Azithromycin forte-obl tablet p/o film 500mg 3 pcs

Compound

The composition of 1 tablet includes: azithromycin dihydrate (at a concentration equal to 250 or 500 mg of azithromycin ), anhydrous lactose, croscarmellose sodium, anhydrous silicon dioxide in colloidal form, magnesium stearate, corn starch, polacrilin potassium, hypromelose, additives E171 and E172, macrogol 4000.
Capsule composition: 250 or 500 mg of active ingredient, lactose in the form of monohydrate, sodium lauryl sulfate, magnesium stearate.

1 gram of powder contains 15, 30 or 75 mg of azithromycin dihydrate . Auxiliary components: xanthan gum, calcium stearate, silicon dioxide, sodium benzoate, anhydrous sodium carbonate, tartrazine, aspartame , ponceau, flavoring additives “Vanillin” and “Apricot”, refined sugar.

Pharmacodynamics and pharmacokinetics

The semisynthetic antibiotic azithromycin is a synthetically produced derivative of erythromycin , which belongs to the group of macrolide and azalide (it is the first representative of the azalides ).

By binding to the 50S ribosomal subunit, it inhibits protein biosynthesis and inhibits the growth of microbes and suppresses their vital activity. In high concentrations it exhibits a bactericidal effect.

The activity of the drug extends to:

• Gram(+) microorganisms (with the exception of erythromycin microflora) - St. aureus and epidermidis; Str. agalactiae, pneumoniae and pyogenes; streptococci belonging to groups C, F and G;
• Gram(-) microorganisms - pertussis bacillus and parapertussis bacillus , diplococci of the genus Neisseria, Haemophilus influenzae , campylobacteria , bacteria of the genus Legionella , bacteria of the monotypic genus Gardnerella and M. catarrhalis;
• anaerobic microflora (Peptostreptococcus spp., B. bivius, C. perfringens, Peptococcus);
• chlamydia (Chl. trachomatis and pneumoniae);
• mycoparasites of the genus Mycobacterium;
• mycoplasmas (Myc. pneumoniae);
• ureaplasma (Ur. urealyticum);
• spirochetes (causative agents of Lyme disease and spirochete pallidum).

Lipophilic, exhibits stability in acidic environments. After taking the tablet/capsule or suspension, it is quickly absorbed from the gastrointestinal tract.

Bioavailability after taking 0.5 g of the drug is 37%, TCmax is 2-3 hours, the rate of binding to plasma proteins is inversely proportional to the concentration of the substance in the blood and varies from 7 to 50%. T1/2 - 68 hours.

The level of azithromycin in the blood plasma stabilizes after 5-7 days of treatment with the drug.

Easily passing through the blood-parenchymal barriers, the substance enters the tissues, where it is transported to the site of infection by polymorphonuclear leukocytes, phagocytes and macrophages and, in the presence of bacteria, is released at the site of the disease.

Penetrates through plasma membranes, which makes the drug effective against infections caused by intracellular pathogens.

The amount of the substance in tissues and cells is 10-15 times higher than the plasma concentration, the concentration in the pathological focus is 24-34% higher than the concentration in healthy tissues.

After the last administration of the drug, the level necessary to maintain the antibacterial effect is maintained for 5-7 days.

In the liver, azithromycin is demethylated and loses activity. Half of the dose taken is excreted with bile (in its pure form), about 6% of the substance is excreted by the kidneys.

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.

Indications for use of Azithromycin. What does the drug treat?

Indications for use of Azithromycin:

• infectious diseases of the respiratory and ENT organs ( tonsillitis , pharyngitis , sinusitis , laryngitis , acute chronic bronchitis , pneumonia , otitis media );
• bacterial infections of the urogenital tract that occur without complications ( cervicitis or urethritis );
• soft tissue infections and skin infections (infectious dermatitis , impetigo , beshikha );
• scarlet fever;
• borreliosis in the initial stage;
• diseases of the stomach and duodenum associated with Helicobacter pylori.

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).

Side effects

The most common side effects of Azithromycin: visual disturbances, nausea, vomiting, abdominal discomfort, diarrhea , decreased concentration of blood bicarbonates, lymphocytopenia .

