Azithromycin for a child: a sure way to overcome bronchitis and pneumonia - an overview for moms. Azithromycin tablets: instructions for use Contraindications and side effects

Azithromycin

International non-proprietary name

Azithromycin

Dosage form

Capsules 250 mg

Composition

One capsule contains

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

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

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

Description

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

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

Pharmacotherapeutic group

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

ATX code J01FA10

Pharmacological properties

Pharmacokinetics

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

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

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

Demethylated in the liver with the formation of inactive metabolites.

It is excreted in 2 stages: the time for reducing the concentration in the blood of the first phase is 14-20 hours, the second phase is 41 hours, which allows you to take the drug 1 time per day.

Pharmacodynamics

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

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

It is inactive against Gram-positive bacteria resistant to erythromycin.

Indications for use

upper infections respiratory tract and ENT organs (angina, sinsuit, tonsillitis, otitis media)

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

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

Urogenital tract infections (uncomplicated urethritis, cervicitis)

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

Dosage and administration

Inside, 1 hour before meals or 2 hours after meals, 1 time per day.

For infections of the upper and lower respiratory tract, infections of the skin and soft tissues, 500 mg / day are prescribed for 3 days (course dose - 1.5 g).

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

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

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

Children from 12 years of age are prescribed at the rate of 10 mg / kg 1 time per day for 3 days or on the first day - 10 mg / kg, then on the 4th day - 5-10 mg / kg / day for 3 days. x days (course dose - 30 mg/kg).

Side effects

Often

Nausea, vomiting, diarrhea, abdominal pain

Seldom

Thromocytopenia

Aggression, agitation, restlessness, nervousness, insomnia, development of suicidal thoughts, suicidal behaviors

Paresthesia, asthenia

Hearing loss, deafness and tinnitus

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

Loss of appetite, flatulence, constipation, pseudomembranous colitis

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

Hypersensitivity reactions (redness, skin rash, itching,

angioedema, photosensitivity), erythema multiforme, Steven-Johnson syndrome and toxic epidermal necrolysis, anaphylactic shock including edema (rarely resulting in death)

Interstitial nephritis, acute renal failure

Very rarely

Fatigue, headache, dizziness, convulsions

Change in taste and smell

Arthralgia

Vaginitis, candidiasis, superinfections

Contraindications

Hypersensitivity to azithromycin and macrolide antibiotics

Severe liver dysfunction

Severe renal dysfunction

Children and adolescents up to 12 years of age

Pregnancy and lactation

Drug Interactions

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

With the joint appointment of warfarin and azithromycin (at usual doses), no change in prothrombin time was detected, however, patients need careful monitoring of prothrombin time.

Increases the concentration of digoxin due to the weakening of its inactivation by the intestinal flora.

With the simultaneous administration of azithromycin with ergotamine and dihydroergotamine, their toxic effects (vasospasm, dysesthesia) may occur.

Reduces clearance and enhances the pharmacological action of triazolam.

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

Lincosamines weaken the effectiveness of azithromycin, tetracycline and chloramphenicol - increase.

Pharmaceutically incompatible with heparin.

special instructions

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

It is necessary to observe a 2-hour break with the simultaneous use of antacids.

The attending physician should be informed about the occurrence of any side effect.

The following side effects have been reported with macrolide antibiotics: ventricular arrhythmia, including ventricular tachycardia and flutter-fibrillation (ventricular), in patients with a prolonged QT interval.

Extremely rarely, during treatment with azithromycin, there may be flutter-flicker (ventricular) and subsequent myocardial infarction in individuals with a history of arrhythmia.

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

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

During treatment with the drug, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities.

Overdose

• Latin name: Azithromycin
• ATX code: J01FA10
• Active substance: Azithromycin (Azithromycin)
• Manufacturer: CJSC FP Obolenskoe, LLC Vertex, JSC Moskhimfarmpreparaty im. N. A. Semashko (Russia), PJSC NPTs Borshchagovsky KhPZ, Pharmaceutical company Zdorovye, OAO KhPZ Krasnaya Zvezda (Ukraine)

Composition

Lineup 1 tablets includes: azithromycin dihydrate (in a concentration equal to 250 or 500 mg azithromycin ), anhydrous lactose, croscarmellose sodium, anhydrous colloidal silicon dioxide, magnesium stearate, corn starch, potassium polacrilin, hypromelose, additives E171 and E172, macrogol 4000.

