Clarithromycin or azithromycin which is better. Why azithromycin remains the drug of choice for community-acquired infections of the lower respiratory tract Erythromycin or clarithromycin which is better

A derivative of erythromycin.

Azithromycin - chemical compound

It belongs to the subclass of azalides, which differ from other macrolides in that a nitrogen atom is added to the 14-membered lactone ring (top-left in the diagram of the azithromycin molecule).

Azithromycin - medicinal product

Azithromycin is also a trade name for the drug.

Indications for the use of azithromycin

Azithromycin use and dosage

Azithromycin in Helicobacter pylori eradication schemes

Azithromycin is a good example to illustrate the possibilities of optimizing the triple therapy eradication regimen. Macrolide antibiotics given in triple regimens, mainly clarithromycin, are most effective. Azithromycin has been tried for a number of years as one of the possible components of therapy, but in early studies a relatively low dose of the drug was used. An increase in the course dose to 3 g led to an increase in the effectiveness of the standard seven-day triple regimen based on a proton pump inhibitor to the required level of more than 80%. At the same time, the undoubted advantage is that as part of a weekly course, the full dose of azithromycin is taken for three days, and once a day. This is convenient for the patient and reduces the percentage of side effects. In addition, in Russia the cost of azithromycin is lower than other modern macrolides (Lapina T.L., Ivashkin V.T.).

All drugs of the macrolide group are characterized by the development of cross-resistance of strains in vitro, but not all macrolides can equally form such resistance in Helicobacter pylori in vivo, since this also depends on the ability of the drug to accumulate in the mucosal layer. Since clarithromycin quickly reaches inhibitory concentrations on the surface of the gastric mucosa, after a course of treatment, 2/3 of non-killed strains Helicobacter pylori become resistant to it. This cannot be said about azithromycin - it has a low eradication efficiency (62%), but secondary resistance develops only in 23% of cases (Kornienko E.A., Parolova N.I.).

Monotherapy Helicobacter pylori azithromycin is not allowed. Azithromycin is not used in eradication Helicobacter pylori outside special schemes, without drugs that reduce the acidity of the stomach. Azithromycin is also not used to treat gastric and duodenal ulcers and gastritis in the absence of Helicobacter pylori in a patient.

Professional medical publications concerning the use of azithromycin in the eradication of Helicobacter pylori

• Teplova N.V., Teplova N.N. Antihelicobacter peptic ulcer therapy with azithromycin and amoxicillin // RMJ. Diseases of the digestive system. - 2004. - v. 6. - No. 2. - 68-70.


• Rusova T.V., Selezneva E.V., Glazova T.G. Clinical examination of children with chronic gastroduodenitis // Questions of children's dietology, 2015, vol. 13, no. 1, pp. 62-69.

Azithromycin as a prokinetic

Erythromycin

It has a wide spectrum of activity, including both gram-positive (staphylococci, producing and not producing penicillinase; streptococci, pneumococci, clostridia, Bacillus anthracis, Corynebacterium diphtheriae), and gram-negative microorganisms (gonococci, hemophilic and pertussis bacilli, brucella, legionella), mycoplasmas, chlamydia , spirochetes, rickettsia.

Resistant to erythromycin Gram-negative rods: coli, Pseudomonas aeruginosa, as well as Shigella, Salmonella, etc.

Indications:
Bacterial infections: diphtheria (including diphtheria carriage), whooping cough (including disease prevention in susceptible individuals at risk of infection), trachoma, brucellosis, legionnaires' disease, scarlet fever, amoebic dysentery, gonorrhea; neonatal conjunctivitis, pneumonia in children and urinary infections in pregnant women caused by Chlamydia trachomatis; primary syphilis (in patients allergic to penicillins), uncomplicated chlamydia in adults (with localization in the lower urinary tract and rectum) with intolerance or ineffectiveness of tetracyclines, etc.; ENT infections (tonsillitis, otitis media, sinusitis), biliary tract infections (cholecystitis), upper and lower respiratory tract infections (tracheitis, bronchitis, pneumonia), skin and soft tissue infections, pustular skin diseases, infected wounds, bedsores, burns II and III stage, trophic ulcers, infections of the mucous membrane of the eyes - caused by pathogens sensitive to the drug; prevention of exacerbations of streptococcal infection (tonsillitis, pharyngitis) in patients with rheumatism, infectious complications during dental interventions in patients with heart defects. It is a reserve antibiotic for the treatment of bacterial infections caused by strains of gram-positive pathogens (in particular staphylococci) resistant to penicillin. In severe forms of infectious diseases, when oral administration of the drug is ineffective or impossible, resort to the / in the introduction of a soluble form of erythromycin - erythromycin phosphate. Erythromycin in suppositories is prescribed in cases where ingestion is difficult.

Rp.:Erythromycini 0.25

D.t.d. N.20 in tab.

S. 2 tablets 4 times a day.

within 14 days

With legionellosis.

Azithromycin(sumamed)

In high concentrations, it has a bactericidal effect against gram-positive cocci: Streptococcus pneumoniae, S.pyogenes, S.agalactiae, streptococci of groups C, F and G, S.viridans, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, B.parapertussis, Legionella pneumophila, H.ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Not active against Gram-positive bacteria resistant to erythromycin.

Indications:

Infections of the upper respiratory tract and ENT organs caused by sensitive microflora: tonsillitis, sinusitis, tonsillitis, otitis media; scarlet fever; infections of the lower respiratory tract: bacterial and atypical pneumonia, bronchitis; skin and soft tissue infections: erysipelas, impetigo, secondarily infected dermatoses; infections of the urogenital tract: gonorrheal and non-gonorrheal urethritis and / or cervicitis; Lyme disease (borreliosis).

Rp.:Azithromycini 0.25

D.t.d. N.10 in caps.

S. On the first day, 1 capsule

morning and evening, from 2nd to

5th day 1 capsule 1 time

in a day. For infections

upper and lower divisions

respiratory tract.

Roxithromycin(rulid)

Sensitive to the drug: Streptococcii groups A and B, incl. Str. pyogenes, Str. agalactiae, Str. mitis, saunguis, viridans, Streptococcus pneumoniae; Neisseria meningitidis; Branhamellacatarrhalis; Bordetella pertussis; Listeria monocytogenes; Corynebacterium diphtheriae; Clostridium; Mycoplasma pneumoniae; Pasteurella multocida; Ureaplasma urealyticum; Clamydia trachomatis, pneumoniae and psittaci; Legionella pneumophila; Campylobacter; Gardnerella vaginalis. Intermittently sensitive: Naemophilus influenzae; Bacteroides fragilis and Vibrio cholerae. Resistant: Enterobacteriaceae, Pseudomonas, Acinetobacter.

Indications:

Treatment of drug-sensitive infections of the upper and lower respiratory tract, skin and soft tissues, genitourinary tract (including sexually transmitted infections, except gonorrhea), infections in dentistry (bronchitis, pneumonia, tonsillitis, scarlet fever, otitis media, sinusitis, diphtheria, whooping cough, trachoma, brucellosis, legionnaires' disease, etc.). Prevention of meningococcal meningitis in persons who have been in contact with the diseased.

Matveev V.A.

Vitebsk State Order of Peoples’ Friendship Medical University, Belarus

The comparative characteristics of clarithromycin in the treatment of respiratory tract infections in children

Summary. The pharmacokinetic and clinical parameters of various 14- and 15-membered macrolides were compared for infections of the upper and lower respiratory tract in children. It has been shown that clarithromycin is the drug of choice for this pathology, which is due to its predominant accumulation in the target organs, optimal spectrum of action, low bacterial resistance-inducing activity, good tolerance, and clinical approbation in various clinical situations.

Keywords: clarithromycin, respiratory infections, children.

summary. The comparison of the pharmacokinetic and clinical properties varies 14- and 15-membered macrolides in the treatment of respiratory tract infections in children was performed. It is shown that clarithromycin is a drug of choice for this pathology that is caused by the next good characteristics: the primary accumulations in target tissues, the optimum spectrum of antibacterial action, the low resistance inducing activity, the good tolerance and broad clinical experience in various clinical situations.

keywords Key words: clarithromycin, respiratory tract infections, children.

Macrolides - chemical structures with a lactone ring in the center, are one of the most long-used and widely used antibiotics (ATBs). The first representative of this group was erythromycin, which was isolated from the culture Streptomyceserythreus and entered clinical practice in 1952. Later, several more natural macrolides were discovered: spiramycin, josamycin, midecamycin. By chemical modification of natural compounds, semi-synthetic preparations were obtained: midecamycin-acetate, roxithromycin, clarithromycin, as well as azalide close to macrolides in structure - azithromycin, which favorably differ from the original ATP in a number of positive qualities: higher bioavailability, stability in the gastrointestinal tract, additional activity against significant pathogens, a slight motilin-like effect.

According to the number of atoms in the lactone ring, 14-, 15- (azalides) and 16-membered macrolides are distinguished. The spectrum of this group of ATP drugs is relatively narrow: the highest activity is observed against gram-positive cocci, especially streptococci, including S. pneumoniae. Staphylococci are much less sensitive. One of the main advantages of macrolides is their activity against atypical bacteria, which is due to their selective intracellular accumulation. Of certain importance is the ability of macrolides to suppress the reproduction of diphtheria bacilli, as well as some gram-negative bacteria, primarily B. pertussis, H.pylory, N. meningitidis, H. influenzae .

Various representatives of the macrolide group are recommended for uncomplicated infections of the skin and soft tissues, toxoplasmosis of newborns and pregnant women, atypical mycobacteriosis, helicobacteriosis of the stomach and duodenum, gynecological infections. However, the main clinical indication for the use of this group of drugs (PM) are infections of the upper and lower respiratory tract in children and adults. At the same time, the activity of various macrolides in this pathology varies significantly. The most optimal properties are 14- and 15-membered macrolides, in the first place - a representative of the "new" semi-synthetic drugs - clarithromycin.

Clarithromycin (6-O-methylerythromycin) was developed as a result of chemical modification of erythromycin by replacing the hydroxyl group in position C 6 with a CH 3 group. This led to better and more stable absorption of the drug in the gastrointestinal tract, increased its acid resistance, ATP activity against a number of microorganisms sensitive to macrolides, including due to stability in the acidic environment of endosomes, which is fundamentally important for the effect on intracellular pathogens.