Less than 1% of patients reported: vaginal infections, oral candidiasis , leukopenia , ephosinophilia , vertigo , dizziness, hypoesthesia , syncope , drowsiness, convulsions (other macrolides also been found to provoke convulsions), headache, distortion/loss of taste and sensations of odors, impaired regularity of bowel movements (rare bowel movements), digestive disorders, anorexia , flatulence , gastritis , increased fatigue, increased AST and ALT, creatinine and bilirubin in the blood, urea , K concentration in the blood; vaginitis , arthralgia , skin rashes and itching.

Less than 0.1% of patients experienced: neutrophilia , thrombocytopenia , hemolytic anemia , mental and motor hyperactivity, nervousness, anxiety, aggressiveness, asthenia , lethargy , neurosis, sleep disturbances, insomnia, discoloration of the tongue, constipation, cholestatic jaundice and hepatitis (including altered FPP indicators), angioedema , interstitial nephritis , acute renal failure, exanthema , urticaria , photosensitivity, Lyell's syndrome , polymorphic and malignant exudative erythema , anaphylaxis , angioedema , candidiasis .

In rare cases, palpitations, ventricular arrhythmia or paroxysmal tachycardia of the “pirouette” type, and chest pain are also possible. It has been found that other macrolide antibiotics . hypotension and QT interval prolongation have also been reported

Side effects that occur with an unknown frequency: myasthenia gravis , agitation , fulminant hepatitis , liver failure , necrotizing hepatitis .

In rare cases, macrolides cause hearing loss. Some patients taking Azithromycin experienced hearing loss, ringing in the ears, and deafness.

Most of these cases were recorded during studies in which the drug was used for a long time in high doses. The reports indicate that the problems described are reversible.

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

Most of the observed adverse reactions are reversible after completion of the course of treatment or discontinuation of the drug.

Classification of the frequency of side effects (WHO): very often (with a frequency of more than 1/10), often (with a frequency of at least 1/100, but less than 1/10), infrequently (with a frequency of at least 1/1000, but less than 1 /100), rare (with a frequency of at least 1/10,000, but less than 1/1000), very rare (with a frequency of less than 1/10,000), including individual messages.

From the circulatory and lymphatic systems: often - lymphocytopenia, eosinophilia; uncommon - leukopenia, neutropenia; rarely - thrombocytopenia, hemolytic anemia.

From the central nervous system: often - dizziness, headache, paresthesia, impaired perception of taste, anorexia; infrequently - anxiety, nervousness, hyposthesia, insomnia, drowsiness; rarely - agitation, delirium, hallucinations; very rarely - fainting, convulsions, psychomotor hyperactivity, aggression, anosmia, loss of taste, parosmia, exacerbation of myasthenia gravis, perversion of smell.

From the senses: infrequently - hearing impairment, vertigo, visual impairment; unknown frequency - hearing impairment, including deafness and/or tinnitus.

From the respiratory system and JIOP organs: infrequently - shortness of breath, nosebleeds.

From the cardiovascular system: infrequently - a feeling of palpitations, “flushes” of blood to the face; very rarely - decreased blood pressure, arrhythmia, ventricular tachycardia, increased QT interval, arrhythmia.

Infectious diseases: infrequently - rhinitis, respiratory diseases, pharyngitis, pneumonia, candidiasis, including the mucous membrane of the oral cavity and genitals, gastroenteritis.

From the digestive system: very often - nausea, diarrhea, abdominal pain, flatulence (bloating), often - vomiting; uncommon - belching, dysphagia, gastritis, constipation, dryness of the oral mucosa, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - discoloration of the tongue, pseudomembranous colitis, pancreatitis.

From the liver and biliary tract: infrequently - hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases; very rarely - cholestatic jaundice, liver failure (in rare cases, fatal, mainly due to liver dysfunction), fulminant hepatitis, liver necrosis.

Allergic reactions: often - itching, rash; uncommon - Stevens-Johnson syndrome, photosensitivity, urticaria; rarely - anaphylactic reactions (including angioedema) in rare cases with fatal outcome, toxic epidermal necrolysis. erythema multiforme.

From the skin and subcutaneous tissues: dry skin, dermatitis, sweating.

From the musculoskeletal system: often - arthralgia; uncommon - osteoarthritis, myalgia, neck pain, back pain.

From the genitourinary system: infrequently - increased residual urea nitrogen and creatinine concentration in the blood plasma, dysuria, pain in the kidneys, metrorrhagia. testicular dysfunction; very rarely - interstitial nephritis, acute renal failure.

Other: often - weakness; uncommon - chest pain, peripheral edema, asthenia (malaise, feeling tired); Uncommon: facial swelling, fever.