Composition capsules: 250 or 500 mg active active substance, lactose monohydrate, sodium lauryl sulfate, magnesium stearate.

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

Release form

• Tablets in p / o and capsules 250 mg or 500 mg. Tablets are packaged in packs of 3 or 6 pieces, capsules - 6 pieces.
• Powder for oral suspension (100 mg/20 ml, 200 mg/20 ml or 500 mg/20 ml; 20 g in plastic vials with measuring cup).

pharmachologic effect

Broad-spectrum antibacterial agent.

Pharmacodynamics and pharmacokinetics

Semi-synthetic antibiotic azithromycin is a synthetic derivative which belongs to the group of antibiotics macrolides and azalides ” (is the first representative azalides ).

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

The activity of the drug extends to:

Lipophilen , exhibits stability in an acidic environment. After taking a tablet / capsule or suspension, it is rapidly absorbed from the gastrointestinal tract.

Bioavailability after taking 0.5 g of the drug is 37%, TCmax - 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 the hematoparenchymal barriers, the substance enters the tissues, where it is transported to the focus of infection by polymorphonuclear leukocytes, phagocytes and macrophages and, in the presence of bacteria, is released in the focus of the disease.

Penetrates through plasma membranes, which makes the drug effective in 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 injection of the drug, the level necessary to maintain the antibacterial effect remains for 5-7 days.

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

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

Indications for the use of Azithromycin:

• infectious diseases of the respiratory and ENT organs ( tonsillitis , , sinusitis , ; exacerbated chronic , pneumonia , );
• proceeding without complications bacterial infections of the urogenital tract (caused by Chlamydia trachomatis cenrvicitis or );
• soft tissue infections and skin infections (infectious , impetigo , beshikha );
• borreliosis in the initial stage;
• associated with Helicobacter pylori diseases of the stomach / 12-colon .

Contraindications

Contraindications: intolerance macrolide antibiotics , severe pathologies of the kidneys and / or liver.

In pediatrics, the suspension is not used to treat children weighing up to 5 kg, capsules and tablets Azithromycin - for children weighing up to 45 kg.

Side effects

The most common side effects of Azithromycin are visual disturbances, nausea, vomiting, abdominal discomfort, , a decrease in the concentration of bicarbonates in the blood, lymphocytopenia .

Less than 1% of patients had: vaginal infections , oral candidiasis , leukopenia , ephosinophilia , vertigo / dizziness, hypoesthesia , syncope , drowsiness, convulsions (it was found that others macrolides also provoke convulsions), headache, distortion/loss of taste and smell, irregular bowel movements (rare bowel movements), digestive disorders, anorexia , , , increased fatigue; increase in ASAT and ALT, And blood, urea , concentration of K 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 , paresthesia , lethargy, neurosis, sleep disturbances, insomnia, discoloration of the tongue, constipation, cholestatic jaundice And hepatitis (including modified FPP indicators), , interstitial nephritis , OPN, exanthema , , photosensitivity, Lyell's syndrome , polymorphic And malignant exudative erythema , anaphylaxis , angioedema , .

In rare cases, there may also be a strong heartbeat, ventricular arrhythmia or paroxysmal tachycardia pirouette type, chest pain. It has been found that other symptoms can also cause similar symptoms. macrolide antibiotics . Cases have also been reported arterial hypotension and prolongation of the QT interval.

Side effects that occur with an unspecified frequency: myasthenia gravis , agitation , fulminant hepatitis , insufficiency of liver function , necrotizing hepatitis .

In rare cases macrolides cause hearing loss. Some patients treated with Azithromycin have impaired hearing, 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. Reports indicate that the problems described are reversible.

Application instruction of Azithromycin

Capsules and tablets Azithromycin: instructions for use

Antibiotic take 1 p./day, one hour before a meal or 2 hours after a meal. The missed dose is taken as soon as possible, while the next dose of the drug should be taken after 24 hours.

According to the instructions for the 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 r. / day. The course lasts 3 days.

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

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

Azithromycin capsules (Astrapharm, Health, BHFZ and other manufacturers) are taken in a similar way.

Instructions for Azithromycin Forte

In 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 treatment acne vulgaris the drug is taken for 3 days at 0.5 g / day, in the next 9 weeks, take 0.5 g / week. (once). The fourth tablet should be drunk on the 8th day of treatment. Subsequent doses are taken at intervals of 7 days.

At uncomplicated cervicitis/urethritis once take 1 g.