Forms of release and dosing

Clarithromycin is available as tablets, powders for oral suspension and infusion solution for parenteral use. The latest dosage form in our country is currently missing.

Tableted clarithromycin exists in the form of immediate release ("Fromilid", tab. 250 mg and 500 mg) and prolonged ("Fromilid-Uno", tab. 500 mg).

In the treatment of infections of the upper and lower respiratory tract in children over 12 years of age and / or weighing > 33 kg, conventional clarithromycin is prescribed 250 mg every 12 hours. For the treatment of acute sinusitis, severe infections and when the process is caused by H. influenzae The dose is 500 mg every 12 hours.

Long-acting clarithromycin in the same age group is prescribed 500 mg every 24 hours. For the treatment of severe infections, the daily dose is increased to 2 tablets of 500 mg every 24 hours. Tablets should not be broken. They are swallowed whole with a small amount of liquid. It is recommended to take the drug during meals. For children under 12 years of age, sustained release clarithromycin is not prescribed.

In children under the age of 12 years and / or weighing less than 33 kg, clarithromycin (Fromilid) is usually used as a suspension at the rate of 15 mg / kg / day in two divided doses (Table 1). It is recommended to drink this drug with a small amount of liquid, since the suspension contains tiny granules that taste bitter. Syringe provided for oral administration drug. One filled syringe holds 5 ml of suspension containing 125 mg of clarithromycin. The syringe should be rinsed after each use.

Table 1. Dosing of suspension "Fromilid" in children depending on body weight

The course of treatment of infections of the upper and lower respiratory tract drugs "Fromilid" and "Fromilid-Uno" is usually 7-14 days.

Mechanism of action and resistance

The effect of clarithromycin, like other macrolides, is due to the suppression of protein synthesis in the microbial cell. The latter is associated with the ability of these ATPs to reversibly bind to various domains of the catalytic peptidyltransferase center of the 50S ribosome subunit. As a result, the course of transpeptidation and translocation reactions is disrupted. A negative effect of macrolides on the assembly process of the 50S subunit itself has also been established. These effects are especially significant in clarithromycin, exceeding those of erythromycin and azithromycin by 2 and 33 times, respectively. Due to differences in the structure of the ribosomes of eukaryotic and prokaryotic cells, the negative effect on protein synthesis affects bacteria to a much greater extent in comparison with the macroorganism. This feature is the reason for the low toxicity of the entire group of macrolides, including clarithromycin.

The effect of clarithromycin on microbial cells is associated not only with the action of ATP itself, but also with its active metabolite: 14-hydroxyclarithromycin (14-hydroxyclarithromycin). This product has a pronounced activity against the most important infectious agent respiratory system - H. influenzae. This property positively distinguishes clarithromycin from most other representatives of the macrolide group, the overwhelming effect of which on the specified pathogen, except for azithromycin, is insufficient.

The action of macrolides on sensitive flora is usually bacteriostatic. However, a bactericidal effect is also possible, for the implementation of which the type of microorganism, the growth phase of bacteria, the size of the lesion and the pH of the medium are important. The bactericidal action is described in relation to S. pyogenes, S. pneumoniae, N. meningitidis, B. pertussis, C. diphtheria, H. influenzae and M. catarrhalis .

Resistance to macrolides is due to two main mechanisms: target modification by methylation of binding points in the ribosome structure (MLS B-phenotype) or activation of the mechanism of removal (efflux) of these ATPs from the bacterial cell (M-phenotype). The first occurs under the influence of the bacterial enzyme methylase and, as a rule, leads to the emergence of high-level resistance (MIC 90> 32-64 mg / l) to all macrolides. This type of stability is typical for S. aureus, M. pneumoniae, S. pneumoniae, S. pyogenes .

Second mechanism, adjustable mef- genes, is significant only for 14- and 15-membered representatives of the macrolide group, the severity of emerging resistance is significantly lower (MIC 90 1-32 mg / l) and, in principle, there is a chance to overcome it with a high dose in case of accumulation of ATP in the focus of the lesion. Efflux is most typical for S. pneumoniae, S. pyogenes, S. aureus, S. epidermidis. It is also believed that, to a large extent, it is due to the activity of this internal pump that most strains H. influenzae have higher MIC values ​​for macrolides compared to S.pneumoniae .

The study of PeGAS-I showed that in the territories closely adjacent to the Republic of Belarus, the M-phenotype of pathogen resistance to macrolides has the main significance (about 75%) .

Pharmacokinetics

Clarithromycin is well absorbed from the gastrointestinal tract. Bioavailability when taken orally reaches 55%, which is significantly higher compared to other "new" macrolides, including azithromycin (37%). The degree of absorption does not depend on food intake, which distinguishes clarithromycin from erythromycin and spiramycin. Communication with proteins is, according to various sources, from 42 to 90%, on average - 65-75%. Approximately 20% of absorbed clarithromycin is immediately metabolized in the liver by cytochrome enzymes CYP 3A4, CYP3A5 and CYP3A7 with the formation of several products, mainly 14-hydroxyclarithromycin. Last in regards to the series pathogenic bacteria, especially H. influenzae, acts in combination with clarithromycin synergistically. Metabolites of other macrolides do not possess similar properties.

Maximum plasma concentration IA is achieved in less than 3 hours after oral administration. Clarithromycin easily penetrates into tissues and body fluids, and accumulates especially actively in lung tissue, where its concentration is 5-6, and in epithelial cells- 20 times higher than in blood plasma (Table 2). Similar indicators for the nasal mucosa and tonsil tissue are 2-4 times. Alveolar macrophages accumulate clarithromycin in amounts exceeding serum level 200-400 times. It is also concentrated in cells immune system. So, in granulocytes, the content of clarithromycin is 20-38, and in mononuclear cells - 16-24 times higher than in the extracellular fluid. Due to this, transport of ATP directly to the focus of inflammation is possible. The active metabolite 14-hydroxyclarithromycin also penetrates well into the fluids and tissues of the respiratory system, although the concentrations achieved are lower compared to the parent substance.

As can be seen from Table. 2, the degree of accumulation of clarithromycin in various fluids and structures of the lung tissue is maximal compared to other 14- and 15-membered macrolides, including azithromycin.

Table 2. Comparative concentrations of clarithromycin and other 14- and 15-membered macrolide antibiotics in serum and lungs after oral administration

Another positive quality of clarithromycin is the maintenance of its relatively high level in plasma / serum during therapy. In contrast, azithromycin, which is characterized by excessive intracellular accumulation, is practically absent in these substrates. Potentially, this distribution the specified drug can increase the risk of adverse outcome in severe lung infections that occur with bacteremia.

The half-life of clarithromycin (T 1 / 2) after taking a dose of 250 mg is from 3 to 4 hours, after taking a dose of 500 mg - from 5 to 7 hours. These figures are significantly lower than those for azithromycin - 48-96 hours. On the one hand, a long half-life allows the use of special regimens for the use of the latter: once a day for only 3-5 days. On the other hand, a significant T 1/2 carries the threat of excessive induction of bacterial resistance. Azithromycin, located almost exclusively inside the cells, is gradually released into the extracellular fluid, where the main pneumopathogens are located, for example S. pneumoniae, S. pyogenes, H. influenzae etc., and suppresses their vital activity. This period of effective action continues after the completion of a short course of therapy for about another 5-7 days. Then, for an extremely long time - up to 4 weeks - the concentration of azithromycin in the extracellular fluid for the main pathogens remains at a subinhibitory level. This is the so-called selective window, which contributes to the vigorous formation of flora resistance, not only in relation to causative ATP, but also to other macrolides. The mechanism of the resulting resistance has not been precisely established, but it is believed that it is associated with efflux activation. On the other hand, azithromycin is a powerful inducer of the methylase enzyme, which provides a particularly unfavorable MLS B-phenotype of resistance to all macrolide ATPs at once.

Due to the short half-life of clarithromycin, these disadvantages are devoid of. In addition, when it is used, the risk of prolonged and delayed allergic reactions, which is described against the background of the use of azithromycin. The post-antibiotic effect of clarithromycin is longer than beta-lactam ATP and in relation to S.pneumoniae- the same azithromycin.

Clarithromycin is excreted primarily in the urine, but also in the bile and intestines. The ratio of the parent substance and its metabolites during excretion is approximately the same. In patients with severe kidney failure(level of excretion of creatinine<30 мл/мин) процесс выделения существенно нарушается и доза кларитромицина должна быть уменьшена .

The pharmacokinetics of clarithromycin when used as a suspension is practically the same as described above, although the amount of metabolite 14-hydroxy-clarithromycin formed during the exchange is slightly less.

Sustained release tablets to improve absorption must be taken with food, while this is not necessary for regular clarithromycin. The maximum concentration (Cmax) in the blood plasma is somewhat lower, it is reached after about 7-8 hours, and its gradual decrease begins only in the second part of the 24-hour interval. Thus, fluctuations in the level of ATP in plasma when taking the prolonged form are significantly (p = 0.0001) less. The indicators for both forms in relation to 14-hydroxy-clarithromycin are close, the concentrations of active components in plasma by the end of the day are similar. Other pharmacokinetic parameters also do not differ significantly, excretion details have not been studied.

Action spectrum

The minimum inhibitory concentrations of clarithromycin for 50 and 90% strains (MIC 50 and MIC 90, respectively) of the most important bacterial pathogens are presented in Table. 3.

Table 3 Comparative activity of clarithromycin and other 14- and 15-membered macrolides against major pathogens in studies in vitro

Note: the level ≤2 mg/l was considered a sign of sensitivity, 2-8 mg/l - moderate sensitivity, >8 mg/l - resistance of pathogens to macrolide antibiotics. PS - penicillin-sensitive strains; PI - strains with intermediate sensitivity to penicillin; PR - penicillin resistant.

