Buy Azithromycin Ecomed film-coated tablets 500 mg No. 3 in pharmacies

Compound:

One tablet contains:

active substance

: azithromycin dihydrate in terms of azithromycin 250 mg/500 mg;

Excipients

: lactitol 300.0 mg / 600.0 mg, calcium phosphate dihydrate 59.8 mg / 119.6 mg, corn starch 24.0 mg / 48.0 mg, croscarmellose sodium 20.0 mg / 40.0 mg, magnesium stearate 6.0 mg / 12.0 mg, hypromellose 5.0 mg / 10.0 mg, sodium lauryl sulfate 1.2 mg / 2.4 mg, microcrystalline cellulose to obtain an uncoated tablet weighing 700 mg / 1400 mg;

Excipients of the shell:

hypromellose 9.49 mg/

18.98 mg, titanium dioxide 5.2 mg/10.4 mg, macrogol-4000 3.744 mg/7.488 mg, talc 1.12 mg/2.24 mg, povidone-K17 0.416 mg/0.832 mg, dye tropeolin O 0.030 mg / 0.060 mg to obtain a coated tablet weighing 720 mg / 1440 mg

Azithromycin ecomed tablet p/o film 500mg 3 pcs

Antacids: Antacids do not affect the bioavailability of azithromycin, but reduce its maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating. Cetirizine: Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not result in a pharmacokinetic interaction or a significant change in the QT interval.

Didanosine (dideoxyinosine): Concomitant use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal a change in the pharmacokinetic indications of didanosine compared with the placebo group.

Digoxin (P-glycoprotein substrates): Concomitant use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine: Concomitant use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear. Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.

Ergot alkaloids: Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended. Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.

Atorvastatin: Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on HMG-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.

Carbamazepine: Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.

Cimetidine: Pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin.

Indirect anticoagulants (coumarin derivatives): In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).

Cyclosporine: In a pharmacokinetic study involving healthy volunteers who took oral azithromycin (500 mg/day once) for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0 was detected. 5 cyclosporine. Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

Efavirenz: Concomitant use of azithromycin (600 mg/day as a single dose) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole: Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance.

Indinavir: Concomitant use of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).

Methylprednisolone: ​​Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir: Concomitant use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in azithromycin Css in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin: Concomitant use of azithromycin and rifabutin does not affect the serum concentrations of either drug. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil: When used in healthy volunteers, there is no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.

Terfenadine: There was no evidence of interaction between azithromycin and terfenadine in pharmacokinetic studies. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.

Theophylline: No interaction has been identified between azithromycin and theophylline.

Triazolam/midazolam: Significant changes in pharmacokinetic parameters were not detected with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses.

Trimethoprim/sulfamethoxazole: Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on the Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.

Description:

Capsule-shaped biconvex tablets, yellow film-coated. On a cross section, two layers are visible, the inner layer is white or almost white.

Pharmacological group:

antibiotic – azalide

ATX code:

J01FA10.

pharmachologic effect

Pharmacological properties

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the macrolide-azalide group. Has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis in microbial cells. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.

It is active against a number of gram-positive, gram-negative, anaerobes, intracellular and other microorganisms.

Microorganisms may initially be resistant to the action of an antibiotic or become resistant to it.

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

In most cases, sensitive microorganisms:

1. Gram-positive aerobes:

• Staphylococcus aureus (methicillin-sensitive)
• Streptococcus pneumoniae (penicillin-sensitive)
• Streptococcus pyogenes

1. Gram-negative aerobes:

• Haemophilus influenzae
• Haemophilus parainfluenzae
• Legionella pneumophila
• Moraxella catarrhalis
• Pasteurella multocida
• Neisseria gonorrhoeae

1. Anaerobes:

• Clostridium perfringens
• Fusobacterium spp.
• Prevotella spp.
• Porphyromonas spp.

1. Other microorganisms:

• Chlamydia trachomatis
• Chlamydia pneumoniae
• Chlamydia psittaci
• Mycoplasma pneumoniae
• Mycoplasma hominis
• Borrelia burgdorferi

Microorganisms that can develop resistance to azithromycin:

gram-positive aerobes:

Streptococcus pneumoniae (penicillin resistant)

Initially resistant microorganisms:

gram-positive aerobes:

Enterococcus faecalis

Staphylococcus (methicillin-resistant staphylococci show a very high degree of resistance to macrolides) gram-positive bacteria resistant to erythromycin

anaerobes

Bacteroides fragilis

Pharmacokinetics

After oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose of 500 mg is 37% (the “first pass” effect), the maximum concentration (0.4 mg/l) in the blood is created after 2-3 hours, the apparent volume of distribution is 31.1 l/kg, protein binding plasma inversely proportional to the concentration in the blood is 7-50%. Penetrates through cell membranes (effective against infections caused by intracellular pathogens).

Transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes histohematic barriers and enters tissues. The concentration in tissues is 10-50 times higher than in plasma, and at the site of infection it is 24-34% higher than in healthy tissues.

Azithromycin has a very long half-life - 35-50 hours. The half-life from tissues is much longer. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainly unchanged - 50% by the intestines, 6% by the kidneys. In the liver it is demethylated, losing activity.

Azithromycin Ecomed – Tablets

Home / Ecoanalogues / Azithromycin Ecomed / Tablets

A broad-spectrum antibacterial drug from the group of macrolides-azalides, it acts bacteriostatically. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and in high concentrations has a bactericidal effect. Acts on extra- and intracellularly located pathogens. Azithromycin Ecomed can be considered as the drug of choice for patients with an allergy to β-lactam antibiotics in respiratory pathology, especially in people with an increased risk of developing dysbiosis.

Registration number: Trade name of the drug: Azithromycin Ecomed® International non-proprietary or generic name: azithromycin Dosage form: film-coated tablets. Description: Yellow film-coated tablets, capsule-shaped, biconvex. The cross section shows two layers. The inner layer is white or almost white. Pharmacotherapeutic group: antibiotic – azalide. ATX code: J01FA10

Expand all

Composition Expand

One tablet contains: Active substance: azithromycin dihydrate in terms of azithromycin 250 mg or 500 mg; Excipients: lactitol 300 mg (or 600 mg), calcium phosphate dihydrate 59.8 mg (or 119.6 mg), corn starch 24.0 mg (or 48.0 mg), hypromellose 5.0 mg (or 10.0 mg), sodium lauryl sulfate 1, 2 mg (or 2.4 mg), croscarmellose sodium 20.0 mg (or 40.0 mg), magnesium stearate 6.0 mg (or 12.0 mg), microcrystalline cellulose to obtain an uncoated tablet weighing 700 mg (or 1400 mg); Excipients of the shell: hypromellose 9.49 mg (or 18.98 mg), titanium dioxide 5.2 mg (or 10.4 mg), macrogol-4000 4.16 mg (or 8.32 mg), talc 1.12 mg (or 2.24 mg) , dye tropeolin-O 0.03 mg (or 0.06 mg), to obtain a coated tablet weighing 720 mg (or 1440 mg).