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

For children, the drug is dosed according to 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.

In the early stages of development 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.

At 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.

At pelvic diseases on the initial stage treatment also shows infusion therapy, 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 a suspension, the powder (2 g) is dissolved in 60 ml of water.

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

If the patient is indicated for infusion therapy, 0.5 g of the powder must be diluted to a concentration of 1 or 2 mg / ml (up to 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 ureaplasma

Simultaneous use Terfenadine with different antibiotics causes prolongation of the QT interval and . Based on this, azithromycin is used with caution in patients who take this drug.

macrolides increase plasma concentration and toxicity, and also slow down excretion , indirect coagulants and drugs subject to microsomal oxidation, however, in the case of azithromycin (and other azalides ) this type of interaction was not recorded.

The effectiveness of the drug is increased in combination with And Tetracycline and decreases in combination with lincosamides .

FROM heparin azithromycin is pharmaceutically incompatible.

Terms of sale

On prescription.

Recipe in Latin (sample):

Rep.: Tab. Azithromycini 0.5 N.3
D.S. 1/day 3 days.

Storage conditions

The drug (in any dosage form) should be stored at a temperature of 15-25˚C in a place protected from moisture and light. The storage temperature of the finished suspension is from 2 to 8°C.

Best before date

For powder and capsules - 2 years. For tablets - 3 years. The suspension is considered fit for use within 3 days.

special instructions

The Vidal guide states that, since azithromycin is metabolized in the liver and the substance is excreted mainly in the 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 violations. heart rate and development torsades de pointes .

The use of Azithromycin IV, 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 how pronounced the changes also depend on its dosage form.

The price of Azithromycin analogues is from 38 UAH (116 rubles).

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 with a dosage of 250 mg or 500 mg.

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

Bad reviews about the treatment of children with Azithromycin are rare. A high concentration of the drug in the focus of inflammation inhibits the activity of bacteria and prevents the infection from spreading further. The child is improving respiratory function, temperature decreases, sore throat and weakness decrease.

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

Alcohol compatibility

The instructions do not indicate the interaction of Azithromycin and alcohol, however, this does not mean that they are allowed to drink alcohol during treatment. Alcoholic drinks reduce the absorption of the drug, slow down the rate of metabolic processes, increase the load on the liver, provoke intoxication and death. hepatocytes .

A single dose of a small dose of alcohol is allowed no earlier than a couple of days after the completion of the course of treatment.

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 the drug for the treatment of expectant mothers.

In all control groups (in the 1st women took azithromycin, in the 2nd - other antibiotics , in the 3rd - did not undergo treatment antimicrobials ) the incidence of severe malformations in the fetus did not differ significantly.

Reviews about Azithromycin

Reviews about Azithromycin with chlamydia , at sore throat , sinusitis , frontite 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 at the same time it is well tolerated by patients, and the side effects associated with its use appear infrequently and completely disappear after stopping treatment.

Published on this page detailed instructions by application Azithromycin. Available dosage forms drug (capsules and tablets 250 mg and 500 mg), as well as its analogues. Provided information about side effects that Azithromycin can cause, about interactions with other drugs. In addition to information about the diseases for the treatment and prevention of which the drug is prescribed (tonsillitis, bronchitis, pneumonia), the algorithms for admission, possible dosages for adults and children are described in detail, the possibility of using during pregnancy and lactation is specified. Annotation to Azithromycin is supplemented by reviews of patients and doctors. Interaction of the drug with alcohol.

Instructions for use and dosage

Inside, 1 hour before or 2 hours after meals 1 time per day.

Adults with infections of the upper and lower respiratory tract - 500 mg per day for 1 dose for 3 days (course dose - 1.5 g).

For infections of the skin and soft tissues - 1000 mg per day on the first day for 1 dose, then 500 mg per day daily from 2 to 5 days (course dose - 3 g).

In acute infections of the genitourinary organs (uncomplicated urethritis or cervicitis) - once 1000 mg.

In Lyme disease (borreliosis) for the treatment of stage 1 (erythema migrans) - 1000 mg on the first day and 500 mg daily from 2 to 5 days (course dose - 3 g).

At peptic ulcer stomach and duodenum associated with Helicobacter pylori - 1 g per day for 3 days as part of a combined anti-Helicobacter therapy. Children over 12 years old (weighing 50 kg or more) with infections of the upper and lower respiratory tract, skin and soft tissues - 500 mg 1 time per day for 3 days.