As can be seen from Table. 3, the spectrum of action of clarithromycin against almost all major pathogenic bacteria is optimal compared to other 14-15-membered macrolides. So, it has the lowest MIC of 50-90 in relation to the most important gram-positive cocci: pneumococci, including those with intermediate sensitivity to penicillin, staphylococci, streptococci gr. A and B, as well as Listeria. The same applies to a significant part of gram-negative bacteria, including the causative agent of such a severe infectious lung lesion as legionellosis. Clarithromycin is effective against most strains Moraxella (Branhamella) catarrhalis, both producing and not producing beta-lactamase. Due to synergism with the 14-hydroxy-clarithromycin metabolite, there is sufficient clinical activity against the most problematic pathogen for macrolides - H.influenzae. Along with azithromycin, clarithromycin is the only one in the ATP group under consideration that has this property. At the same time, the suppressive effect is also noted in relation to strains of the specified pathogen producing beta-lactamase. The activity of clarithromycin against atypical bacteria is also extremely high. In particular, its MIC for chlamydia in this ATP group is minimal. It surpasses, with the exception of azithromycin, other 14 and 15-membered macrolides in terms of effects on M. Rneumoniae.

At the same time, it is necessary to take into account the following practical facts. Methicillin-resistant (MRSA and MRSE) staphylococci are not sensitive to clarithromycin, as well as to all other macrolides. High activity of clarithromycin is observed mainly in relation to erythromycin-sensitive streptococci and staphylococci. Erythromycin-resistant ones are much more resistant, but this is also true for most other members of the macrolide group, including azithromycin. At the same time, in the case of the MLS B variant, the level of resistance is very high, while against the background of the activation of the efflux mechanism, the moderate effectiveness of clarithromycin due to the achievement of high concentrations in the affected areas can be maintained.

Clinical efficacy of clarithromycin in respiratory tract infections in children

The effectiveness of clarithromycin has been proven in the defeat of various parts of the respiratory system in children.

Streptococcal tonsillitis/pharyngitis. As with other infectious lesions of the lower and upper respiratory tract, in this pathology, macrolides, including clarithromycin, are more often prescribed for allergies to beta-lactam ATPs. However, given the extremely high activity against S. pyogenes, in this case they can be considered as drugs of choice. In addition, modern macrolides provide more reliable eradication of the pathogen from the nasopharynx, reaching 90-95%, which is important for the prevention of late complications of streptococcal infection: glomerulonephritis and rheumatism.

The effectiveness of clarithromycin in streptococcal processes is beyond doubt. For example, in a study by J.G. Still et al. in the treatment of 191 children aged 6 months. up to 12 years of age with streptococcal pharyngitis, clinical efficacy reached 96%, bacteriological - 92%. The latter indicator significantly exceeded that for phenoxymethylpenicillin - 81%. When compared with other anti-TB drugs, clarithromycin was as clinically effective as cefadroxil, lincomycin, or benzathine-penicillin, and clinical symptoms stopped earlier than with amoxicillin/clavulanate. Eradication rate S. pyogenes 94.7% are also given by researchers from Japan. N.L. Kearsley et al. demonstrated equal clinical efficacy of clarithromycin (98%) and amoxicillin (97%) in 229 children with streptococcal tonsillitis/pharyngitis in England. In the treatment of more than 1000 children in Italy, the clinical efficacy of clarithromycin reached 90.9%. At the same time, in this study a relatively high level of resistance of streptococci to macrolides was recorded, due to various mechanisms. This confirms the danger of using representatives of the group that cause an intensive increase in the resistance of pathogenic bacteria, primarily azithromycin.

The evidence base for extended-release clarithromycin is not so extensive, however, in a randomized, double-blind, multicenter study, using this drug for 5 days at 500 mg / day once in 539 patients with streptococcal tonsillopharyngitis, which included children from 12 years of age, clinical effect reached 94%, and the eradication rate S. pyogenes- 89%, which did not differ from the results of a 10-day course of phenoxymethylpenicillin.

Rhinosinusitis/otitis media. Etiologically the main role in otitis media and ri nosinusitis plays no longerS. pyogenes, and other microorganisms: S. pneumoniae, Moraxella (Branhamella) catarrhalis, H. influenzae, Staph. spp., however, most of them are also included in the spectrum of action of clarithromycin. In addition, this drug accumulates in the middle ear cavity, nasal mucosa and paranasal sinuses in concentrations significantly higher than serum levels, which ensures the optimal clinical effect.

According to A. Arguedas et al., the clinical efficacy of a 10-day course of clarithromycin in acute otitis media in children over 6 months of age. up to 12 years was 95.7%. Numerous studies suggest that clarithromycin is at least as effective in this pathology as amoxicillin, amoxicillin/clavulanate, cefuroxime axetil, or cefaclor. So 5-day courses of clarithromycin and amoxicillin / clavulanate had a clinical efficacy of 92 and 95%, respectively, 10-day courses of clarithromycin and amoxicillin - 95 and 92%, respectively, and the level of bacteriological sanitation reached 100 and 89%, respectively. At the same time, the tolerability of clarithromycin in children was the best compared to other ATPs, especially those protected by aminopenicillins. At the same time, it must be borne in mind that in this pathology, a steadily increasing resistance of pathogens to macrolide ATPs has been recorded.

Experience with clarithromycin in paranasal sinus infections has also been generally positive. In particular, a multicenter European study, which included 310 children, demonstrated the effectiveness of this drug at the level of 97.3%. As a result, clarithromycin is considered the ATP of choice for acute and chronic rhinosinusitis in children allergic to beta-lactam ATPs. In a non-comparative study in Japan, clarithromycin 10 mg/kg twice daily improved clinical symptoms was observed in 89% of 36 children with sinusitis and otitis media, and an improvement in the x-ray picture - in 82%. Multicentre, randomized, double-blind studies have shown comparable activity for clarithromycin, cefuroxime axetil, levofloxacin, sparfloxacin, and ciprofloxacin in acute adult sinusitis. The presence of any differences in this regard in children is unlikely. The use of conventional clarithromycin and extended release clarithromycin in 39 adolescents diagnosed with sinusitis demonstrated a clinical efficacy rate of 90%.

When using clarithromycin in children with chronic ENT processes, it is necessary to take into account the increased risk of the presence of pathogens highly resistant to macrolide ATP, including anaerobes - b.fragilis .

Bronchitis and pneumonia. Clarithromycin is highly active against most pathogens of infectious lesions of the lower respiratory tract, including those caused by atypical flora: M. pneumoniae, Chl. pneumoniae. As for the level of clinical efficacy, although the main studies were conducted on adult patients, there is evidence from pediatric practice(Table 4).

Table 4. Efficacy of clarithromycin in lower respiratory infections in children (adapted in part from )

As can be seen from Table. 4, the effectiveness of clarithromycin in lower respiratory tract infections in children was quite high, both in clinical terms and in terms of eradication of causative pathogens, especially chlamydia and mycoplasmas. At the same time, the effectiveness of treatment was not inferior to other widely used ATP drugs, such as amoxicillin/clavulanate or cefuroxime. Tolerability of clarithromycin was good, significant side effects, unlike erythromycin, were not observed. A positive factor was the high rate of onset of the result, often exceeding that of penicillin, amoxicillin and some cephalosporins, which positively affects the pharmacoeconomic indicators of the use of clarithromycin.

Pediatric experience with sustained release clarithromycin for lower respiratory tract infections is limited and, due to available prescribing recommendations, is practically limited to adolescents. However, S.L. Block showed equal (90%) efficacy of this dosage form and conventional clarithromycin in patients aged 6-16 years with community-acquired pneumonia, with fewer side effects in the latter.

Thus, clarithromycin is a highly effective and widely tested drug. Due to the accumulation in the tissues and fluids of the respiratory system, the optimal spectrum of action, proven clinical efficacy, ease of use, it should be considered as the drug of choice among the entire family of macrolides for infectious lesions of the upper and lower respiratory tract in children.

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21.Nishimura T. , Sugita K. , Taniguchi K. et al. // Jpn. J. Antibiot. - 2003. - Vol. 56, No. 4. - P. 281-288.

22.Kearsley N.L., Campbell A., Sanderson A.A.. et al. // Br. J.Clin. Pract. - 1997. - Vol. 51, No. 3. - P. 133-137.

23.Rondini G., Cocuzza C.E., Cianflone ​​M. et al. // Int. J. Antimicrob. agents. - 2001. - Vol. 18, No. 1. - P. 9-17.

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26.Ramet J. // Poster presented at the Third International Conference on Macrolides, Azalides and Streptogramins. - Lisbon, 1996.

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Attention! The article is addressed to medical specialists. Reprinting this article or its fragments on the Internet without a hyperlink to the original source is considered a copyright infringement.

The spectrum of application of azithromycin is very wide, therefore, there are quite a lot of dosage forms of this drug. These are powder for dilution with water and oral consumption, granules for dilution with water and oral consumption, a special form for dilution and use as injections, capsules and tablets for oral consumption.

Azithromycin is able to both slow down the reproduction of the pathogen, and completely destroy it. The effect depends on the prescribed dosage. Azithromycin can destroy most gram-positive and gram-negative microbes, some anaerobic microbes. DO NOT ATTEMPT TO TAKE AZITHROMYCIN AGAINST THE GERMS WHICH ERYTHROMYCIN "DOES NOT TAKE".

What diseases are prescribed azithromycin?

These are infectious diseases of the organs of the ear-nose-throat system, upper and lower respiratory tract. Also, azithromycin is effective for erysipelas, impetigo, dermatoses infected with an infection. Azithromycin is also used for infectious diseases of the genitourinary system, such as urethritis (both with the formation of pus and without it), cervicitis. Together with some other drugs, azithromycin is prescribed for the complex treatment of peptic ulcers of the digestive system caused by Helicobacter pylori.

Who should not take azithromycin?

Azithromycin is not prescribed to newborn babies, as well as to small patients with kidney or liver dysfunction. Certain types of azithromycin are not approved for use by patients under the age of sixteen. Azithromycin is not prescribed for individual intolerance to azalides and macrolides, with severe disorders of the kidneys and liver. Pregnant women are sometimes prescribed azithromycin, but there is still some risk. It is not allowed to take azithromycin during breastfeeding. In addition, even a perfectly healthy person with heart rhythm disturbances is forbidden to use azithromycin.

Can azithromycin cause side effects, and which ones?

Unfortunately, all antibiotics cause side effects. Some more, some less. In the case of oral administration, azithromycin causes diarrhea in five percent of patients, nausea in three percent, discomfort in the stomach in three percent. Such unpleasant disorders as bloating, vomiting appear in less than one percent of patients.

In the treatment of azithromycin, migraine-like pain, lack of coordination, and lethargy may occur. In addition, azithromycin can cause various kinds of allergic manifestations, such as skin rashes, swelling of the larynx. With the introduction of azithromycin intravenously, inflammation may appear at the injection site.