Laboratory data: often - an increase in the number of basophils, monocytes, neutrophils, a decrease in the concentration of bicarbonates in the blood plasma; infrequently - increased alkaline phosphatase activity, increased chlorine content, increased glucose concentration, increased bicarbonate concentration in the blood plasma, increased platelet count, increased hematocrit, change in sodium content in the blood plasma, change in the concentration of potassium in the blood plasma.

Any side effect should be reported to your doctor.

Instructions for use of Azithromycin (Method and dosage)

Azithromycin capsules and tablets, instructions for use

The antibiotic is taken 1 time per day, an hour before meals or 2 hours after meals. The missed dose is taken as quickly as possible, and the next dose of medication should be taken 24 hours later.

According to the instructions for use of Azithromycin, for children weighing more than 45 kg and adult patients, the optimal dosage for soft tissue diseases, respiratory diseases and skin diseases is 500 mg 1 time per day. The course lasts 3 days.

For Lipschutz migratory erythema , take 2 tablets of Azithromycin 500 mg on the first day, from days 2 to 5 inclusive - 500 mg/day.

For uncomplicated cervicitis/urethritis, take 1 g of the drug once.

Azithromycin capsules (Astrapharm, Zdorovye, BHFZ and other manufacturers) are taken according to a similar scheme.

Instructions for Azithromycin Forte

For diseases of soft tissues, respiratory organs and skin, the recommended dose per course is 1.5 g (it should be divided into 3 doses with intervals of 24 hours between them).

For the treatment of acne , the drug is taken at a dose of 0.5 g/day for 3 days, followed by 0.5 g/week for the next 9 weeks. (one time). The fourth tablet should be taken on the 8th day of treatment. Subsequent doses are taken at intervals of 7 days.

For uncomplicated cervicitis/urethritis, take 1 g once.

For Lyme disease, the patient is prescribed 1 g on the first day, from days 2 to 5 - 0.5 g. For the full course, the patient takes a total of 3 g of Azithromycin.

For children, the drug is dosed depending on weight. The standard dose is 10 mg/kg/day. The treatment regimen may be as follows:

• 3 doses of 10 mg/kg at intervals of 24 hours;
• 1 dose of 10 mg/kg and 4 doses of 5-10 mg/kg.

At the initial stages of the development of Lyme disease , the first dose of the drug for a child is 20 mg/kg; in the next 4 days, children's Azithromycin Forte is taken at 10 mg/kg.

For pneumonia, treatment begins with intravenous administration of the drug (at least 2 days, 0.5 g/day). Then they switch to taking capsules. The course lasts from 1 to 1.5 weeks. Therapeutic dose - 500 mg/day.

For pelvic diseases , infusion therapy is also indicated at the initial stage of treatment, then the patient should switch to taking 250 mg capsules (2 per day for a week).

The timing of the transition to tablets/capsules is determined depending on the dynamics of laboratory and clinical parameters.

To prepare the suspension, the powder (2 g) is dissolved in 60 ml of water.

To prepare an injection solution, 0.5 g of powder is diluted in 4.8 ml of water for injection.

If the patient is indicated for infusion therapy, 0.5 g of powder must be diluted to a concentration of 1 or 2 mg/ml (500 or 250 ml, respectively) with Ringer's solution, NaCl 0.9% or dextrose 5%. In the first case, the duration of the infusion is 3 hours, in the second - 1 hour.

Treatment regimen for ureaplasmosis

For ureaplasmosis, treatment should be carried out according to the principle of complexity.

A few days before starting Azithromycin, the patient is prescribed immunomodulators. The drug is injected into the muscle 1 r./day. with an interval of 1 day. Injections continue to be given throughout the course of treatment.

Simultaneously with the 2nd dose of the immunomodulator, a bactericidal antibiotic . When it is completed, switch to Azithromycin. During the first 5 days, the drug is taken daily 1.5 hours before breakfast, 1 g.

After this time, take a 5-day break and again, following the recommendations in the instructions for the drug, take 1 g. After another 5 days, Azithromycin is taken for the 3rd and last time. The dose is the same - 1 g.

For 15-16 days, while treatment with Azithromycin continues, the patient should also take 2-3 times a day. take stimulators of the synthesis of your own interferons , as well as antimycotics of the polyene series .

After a course of antibiotics, restorative therapy is indicated using drugs that normalize the function of the gastrointestinal tract and help restore its microflora. Maintenance treatment is continued for 2 weeks or more.