In the treatment of erythema migrans in children, the dose is 1000 mg on the first day and 500 mg daily from days 2 to 5.

Release form

Film-coated tablets 250 mg and 500 mg.

Capsules 250 mg and 500 mg.

Azithromycin- a broad-spectrum antibiotic. It is a representative of a subgroup of macrolide antibiotics - azalides, acts bacteriostatically. When creating high concentrations in the focus of inflammation, it has a bactericidal effect.

Acts on extra- and intracellular pathogens. Gram-positive and gram-negative microorganisms are sensitive to azithromycin; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp; as well as Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. Azithromycin is not active against Gram-positive bacteria resistant to erythromycin.

It is also active against Toxoplasma gondii.

Pharmacokinetics

Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in an acidic environment and lipophilicity. Azithromycin penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), into the skin and soft tissues. 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 the sites of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (on average by 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function. Azithromycin persists at bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) courses of treatment. Demethylated in the liver, the resulting metabolites are not active. 50% is excreted unchanged in the bile, 6% - by the kidneys.

Indications

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

• infections of the upper respiratory tract and ENT organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);
• scarlet fever;
• infections of the lower respiratory tract (including those caused by atypical pathogens);
• infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
• infections of the urogenital tract (uncomplicated urethritis and / or cervicitis);
• Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
• diseases of the stomach and duodenum associated with Heliobactcr pylori (as part of combination therapy).

Contraindications

• hepatic and / or renal failure;
• lactation period;
• children's age up to 12 years;
• hypersensitivity (including to other macrolides).

special instructions

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

It is necessary to observe a break of 2 hours with the simultaneous use of antacids. After discontinuation of treatment, hypersensitivity reactions may persist in some patients, which requires specific therapy under medical supervision.

Side effect

• diarrhea;
• nausea;
• abdominal pain;
• dyspepsia (flatulence, vomiting);
• constipation;
• anorexia;
• taste change;
• candidiasis of the oral mucosa;
• heartbeat;
• chest pain;
• dizziness;
• headache;
• drowsiness;
• neurosis;
• sleep disturbance;
• vaginal candidiasis;
• rash;
• angioedema;
• skin itching;
• hives;
• conjunctivitis;
• increased fatigue;
• photosensitivity.

drug interaction

Antacids (aluminum and magnesium containing), ethanol (alcohol) and food slow down and reduce absorption. With the joint appointment of warfarin and azithromycin (in normal doses), no change in prothrombin time was detected, however, given that the interaction of macrolides and warfarin may increase the anticoagulant effect, patients need careful monitoring of prothrombin time.

Digoxin: increased concentration of digoxin.

Ergotamine and dihydroergotamine: increased toxic effect (vasospasm, dysesthesia).

Triazolam: decreased clearance and increased pharmacological action triazolam. Slows down the excretion and increases the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexo-barbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, theophylline and other xanthine derivatives) - due to the inhibition of microsomal oxidation in hepatocytes by azithromycin.

Lincosamines weaken the effectiveness, tetracycline and chloramphenicol - increase.

Analogues medicinal product Azithromycin

Structural analogues for the active substance:

• Azivok;
• Azimicin;
• Azitral;
• Azitrox;
• Azithromycin Forte;
• Azithromycin OBL;
• Azithromycin McLeods;
• Azithromycin dihydrate;
• AzitRus;
• AzitRus forte;
• Azicide;
• Vero Azithromycin;
• Zetamax retard;
• Zitnob;
• Zitrolide;
• Zitrolide forte;
• Zitrocin;
• Sumazid;
• Sumaclid;
• Sumamed;
• Sumamed forte;
• sumamecin;
• sumamecin forte;
• Sumamox;
• Sumatrolide solutab;
• Tremak Sanovel;
• Hemomycin;
• Ecomed.

Use in children

Contraindicated in children under 12 years of age.

Use during pregnancy and lactation

Azithromycin may be used during pregnancy when the benefits far outweigh the risks associated with the use of any drug during pregnancy.

If it is necessary to prescribe the drug during lactation, it is necessary to resolve the issue of stopping breastfeeding.

Description

Blue film-coated tablets, round, with a biconvex surface, scored.