How much azithromycin is prescribed?

The dosage depends on the disease and the condition of the patient. Oral azithromycin is taken once a day, one hour before a meal or two hours after a meal.

Intravenous injections of azithromycin are prescribed, as a rule, for pneumonia and other serious diseases for the first two days of treatment. Then the patient switches to taking azithromycin in the form of tablets or capsules orally.

How is azithromycin combined with other drugs?

The use of azithromycin along with alcohol and food inhibits the absorption of azithromycin. With simultaneous treatment with azithromycin and warfarin, it is necessary to monitor the number of platelets in the blood. With the simultaneous use of azithromycin and cycloserine, the activity of the latter increases. With simultaneous use with tetracycline and chloramphenicol, the activity of azithromycin is enhanced. It is forbidden to apply simultaneously with heparin.

When treating with azithromycin, it is recommended to take vitamin dietary supplements (biologically active supplements) to maintain the body.

Which is better: clarithromycin or azithromycin?

Azithromycin and clarithromycin belong to the macrolide class of antibiotics. This group has a wide spectrum of action, copes with intracellular microbes and is actively used today.

Macrolides

All drugs from this group are divided into several types. The classification is based on the chemical structure and natural origin.

The first natural macrolide antibiotic is erythromycin, all other drugs are compared with it. It has the smallest spectrum of activity, is poorly absorbed and is excreted from the body for a long time. Therefore, when choosing: clarithromycin, azithromycin or erythromycin, the latter should not be preferred.

The drugs we are considering are representatives of semi-synthetic macrolides, which were created artificially in order to improve the properties of the drug.

At the same time, clarithromycin is a 14-membered molecule in chemical structure, and azithromycin is 15-membered. This, of course, affects their properties and action in the body.

Let's try to find out, clarithromycin or azithromycin: which is better?

Clarithromycin

The mechanism of action of all substances of this group is the same. Azithromycin or clarithromycin, when interacting with a microbe, will first stop its reproduction, and in high concentrations, kill it. However, these antibiotics differ from each other in some features.

Clarithromycin has the following benefits:

• The highest bioavailability among all macrolides. The agent easily penetrates into the bloodstream when taken orally and is distributed throughout the body.
• Fast half-life. In just 5-7 hours, half of the drug will already be processed and removed from the body.
• There are intravenous and oral forms. The drug is available in tablets and powder for suspension.
• More active against Helicobacter, therefore it is used in the treatment peptic ulcer and gastritis.
• Able to destroy atypical microorganisms faster than other macrolides.

This drug also has certain disadvantages:

• It does not act on its own, but due to the active metabolite, which is already formed in the body.
• If the patient has kidney disease, the elimination of the drug is seriously slowed down.
• Cannot be used during pregnancy, lactation and in babies under 6 months of age.

Before choosing clarithromycin or azithromycin, you need to familiarize yourself with the features of each drug.

Azithromycin

This drug already has a different chemical structure than clarithromycin. Its spectrum of activity and features of distribution in the body are different.

• A large number of dosage forms for oral administration: tablets, capsules, powders, syrups.
• Able to destroy enterobacteria and more actively affects Pseudomonas aeruginosa.
• Can be used with or without food.
• Creates the highest concentration in tissues among all macrolides, causes the effect faster.
• The drug is well tolerated, unlike many other antibiotics.
• It is taken only 1 time per day, which makes it easier for patients to use.
• Can be used in the form of short courses - only 3-5 days. In children, a single use is possible.

• It is used exclusively inside. Cannot be used to treat sepsis, endocarditis and other systemic diseases.
• It has two times lower bioavailability than clarithromycin.
• It takes a long time to be excreted from the body. For two days, on average, only half of the incoming substance is processed.

Now you know the advantages and disadvantages of both drugs and it has become easier to make a choice: azithromycin or clarithromycin. It is recommended to choose an antibiotic together with a doctor who knows the spectrum of activity of each remedy.

20 real analogues of the antibiotic clarithromycin

Clarithromycin binds to the 50S subunit of the ribosome membrane of the bacterial cell and inhibits protein biosynthesis. Active against intracellular pathogens.

The drug is superior to erythromycin in pharmacokinetic and antibacterial properties. The antibiotic is stable in an acidic environment. When taken orally, it is absorbed fairly quickly. Cmax is reached after about 2.5 hours.

The drug is used in the first line of Helicobacter pylori eradication. The antibiotic causes side effects from the nervous system, digestive tract and hematopoietic organs. The original drug clarithromycin affects the senses. The antibiotic is contraindicated in children under 12 years of age and in patients with hypersensitivity to at least one component in the composition.

Clarithromycin analogues

Binoclair is active against gram+ (staphylococci, streptococci), gram- (hemophilic bacillus, hemophilus, gonococcus, legionella pneumophila, campylobacter jejuni) foreign agents, as well as anaerobes (bacteroids, clostridia, peptostreptococci). Rapidly absorbed from the gastrointestinal tract. Bioavailability reaches 50 percent. The half-life is about 4 hours.

Klabaks is a semi-synthetic macrolide of the latest generation. Klabaks is effective in the treatment of tonsillitis, pneumonia, furunculosis. The antibiotic is taken at 250 mg twice a day, with severe infections, the dosage is increased by 2 times. The course of treatment is from 1 to 2 weeks.

Klabax OD is a broad-spectrum macrolide, belongs to the 2nd generation, acts bacteriostatically.

Klabax OD is forbidden to be taken simultaneously with some antihistamines and serotonergic drugs, as well as antipsychotics. The drug is contraindicated in severe pathologies of the kidneys and liver, as well as in patients with porphyrin disease.

Klarbakt also affects protein synthesis of pathogenic microorganisms. It is active against all mycobacteria, except for Koch's Wands.

Klarbakt is absorbed quickly. Eating slows down absorption. Prolonged antibiotic therapy is fraught with the development of superinfection (candidiasis). The antibiotic penetrates into women's milk, so the treatment of lactating women is possible with the abolition of breastfeeding.

Clarithrosin is available in the form of yellow film-coated tablets. The medication is taken orally, regardless of food intake.

Clarithrosin is prescribed for inflammation of the bronchial mucosa, lymphoid tissue of the pharynx, palatine tonsils, paranasal sinuses, nosocomial pneumonia, hair follicle and infections of the oral cavity. The drug is taken to prevent the recurrence of peptic ulcer.

Klacid interacts with the 50S ribosomal subunit. The drug can be taken in the treatment of three-year-old children. The drug is rapidly absorbed in the gastrointestinal tract. Bioavailability reaches 50 percent. The production of β-lactamase does not affect the activity of Klacid. Most strains of Staphylococcus are resistant to the antibiotic.

Clerimed belongs to macrolides, its main active ingredient is clarithromycin. The antimicrobial mechanism is based on the ability of the antibiotic to interact with the 50S-ribosomal subunit, which negatively affects protein synthesis in the cell. The antibiotic crosses the protective barrier between maternal and fetal blood in the placenta.

Crixan is prescribed by doctors for infections of the respiratory tract, skin and inflammation of the ear. Indications also include chlamydia and mycobacteriosis. Drugs are taken with caution in renal or hepatic insufficiency. When taken together with drugs that inhibit the activity of the blood coagulation system and prevent the formation of blood clots, it is necessary to control the prothrombin time.

Lecoclar should not be prescribed to children under six months of age, as there is insufficient data on its efficacy and safety at this time. The antibiotic is contraindicated in patients with a history of hepatitis. The drug has an extensive list of side effects: from dyspeptic disorders to hearing loss.

Fromilid exhibits a bacteriostatic effect, but it has a bactericidal effect on some strains. Fromilid is prescribed to patients with acquired immune deficiency syndrome. HP is well absorbed when taken orally. The elimination half-life averages about 5 hours.

Fromilid UNO is contraindicated in lactose intolerance. Drugs are not prescribed to patients under 18 years of age. Fromilid UNO causes side effects from the gastrointestinal tract, skin and subcutaneous tissue, nervous and urinary systems, sensory organs and hematopoiesis, heart, musculoskeletal system. At admission, changes in laboratory parameters are noted. Medicine is released only according to the recipe.

Analogues include Vero-Clarithromycin, Clarithromycin Protech, Clarithromycin SR, Clarithromycin Ecocitrin, Clarithromycin-OBL, Clarithromycin-Verte. All drugs act bacteriostatically, they are active against gram + cocci and intracellular and membrane pathogens, reach high concentrations in tissues, have a low risk of developing cross-allergy with beta-lactams when taken.

Semi-synthetic 14-mer macrolides

When deciding how to replace Clarithromycin, doctors often prescribe the following drugs:

Rulid belongs to the pharmacological group of macrolides and azalides. The main active ingredient is roxithromycin. It is superior to erythromycin in terms of pharmacokinetic and microbiological parameters. Increasing the dosage allows you to achieve a bactericidal effect.

The antibiotic has low toxicity. Active against Streptococcus, Listeria, Staphylococcus, Corynebacterium diphtheriae, Neisseria meningitidis, Legionella and Mollicutes. Drugs are prescribed for whooping cough, acute pharyngitis, chronic obstructive pulmonary disease, cercevit, as well as

genital and dental infections.

Esparoxy is effective in the treatment of diseases of bacterial etiology of the respiratory tract (pneumonia), ENT organs (otitis, sinusitis), skin (erysipelas) and urinary tract (urethritis). Therapy with this generic Clarithromycin is carried out only after 12 years. The antibiotic is taken once a day at 300 mg or twice a day at 150 mg. If antibiotic therapy lasts more than 2 weeks, then a clinical blood test is performed. The drug affects the concentration of attention and reduces psychomotor reactions.

Roxithromycin is a semi-synthetic macrolide, the action of which depends on the dosage: in high doses, a bactericidal effect is achieved. Pathogens that synthesize enzymes that can break down beta-lactam antibiotics are sensitive to it. It is prescribed as a prophylaxis of bacteremia after dental interventions. The antimicrobial agent is widely used in pediatric practice and is prescribed to children from two months.

Clarithromycin or Azithromycin: which is better and what is the difference?

Azithromycin is a semi-synthetic broad-spectrum antibiotic belonging to the azalide group. In its structure, Azithromycin differs from classical macrolides. It was first synthesized by the Croatian pharmaceutical company Pliva in the 1980s.