Pharmacological action Expand

A broad-spectrum antibacterial drug from the group of macrolides-azalides, has a bacteriostatic effect. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and in high concentrations has a bactericidal effect. Acts on extra- and intracellularly located pathogens. Microorganisms may be initially resistant to the action of an antibiotic or may acquire resistance to it. Scale of sensitivity of microorganisms to azithromycin (Minimum inhibitory concentration, mg/l): Staphylococcus: sensitive ≥1 mg/l, resistant >2 mg/l; Streptococcus A, B, C, G: sensitive ≤0.25 mg/l, resistant >0.5 mg/l; Streptococcus pneumoniae: sensitive ≥0.25 mg/l, resistant >0.5 mg/l; Haemophilus influenzae: sensitive ?0.12 mg/l, resistant >4 mg/l; Moraxella catarrhalis: sensitive ≤0.5 mg/l, resistant >0.5 mg/l; Neisseria gonorrhoeae: sensitive ≤0.25 mg/l, resistant >0.5 mg/l; Sensitive:

• aerobic gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes;

• aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;

• anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.;

• other: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Moderately sensitive or insensitive:

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

Resistant:

• aerobic gram-positive microorganisms: Enterococcus faecalis, Staphylococci spp. (methicillin-resistant).

• anaerobes: Bacteroides fragilis group. Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. group A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-sensitive strains), resistant to erythromycin and other macrolides, lincosamides, and resistant to azithromycin.

Pharmacokinetics Expand

After oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose of 0.5 g is 37% (the “first pass” effect through the liver), maximum concentration (Cmax) after oral administration of 0.5 g is 0.4 mg/l, time to reach maximum concentration (TCmax) is 2-3 hours. The concentration in tissues and cells is 10-50 times higher than in blood serum. The volume of distribution is 31.1 l/kg, binding to plasma proteins is inversely proportional to the concentration in the blood and remains 7-50%. Azithromycin is acid-stable, lipophilic. Easily passes through histohematic barriers, penetrates well into the respiratory tract, genitourinary organs and tissues, incl. into the prostate gland, skin and soft tissues. It is also transported to the site of infection by phagocytes, polymorphonuclear leukocytes and macrophages, where it is released in the presence of bacteria. Penetrates through cell membranes and creates high concentrations in them, which is especially important for the eradication of intracellular pathogens. In foci of infection, the concentration is 24-34% higher than in healthy tissues and correlates with the severity of the inflammatory process. Remains in effective concentrations for 5-7 days after taking the last dose. It is demethylated in the liver, the resulting metabolites are not active. The metabolism of the drug involves isoenzymes CYP3A4, CYP3A5, CYP3A7, of which it is an inhibitor. Plasma clearance - 630 ml/min: half-life between 8 and 24 hours after administration - 14-20 hours, half-life in the range from 24 to 72 hours - 41 hours. More than 50% of the drug is excreted unchanged by the intestines, 6% by the kidneys . Food intake significantly changes pharmacokinetics: Cmax increases (by 31%), the area under the concentration-time curve (AUC) does not change. In elderly men (65-85 years old), the pharmacokinetic parameters do not change; in women, Cmax increases (by 30-50%).

Indications for use Expand

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

• infections of the upper respiratory tract and ENT organs: pharyngitis, tonsillitis, sinusitis, otitis media;

• lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl. caused by atypical pathogens;

• infections of the skin and soft tissues: acne vulgaris of moderate severity, erysipelas, impetigo, secondary infected dermatoses;

• the initial stage of Lyme disease (borreliosis) – erythema migrans;

• urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis).

Contraindications Expand

Contraindications:

• hypersensitivity to macrolide antibiotics;

• severe liver and/or kidney failure;

• children under 12 years of age with body weight less than 45 kg (for this dosage form);

• breast-feeding;

• simultaneous use with ergotamine and dihydroergotamine;

Carefully:

• moderate dysfunction of the liver and kidneys;

• with arrhythmias or predisposition to arrhythmias and prolongation of the QT interval;

• with the combined use of terfenadine, warfarin, digoxin;

Use during pregnancy and lactation Expand

Azithromycin is recommended to be prescribed during pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. During treatment with azithromycin, breastfeeding is suspended.

Dosing regimen Expand

Azithromycin Ecomed® is taken orally, without chewing, 1 time per day, regardless of meals. Adults (including elderly people) and children over 12 years of age weighing over 45 kg. For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 0.5 g per day for 3 days (course dose – 1.5 g). For moderate acne: 0.5 g per day for 3 days, then 0.5 g once a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (8th day from the start of treatment), the subsequent 8 weekly tablets should be taken at intervals of 7 days. Course dose 6.0 g. For migratory erythema: 1 time per day for 5 days, 1st day 1.0 g, then from 2nd to 5th day 0.5 g. Course dose 3.0 g. For urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): 1.0 g once. Prescription for patients with impaired renal function. For patients with moderate renal impairment (creatinine clearance > 40 ml/min), no dose adjustment is necessary.

Side effect Expand

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, loose stools, flatulence, indigestion, anorexia, constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver function, liver failure, liver necrosis (possibly fatal). Allergic reactions: itching, skin rashes, angioedema, urticaria, photosensitivity, anaphylactic reaction (in rare cases fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. From the cardiovascular system: palpitations, arrhythmia, ventricular tachycardia, increased QT interval, bidirectional ventricular tachycardia. From the nervous system: dizziness/vertigo, headache, convulsions, drowsiness, paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness. From the senses: tinnitus, reversible hearing impairment up to deafness (when taking high doses for a long time), impaired perception of taste and smell. From the circulatory and lymphatic systems: thrombocytopenia, neutropenia, eosinophilia. From the musculoskeletal system: arthralgia. From the genitourinary system: interstitial nephritis, acute renal failure. Other: vaginitis, candidiasis.

Overdose Expand

Symptoms: temporary hearing loss, nausea, vomiting, diarrhea. Treatment is symptomatic.

Interaction with other drugs Expand

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating. When used parenterally, azithromycin does not affect the plasma concentrations of cimetidine, efavirenz, fluconazole, indinavir, midazolam, triazolam, co-trimoxazole when used together, however, the possibility of such interactions should not be excluded when azithromycin is administered orally. If combined use with cyclosporine is necessary, it is recommended to monitor the level of cyclosporine in the blood. When taking digoxin and azithromycin together, it is necessary to monitor the concentration of digoxin in the blood, because many macrolides increase the absorption of digoxin in the intestine, thereby increasing its concentration in the blood plasma. If co-administration with warfarin is necessary, careful monitoring of prothrombin time is recommended. Concomitant use of terfenadine and macrolide antibiotics causes arrhythmia and prolongation of the QT interval. Based on this, the above complications cannot be excluded when taking terfenadine and azithromycin together. Since there is a possibility of inhibition of the CYP3A4 isoenzyme by azithromycin in parenteral form when used together with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs whose metabolism occurs with the participation of this isoenzyme, the possibility of such interaction should be taken into account when prescribing azithromycin for administration inside. When azithromycin and zidovudine are taken together, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or the renal excretion of it and its glucuronidated metabolite. However, the concentration of the active metabolite, phosphorylated zidovudine, increases in mononuclear cells of peripheral vessels. The clinical significance of this fact is not clear. When macrolides are taken simultaneously with ergotamine and dihydroergotamine, their toxic effects may occur.