Composition

One tablet contains: active substance: azithromycin - 500 mg; Excipients: calcium hydrophosphate dihydrate, hypromellose, corn starch, starch 1500, partially pregelatinized corn starch, sodium lauryl sulfate, magnesium stearate, microcrystalline cellulose, opadry II (including polyvinyl alcohol, talc, macrogol 3350, lecithin (soy), titanium dioxide E 171, iron oxide yellow E 172, aluminum varnish based on indigo carmine E 132).

Pharmacotherapeutic group

Antibacterial agents for systemic use. Macrolides.
ATX code– J01FA10.

Pharmacological properties"type="checkbox">

Pharmacological properties

Pharmacodynamics
Mechanism of action
Azithromycin is a broad-spectrum antibiotic, the first member of a new subgroup of macrolide antibiotics called azalides. The molecule is constructed by adding an oxygen atom to the lactone ring of erythromycin A. The chemical name of azithromycin is: 9-deoxy-9a-aza-9a-methyl-9a-homoerythromycin A. The molecular weight is 749.0.
The mechanism of action of azithromycin is binding to the 50 S unit of the ribosome, which prevents the synthesis of bactericidal proteins and translocation of peptides.
Mechanism of resistance
Resistance to azithromycin may be natural or acquired. The three main mechanisms of resistance in bacteria are: target-side alteration, alteration to antibiotic transport, and antibiotic modification.
Complete cross-resistance exists between the following microorganisms: Streptococcus pneumoniae, group A beta hemolytic streptococcus, Enterococcus faecalis and Staphylococcus aureus, including methicillin resistant S aureus (MRSA) to erythromycin, azithromycin, other macrolides and lincosamides.
Limit concentrations (Breakpoints)
Limit concentrations of sensitivity to azithromycin for typical pathogens are:
EUCAST (European Committee on Antimicrobial Susceptibility Testing) limit values ​​for minimum inhibitory concentrations (MICs):
Erythromycin can be used to determine the sensitivity of these bacteria to other macrolides (azithromycin, clarithromycin, and roxithromycin).
At intravenous administration macrolides have an effect on Legionella pneumophila < 1 мг/л для штаммов дикого типа).
Macrolides are used in the treatment of infections caused by Campylobacter jejuni(minimum inhibitory concentration of erythromycin< 1 мг/л для штаммов дикого типа). Азитромицин используется для лечения инфекций, вызванных S.typhy(minimum inhibitory concentration ≤ 16 mg/l for wild-type strains) and Shigella spp..
Sensitivity
The incidence of acquired resistance may differ both geographically and temporally for selected specimens, and local information on resistance would be highly desirable, especially in the treatment of severe infections. A specialist should be consulted when the incidence of acquired resistance is such that the very use of the drug in the last few types of infections becomes questionable.
Antimicrobial spectrum of azithromycin:
GENERALLY SENSITIVE MICROORGANISMS
- aerobic gram-positive microorganisms:
- Staphylococcus aureus(methicillin-sensitive);
-Streptococcus pneumoniae(penicillin-sensitive);
-Streptococcus pyogenes;
- aerobic Gram-negative microorganisms:
- haemuphilis influenzae;
- haemophilus parainfluenzae;
- Legionella pneumophila;
- Moraxella calarrhalls;
- Moraxella catarrhalis;
-Pasteurela multocida;
- anaerobic microorganisms:
- Clostridium perfrmgens;
- Fusobacterium spp.;
- Prevotella spp..;
-Porphyriomonas spp.;
- Other microorganisms:
- Chlamydia trachomatis;
MICROORGANISMS WITH ACQUIRED RESISTANCE
- Aerobic gram-positive microorganisms
- Streptococcus pneumoniae(penicillin intermediate resistant, penicillin resistant).
NATURALLY RESISTANT MICROORGANISMS
- Aerobic gram-positive microorganisms:
- Enterococcus faecalis;
- Staphylococcus MRS A, MRSE(Methicillin-resistant staphylococci have acquired resistance to macrolides and are listed here because they are rarely sensitive to azithromycin.)
- Anaerobic microorganisms:
- Bacteriodis fragilis group
Pharmacokinetics
Suction
After oral administration, azithromycin is well absorbed and rapidly distributed in the body. After a single dose of 500 mg, bioavailability is 37% due to the first pass effect through the liver. Cmax in blood plasma is reached after 2-3 hours and is 0.4 mg / l.
Distribution
Protein binding is inversely proportional to plasma concentration and is 7-50%. The apparent Vd is 31.1 l/kg. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily penetrates through histohematic barriers and enters the tissues. The concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection it is 24-34% higher than in healthy tissues.
Metabolism
Demethylated in the liver, losing activity.
breeding
T1 / 2 is long - 35-50 hours. T1 / 2 from tissues is much larger. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mainly unchanged - 50% through the intestines, 6% by the kidneys.