Treatment regimen for chlamydia. Capsules and tablets - why are they effective for chlamydia?

Azithromycin is the drug of choice for chlamydia of the lower genitourinary system, as it is well tolerated by patients, and, in addition, can be used to treat adolescents and during pregnancy .

For this form of infection, it is taken 1 time in a dose of 1 g.

If chlamydial infection , treatment is carried out in short courses, and long intervals are maintained between courses.

The course of treatment is designed for 3 doses. The dose for 1 dose is 1 g. The interval between doses is 7 days, that is, the medicine is taken on days 1, 7 and 14. This regimen has been approved by the Russian Ministry of Health for the treatment of persistent/complicated forms of chlamydia.

How to take Azithromycin for sore throat?

All antibiotics intended for the treatment of sore throat are taken in a ten-day course. Azithromycin is an exception to this rule - it is prescribed for 3-5 days.

Another advantage of the drug is that it is tolerated by patients much better than penicillin drugs ( macrolides are considered the least toxic antibiotics).

Adults and children whose weight exceeds 45 kg are prescribed to take 500 mg/day. If for some reason a dose is missed, the next dose is taken as soon as this circumstance is discovered, and the next dose is taken at 24-hour intervals.

Children aged six months to 12 years are advised to take the suspension. You should take an antibiotic once a day. Treatment lasts at least 3 days, the dose is selected individually.

Reviews of Azithromycin for angina are positive, since even with purulent angina, the patient’s condition improves significantly within 5-6 hours after the first tablet was taken.

Antibiotics for sinusitis. Azithromycin - what are these tablets for for sinusitis?

Azithromycin for sinusitis is used according to one of the following regimens:

• loading dose (500 mg) on ​​the first day, then 500 mg for 3 days;
• loading dose (500 mg) and another 4 days of 250 mg.

Children under 12 years of age are prescribed a suspension. The drug is dosed at the rate of 10 mg per 1 kg of child weight. The medicine is given to the patient 1 time per day. three-day course. In some cases, on the first day it is recommended to give the child 10 mg/kg Azithromycin, and in the next 4 days reduce the dose to 5 mg/kg. The highest dose per course is 30 mg/kg.

Azithromycin for sinusitis , accumulating at the site of the disease, suppresses Gram (+) bacteria, which are the main cause of its development, and effectively relieves inflammation in the sinuses.

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.

Interaction

Absorption of the drug is reduced in combination with Al3+ and Mg2+-containing antacids, food and ethanol .

The combination of macrolides + Warfarin can provoke an increase in the anticoagulant effect, so patients taking Azithromycin in combination with Warfarin - despite the fact that studies have not shown changes in prothrombin time when taken in usual doses - require careful monitoring of this indicator.

Unlike other macrolides, it does not interact with terfenadine , triazolam , Theophylline , Digoxin , Carbamazepine .

The simultaneous use of terfenadine with various antibiotics provokes prolongation of the QT interval and arrhythmia . Based on this, Azithromycin is used with caution in patients taking this drug.

Macrolides increase plasma concentration and toxicity, and also slow down the excretion of methylprednisolone , Cycloserine , Felodipine , indirect coagulants and drugs subject to microsomal oxidation, however, in the case of the use of Azithromycin (and other azalides), this type of interaction has not been recorded.

The effectiveness of the drug increases in combination with chloramphenicol and tetracycline and decreases in combination with lincosamides .

Azithromycin is pharmaceutically incompatible with Heparin

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.

special instructions

The Vidal reference book states that since Azithromycin is metabolized in the liver and the substance is excreted primarily in bile, the drug should not be used to treat patients with severely impaired liver function.

Elderly patients do not need to adjust the dose. However, since the electrical conduction of the heart may be impaired in older people, prescribing the drug to them may increase the risk of heart rhythm disturbances and the development of torsades de pointes .

The use of intravenous Azithromycin, according to Wikipedia, is contraindicated in patients under 16 years of age.

Features of the pharmacokinetic profile of the drug

The pharmacokinetic parameters of the drug are largely influenced by food intake, and the extent to which the changes are pronounced also depends on its dosage form.

Thus, food intake helps to reduce the Cmax of azithromycin in capsule form and increases this indicator for the tablet form. In the first case, there is a simultaneous decrease in AUC, in the second, this indicator remains unchanged.

In old age, in women, unlike men of the same age group, pharmacokinetic parameters change, namely, Cmax increases.