Special instructions Expand

If you miss taking an antibiotic, the missed dose should be taken as soon as possible, with subsequent doses taken at intervals of 24 hours. After discontinuation of azithromycin therapy, hypersensitivity reactions in some patients may persist for a long time and may require specific therapy under medical supervision. Given the likelihood of developing side effects from the central nervous system, caution should be exercised when driving vehicles and operating machinery.

Release form Expand

Film-coated tablets 250 mg, 500 mg. 6 tablets with a dosage of 250 mg, 3 tablets with a dosage of 500 mg are placed in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 6 tablets with a dosage of 250 mg, 3 tablets with a dosage of 500 mg in plastic bottles or polymer bottles. Each bottle, 1 blister pack together with instructions for use are placed in a cardboard pack.

Expiration date Expand

2 years. Do not use after expiration date.

Storage conditions Expand

In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Vacation conditions Expand

On prescription.

Manufacturer/organization receiving claims Expand

JSC "AVVA RUS", Russia, 610044 Kirov, st. Luganskaya, 53A. Tel., www.avva-rus.ru, www.ecoantibiotic.ru Send consumer complaints to the manufacturer.

Share information:

Indications for use

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

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

Carefully

• myasthenia gravis;
• mild to moderate liver dysfunction;
• mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min);
• in patients with the presence of proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances in water and electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure;
• simultaneous use of terfenadine, warfarin, digoxin, cyclosporine.

Buy Azithromycin Ecomed powder for oral suspension 200mg/5ml 16.5g in pharmacies

Dosage form:

powder for the preparation of suspension for oral administration

Composition of components in 5 ml suspension:

Description

White or yellowish-white powder with a faint fruity odor. Ready suspension: white to light yellow, homogeneous with a faint fruity odor.

Pharmacological group antibiotic – azalide.

Pharmacological properties

Pharmacodynamics

A broad-spectrum antibacterial drug from the group of macrolides-azalides, has a bacteriostatic effect. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage, suppresses protein synthesis, slows down the growth and reproduction of bacteria, and in high concentrations has a bactericidal effect. Acts on extra- and intracellularly located pathogens.

Microorganisms may be initially resistant to the action of an antibiotic or may acquire resistance to it.

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

Sensitive:

aerobic gram-positive microorganisms:

Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes;

aerobic gram-negative microorganisms:

Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;

anaerobic microorganisms:

Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.;

others:

Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

Moderately sensitive or insensitive:

aerobic gram-positive microorganisms:

Streptococcus pneumoniae (moderately sensitive or resistant to penicillin).

Resistant: aerobic gram-positive microorganisms:

Enterococcus faecalis, Methicillin-resistant strains of Staphylococcus aureus.

Anaerobes: Bacteroides fragilis group.

Streptococcus pneumoniae, beta-hemolytic Streptococcus spp. group A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-sensitive strains), resistant to erythromycin and other macrolides, lincosamides, and resistant to azithromycin.

Pharmacokinetics

After oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose of 0.5 g is 37% (the “first pass” effect through the liver), maximum concentration (Cmax) after oral administration of 0.5 g is 0.4 mg/l, time to reach maximum concentration (TCmax) is 2 -3 hours. Concentration in tissues and cells is 10-50 times higher than in serum. The volume of distribution is 31.1 l/kg, binding to plasma proteins is inversely proportional to the concentration in the blood and amounts to 7-50%. Azithromycin is acid-stable and lipophilic. Easily passes through histohematic barriers, penetrates well into the respiratory tract, internal organs and tissues, including the prostate gland, skin and soft tissues. It is also transported to the site of infection by phagocytes, polymorphonuclear leukocytes and macrophages, where it is released in the presence of bacteria. Penetrates through cell membranes and creates high concentrations in them, which is especially important for the eradication of intracellular pathogens.

In foci of infection, the concentration is 24-34% higher than in healthy tissues and correlates with the severity of the inflammatory process. Remains in effective concentrations for 5-7 days after taking the last dose.

It is demethylated in the liver, the resulting metabolites are not active. The metabolism of the drug involves isoenzymes CYP3A4, CYP3A5, CYP3A7, of which it is an inhibitor. Plasma clearance - 630 ml/min: half-life between 8 and 24 hours after administration - 14-20 hours, half-life in the range from 24 to 72 hours - 41 hours. More than 50% of the drug is excreted through the intestines unchanged, 6% - kidneys.

Food intake significantly changes pharmacokinetics: Cmax increases (by 31%), the area under the concentration-time curve (AUC) does not change.

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

Indications for use

Infectious and inflammatory diseases caused by microorganisms sensitive to azithromycin:

infections of the upper respiratory tract and ENT organs: pharyngitis, tonsillitis, sinusitis, otitis media; lower respiratory tract infections: acute bronchitis, exacerbation of chronic bronchitis, pneumonia, incl. caused by atypical pathogens; infections of the skin and soft tissues: erysipelas, impetigo, secondary infected dermatoses; the initial stage of Lyme disease (borreliosis) – erythema migrans;

Contraindications

hypersensitivity to azithromycin (including other macrolides) or other components of the drug; severe renal failure (creatinine clearance (CC) less than 40 ml/min); severe liver failure (class C on the Child-Pugh scale); breast-feeding; simultaneous use with ergotamine and dihydroergotamine; children up to 6 months; sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption; hypersensitivity to erythromycin; ketolides.

Carefully

Pregnancy, myasthenia gravis, mild to moderate liver dysfunction, mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min), diabetes mellitus, in patients with the presence of proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin) , with disturbances in water and electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of digoxin, warfarin, cyclosporine.

Use during pregnancy and breastfeeding

Pregnancy

During pregnancy, azithromycin is used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding period

During breastfeeding, it is used only if the expected benefit to the mother outweighs the potential risk to the child. If it is necessary to use azithromycin during breastfeeding, it is recommended to stop breastfeeding.

Directions for use and doses

Orally (the method of administration is determined by the release form), 1 time per day, 1 hour before or 2 hours after meals.

After taking the drug, the child must be offered to drink a few sips of water so that he can swallow the remainder of the suspension.

Before each dose of the drug, it must be shaken thoroughly until a homogeneous suspension is obtained. If the required volume of suspension has not been taken within 20 minutes after shaking, the suspension should be shaken again, the required volume taken and given to the child.

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues

At the rate of 10 mg/kg body weight 1 time per day for 3 days (course dose 30 mg/kg).

To accurately dose azithromycin according to your child's body weight, use the table below.

Children weighing up to 10 kg should take azithromycin in powder form to prepare an oral suspension with a concentration of 100 mg/5 ml.

To accurately dose azithromycin according to your child's body weight, use the table below.

For pharyngitis/tonsillitis caused by Streptococcus pyogenes, azithromycin is used at a dose of 20 mg/kg/day for 3 days (course dose 60 mg/kg). The maximum daily dose is 500 mg.

For Lyme disease (the initial stage of borreliosis) - erythema migrans

On the 1st day at a dose of 20 mg/kg/day, then from the 2nd to the 5th day at a dose of 10 mg/kg/day (course dose 60 mg/kg).

If kidney function is impaired

In patients with GFR (glomerular filtration rate) 10-80 ml/min, no dose adjustment is required.