Indications for use

Upper respiratory infections (acute and chronic tonsillopharyngitis, acute and chronic recurrent sinusitis, acute otitis media).
Infections of the lower respiratory tract (acute bacterial bronchitis, exacerbation chronic bronchitis community-acquired bacterial pneumonia).
Skin and soft tissue infections: uncomplicated forms acne vulgaris, chronic erythema migrans ( initial stage Lyme disease), erysipelas, impetigo, pyoderma.
Sexually transmitted diseases (urethritis, cervicitis).
Diseases of the stomach and duodenum associated with Helicobacter pylori.

Contraindications

Hypersensitivity to macrolide antibiotics.
Because of the theoretical possibility of ergotism, azithromycin should not be co-administered with ergotamine derivatives.

Dosage and administration

Inside, once a day, 1 hour before a meal or 2 hours after it, with water.
For infections of the upper and lower respiratory tract, skin and soft tissues (with the exception of chronic erythema migrans): 500 mg once a day for 3 days; the total dose is 1500 mg.
For uncomplicated forms acne vulgaris: the course dose is 6 g. The first 3 days are prescribed 1 tablet 500 mg 1 time per day, in the next 9 weeks - 1 tablet 500 mg 1 time per week, and in the second week the tablet is taken 7 days after the previous dose . For chronic erythema migrans: 1 g (2 tablets of 500 mg at the same time) on the first day and 500 mg daily once a day from the second to the fifth day.
For sexually transmitted infections: uncomplicated urethritis / cervicitis - 1 g once.
Diseases of the stomach and duodenum associated with Helicobacter pylori: 1 g (2 tablets of 500 mg) daily, in combination with anti-secretory drugs and others medicines, as directed by a physician.
Azithromycin tablets 500 mg can be administered to children weighing more than 45 kg.
The score on the tablet is not intended to be divided into two equal doses.
Insufficiency of renal function
Patients with creatinine clearance >40 ml/min dose adjustment is not required. Studies of patients with creatinine clearance<40 мл/мин, не проводились. Таким пациентам нужно применять азитромицин с осторожно-стью.
Hepatic insufficiency
Use with caution in patients with severe hepatic impairment.

Side effect

Azithromycin rarely causes adverse reactions.
The table shows side effects by disease and frequency of manifestations. Side effects are classified by frequency as follows: very often (≥ 1/10); often (≥ 1/100 to<1/10); нечасто (≥ 1/1000 до <1/100); редко (≥ 1/10 000 до <1/1 000); очень редко (<1/10 000), неизвестно (невозможно оценить на основании имеющихся данных). Побочные действия в каждой группе в отношении частоты указываются по шкале от более частых к менее частым.