• The drug has a wide spectrum of activity. Azithromycin has several dosage forms: powder, capsules, tablets and syrup (each trade name has its own release form). It is inactive against Gram+ microorganisms resistant to erythromycin.
• The drug is widely used in gastroenterology (it is part of the complex therapy of stomach ulcers), urology and gynecology (inflammation of the urethra and cervix), dermatology (impetigo) and otolaryngology (infectious diseases of the ENT organs).
• Azithromycin is not prescribed to newborns and children with liver or kidney dysfunction. Treatment of pregnant women is possible only when the benefits of using an antibiotic outweigh the possible risks. Patients with cardiac arrhythmias should take Azithromycin with caution. The lactation period is a contraindication.
• When taken orally, the antibiotic causes diarrhea in about 5% of patients. Vomiting, flatulence and nausea appear much less frequently. Nephritis and vaginal candidiasis are diagnosed in 1% of patients. Against the background of antibiotic therapy with Azithromycin, migraine-like headaches may occur.

The dosage is determined by the patient's condition and depends on the severity of the infectious process. The antibiotic is taken one hour before meals or two hours after the last meal. Injection is practiced for pneumonia (first days of therapy). The antimicrobial drug and ethyl alcohol are incompatible: alcohol reduces the absorption of drugs, which contributes to the progression of the infection. To eliminate the latter, stronger antimicrobial agents will be needed. An analogue of Clarithromycin is twice cheaper than the original drug.

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List of over-the-counter antibiotics + reasons for the ban on their free circulation

In the forties of the last century, humanity received a powerful weapon against many deadly infections. Antibiotics were sold without prescriptions and allowed

Source:

Azithromycin instructions for use price reviews analogues

Many drugs have a wide range of effects, allowing you to get rid of numerous diseases. One popular antibiotic is azithromycin. Instructions for use, price, reviews, analogues - all this will be discussed in the material presented. The tool has a semi-synthetic origin and has a wide range of effects on the body. The structure has its own characteristics; for ease of use, several convenient forms are assumed.

What does azithromycin help with?

Azithromycin is a drug that has a special effect in relation to gram-positive and gram-negative bacteria. The drug is widely used in the treatment of a number of infectious and inflammatory processes, the properties of which were derived from pathogens of various kinds. In the course of entering the body, the antibiotic creates increased concentrations of the main substance in the focus of the inflammatory process - azithromycin dihydrate. It is not susceptible to the negative factors of an acidic environment and is soluble in fats, therefore it is able to easily penetrate into soft tissues, various liquids of biological origin, and the respiratory tract. After a two-hour period of time after administration, the agent reaches its maximum content in concentration.

Analogues and varieties of the drug

Pharmaceutics offers several manufactured forms of the drug:

• Tablets (film shell);
• capsules with gelatin content;
• suspension powder.

Tablet forms suggest 250 mg and 500 mg of the main active ingredient in addition to auxiliary elements. Packaging is carried out in special cardboard packs of three tablets.

Indications for the use of the remedy

• Infectious processes in the respiratory organs and tracts;
• infections and various kinds of lesions in the area of ​​soft tissues and integuments of the skin (they help well with acne, redness);
• diseases associated with the functioning of the reproductive system and genitourinary features (tablets help with cystitis and other kidney and genital infections and inflammations);
• problems associated with ENT organs (drugs for flu, sore throat, sinusitis and other diseases help);
• dermatological processes during secondary infection with bacteria;
• combined methods of treatment for diseases of the gastrointestinal tract.

The appointment of antibiotic groups is solely the responsibility of a specialist, taking into account the individual characteristics of the organism, the presence of pathologies and other phenomena.

Contraindications for use

There are no particular difficulties when taking it, but if you have sensitivity to the components, you should stop taking it. If there are allergic reactions, it is better not to start treatment. Special contraindications include the state of pregnancy, feeding, children under 12 years of age.

Azithromycin instructions for use capsules 500 mg

The drug is taken once a day for an hour or 2 hours before or after a meal.

• Adults in case of detection of infectious processes in the respiratory tract 500 mg per day once, for 3 days (total course dosage - 1.5 g).
• For infections of the skin and soft tissues, the following medication regimen is indicated: on the 1st day of treatment, the drug is 1000 mg (two 500 mg capsules) once. And starting from the second day to the 5th day - take the drug dosage of 500 mg (1 capsule) per daily period.
• If chronic erythema migratory type is found, it is necessary to take the remedy according to a certain scheme. On the 1st day, 4 capsules (250 mg) are taken - 1 g once. Starting from the second day to the fifth day - 500 capsules (the course - in total, it turns out, 4 days) in the amount of 2 pieces per day.
• In case of detection of urethritis, cervicitis, a single dose of 1 g of 250 mg is taken.
• If gastric diseases are detected, as well as pathologies in the field of functioning duodenum, is prescribed 1 g (4 capsules of 250 mg) per day for 3 days. And this is not the main, but part of the combination therapy.

With angina and other ENT diseases (for example, with sinusitis), you must strictly follow the doctor's instructions. Since the dosages are significantly influenced by the individual characteristics of the organism. If one of the dosages of the remedy is missed, it is necessary to take it as soon as possible. And subsequent doses are drunk with a break of 24 hours. The described dosages are relevant for admission by representatives of the adult and child population weighing more than 45 kg.

Azithromycin instructions for use for children 250

As part of the instructions, children under the age of 12 are prohibited from using tablets. They are successfully replaced by a suspension for children or a special syrup designed to give in to the most successful dosing.

• For infants under six months of age, the antibiotic substance is completely contraindicated, since side effects and complications may occur.
• Children for the treatment of inflammation in the upper respiratory tract, otitis, pneumonia, are prescribed a single dose of medication in the amount of 10 mg / kg.
• Children over 14 years of age use tablets weighing 125 mg or 250 mg, as well as a special syrup. They are assigned 1-2 tsp. composition based on body weight. Over the following days, the treatment process continues at a lower dosage of 5 mg / kg.

Azithromycin tablet price 500 mg price

As already noted, the packaging of the product is carried out in 3 tablets. In general, in Russia the cost of this drug ranges from 32 to 190 rubles. However, it is dose dependent. The 500 mg remedy costs no more than rubles per package.

Azithromycin analogues of the drug cheap

The drug can have a good replacement in the form of budget analogues. Which are cheaper, and in terms of efficiency (in suspension or tablets) are not inferior to the standard sample.

• AZAX is a drug based on azithromycin with a wide spectrum of action.
• AZIMED - this composition is also widely used to treat a large number of diseases. It costs from 100 rubles per pack, which is cheaper than azithromycin.
• AZITRAL is a good choice, the price ranges from 248 rubles to 335 rubles, so the tablets are expensive. The side effects and contraindications are identical.
• ZETAMAKS is a broad-spectrum agent, affordable and topical in effect.
• SUMAMED is an effective analogue of azithromycin costing from 203 rubles per pack of tablets.

Azithromycin compatibility with other drugs

The drug can be used as an independent element of therapy, and in combination with other formulations. It is important to know the features of its compatibility with other drugs.

Azithromycin and cycloferon

The drug cycloferon has excellent compatibility with all means, so the drug in question (antibiotic) is no exception. When used together, medical advice is required.

Azithromycin and paracetamol

Paracetamol is an antipyretic, so it can be perfectly combined with many antibacterial agents of nature and orientation.

Azithromycin and amoxicillin

Azithromycin helps to weaken the powerful bactericidal action of the drug amoxicillin, so sharing is undesirable.

Azithromycin and Ingavirin

No violations were found while taking the drugs, but to clarify the dosages of Ingavirin, it is worth consulting with your doctor.

Azithromycin and ibuprofen

Ibuprofen is a universal drug, therefore, there are practically no drugs with which its simultaneous administration would be inappropriate.

Azithromycin and Kagocel

Kagocel can be used at advanced stages of treatment and can sometimes be used after a course of treatment with azithromycin and simultaneously with it.

Azithromycin what is the difference with other drugs

• Unlike the drug sumamed, azithromycin is a generic, while its analogue is original, and therefore costs much more. There are some differences in side effects and system of contraindications.
• If we compare the drug with Azitrox, it can be noted that one drug acts as a budget analogue of the second. The most optimal option is chosen by the doctor.
• Amoxiclav is another antibiotic that effectively fights broad-spectrum bacterial infections.

Azithromycin and clarithromycin which is more effective

Both drugs are in the top ten drugs against the diseases in question. The differences between azithromycin and clarithromycin, when compared, are in several aspects.

• azithromycin has a shorter course of treatment;
• can be taken once a day and have an effect;
• easier to carry and is the safest.

The difference is small in principle, but it exists. However, self-treatment will not help here, so it is important to contact a specialist who will prescribe an effective drug.

Azithromycin and alcohol compatibility

Using the drug together with alcoholic beverages, you can provoke the transition of many diseases into a chronic form. Therefore, the answer to the question of how long a patient can drink beer lies in the fact that all the symptoms of the disease have passed. Otherwise, consequences may start in the form of pathological complications, pain in the head.

Have you taken azithromycin? Instructions for use, price, reviews, analogues information useful? Leave your opinion or feedback for everyone on the forum!

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Why azithromycin remains the drug of choice for community-acquired lower respiratory tract infections

Infectious and inflammatory diseases of the respiratory tract occupy the first place in the structure of infectious pathology. Pneumonia is the most common infectious cause of death in the world.

Infectious and inflammatory diseases of the respiratory tract occupy the first place in the structure of infectious pathology. Pneumonia is the most common infectious cause of death in the world. In Russia, about 1.5 million people suffer from pneumonia every year. In this regard, the problem of the rational choice of an antibacterial agent for the treatment of lower respiratory tract infections remains relevant. The choice of a drug for antibacterial therapy should be based on its spectrum of action, covering the isolated or suspected pathogen sensitive to this antibiotic, the pharmacokinetic properties of the antibacterial agent, ensuring its penetration at a therapeutic concentration into the corresponding tissues, cells and body fluids, data on the safety of the antibiotic (side effects , contraindications and possible undesirable interactions with other drugs), characteristics of the dosage form, route of administration and dosing regimen that ensure high compliance with therapy, pharmacoeconomic aspects of treatment.