In case of liver dysfunction

When used in patients with mild to moderate liver dysfunction, no dose adjustment is required.

Elderly patients

No dose adjustment is required. In elderly patients, special caution is recommended when using azithromycin due to the possible presence of proarrhythmogenic factors that may increase the risk of developing cardiac arrhythmia and arrhythmias.

Method of preparing the suspension

The suspension is prepared immediately before use.

The powder in the bottle is first shaken, 12 ml of boiled and cooled to room temperature water is added using a dosing syringe, mixed to obtain a homogeneous suspension.

To accurately dose the suspension, you should use a syringe, which should be rinsed well with water after each use. After dilution, the prepared suspension should be stored for no more than 5 days in the refrigerator, but not frozen.

When used in patients with mild to moderate renal impairment, no dose adjustment is required; When used in patients with mild to moderate liver dysfunction, no dose adjustment is required in elderly patients.

Side effects

Infectious and parasitic diseases

uncommon: candidiasis, including oral mucosa, vaginal infection, pneumonia, fungal infection, bacterial infection, pharyngitis, gastroenteritis, respiratory diseases, rhinitis unknown frequency: pseudomembranous colitis

Blood and lymphatic system disorders

uncommon: leukopenia, neutropenia, eosinophilia very rare: thrombocytopenia, hemolytic anemia

Metabolic and nutritional disorders

uncommon: anorexia

Immune system disorders

uncommon: angioedema, hypersensitivity reaction unknown frequency: anaphylactic reaction

Nervous system disorders

often: headache uncommon: dizziness, disturbance of taste, paresthesia, drowsiness, insomnia, nervousness rare: agitation unknown frequency: hypoesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perverted sense of smell, loss of taste, myasthenia gravis, delusions, hallucinations

Visual disorders

common: visual impairment

Hearing and labyrinth disorders

Uncommon: Hearing impairment, vertigo Unknown Frequency: Hearing impairment, including deafness and/or tinnitus

Cardiovascular disorders

uncommon: palpitations very rare: arrhythmia unknown frequency: increased QT interval on the electrocardiogram, arrhythmia, ventricular tachycardia

Vascular disorders

uncommon: flushing of the face unknown frequency: decreased blood pressure

Respiratory, thoracic and mediastinal disorders

uncommon: shortness of breath, nosebleeds

Gastrointestinal disorders

very common: diarrhea common: nausea, vomiting, abdominal pain uncommon: flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands very rare: change tongue colors, pancreatitis

Disorders of the liver and biliary tract

uncommon: hepatitis rare: liver dysfunction, cholestatic jaundice unknown frequency: liver failure (in rare cases, fatal, mainly due to severe liver dysfunction); liver necrosis, fulminant hepatitis

Skin and subcutaneous tissue disorders

uncommon: skin rash, itching, urticaria, dermatitis, dry skin, sweating rare: photosensitivity reaction unknown frequency: Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS syndrome)

Musculoskeletal and connective tissue disorders

uncommon: osteoarthritis, myalgia, back pain, neck pain unknown frequency: arthralgia

Renal and urinary tract disorders

uncommon: dysuria, pain in the kidney area unknown frequency: interstitial nephritis, acute renal failure

Genital and breast disorders

uncommon: metrorrhagia, testicular dysfunction

General and administration site disorders

uncommon: edema, asthenia, malaise, feeling tired, facial swelling, chest pain, fever, peripheral edema

Influence on the results of laboratory and instrumental studies

often: decreased number of lymphocytes, increased number of eosinophils, increased number of basophils, increased number of monocytes, increased number of neutrophils, decreased concentration of bicarbonates in the blood plasma; infrequently: increased activity of aspartate aminotransferase, alanine aminotransferase, increased concentration of bilirubin in the blood plasma, increased concentration of urea in the blood plasma, increase in plasma creatinine concentration, change in plasma potassium content, increase in plasma alkaline phosphatase activity, increase in plasma chloride content, increase in blood glucose concentration, increase in platelet count, decrease in hematocrit, increase in plasma bicarbonate concentration, change sodium content in blood plasma

Overdose

Symptoms: temporary hearing loss, nausea, vomiting, diarrhea.

Treatment is symptomatic.

Interaction with other drugs

Antacids (aluminum and magnesium containing) do not affect bioavailability, but reduce the concentration of azithromycin in the blood by 30%, so the interval between their administration should be 1 hour before or 2 hours after taking these drugs.

When used simultaneously with ergotamine and dihydroergotamine derivatives, the toxic effect of the latter may be enhanced (vasospasm, dysesthesia).

When used together with indirect coumarin anticoagulants (warfarin), patients need careful monitoring of prothrombin time.

Caution must be exercised when co-prescribing terfenadine and azithromycin, since it has been found that the simultaneous use of terfenadine and macrolides causes arrhythmia and prolongation of the QT interval. Based on this, the above complications cannot be excluded when taking terfenadine and azithromycin together.

When used simultaneously with cyclosporine, it is necessary to monitor the concentration of cyclosporine in the blood. When azithromycin and cyclosporine are used simultaneously, a dose adjustment of cyclosporine is necessary. When used simultaneously with digoxin, it is necessary to control the concentration of digoxin in the blood (it is possible to increase the absorption of digoxin in the intestine). The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentration of azithromycin in the blood plasma; no clinically significant side effects were observed and no dose adjustment of azithromycin is required when used simultaneously with nefinavir.

When used concomitantly with zidovudine, azithromycin has little effect on the pharmacokinetics, including renal excretion, of zidovudine or its glucuronide metabolite.

Azithromycin weakly interacts with cytochrome P450 isoenzymes; it has not been revealed that azithromycin is involved in pharmacokinetic interactions similar to erythromycin and other macrolides; azithromycin is not an inducer or inhibitor of the cytochrome P450 isoenzyme.

Neutropenia has occasionally been observed with concomitant use of azithromycin and rifabutin, although neutropenia has been associated with the use of rifabutin; a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Azithromycin does not affect the blood concentrations of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim/sulfamethoxazole, cetirizine, sildenafil, atorvastatin, rifabutin and methylprednisolone when used simultaneously.

There have been isolated case reports of rhabdomyolysis in patients taking azithromycin and statins concomitantly.

special instructions

If you miss one dose of azithromycin, the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.

Azithromycin should be taken at least one hour before or two hours after taking antacids.

Azithromycin should be used with caution in patients with mild to moderate hepatic impairment due to the possibility of developing fulminant hepatitis and severe hepatic failure.

If there are symptoms of liver dysfunction, such as rapidly increasing asthenia, jaundice, dark urine, bleeding tendency, hepatic encephalopathy, azithromycin therapy should be discontinued and a study of the functional state of the liver should be performed.

In case of impaired renal function: in patients with GFR (glomerular filtration rate) 10-80 ml/min, no dose adjustment is required, azithromycin therapy should be carried out with caution under monitoring the state of renal function

As with the use of other antibacterial drugs, during therapy with azithromycin, patients should be regularly examined for the presence of non-susceptible microorganisms and signs of the development of superinfections, including fungal ones.

Azithromycin should not be used in longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.

There is no data on a possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism with the simultaneous use of macrolides with ergotamine and dihydroergotamine derivatives, this combination is contraindicated

With long-term use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis, is possible. If antibiotic-associated diarrhea develops while taking azithromycin, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. Do not use drugs that inhibit intestinal motility.

