneous use of azithromycin and rifabutin does not affect the concentration of either drug in the blood plasma. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established. Sildenafil: When used in healthy volunteers, there is no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite. Terfenadine: There was no evidence of interaction between azithromycin and terfenadine in pharmacokinetic studies. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval. Theophylline: No interaction has been identified between azithromycin and theophylline. Triazolam/midazolam: No significant changes in pharmacokinetic parameters were detected with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses. Trimethoprim/sulfamethoxazole: Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin plasma concentrations were consistent with those found in other studies. Ergot alkaloids: Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Azithromycin belongs to the group of macrolide antibiotics and is widely used to treat various infectious processes in children. The drug is characterized by low toxicity and a low risk of side effects, which allows it to be prescribed already in the first year of a child’s life. Azithromycin was first synthesized in 1980 by the Croatian pharmaceutical company Pliva. After some time, the World Health Organization included this antibiotic in the list of the most important medicines.

Pharmacological properties

Azithromycin is the first representative of the azalide class. Like other drugs in the macrolide group, it has a bacteriostatic effect on pathogenic bacteria. The drug has no effect on fungi and viruses. Azithromycin is able to bind to the 50S ribosomal subunit of the pathogen and thereby inhibit protein production by the cell. As a result, the bacterium loses its ability to reproduce and becomes more vulnerable to the body’s immune defense factors. Those who are sensitive to this drug are:

Azithromycin after oral administration is quickly absorbed by the mucous membrane of the herbal tract. However, most of the drug is immediately metabolized by the liver and only a little more than a third (37%) of the initial dose enters the systemic circulation. The maximum concentration is recorded 180 minutes after administration.

A special feature of the drug is the fact that it penetrates human tissues and cells and is transported by leukocytes and macrophages to the site of inflammation.

Therefore, at the site of the pathological process, sometimes the concentration of azithromycin is 10-50 times higher than in the blood plasma. This allows the drug to retain antimicrobial activity in the body for up to 5 days after the last use.

Food intake negatively affects the pharmacokinetics of azithromycin. Its absorption into the patient’s body decreases, so doctors strongly recommend taking the antibiotic “on an empty stomach.” Azithromycin is gradually inactivated in the patient's liver cells. About half of the drug is excreted unchanged through bile.

Indications for the use of azithromycin

Azithromycin is prescribed to children for the following conditions:

Contraindications to taking the drug

Azithromycin should not be prescribed or used if the child has the following contraindications:

• hypersensitivity to your favorite macrolide drugs;
• end-stage liver failure;
• children up to 4 months;
• malabsorption syndrome;
• intolerance to sucrase or fructose;
• simultaneous administration of ergotamine.

Prescription restrictions

In some cases, azithromycin should be prescribed with caution. This is allowed to be done in situations where the benefits of taking this medication outweigh the possible harm. It is also recommended to use azithromycin for children if the pathogen has developed resistance to other antibiotics.

Since the drug sometimes leads to the development of tachycardia, arrhythmias and an increase in the Q-T interval, it should be used for congenital or acquired heart pathologies under careful control of frequency and rhythm.

There is evidence that with a significant decrease in renal filtration rates, additional accumulation of azithromycin occurs in the body. Therefore, you need to either choose a different drug or use reduced doses.

Release form of the drug

Azithromycin is available in the form of capsules or tablets containing the active substance 125, 250 and 500 mg. In addition, powder for making syrup is produced especially for children. The content of azithromycin is 100 or 200 mg in 5 ml of the finished suspension.

After preparation, the syrup has the taste and smell of cherries, bananas, strawberries or raspberries.

The original drug is considered to be “Sumamed”, which is manufactured by the Croatian company “Pliva”. But besides it, there are more affordable analogues on the market: Zitrox, Azinort, Azitral, Azithromax, Azithromycin, Azithromycin-Norton and others.

Side effects

Even with short-term use of the drug, bacterial resistance to the drug may develop. Also, secondary fungal (candidiasis) or microbial infection is rarely associated. Cases of the development of pseudomembranous colitis caused by C. dificcile have been described. The severity of this complication varies. Some children have only diarrhea, while others have severe damage to the digestive tract.

In some children (especially young children), cases of neurological symptoms have been described. In them, taking the drug was accompanied by headache, dizziness, paresthesia of the limbs, drowsiness, depression, convulsions, nervousness, hyperactivity and hearing impairment. In the presence of cardiac pathology, the risk of rhythm disturbances, tachycardias and arrhythmias increases.

Sometimes azithromycin inhibits hematopoiesis in the patient's bone marrow. In the laboratory, this is manifested by a decrease in the number of red blood cells, leukocytes and platelets in the peripheral blood. The patient experiences symptoms of anemia, secondary infection, hemorrhages in the skin and mucous membranes. Cases of allergic reactions of varying severity have been described.

When taking the drug in children with impaired liver function, cases of toxic hepatitis and worsening organ failure were recorded.

Interaction with other drugs

Like other macrolides, azithromycin cannot be combined with bactericidal antibiotics, since their effectiveness is reduced. You should also avoid taking the drug simultaneously with antacids, since they can bind and remove the antibiotic from the patient's body.

Azithromycin also leads to an increase in the concentration of cardiac glycosides (digoxin) in the blood plasma, which must be taken into account when choosing drug doses.

This drug has a similar effect on indirect anticoagulants (coumarin derivatives) and cyclosporine.

How to use azithromycin

Suspension

Mostly children are prescribed the drug in syrup form. This allows not only to accurately dose the required amount of azithromycin, but is also more positively perceived by children and their parents. The syrup is taken orally once a day, having previously measured out the required volume of antibiotic using a spoon or a special syringe.

The intake should take place no sooner than 60 minutes before a meal, or 2 hours after it. After this, be sure to give the child a small amount of plain water to drink. If you miss a dose, you need to take it as quickly as possible, and take the next dose of azithromycin after 24 hours.

The drug is dosed to children depending on their body weight. Below are these calculations for 200 mg/5 ml syrup. The daily amount of azithromycin suspension for children weighing 15-24 kg is 5 ml, 25-34 kg - 7.5 ml, 35-44 kg - 10 ml, over 45 kg - 12.5 ml suspension. These indicators are most relevant for bacterial infections of the upper respiratory tract. For erythema migrans, a twice as high dose of antibiotic is prescribed. The course of therapy usually lasts 3 days, but can be continued by the doctor up to 5.

The 100 mg/5 ml suspension form is intended for children of the first year of life. The drug is also taken once a day. The dosage of the antibiotic is as follows: 0.5 ml of syrup per 1 kg of body weight. In this case, the drug can be used only if the child is not lighter than 5 kg.

Tablet form

Azithromycin tablets can be prescribed from the age of three. The main criterion is a body weight of more than 12.5 kg and the ability to adequately swallow this form of the drug.

It was for children that tablets containing 125 and 250 mg of azithromycin were developed. The antibiotic dosage is 10 mg per 1 kg of body weight per day. The course of therapy also lasts 3 days. The basic rules for administration do not differ from those for syrup. After reaching 45 kg, the child is prescribed an adult dose of 500 mg.