Lower respiratory tract infections and principles of antibiotic choice

In non-specific community-acquired infections, the choice of an antibacterial drug in most cases is based on statistical data on their most common pathogens, as well as information on the effectiveness of certain antibiotics confirmed in controlled clinical trials in infections of known etiology. The forced empirical approach to treatment is associated with the lack of the possibility of microbiological examination in outpatient medical institutions, the duration of bacteriological identification of the pathogen and determination of its sensitivity to antibiotics (3-5 days, and in the case of "atypical" pathogens and more), the impossibility in some cases to obtain biological material for sowing or bacterioscopy (for example, about 30% of patients with pneumonia have an unproductive cough, which does not allow examination of sputum), difficulties in distinguishing between true pathogens and saprophytes (usually oropharyngeal microorganisms that enter the test material). Difficulties in choosing a drug on an outpatient basis are also determined by the lack of full monitoring of the course of the disease and, therefore, timely correction of treatment if it is ineffective. Antibiotics penetrate different tissues and body fluids in different ways. Only some of them penetrate well into the cell (macrolides, tetracyclines, fluoroquinolones, to a lesser extent - clindamycin and sulfonamides). Therefore, even if the drug in vitro shows high activity against this pathogen, but does not reach a level in the place of its localization that exceeds the minimum inhibitory concentration (MIC) for this microorganism, it will not have a clinical effect, although microbial resistance to it will be developed. An equally important aspect of antibiotic therapy is its safety, especially for an outpatient who is deprived of routine medical supervision. In the outpatient setting, oral antibiotics should be preferred. In pediatric practice, the organoleptic properties of the drug are important. To increase the patient's compliance with medical prescriptions, the antibiotic dosing regimen should be as simple as possible, i.e. drugs with a minimum frequency of administration and a short course of treatment are preferable.

Causative agents of non-specific community-acquired infections of the lower respiratory tract

Acute respiratory viral infections (ARVI) occurring with bronchitis syndrome, in some cases, more often in childhood, may be complicated by the addition of bacterial flora with the development of acute bronchitis. The causative agents of acute bacterial bronchitis in childhood are pneumococcus, mycoplasma or chlamydia, less often Haemophilus influenzae, moraxella or staphylococcus aureus. Acute bacterial bronchiolitis in children is caused by moraxella, mycoplasma, and whooping cough. Acute purulent tracheobronchitis in adults in 50% of cases is caused by Haemophilus influenzae, in other cases pneumococcus, less often moraxella (5-8% of cases) or intracellular microorganisms (5% of cases).

Among the bacterial pathogens of exacerbations of chronic bronchitis, Haemophilus influenzae (30-70% of cases), Streptococcus pneumoniae and Moraxella catarrhalis play the main role. For smokers, the association of H. influenzae and M. catarrhalis is most characteristic. In aggravated clinical situations (age over 65 years, long-term course of the disease - more than 10 years, frequent exacerbations - more than 4 times a year, concomitant diseases, severe bronchial obstruction - forced expiratory volume in the first second (FEV1)< 50% должных величин, постоянное отделение гнойной мокроты, алкоголизм, иммунодефицитные состояния) преобладают продуцирующие бета-лактамазу штаммы H. influenzae и M. catarrhalis, этиологическое значение приобретают Enterobacteriaceae (Klebsiella pneumoniae), Pseudomonas aeruginosa, Staphylococcus aureus.

The most common causative agent of community-acquired pneumonia in adults remains pneumococcus (30.5% of cases), less often etiological agents are mycoplasmas (from 12.5% ​​to 20-30%), chlamydia (from 2-8% to 12.5%) or hemophilic wand. In young people, pneumonia is more often caused by a monoculture of the pathogen (usually S. pneumoniae), and in older people or patients with risk factors - associations of bacteria, often represented by a combination of gram-positive and gram-negative microorganisms (21% - C. pneumoniae, 16% - M. pneumoniae , 6% - Legionella pneumophila, up to 11% - H. influenzae). Croupous (lobar) pneumonia in 100% of cases is caused by pneumococcus. M. pneumoniae or C. pneumoniae are common in people under the age of 35 (up to 20-30%), and their etiological role in patients of older age groups is less significant (1-9%). H. influenzae (4.5-18% of cases) often causes pneumonia in smokers, as well as against the background of chronic obstructive bronchitis. In them, in 1–2% of cases, the etiological agent is M. catarrhalis. L. pneumophila is a rare causative agent of community-acquired pneumonia (2–10%, on average 4.8% of cases), but legionella pneumonia ranks second (after pneumococcal) in mortality. Enterobacteriaceae (3-5% of cases), such as K. pneumoniae, Escherichia coli, extremely rarely other enterobacteria, occur in patients with risk factors (age over 65 years, immunodeficiency states, diabetes mellitus, alcoholism, renal, hepatic or congestive heart failure , chronic obstructive pulmonary disease, use of antibiotics in the previous three months, etc.). S. aureus is a rare causative agent of "domestic" pneumonia (less than 5%). The likelihood of staphylococcal pneumonia increases in elderly patients, with drug or alcohol addiction, in patients on hemodialysis, or in people with influenza. Other pathogens are found in no more than 2% of cases. In 39.5% of cases, the pathogen cannot be isolated. In this case, one should take into account the increased role of atypical pathogens (chlamydia and mycoplasmas), the bacteriological isolation of which requires special conditions.

Antibacterial activity of azithromycin

The spectrum of antimicrobial action of all macrolides is the same (Table 1). Although the nature of the action of macrolides is mainly bacteriostatic, azithromycin, which creates high concentrations in tissues, exhibits bactericidal activity against a number of pathogens: H. influenzae, M. catarrhalis, N. gonorrhoeae, S. pneumoniae, S. pyogenes, S. agalactiae, Campylobacter spp ., H. pylori, B. pertussis, C. diphtheriae.

Azithromycin is highly active against probable pathogens of lower respiratory tract infections: pneumococcus (MIC 0.03–0.12 μg / ml), mycoplasma (MIC 0.001–0.01 μg / ml), chlamydia (MIC 0.06–0.25 μg / ml), Haemophilus influenzae (MIC 0.25–1 µg/ml), Moraxella (MIC 0.03–0.06 µg/ml), Staphylococcus (MIC 0.06–0.5 µg/ml), Legionella ( MIC 0.5 µg/ml).

Azithromycin ranks first among macrolides in terms of activity against H. influenzae, M. catarrhalis, N. gonorrhoeae, R. rickettsii, B. melitensis, including their beta-lactomase-producing strains. In terms of its effect on H. influenzae, it is inferior to aminopenicillins and cephalosporins, but exceeds erythromycin by 2–8 times. At a concentration of 1 μg / ml, azithromycin inhibits the growth of 100%, erythromycin - 16%, and roxithromycin - 5% of H. influenzae strains. The minimum bactericidal concentration (MBC), leading to the death of 99.9% of Haemophilus influenzae strains, for azithromycin is 4 μg / ml, for erythromycin - 16 μg / ml, for roxithromycin - 64 μg / ml.

Although azithromycin is second only to clarithromycin in vitro against chlamydia, mycoplasmas, ureaplasmas, and legionella, its in vivo activity against these intracellular pathogens exceeds that of other macrolides due to its extremely high ability to penetrate into cells. MBC of azithromycin against C. pneumoniae ranges from 0.06 to 0.125 µg/ml. Azithromycin is superior to clarithromycin in activity against Coxiella burnetii, which causes SARS. In terms of action on mycoplasmas, azithromycin is superior to doxycycline.

Azithromycin and other macrolides are characterized by a post-antibiotic effect, i.e., the preservation of the antimicrobial effect of the drug after its removal from the environment. This is due to irreversible changes in the ribosome of the pathogen, leading to blocking of the translocation. Azithromycin (to a lesser extent erythromycin and clarithromycin) also has a sub-MIC-post-antibiotic effect - an effect on microorganisms after exposure to sub-inhibitory concentrations of the antibiotic. Under the influence of concentrations of these drugs, even below the MIC, microorganisms, including those usually resistant to them (Pseudomonas aeruginosa), become more sensitive to immune defense factors. Azithromycin exhibits a post-antibiotic and sub-MIC-post-antibiotic effect against S. pyogenes, S. pneumoniae, H. influenzae, L. pneumophila, the duration of which is superior to that of clarithromycin.

Azithromycin and other macrolides have immunomodulatory and anti-inflammatory effects. Macrolides increase the activity of T-killers. In particular, an increase in the killing of chlamydia under the action of azithromycin has been established. Macrolides accumulate in neutrophils, monocytes and macrophages, enhance their migration to the inflammation site, increase their phagocytic activity, stimulate the secretion of interleukins IL-1, IL-2, IL-4. Macrolides affect oxidative reactions in phagocytes (increase the production of superoxide by neutrophils) and contribute to their degranulation. Azithromycin also accelerates neutrophil apoptosis after pathogen eradication. After sanitation of the focus of infection, macrolides increase the production of anti-inflammatory cytokine (interleukin IL-10) by monocytes, reduce the production of pro-inflammatory cytokines (interleukins IL-1, IL-2, IL-6, IL-8, TNF-alpha) by monocytes and lymphocytes, reduce the formation of highly active oxygen compounds (NO) and inflammatory mediators - prostaglandins, leukotrienes and thromboxanes, which helps to stop the inflammatory response. The anti-inflammatory effect is manifested even at subtherapeutic concentrations of macrolides and is comparable to the effect of non-steroidal anti-inflammatory drugs. It is associated with a decrease under the action of macrolides of airway hyperreactivity, which always accompanies bronchopulmonary infections.

All macrolides are ineffective against microorganisms naturally resistant to erythromycin. With the formation of acquired resistance to macrolides after the termination of contact with the antibiotic, sensitivity to it is restored over time. The resistance of microorganisms to macrolides is intragroup cross. Cross-resistance with macrolides is also observed in lincosamides. 90–95% of hospital strains of pneumococcus resistant to penicillin are also resistant to macrolides. The resistance of gram-positive cocci to macrolides in Russia is much lower than in other countries. According to the results of the PROTEKT International Multicentre Study (2002), the prevalence of erythromycin-resistant S. pneumoniae in Western European countries averages 31.5% (1–4% in Sweden and the Netherlands, 12.2% in the UK, 36.6% - in Spain, 58.1% - in France). In Hong Kong and Singapore it reaches 80%. The resistance of pneumococcus to penicillin and macrolides in our country is low, but there is a significant resistance to tetracycline and co-trimoxazole (Table 2). The resistance of pneumococcus to doxycycline in Russia exceeds 25%. Methicillin-resistant strains of staphylococcus are resistant to all macrolides. Unlike gram-positive microorganisms, no development of acquired resistance to macrolides was detected in H. influenzae, M. catarrhalis and intracellular pathogens (mycoplasmas, chlamydia, legionella).