When treated with macrolides, including azithromycin, prolongation of cardiac repolarization and QT interval was observed, increasing the risk of developing cardiac arrhythmias, including arrhythmias, which can lead to cardiac arrest.

Caution should be exercised when using azithromycin in patients with the presence of proarrhythmogenic factors (especially in elderly patients), including congenital or acquired prolongation of the QT interval, in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with fluid and electrolyte imbalance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure .

The use of azithromycin may provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Impact on the ability to drive vehicles and machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form

Powder for the preparation of suspension for oral administration 100 mg/5 ml, 200 mg/5 ml.

16.5 g in 60 ml dark glass bottles with a screw-on plastic cap with a silica gel insert.

1 bottle along with a syringe for dosing and instructions for use is placed in a cardboard pack.

Best before date

2 years.

Ready suspension – 5 days.

Do not use after expiration date.

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 ° C.

The prepared suspension is stored at a temperature from 2 ºС to 8 ºС in a tightly closed bottle.

Keep out of the reach of children.

Vacation conditions

On prescription.

Directions for use and doses

Azithromycin Ecomed® is taken orally, without chewing, 1 time per day, regardless of meals. The drug is taken at least 1 hour before or 2 hours after meals.

Adults (including elderly people) and children over 12 years of age weighing over 45 kg.

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 0.5 g per day for 3 days (course dose – 1.5 g).

For moderate acne: 0.5 g per day for 3 days, then 0.5 g once a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (8th day from the start of treatment), the subsequent 8 weekly tablets should be taken at intervals of 7 days. Course dose 6.0 g.

For migratory erythema: 1 time per day for 5 days, 1st day 1.0 g, then from 2nd to 5th day 0.5 g. Course dose 3.0 g.

For urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): 1.0 g once.

When used in patients with mild renal impairment, no dose adjustment is required.

When used in patients with mild to moderate liver dysfunction, no dose adjustment is required in elderly patients.

Elderly patients: no dose adjustment is required. Caution should be exercised in elderly patients with persistent proarrhythmogenic factors due to the high risk of developing arrhythmias, including arrhythmias.

AZITHROMYCIN ECOMED por. d/prig. susp. 200 mg/5 ml vial. 16.5 g

Side effects

Infectious and parasitic diseases uncommon: candidiasis, including oral mucosa, vaginal infection, pneumonia, fungal infection, bacterial infection, pharyngitis, gastroenteritis, respiratory diseases, rhinitis unknown frequency: pseudomembranous colitis Blood and lymphatic system disorders uncommon: leukopenia , neutropenia, eosinophilia very rare: thrombocytopenia, hemolytic anemia Metabolic and nutritional disorders uncommon: anorexia Immune system disorders uncommon: angioedema, hypersensitivity reaction unknown frequency: anaphylactic reaction Nervous system disorders common: headache uncommon: dizziness , disturbance of taste, paresthesia, drowsiness, insomnia, nervousness rarely: agitation unknown frequency: hypoesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perverted sense of smell, loss of taste, myasthenia gravis, delirium, hallucinations Organ disorders vision common: visual impairment Hearing and labyrinthine disorders uncommon: hearing impairment, vertigo unknown frequency: hearing impairment, including deafness and/or tinnitus Disorders of the cardiovascular system uncommon: palpitations very rare: arrhythmia unknown frequency: increase in the QT interval on the electrocardiogram, arrhythmia, ventricular tachycardia Vascular disorders infrequently: flushing of the face unknown frequency: decreased blood pressure Disorders of the respiratory system, chest and mediastinal organs infrequently: shortness of breath, nosebleeds parts of the gastrointestinal tract very often: diarrhea often: nausea, vomiting, abdominal pain infrequently: flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased salivary secretion glands very rare: discoloration of the tongue, pancreatitis Disorders of the liver and biliary tract uncommon: hepatitis rare: impaired liver function, cholestatic jaundice unknown frequency: liver failure (in rare cases - fatal, mainly due to severe liver dysfunction) ; liver necrosis, fulminant hepatitis Skin and subcutaneous tissue disorders uncommon: skin rash, itching, urticaria, dermatitis, dry skin, sweating rare: photosensitivity reaction unknown frequency: Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, drug rash with eosinophilia and systemic manifestations (DRESS syndrome) Musculoskeletal and connective tissue disorders uncommon: osteoarthritis, myalgia, back pain, neck pain unknown frequency: arthralgia Renal and urinary tract disorders uncommon: dysuria, pain in the kidney area unknown frequency: interstitial nephritis, acute renal failure Genital and breast disorders uncommon: metrorrhagia, testicular dysfunction General disorders and administration site disorders uncommon: edema, asthenia, malaise, feeling tired, facial swelling, chest pain, fever, peripheral edema Impact on the results of laboratory and instrumental studies often: decrease in the number of lymphocytes, increase in the number of eosinophils, increase in the number of basophils, increase in the number of monocytes, increase in the number of neutrophils, decrease in the concentration of bicarbonates in the blood plasma infrequently: increase in the activity of aspartate aminotransferase, alanine aminotransferase, increase in the concentration of bilirubin in plasma blood, increased urea concentration in blood plasma, increased creatinine concentration in blood plasma, change in potassium content in blood plasma, increased alkaline phosphatase activity in blood plasma, increased chloride content in blood plasma, increased blood glucose concentration, increased platelet count, decreased hematocrit , increase in the concentration of bicarbonates in the blood plasma, changes in the sodium content in the blood plasma

Side effect

The frequency of side effects is classified in accordance with WHO recommendations: very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%; unknown frequency—cannot be estimated from available data.

Infectious diseases:

uncommon - candidiasis, incl. mucous membrane of the oral cavity and genitals, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; unknown frequency - pseudomembranous colitis.

From the blood and lymphatic system:

uncommon - leukopenia, neutropenia, eosinophilia; very rarely - thrombocytopenia, hemolytic anemia.

Metabolism and nutrition:

infrequently - anorexia.

Allergic reactions:

uncommon - angioedema, hypersensitivity reaction; unknown frequency - anaphylactic reaction.

From the nervous system:

often - headache; infrequently - dizziness, disturbance of taste, paresthesia, drowsiness, insomnia, nervousness; rarely - agitation; unknown frequency - hypoesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perversion of smell, loss of taste, myasthenia gravis, delirium, hallucinations.

From the side of the organ of vision:

infrequently - visual impairment.

Hearing and labyrinth disorders:

uncommon - hearing loss, vertigo; unknown frequency - hearing loss, incl. deafness and/or tinnitus.

From the cardiovascular system:

infrequently - palpitations, flushing of the face; unknown frequency - decreased blood pressure, increased QT interval on ECG, ari, ventricular tachycardia.

From the respiratory system:

infrequently - shortness of breath, nosebleeds.

From the gastrointestinal tract:

very often - diarrhea; often - nausea, vomiting, abdominal pain; uncommon - flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - change in tongue color, pancreatitis.

From the liver and biliary tract:

uncommon - hepatitis; rarely - impaired liver function, cholestatic jaundice; unknown frequency - liver failure (in rare cases with death, mainly due to severe liver dysfunction); liver necrosis, fulminant hepatitis.