In children from 12 months to 5 years, there is a decrease in AUC, Cmax, T1/2.

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 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 analogs

Level 4 ATC code matches:
Ecositrin

Azicine

Rovamycin

AzitRus

Safocid

Clarithromycin

Sumamed Forte

Klarbakt

Azitro Sandoz

Sumamed

ZI-Factor

Azitral

Azimed

Azicide

Spiramycin-vero

Zitrolide

Ecomed

Macropen

Klacid SR

Klacid

• Azivok
• Azitral
• Azithromycin-Astrapharm
• AzitRus
• Azithromycin Forte
• Zitrolide
• Tremak-sanovel
• Hemomycin
• Sumamed
• Sumamox
• Sumaclid 1000

Azithromycin for children

The use of tablets and capsules is possible if the child’s body weight exceeds 45 kg. The dosage of Azithromycin for children weighing 45 kg is determined depending on the indications.

Children weighing more than 45 kg are prescribed capsules or tablets at a dosage of 250 mg or 500 mg.

At a young age, the optimal dosage form for children is a suspension.

Bad reviews about the treatment of children with Azithromycin are very rare. A high concentration of the drug at the site of inflammation suppresses the activity of bacteria and prevents the infection from spreading further. The child's respiratory function improves, the temperature decreases, sore throat and weakness decrease.

An important feature of the medicine is that to achieve a therapeutic effect, 3-5 days of treatment are enough, since the drug continues to act for another week after completion of the course.

Azithromycin during pregnancy

During pregnancy and breastfeeding, the drug is prescribed when the benefits of treatment for the mother outweigh the potential risks of using Azithromycin for the fetus/child.

Reviews of Azithromycin during pregnancy, compiled by Canadian researchers as part of the Motherisk Program, convincingly prove the safety of using the drug for the treatment of expectant mothers.

In all control groups (women in the 1st group took Azithromycin, in the 2nd group - other antibiotics, in the 3rd group - they were not treated with antimicrobial drugs), the incidence of severe malformations in the fetus did not differ significantly.

Reviews about Azithromycin

Reviews of Azithromycin for chlamydia , sore throat , sinusitis , frontal sinusitis and other diseases that are caused by microbes sensitive to the drug are overwhelmingly good.

The drug is a powerful tool for combating bacterial infection and is well tolerated by patients, and the side effects associated with its use appear infrequently and completely disappear after cessation of treatment.

Reviews from doctors about the drug are also positive. The main advantages of Azithromycin, according to doctors, are that it:

• has anti-inflammatory and immunomodulatory effects;
• characterized by high activity against probable pathogens of infectious respiratory diseases;
• creating high concentrations in tissues, exhibits bactericidal properties against H. pylori, H. influenzae, N. gonorrhoeae, M. catarrhalis S. pyogenes, S. pneumoniae, S. agalactiae, B. pertussis, Campylobacter spp., C. diphtheriae;
• effective against atypical pathogens that reproduce inside cells (in particular, against mycoplasmas and chlamydia );
• can be used during pregnancy ;
• has a dosage form suitable for children.

Azithromycin has a post-antibiotic effect , which allows it to be used in short courses. In addition, under the influence of the drug, even microbes resistant to it become more sensitive to the effects of immune defense factors.

Unlike Erythromycin , which is the basis of macrolide antibiotics, Azithromycin does not decompose in the acidic environment of the stomach and has a lesser effect on gastrointestinal motility.

Azithromycin forte-obl tablet p/o film 500mg 3 pcs

Pharmacological group:

Antibiotic azalide.
Pharmacodynamics:
Azithromycin is a broad-spectrum bacteriostatic antibiotic from the group of macrolides-azalides. 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 subunit of the ribosome, 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, anaerobic, intracellular and other microorganisms.

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

In most cases, sensitive microorganisms 1. Gram-positive aerobes Staphylococcusaureus 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.; Porphyriomonas 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-sensitive.

Initially resistant microorganisms

Gram-positive aerobes Enterococcus faecalis; Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides); gram-positive bacteria resistant to erythromycin.

Anaerobes Bacteroidesfragilis.

Pharmacokinetics:

Azithromycin is rapidly absorbed from the gastrointestinal tract due to its stability in an acidic environment and lipophilicity. It is quickly distributed throughout the body, while high concentrations of the antibiotic are achieved in the tissues. After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is reached after 2.5-2.9 hours and is 0.4 mg/l. Bioavailability is 37.5%.

Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, the prostate gland), skin and soft tissues. The high concentration in tissues (10-50 times higher than in plasma) and the long half-life are due to the low binding of azithromycin to plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in the low pH environment surrounding lysosomes. This, in turn, determines the large apparent volume of distribution (31.1 l/kg) and high plasma clearance. The ability of azithromycin to accumulate predominantly in lysosomes is especially important for the elimination of intracellular pathogens. It has been proven that phagocytes deliver azithromycin to sites of infection, where it is released during the process of phagocytosis. The concentration of azithromycin in foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which has made it possible to develop short (3-day and 5-day) courses of treatment.

It is demethylated in the liver, the resulting metabolites are not active.

The elimination of azithromycin from blood plasma occurs in 2 stages: the half-life is 14-20 hours in the range from 8 to 24 hours after taking the drug and 41 hours in the range from 24 to 72 hours, which allows the drug to be used once a day.

The drug is excreted mainly in bile unchanged, a small part is excreted by the kidneys.

How much does Azithromycin cost?

In Russian pharmacies, the cost of tablets (250 mg No. 6) is from 50 rubles, the price of Azithromycin in tablets of 500 mg (package No. 3) is about 200 rubles. The price of Azithromycin analogues is approximately the same.

The average price of Azithromycin in Ukraine (250 mg No. 6 tablets) is 30 UAH, 3 antibiotic tablets at a dosage of 500 mg can be bought for 50-70 UAH.

The price of Azithromycin in Belarus is from 15 to 200 thousand rubles (depending on the dosage of the active substance and the number of tablets/capsules in the package). The price of the suspension for children is from 15 to 110 thousand rubles.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Azitrox por.
  for prig. susp. for oral administration, azithromycin, 100 mg/5 ml 15.9 Pharmstandard-Leksredstva OJSC 146 rub. order
• Azitrox por. for prig. susp. for oral administration, azithromycin, 200 mg/5 ml 15.9 Pharmstandard-Leksredstva OJSC

  RUB 217 order

• Azitrox (azithromycin) 500 mg caps. 2 pcs. Pharmstandard-Leksredstva OJSC

  RUB 224 order

• Azithromycin tablets p.p.o. 500 mg 3 pcs. VertexVertex JSC

  RUB 215 order

• Azitrox (azithromycin) 500 mg caps. 3 pcs. Pharmstandard-Leksredstva OJSC

  RUB 323 order

Pharmacy Dialogue

• Azithromycin (caps. 500 mg No. 3)Medicine production

  81 RUR order

• Azithromycin Avexima (tab.p.reg. 500 mg No. 3) Irbitsky HFZ

  132 RUR order

• Azithromycin-OBL (caps. 250 mg No. 6) Obolenskoe pharmaceutical company.

  RUB 157 order

• Azithromycin (tablet p/o 500 mg No. 3)Vertex

  RUB 216 order

• Azithromycin (caps. 250 mg No. 6)Vertex

  200 rub. order

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Pharmacy24

• Azithromycin 250 mg N6 capsules PAT NEC "Borshchagivsky chemical-pharmaceutical plant", Kiev, Ukraine
  42 UAH. order
• Azithromycin 500 mg No. 3 tablets Flamingo Pharmaceuticals Ltd., India

  34 UAH order

• Azithromycin 250 mg No. 6 capsules TOV Pharmaceutical company “Zdorovya”, Kharkiv, Ukraine

  47 UAH order

• Azithromycin Grindeks 500 mg No. 3 tablets Blupharma - Pharmaceutical Industry, S.A., Portugal

  103 UAH order

• Azithromycin 500 mg No. 3 capsules TOV Astrapharm, Ukraine

  34 UAH order

PaniPharmacy

• Azithromycin-KR por.gr.d/oral.susp.200mg/5ml 25.4g No. 1 Ukraine, Krasnaya Zvezda

  88 UAH order

• AZITHROMYCIN tablets Azithromycin Grindeks tablets 500 mg No. 3 Portugal, Bluepharma

  113 UAH order

• AZITHROMYCIN capsule Azithromycin capsules 500 mg No. 3 Ukraine, Health LLC

  62 UAH.order

• AZITHROMYCIN capsule Azithromycin-KR caps. 500 mg No. 3 Ukraine, Red Star OJSC

  42 UAH order

• AZITHROMYCIN capsule Azithromycin capsules 0.25g No. 6 Ukraine, Astrapharm LLC

  36 UAH order

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