Features of the pharmacokinetics of azithromycin

Azithromycin is characterized by a higher acid resistance (300 times greater than that of erythromycin) than other macrolides, which are partially inactivated by gastric hydrochloric acid. All macrolides are highly lipid soluble and well absorbed from the intestine, but partially undergo first-pass biotransformation. The bioavailability of azithromycin is 37%; for other drugs in this group, it ranges from 10 to 68%. The maximum concentration of azithromycin in the blood plasma after oral administration is 0.3-0.62 μg / ml and is reached after 2.5-2.9 hours (after taking 500 mg, the maximum concentration of 0.41-0.5 μg / ml is created after 2.2 h). After a single dose, two peaks of maximum concentration are recorded. The second peak (often exceeding the first) is due to the ability of macrolides to accumulate in bile with subsequent reabsorption from the intestine. After intravenous drip infusion for 1 hour, the concentration of azithromycin in the blood reaches 3.6 μg / ml, decreasing after 24 hours to 0.2 μg / ml.

The degree of binding of azithromycin to plasma proteins is relatively low and varies from 7% (at a concentration of 1–2 μg / ml) to 51% (at a concentration of 0.02–0.1 μg / ml). As you know, the lower the degree of drug binding to protein, the greater its active concentration and the sooner it leaves the vascular bed, penetrating into the tissues. For comparison, among macrolides, roxithromycin binds to the greatest extent with serum proteins (by 92-96%). Due to its good lipid solubility, azithromycin easily penetrates into tissues, accumulating in them, as evidenced by a large volume of distribution - 31.1 l / kg. AUC0-24 azithromycin 4.3 µg´h/ml. Azithromycin is superior to beta-lactams and aminoglycosides in its ability to penetrate blood-tissue barriers (except for the blood-brain barrier). Among macrolides, azithromycin creates the highest tissue concentration (tens and hundreds of times higher than serum, in most tissues from 1 to 9 μg / g), so its level in blood plasma is low. The highest serum concentration is noted when taking roxithromycin, due to its lower penetration into tissues. Azithromycin is found in high concentrations in the lungs, sputum, and alveolar fluid. 48-96 hours after a single dose of 500 mg of azithromycin, its concentration in the bronchial mucosa is 195-240 times, in the lung tissue - more than 100 times, and in bronchial secretion - 80-82 times higher than serum.

Unlike most other antibiotics, macrolides (azithromycin to the greatest extent) penetrate cells well and create long-lasting high intracellular concentrations. In erythromycin, they are 17 times, in clarithromycin - 16–24 times, in azithromycin - 1200 times higher than the concentration in the blood. Macrolides accumulate in various cells, including fibroblasts, epithelial cells, and macrophages. In especially large quantities, they accumulate in the phospholipid layer of the membranes of lysosomes of phagocytic blood cells (neutrophils, monocytes) and tissues (alveolar macrophages) (Table 3). Phagocytes loaded with macrolides, when migrating under the influence of chemotactic factors secreted by bacteria, transport them to the infectious-inflammatory focus, creating in it the concentration of the antibiotic higher than in healthy tissues. It correlates with the severity of inflammatory edema. The diffusion process in macrophages of roxithromycin and clarithromycin takes 15-20 minutes, azithromycin - up to 24 hours, but its maximum concentration in cells remains for about 48 hours. Macrolides are released from macrophages, neutrophils and monocytes during phagocytosis under the influence of bacterial stimuli. Some of them are absorbed again, some of the macrolides that have entered the macrophages irreversibly bind to lysosome proteins. Targeted antibiotic delivery is of particular importance in the case of infection at restricted sites.

Azithromycin has the longest T1 / 2 (after the first dose, 10-14 hours, in the range from 8 to 24 hours after taking - 14-20 hours, from 24 to 72 hours - 35-55 hours, with multiple doses - 48-96 hours , on average 68-71 hours), which allows you to prescribe an antibiotic only once a day. The elimination half-life from tissues is much longer. Therapeutic concentration of azithromycin in tissues persists for 5-7 days after withdrawal (erythromycin - 1-3 days). Macrolides have a predominantly extrarenal route of elimination. They undergo biotransformation (demethylation, hydroxylation) in the liver with the participation of cytochrome P-450 (mainly its CYP3A4 isoenzyme) and are excreted in the bile in high concentrations as active (clarithromycin, midecamycin) or inactive metabolites and unchanged. Azithromycin is partially biotransformed in the liver (10 of its metabolites are known), and 50% of the dose is excreted in the bile unchanged. A small part of the dose (for azithromycin - 6% of the oral and 11-14% of the intravenous dose) is excreted in the urine.

Renal failure and liver cirrhosis do not affect the pharmacokinetics of azithromycin. For other macrolides, dosage adjustment may be required. In elderly patients, the pharmacokinetics of macrolides does not change significantly and correction of the dosing regimen is not required for them.

Azithromycin, like macrolides in general, is one of the least toxic antibiotics. The overall incidence of side effects of azithromycin is about 9% (when using erythromycin - 30-40%, clarithromycin - 16%). The frequency of side effects of azithromycin, requiring discontinuation of the drug, averages 0.8%.

Data from a meta-analysis of studies conducted in Western Europe, North and South America, Africa and Asia showed that azithromycin was associated with a significantly lower incidence of adverse effects than comparators in the treatment of both adults and children (7.6% and 8 .7% for azithromycin, 9.8% and 13.8% for other antibiotics). Early termination of treatment was required in 0.1-1.3% of patients receiving azithromycin, and in 1-2.6% of patients receiving comparators.

The safety of azithromycin was also studied in 46 studies conducted in Central and Eastern Europe. They included 2650 adults and 1006 children treated with azithromycin and 831 adults and 375 children treated with erythromycin, roxithromycin, clarithromycin, midecamycin, josamycin, phenoxymethylpenicillin, amoxicillin, co-amoxiclav, cefaclor, doxycycline, or ciprofloxacin. Adverse effects were noted in 5.3% of adults and 7.2% of children treated with azithromycin, and in 14.9% of adults and 19.2% of children treated with comparators. Early discontinuation of treatment was required in 0.09% of adults and 0.4% of children treated with azithromycin, and in 2.3% of adults and 2.1% of children treated with other antibiotics.

The other 15 studies included 1616 patients treated with azithromycin and 1613 patients treated with roxithromycin, clarithromycin, amoxicillin, co-amoxiclav, or cefaclor. Undesirable effects were noted in 10.5% of patients treated with azithromycin, and in 11.5% of patients treated with comparators. Early discontinuation of treatment was required in 0.4% of patients treated with azithromycin and in 2.1% of patients treated with comparators.

In a double-blind clinical study of azithromycin tolerance in 2598 children, side effects were observed in 8.4% of patients. They were significantly more common in children treated with reference drugs (12.9%) - co-amoxiclav, ampicillin, phenoxymethylpenicillin, cephalexin, cefaclor, doxycycline, dicloxacillin, flucloxacillin, josamycin and erythromycin.

On the part of the gastrointestinal tract, adverse events with the use of azithromycin occur in 6-9% of cases, clarithromycin - in 12%, erythromycin - in 20-32%. In the treatment of azithromycin, mild or moderate abdominal pain, nausea, vomiting or diarrhea were observed in 5% of children (when taking erythromycin and other 14-mer macrolides that are stimulants of motilin receptors, diarrhea is much more common).

Hepatotoxicity is uncharacteristic of azithromycin, but is possible in rare cases with long-term use of josamycin, spiramycin, clarithromycin and high doses of erythromycin.

Undesirable effects from the central nervous and cardiovascular systems are not severe and occur in less than 1% of cases.

Unlike therapy with beta-lactam antibiotics, dysbacteriosis and associated complications in the treatment of azithromycin are uncharacteristic, since it, like other macrolides, does not affect the normal intestinal microflora.

Allergic reactions to azithromycin and other macrolides are very rare (less than 1% of cases) and are usually limited to skin manifestations. At the same time, they develop on penicillins in 10%, and on cephalosporins - in 4% of patients. There is no cross-allergy with penicillins and cephalosporins, but there is a cross-allergy with other macrolides.

Azithromycin is contraindicated only in case of hypersensitivity to macrolides, liver failure, in the first trimester of pregnancy (unless the expected benefit to the mother outweighs the potential risk to the fetus) and during lactation.

The interaction at the level of biotransformation in the liver is most clinically significant for erythromycin, oleandomycin, clarithromycin and josamycin, to a lesser extent for roxithromycin and midecamycin and is uncharacteristic for azithromycin, dirithromycin and spiramycin. When using macrolides in patients simultaneously taking drugs that are metabolized with the participation of cytochrome P-450, their elimination may be slowed down. This leads to an increase in the serum concentration of these drugs and an increased risk of side effects. At the same time, in particular, the anticoagulant effect of indirect anticoagulants (warfarin, acenocoumarol, phenindione, ethyl biscumacetate), the nephrotoxic effect of immunosuppressants (cyclosporine and tacrolimus), the duration of action of glucocorticoids increases, the risk of developing rhabdomyolysis under the action of statins increases, the frequency of side effects of disopyramide, antagonists calcium (nifedipine and verapamil), bromocriptine, antiviral drugs used in HIV infection, hypnotics and anticonvulsants (carbamazepine, valproic acid, phenytoin), tranquilizers (midazolam, triazolam, zopiclone), increased plasma levels of cisapride, pimozide, antihistamines ( terfenadine, astemizole, ebastine). This can lead to prolongation of the QT interval on the ECG and cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation, ventricular flutter or fibrillation. Macrolides (except azithromycin and midecamycin) cause an increase in theophylline concentration in blood serum (by 10-50%) and theophylline intoxication.

Due to the fact that azithromycin is not an inhibitor of cytochrome P-450, it does not interact with theophylline, hypnotics and anticonvulsants, tranquilizers, indirect anticoagulants, antihistamines. This has been reliably confirmed in specially conducted controlled studies.