For the skin and subcutaneous tissues:

uncommon - skin rash, itching, urticaria, dermatitis, dry skin, sweating; rarely - photosensitivity reaction; unknown frequency - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.

From the musculoskeletal system:

uncommon - osteoarthritis, myalgia, back pain, neck pain; unknown frequency - arthralgia.

From the kidneys and urinary tract:

uncommon - dysuria, pain in the kidney area; unknown frequency - interstitial nephritis, acute renal failure.

From the genital organs and breast:

infrequently - metrorrhagia, testicular dysfunction.

Other:

uncommon - asthenia, malaise, feeling of fatigue, facial swelling, chest pain, fever, peripheral edema.

Laboratory data:

often - a decrease in the number of lymphocytes, an increase in the number of eosinophils, an increase in the number of basophils, an increase in the number of monocytes, an increase in the number of neutrophils, a decrease in the concentration of bicarbonates in the blood plasma; infrequently - increased activity of AST, ALT, increased concentration of bilirubin in the blood plasma, increased concentration of urea in the blood plasma, increased concentration of creatinine in the blood plasma, change in the potassium content in the blood plasma, increased activity of alkaline phosphatase in the blood plasma, increased chlorine content in the blood plasma, increased blood glucose concentration, increased platelet count, increased hematocrit, increased plasma bicarbonate concentration, change in plasma sodium content.

Buy Azithromycin Ecomed film-coated tablets 500 mg No. 3 in pharmacies

Dosage form:

film-coated tablets

Compound:

Composition per tablet:

Description:

Capsule-shaped biconvex tablets, yellow film-coated. On a cross section, two layers are visible, the inner layer is white or almost white.

Pharmacological group:

antibiotic – azalide

Pharmacological properties

Pharmacodynamics

Azithromycin is a broad-spectrum bacteriostatic antibiotic from the macrolide-azalide group. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis in microbial cells. By binding to the 50S ribosomal subunit, it inhibits peptide translocase at the translation stage and suppresses protein synthesis, slowing down the growth and reproduction of bacteria. In high concentrations it has a bactericidal effect.

It is active against a number of gram-positive, gram-negative, anaerobes, intracellular and other microorganisms.

Microorganisms may initially be resistant to the action of an antibiotic or become resistant to it.

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

In most cases, sensitive microorganisms:

1. Gram-positive aerobes:

Staphylococcus aureus (methicillin-sensitive) Streptococcus pneumoniae (penicillin-sensitive) Streptococcus pyogenes

2. Gram-negative aerobes:

Haemophilus influenzae Haemophilus parainfluenzae Legionella pneumophila Moraxella catarrhalis Pasteurella multocida Neisseria gonorrhoeae

3. Anaerobes:

Clostridium perfringens Fusobacterium spp. Prevotella spp. Porphyromonas spp.

4. Other microorganisms:

Chlamydia trachomatis Chlamydia pneumoniae Chlamydia psittaci Mycoplasma pneumoniae Mycoplasma hominis Borrelia burgdorferi

Microorganisms that can develop resistance to azithromycin: gram-positive aerobes:

Streptococcus pneumoniae (penicillin resistant)

Initially resistant microorganisms: gram-positive aerobes:

Enterococcus faecalis Staphylococcus (methicillin-resistant staphylococci show a very high degree of resistance to macrolides)

gram-positive bacteria, erythromycin-resistant anaerobes

Bacteroides fragilis

Pharmacokinetics

After oral administration, azithromycin is well absorbed and quickly distributed in the body. Bioavailability after a single dose of 500 mg is 37% (the “first pass” effect), the maximum concentration (0.4 mg/l) in the blood is created after 2-3 hours, the apparent volume of distribution is 31.1 l/kg, binding with plasma proteins is inversely proportional to the concentration in the blood, 7-50%. Penetrates through cell membranes (effective against infections caused by intracellular pathogens).

Transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes histohematic barriers and enters tissues. The concentration in tissues is 10–50 times higher than in plasma, and at the site of infection it is 24–34% higher than in healthy tissues.

Azithromycin has a very long half-life - 35-50 hours. The half-life from tissues is much longer. The therapeutic concentration of azithromycin lasts up to 5-7 days after taking the last dose. Azithromycin is excreted mainly unchanged - 50% by the intestines, 6% by the kidneys. In the liver it is demethylated, losing activity.

Indications for use

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

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

Contraindications

- hypersensitivity to macrolide antibiotics; - hypersensitivity to other components of the drug; - severe liver failure; - severe renal failure (creatinine clearance below 40 ml/min); - children under 12 years of age with body weight less than 45 kg (for this dosage form); - breast-feeding; - simultaneous use with ergotamine and dihydroergotamine.

Carefully

- myasthenia; - liver dysfunction of mild to moderate severity; - mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min); - in patients with the presence of proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients receiving therapy with antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with water and electrolyte imbalance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; - simultaneous use of terfenadine, warfarin, digoxin, cyclosporine.

Use during pregnancy and lactation.

Azithromycin is recommended to be prescribed during pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

During treatment with azithromycin, breastfeeding is suspended.

Directions for use and doses

Azithromycin Ecomed® is taken orally, without chewing, 1 time per day. The drug is taken at least 1 hour before or 2 hours after meals.

Adults (including elderly people) and children over 12 years of age weighing over 45 kg.

For infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 0.5 g per day for 3 days (course dose – 1.5 g).

For moderate acne: 0.5 g per day for 3 days, then 0.5 g once a week for 9 weeks. The first weekly tablet should be taken 7 days after taking the first daily tablet (8th day from the start of treatment), the subsequent 8 weekly tablets should be taken at intervals of 7 days. Course dose 6.0 g.

For migratory erythema: 1 time per day for 5 days, 1st day 1.0 g, then from 2nd to 5th day 0.5 g. Course dose 3.0 g.

For urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): 1.0 g once.

When used in patients with mild renal impairment: no dose adjustment is required.

When used in patients with mild to moderate liver dysfunction, in elderly patients: no dose adjustment is required.

Elderly patients: no dose adjustment is required. Caution should be exercised in elderly patients with persistent proarrhythmogenic factors due to the high risk of developing arrhythmias, including arrhythmias.

Side effect

The frequency of side effects is classified in accordance with WHO recommendations: very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%; unknown frequency—cannot be estimated from available data.

Infectious diseases:

uncommon - candidiasis, incl. mucous membrane of the oral cavity and genitals, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; unknown frequency - pseudomembranous colitis.

From the blood and lymphatic system:

uncommon - leukopenia, neutropenia, eosinophilia; very rarely - thrombocytopenia, hemolytic anemia.

Metabolism and nutrition:

infrequently - anorexia.

Allergic reactions:

uncommon - angioedema, hypersensitivity reaction; unknown frequency - anaphylactic reaction.

From the nervous system:

often - headache; infrequently - dizziness, disturbance of taste, paresthesia, drowsiness, insomnia, nervousness; rarely - agitation; unknown frequency - hypoesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perversion of smell, loss of taste, myasthenia gravis, delirium, hallucinations.

From the side of the organ of vision:

infrequently - visual impairment.

Hearing and labyrinth disorders:

uncommon - hearing loss, vertigo; unknown frequency - hearing loss, incl. deafness and/or tinnitus.

From the cardiovascular system:

infrequently - palpitations, flushing of the face; unknown frequency - decreased blood pressure, increased QT interval on ECG, ari, ventricular tachycardia.

From the respiratory system:

infrequently - shortness of breath, nosebleeds.

From the gastrointestinal tract:

very often - diarrhea; often - nausea, vomiting, abdominal pain; uncommon - flatulence, dyspepsia, constipation, gastritis, dysphagia, bloating, dry oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - change in tongue color, pancreatitis.

From the liver and biliary tract:

uncommon - hepatitis; rarely - impaired liver function, cholestatic jaundice; unknown frequency - liver failure (in rare cases with death, mainly due to severe liver dysfunction); liver necrosis, fulminant hepatitis.

For the skin and subcutaneous tissues:

uncommon - skin rash, itching, urticaria, dermatitis, dry skin, sweating; rarely - photosensitivity reaction; unknown frequency - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.

From the musculoskeletal system:

uncommon - osteoarthritis, myalgia, back pain, neck pain; unknown frequency - arthralgia.

From the kidneys and urinary tract:

uncommon - dysuria, pain in the kidney area; unknown frequency - interstitial nephritis, acute renal failure.

From the genital organs and breast:

infrequently - metrorrhagia, testicular dysfunction.

Other:

uncommon - asthenia, malaise, feeling of fatigue, facial swelling, chest pain, fever, peripheral edema.

Laboratory data:

often - a decrease in the number of lymphocytes, an increase in the number of eosinophils, an increase in the number of basophils, an increase in the number of monocytes, an increase in the number of neutrophils, a decrease in the concentration of bicarbonates in the blood plasma; infrequently - increased activity of AST, ALT, increased concentration of bilirubin in the blood plasma, increased concentration of urea in the blood plasma, increased concentration of creatinine in the blood plasma, change in the potassium content in the blood plasma, increased activity of alkaline phosphatase in the blood plasma, increased chlorine content in the blood plasma, increased blood glucose concentration, increased platelet count, increased hematocrit, increased plasma bicarbonate concentration, change in plasma sodium content.

Overdose

Symptoms: temporary hearing loss, nausea, vomiting, diarrhea.

Treatment is symptomatic.

Interaction with other drugs

Antacids

Antacids do not affect the bioavailability of azithromycin, but reduce its maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating.

Cetirizine

Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.

Didanosine (dideoxyinosine)

The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal any changes in the pharmacokinetic indications of didanosine compared to the placebo group.

Digoxin (P-glycoprotein substrates)

Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.

Ergot alkaloids

Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on HMG-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.

Carbamazepine

Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.

Cimetidine

Pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin.

Indirect anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).

Cyclosporine

In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. . Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

Efavirenz

Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole

Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which had no clinical significance.

Indinavir

The simultaneous use of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).

Methylprednisolone

Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin

The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil

When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.

Terfenadine

Pharmacokinetic studies have not provided evidence of an interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.

Theophylline

No interaction has been detected between azithromycin and theophylline.

Triazolam/midazolam

Significant changes in pharmacokinetic parameters with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses were not detected.

Trimethoprim/sulfamethoxazole

Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.

special instructions

If you miss one dose, the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.

The drug should be taken at least one hour before or two hours after taking antacids.

The drug should be used with caution in patients with mild to moderate liver dysfunction due to the possibility of developing fulminant hepatitis and severe liver failure.

If there are symptoms of liver dysfunction, such as rapidly increasing asthenia, jaundice, darkening of urine, tendency to bleeding, hepatic encephalopathy, drug therapy should be stopped and a study of the functional state of the liver should be performed.

In case of mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min), azithromycin therapy should be carried out with caution under monitoring the state of renal function.

As with the use of other antibacterial drugs, during therapy with azithromycin, patients should be regularly examined for the presence of non-susceptible microorganisms and signs of the development of superinfections, including fungal ones.

The drug should not be used for longer courses than indicated in the instructions, because The pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.

There is no data on a possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism with the simultaneous use of macrolides with ergotamine and dihydroergotamine derivatives, this combination is not recommended.

With long-term use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis, is possible. If antibiotic-associated diarrhea develops while taking the drug, as well as after 2 months. after completion of therapy, clostridial pseudomembranous colitis should be excluded.

When treated with macrolides, incl. azithromycin, prolongation of cardiac repolarization and QT interval was observed, increasing the risk of developing cardiac arrhythmias, incl. ari.

Caution should be exercised when using the drug in patients with the presence of proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with fluid and electrolyte imbalance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure.

The use of azithromycin may provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis. Impact on the ability to drive vehicles and operate machinery.

If undesirable effects on the nervous system and visual organs develop, caution should be exercised when performing actions that require increased concentration and speed of psychomotor reactions.

Release form

Film-coated tablets, 250 mg and 500 mg.

6 tablets with a dosage of 250 mg, 3 tablets with a dosage of 500 mg in a blister pack made of polyvinyl chloride/polyvinylidene chloride film and printed varnished aluminum foil.

1 blister pack along with instructions for use is placed in a cardboard pack.

Best before date

2 years. Do not use after expiration date.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Conditions for dispensing from pharmacies

On prescription.

Interaction with other drugs.

Antacids

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating.

Cetirizine

Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.

Didanosine (dideoxyinosine)

The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal any changes in the pharmacokinetic indications of didanosine compared to the placebo group.

Digoxin (P-glycoprotein substrates)

Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.

Ergot alkaloids

Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on HMG-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.

Carbamazepine

Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.

Cimetidine

Pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin.

Indirect anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).

Cyclosporine

In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, followed by cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. . Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

Efavirenz

Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole

Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which was not clinically significant.

Indinavir

The simultaneous use of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).

Methylprednisolone

Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin

The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil

When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.

Terfenadine

Pharmacokinetic studies have not provided evidence of an interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.

Theophylline

No interaction has been detected between azithromycin and theophylline.

Triazolam/midazolam

Significant changes in pharmacokinetic parameters with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses were not detected.

Trimethoprim/sulfamethoxazole

Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not show a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.

Azithromycin Ecomed®

Antacids

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating.

Cetirizine

Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.

Didanosine (dideoxyinosine)

The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal any changes in the pharmacokinetic indications of didanosine compared to the placebo group.

Digoxin (P-glycoprotein substrates)

Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.

Ergot alkaloids

Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on HMG-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.

Carbamazepine

Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.

Cimetidine

Pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin.

Indirect anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).

Cyclosporine

In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, and then cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. . Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

Efavirenz

Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole

Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which did not have clinical significance.

Indinavir

The simultaneous use of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).

Methylprednisolone

Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin

The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil

When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.

Terfenadine

Pharmacokinetic studies have not provided evidence of an interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.

Theophylline

No interaction has been detected between azithromycin and theophylline.

Triazolam/midazolam

Significant changes in pharmacokinetic parameters with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses were not detected.

Trimethoprim/sulfamethoxazole

Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not reveal a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.

special instructions

If you miss one dose, the missed dose should be taken as soon as possible, and subsequent doses should be taken at intervals of 24 hours.

The drug should be taken at least one hour before or two hours after taking anatacid medications.