Over the course of 10 years, the effectiveness of azithromycin in lower respiratory tract infections (see Table 4 and Table on page 26 "Efficacy of azithromycin in lower respiratory tract infections in adults") was studied in 29 large randomized controlled trials in 5901 patients, including 762 children. 12 studies included patients with various infections, 9 - patients with exacerbation of chronic bronchitis, 9 - patients with pneumonia. Twenty-two studies examined the efficacy of a 3-day course of azithromycin therapy, 5-5 days, 2-step therapy (intravenously, then orally) and 1 single dose. Macrolides (erythromycin, clarithromycin, roxithromycin, dirithromycin) were used as reference drugs in 8 studies, penicillins (co-amoxiclav, amoxicillin, benzylpenicillin) were used in 13 studies, oral cephalosporins (cefaclor, cefuroxime axetil, ceftibuten) were used in 4 studies, and fluoroquinolones (moxifloxacin). Most often (in 9 studies), azithromycin was compared with co-amoxiclav. The duration of use of comparators was usually 10 days. The effectiveness of both 3-day and 5-day courses of azithromycin therapy was high and in most studies was comparable to that of 10-day courses of treatment with comparator drugs. In 5 studies, azithromycin outperformed comparators (co-amoxiclav, erythromycin, benzylpenicillin, and ceftibuten). The tolerability of therapy in the main and control groups was generally comparable, although in 4 studies azithromycin caused adverse effects less frequently than co-amoxiclav or cefuroxime axetil. The difference was mainly due to the lower incidence of gastrointestinal disorders with azithromycin treatment.

In one of the last large international double-blind randomized trials, azithromycin (500 mg once daily for 3 days) was compared with clarithromycin (500 mg twice daily for 10 days) in exacerbation of chronic obstructive pulmonary disease (COPD). The clinical efficacy of azithromycin and clarithromycin in the following pathogens, respectively, was: with H. influenzae - 85.7% and 87.5%, M. catarrhalis - 91.7% and 80%, S. pneumoniae - 90.6% and 77.8 %.

The effectiveness of azithromycin in lower respiratory tract infections in children, such as acute purulent bronchitis and community-acquired pneumonia, is as high as in adults. The results of comparative controlled studies indicate that in terms of clinical efficacy, which exceeds 90%, azithromycin in such infections is not inferior to erythromycin, josamycin, co-amoxiclav and cefaclor.

In particular, a multicenter double-blind study revealed the high efficacy of azithromycin in mycoplasmal pneumonia in children. With community-acquired pneumonia in children (39 people received azithromycin 10 mg/kg once a day and 34 - co-amoxiclav 40 mg/kg in 3 doses), the clinical efficacy was 100% and 94%, respectively. In a comparative study of azithromycin (10 mg / kg 1 time per day) and co-amoxiclav (40 mg / kg in 3 doses) in 97 and 96 children with lower respiratory tract infections, the clinical efficacy was 97% and 96%, respectively. At the same time, in children treated with azithromycin, recovery occurred significantly faster, and the frequency of side effects of therapy was less. In general, the effectiveness of a short course of azithromycin and traditional courses of treatment of community-acquired pneumonia in children has been shown to be equal.

Evidence of the high efficiency of short courses of azithromycin (3-day course when administered orally 1 time per day 500 mg for adults and 10 mg / kg for children) in the treatment of acute infections of the upper and lower respiratory tract of various localization are the results of a prospective non-comparative study of the drug in 235 medical centers in 1574 adults and 781 children. Cure or rapid improvement was observed in more than 96% of cases, eradication of pathogens - in 85.4%.

As a result, comparative studies of macrolides demonstrated similar clinical and bacteriological efficacy of azithromycin, clarithromycin, dirithromycin, midecamycin, midecamycin acetate, roxithromycin, josamycin, erythromycin in adults and children with infections of the lower respiratory tract, including acute bronchitis, exacerbation of chronic bronchitis, community-acquired pneumonia, in including mycoplasma. However, dyspeptic symptoms caused by erythromycin often required drug replacement.

Adherence to treatment (compliance)

One of the conditions for the effectiveness of antibiotic therapy is the fulfillment by patients of doctor's prescriptions. It is estimated that 40% of patients do not comply with the prescribed antibiotic regimen. This is especially true for outpatient practice. Typical violations include skipping a dose, changing the dose or time of taking, premature withdrawal of the drug when you feel better. Of the patients who took less than 80% of the prescribed course of therapy, only 59% achieved the desired effect of the antibiotic. For the rest, the recovery period may be prolonged, complications, relapses, microbial resistance, chronicity of the infectious and inflammatory process may develop, another antibiotic may be required, and, ultimately, the patient's confidence in the doctor's recommendations is undermined. Compliance with the prescribed schedule for taking an antibiotic directly depends on its convenience for the patient. It is known that the lower the frequency of administration and the shorter the course of treatment, the more patients comply with medical prescriptions. Thus, among macrolides, azithromycin has the best compliance, since it is used only once a day, on average for 3 days.

In the standard of care for patients with pneumonia (Order of the Ministry of Health and Social Development of the Russian Federation of November 23, 2004 No. 263), azithromycin is defined as a means of drug treatment of pneumonia along with clarithromycin, amoxicillin with clavulanic acid, cefotaxime, moxifloxacin. In the standard of care for patients with COPD (Order of the Ministry of Health and Social Development of the Russian Federation dated November 23, 2004 No. 271), azithromycin is listed among the antibiotics for the treatment of exacerbations along with clarithromycin, amoxicillin with clavulanic acid, moxifloxacin.

Thus, azithromycin has a high activity against almost all probable non-specific bacterial pathogens of community-acquired infections of the lower respiratory tract. Unlike beta-lactam antibiotics, it is effective against intracellular pathogens, and compared to other macrolides, it has a pronounced activity against Haemophilus influenzae. Acquired microbial resistance to azithromycin in Russia remains at a low level. Azithromycin differs significantly from other antibiotics in its pharmacokinetics, primarily accumulation in high concentrations in tissues, especially in cells, and a long half-life from the body. This allows you to use azithromycin 1 time per day in a short course. Side effects of azithromycin are mild and rare. It interacts little with other drugs and has minimal contraindications. All this ensures good tolerability and adherence of patients to treatment. The clinical efficacy and safety of azithromycin (Sumamed) in lower respiratory tract infections has been proven in numerous high-quality clinical studies. Azithromycin is included in the approved standards of care.

Azithromycin is indicated for monotherapy of acute bronchitis and bronchiolitis of bacterial etiology. With exacerbation of chronic bronchitis, azithromycin, due to its activity against Haemophilus influenzae, is an alternative drug. In mild community-acquired pneumonia, azithromycin is a first-line drug for monotherapy. In the presence of clinical or epidemiological data on mycoplasmal, chlamydial or legionella (atypical) pneumonia, it is the drug of choice. In severe pneumonia, azithromycin may supplement parenteral administration of beta-lactam antibiotics.

S. V. Lukyanov, Doctor of Medical Sciences, Professor of Federal State Institution "Consulting and Methodological Licensing Center" of Roszdravnadzor, Moscow

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Macrolides, lincosamides and streptogramins (MLS antibiotics) are chemically unrelated antibiotics with a similar mechanism of action and antimicrobial activity with a similar resistance profile. They bind reversibly to the 50S ribosomal subunit, blocking translocation. MLS antibiotics are considered to be bacteriostatic antibiotics, they are bactericidal against specific isolates. The main mechanism of acquired resistance is a specific mutation of the 50S ribosomal RNA subunit. Resistance to one member of the MLS class is not necessarily accompanied by resistance to others.

Macrolides have a macrocyclic lactone ring. The prototype of the macrolide is erythromycin, represented by various salts. In recent years, new macrolides have been introduced into clinical practice in the United States, including clarithromycin, azithromycin, and dirithromycin. Other macrolides are available in Europe and Asia. They are usually taken orally, although intravenous formulations of erythromycin and azithromycin exist, and erythromycin lotion is used to treat aspe vulgaris. Macrolides are metabolized in the liver and do not penetrate into the CSF in quantities sufficient to create therapeutic concentrations.

Erythromycin active against streptococci, staphylococci, Bordetella pertussis, Corynebacterium diphtheriae, Campylobacter jejuni, Mycoplasma pneumoniae, Ureaplasma urealyticum, Legionella and Chlamydia. Erythromycin and dirithromycin have limited activity against H. influenzae, but clarithromycin and azithromycin are significantly more effective against this microorganism. Macrolides do not work against Enterobacteriaceae, P. aeruginosa or Mycoplasma hominis.

Macrolides used primarily to treat respiratory tract infections. In addition, macrolides can be used instead of penicillin for streptococcal pharyngitis, especially in patients allergic to penicillin.

Macrolides are the drugs of choice in the treatment of pneumonia, tk. they are active against pneumococci, C. pneumoniae, M. pneumoniae and Legionella. In cases where the infection can be caused by Haemophilus influenzae, it is preferable to use clarithromycin or azithromycin.

Erythromycin- the drug of choice for the treatment of whooping cough, legionnaires' disease, infection caused by Chlamydia trachomatis (during pregnancy, when tetracyclines are contraindicated), and as effectively as penicillin, eliminates the state of carriage in diphtheria. Erythromycin is used with the same success as tetracycline in the treatment of infections caused by M. pneumoniae, is used in enteritis caused by C. jejuni, and can be used instead of beta-lactams in moderate infections of the skin and soft tissues (S. pyogenes and S. aureus).

Clarithromycin and azithromycin

Clarithromycin and azithromycin more active against some pathogens than erythromycin. Clarithromycin and azithromycin (but not dirithromycin) are more active than erythromycin against H. influenzae and are more suitable as an empiric treatment for respiratory tract infections when H. influenzae is the possible pathogen.

And clarithromycin, and azithromycin are active against the Mycobacterium avium complex, an important pathogen in patients. Clarithromycin is useful in controlling most other, nontuberculous mycobacteria. It is also very active against Helicobacter pylori and is a component of a complex of drugs commonly used for polytherapy of duodenal ulcer caused by H. pylori. Azithromycin acts on Chlamydia trachomatis and is the only drug that can cure urethritis and cervicitis caused by this pathogen with a single application.