The drug should be used with caution in patients with mild to moderate liver dysfunction due to the possibility of developing fulminant hepatitis and severe liver failure.

If there are symptoms of liver dysfunction, such as rapidly increasing asthenia, jaundice, darkening of urine, tendency to bleeding, hepatic encephalopathy, drug therapy should be stopped and a study of the functional state of the liver should be performed.

In case of mild to moderate renal dysfunction (creatinine clearance more than 40 ml/min), azithromycin therapy should be carried out with caution under monitoring the state of renal function.

As with the use of other antibacterial drugs, during therapy with azithromycin, patients should be regularly examined for the presence of non-susceptible microorganisms and signs of the development of superinfections, including fungal ones.

The drug should not be used for longer courses than indicated in the instructions, because The pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosage regimen.

There is no data on a possible interaction between azithromycin and ergotamine and dihydroergotamine derivatives, but due to the development of ergotism with the simultaneous use of macrolides with ergotamine and dihydroergotamine derivatives, this combination is not recommended.

With long-term use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea and severe colitis, is possible. If antibiotic-associated diarrhea develops while taking the drug, as well as 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded.

When treated with macrolides, incl. azithromycin, prolongation of cardiac repolarization and QT interval was observed, increasing the risk of developing cardiac arrhythmias, incl. ari.

Caution should be exercised when using the drug in patients with the presence of proarrhythmogenic factors (especially in elderly patients): with congenital or acquired prolongation of the QT interval, in patients taking antiarrhythmic drugs of classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with fluid and electrolyte imbalance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure.

The use of azithromycin may provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

Azithromycin Ecomed, 3 pcs., 500 mg, film-coated tablets

Antacids

Antacids do not affect the bioavailability of azithromycin, but reduce the maximum blood concentration by 30%, so the drug should be taken at least one hour before or two hours after taking these drugs and eating.

Cetirizine

Concomitant use of azithromycin with cetirizine (20 mg) for 5 days in healthy volunteers did not lead to pharmacokinetic interaction or a significant change in the QT interval.

Didanosine (dideoxyinosine)

The simultaneous use of azithromycin (1200 mg/day) and didanosine (400 mg/day) in 6 HIV-infected patients did not reveal any changes in the pharmacokinetic indications of didanosine compared to the placebo group.

Digoxin (P-glycoprotein substrates)

Simultaneous use of macrolide antibiotics, incl. azithromycin, with P-glycoprotein substrates such as digoxin, leads to increased concentrations of P-glycoprotein substrate in the blood serum. Thus, with the simultaneous use of azithromycin and digoxin, it is necessary to take into account the possibility of increasing the concentration of digoxin in the blood serum.

Zidovudine

The simultaneous use of azithromycin (single dose of 1000 mg and multiple doses of 1200 or 600 mg) has a minor effect on pharmacokinetics, incl. renal excretion of zidovudine or its glucuronide metabolite. However, the use of azithromycin caused an increase in the concentration of phosphorylated zidovudine, a clinically active metabolite in peripheral blood mononuclear cells. The clinical significance of this fact is unclear.

Azithromycin interacts weakly with isoenzymes of the cytochrome P450 system. Azithromycin has not been shown to participate in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin is not an inhibitor or inducer of cytochrome P450 isoenzymes.

Ergot alkaloids

Given the theoretical possibility of ergotism, the simultaneous use of azithromycin with ergot alkaloid derivatives is not recommended.

Pharmacokinetic studies were conducted on the simultaneous use of azithromycin and drugs whose metabolism occurs with the participation of isoenzymes of the cytochrome P450 system.

Atorvastatin

Concomitant use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause changes in atorvastatin plasma concentrations (based on HMG-CoA reductase inhibition assay). However, in the post-marketing period, isolated case reports of rhabdomyolysis have been received in patients receiving concomitant azithromycin and statins.

Carbamazepine

Pharmacokinetic studies involving healthy volunteers did not reveal a significant effect on the plasma concentrations of carbamazepine and its active metabolite in patients receiving concomitant azithromycin.

Cimetidine

Pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin did not reveal changes in the pharmacokinetics of azithromycin, provided that cimetidine was used 2 hours before azithromycin.

Indirect anticoagulants (coumarin derivatives)

In pharmacokinetic studies, azithromycin did not affect the anticoagulant effect of a single 15 mg dose of warfarin administered to healthy volunteers. Potentiation of the anticoagulant effect has been reported after simultaneous use of azithromycin and indirect anticoagulants (coumarin derivatives). Although a causal relationship has not been established, the need for frequent monitoring of PT should be considered when using azithromycin in patients receiving indirect oral anticoagulants (coumarin derivatives).

Cyclosporine

In a pharmacokinetic study involving healthy volunteers who took azithromycin (500 mg/day once) orally for 3 days, and then cyclosporine (10 mg/kg/day once), a significant increase in plasma Cmax and AUC0-5 of cyclosporine was detected. . Caution is advised when using these drugs together. If simultaneous use of these drugs is necessary, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

Efavirenz

Concomitant use of azithromycin (600 mg/day once) and efavirenz (400 mg/day) daily for 7 days did not cause any clinically significant pharmacokinetic interaction.

Fluconazole

Concomitant use of azithromycin (1200 mg once) did not change the pharmacokinetics of fluconazole (800 mg once). The total exposure and T1/2 of azithromycin did not change with simultaneous use of fluconazole, however, a decrease in Cmax of azithromycin was observed (by 18%), which did not have clinical significance.

Indinavir

The simultaneous use of azithromycin (1200 mg once) did not have a statistically significant effect on the pharmacokinetics of indinavir (800 mg 3 times a day for 5 days).

Methylprednisolone

Azithromycin does not have a significant effect on the pharmacokinetics of methylprednisolone.

Nelfinavir

The simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the Css of azithromycin in the blood serum. No clinically significant side effects were observed, and no dose adjustment of azithromycin is required when used concomitantly with nelfinavir.

Rifabutin

The simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood serum. Neutropenia has sometimes been observed with simultaneous use of azithromycin and rifabutin. Although neutropenia has been associated with the use of rifabutin, a causal relationship between the use of the combination of azithromycin and rifabutin and neutropenia has not been established.

Sildenafil

When used in healthy volunteers, there was no evidence of the effect of azithromycin (500 mg/day daily for 3 days) on the AUC and Cmax of sildenafil or its main circulating metabolite.

Terfenadine

Pharmacokinetic studies have not provided evidence of an interaction between azithromycin and terfenadine. There have been isolated cases reported where the possibility of such an interaction could not be completely excluded, but there was no concrete evidence that such an interaction occurred. It has been found that the simultaneous use of terfenadine and macrolides can cause arrhythmia and prolongation of the QT interval.

Theophylline

No interaction has been detected between azithromycin and theophylline.

Triazolam/midazolam

Significant changes in pharmacokinetic parameters with simultaneous use of azithromycin with triazolam or midazolam in therapeutic doses were not detected.

Trimethoprim/sulfamethoxazole

Concomitant use of trimethoprim/sulfamethoxazole with azithromycin did not reveal a significant effect on Cmax, total exposure or renal excretion of trimethoprim or sulfamethoxazole. Azithromycin serum concentrations were consistent with those found in other studies.