Interaction with other drugs

Food reduces the absorption of azithromycin.
Antacids: antacids slow down the absorption of azithromycin. The recommended interval between taking the drug and antacids is at least two hours.
cetirizine: simultaneous administration of azithromycin and cetirizine at a dose of 20 mg for 5 days to healthy volunteers did not lead to a change in pharmacokinetics or a significant change in the QT interval.
Didanosine: the simultaneous use of azithromycin at a daily dose of 1200 mg and didanosine in 6 subjects did not affect the pharmacokinetics of didanosine compared with placebo.
Digoxin: since there is evidence of a change in the metabolism of digoxin in patients who take macrolide antibiotics, caution is needed when they are taken simultaneously.
Zidovudine: Azithromycin at a single dose at a dose of 1000 mg and at multiple doses of 1200 mg did not affect the pharmacokinetics, as well as the release of zidovudine and its metabolites.
Ergotamine derivatives: due to the theoretical possibility of ergotism, azithromycin cannot be used together with ergotamine derivatives.
Atorvastatin: with the simultaneous use of atorvastatin (10 mg per day) and azithromycin (500 mg per day), azithromycin did not affect the concentration of atorvastatin in plasma.
Carbamazepine: in pharmacokinetic studies conducted on healthy volunteers, azithromycin had no significant effect on plasma levels of carbamazepine or its active metabolite.
Cimetidine: when taking cimetidine two hours before taking azithromycin, no changes in the pharmacokinetics of azithromycin were observed.
Coumarin oral anticoagulants: in a pharmacokinetic interaction study, azithromycin did not alter the effect of warfarin anticoagulants when taken at a dose of 15 mg in healthy volunteers. After the joint administration of azithromycin and coumarin anticoagulants, the anticoagulant effect increased. Although a causal relationship has not been established, the frequency of prothrombin time checks should be considered when azithromycin is taken by patients taking coumarin anticoagulants.
Cyclosporine: some macrolide antibiotics interfere with the metabolism of ciclosporin. While taking azithromycin and cyclosporine, it is necessary to control the concentration of cyclosporine.
Efavirenz: co-administration of a single dose of azithromycin 500 mg and efavirenz 400 mg daily for 7 days did not result in a clinically significant pharmacokinetic interaction.
Fluconazole: the simultaneous use of a single dose of 1200 mg of azithromycin does not change the pharmacokinetics of a single dose of 800 mg of fluconazole. The total concentration and half-life of azithromycin did not change with the simultaneous use of fluconazole. However, there was a clinically significant decrease in Cmax (18%) of azithromycin.
Indinavir: the simultaneous use of a single dose of 1200 mg of azithromycin does not significantly affect the pharmacokinetics of indinavir when taken at a dose of 800 mg three times a day for 5 days.
Methylprednisolone: in a pharmacokinetic study of drug interactions in healthy volunteers, azithromycin had no significant effect on the pharmacokinetics of methylprednisolone.
Midazolam: in healthy volunteers, simultaneous administration of azithromycin 500 mg daily for 3 days does not cause clinically significant changes in the pharmacokinetics and pharmacodynamics of midazolam when taken once 15 mg.
Nelfinavir: the simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg three times a day) leads to an increase in the concentration of azithromycin. No clinically significant side effects were identified. There is no need to adjust the dose.
Rifabutin: The simultaneous use of azithromycin and rifabutin did not affect the concentration of either of the two drugs in the blood serum. With the simultaneous use of azithromycin and rifabutin, neutropenia was observed in patients. Neutropenia is associated with the use of rifabutin, a causal relationship when taken in combination with azithromycin has not been established.
Sildenafil: there was no evidence of an effect of azithromycin (when taking 500 mg daily for 3 days) on the AUC and Cmax values ​​\u200b\u200bof sildenafil or its main metabolites in the blood.
Terfenadine: interaction of terfenadine and azithromycin was not revealed. In some cases, such an interaction cannot be completely excluded. Yet there is no evidence of such a reaction. As with other macrolides, azithromycin and terfenadine should be used with caution at the same time.
Theophylline: Azithromycin does not affect the pharmacokinetics of theophylline in healthy volunteers. The simultaneous use of theophylline and other macrolide antibiotics sometimes leads to an increase in the concentration of theophylline in the blood serum.
Triazolam: Co-administration of azithromycin 500 mg on Day 1 and 250 mg on Day 2 and triazolam 0.125 mg on Day 2 in 14 healthy volunteers had no significant effect on the pharmacokinetic parameters of triazolam compared with concomitant administration of triazolam and placebo .
Trimethoprim/sulfamethoxazole: Co-administration of trimethoprim/sulfamethoxazole DS (160 mg/800 mg) for 7 days and azithromycin 1200 mg on day 7 did not significantly affect peak concentrations, total exposure, or elimination of trimethoprim and sulfamethoxazole.

Precautionary measures

allergic reactions: In rare cases, severe allergic reactions, anaphylactic edema and anaphylaxis have been reported. Some of these reactions are accompanied by recurrent symptoms and require longer monitoring and treatment.
Hypersensitivity: as with erythromycin and other macrolides, there have been reports of rare serious allergic reactions, including angioedema and anaphylaxis (rarely fatal), skin reactions, including acute generalized exanthematous pustulosis (AGEP), Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reactions with rash, eosinophilia and systemic symptoms (DRESS syndrome). The use of azithromycin leads to a recurrence of the symptoms of some of the above reactions, which requires a longer period of observation and treatment.
If an allergic reaction develops, azithromycin should be discontinued immediately and appropriate treatment instituted. The doctor needs to know that it is possible to re-develop the symptoms of allergic reactions after the cessation of symptomatic treatment.
Hepatic impairment: Azithromycin should be used with caution in patients with severe liver disease. It is necessary to check the liver function if symptoms of dysfunction appear, such as the rapid development of asthenia associated with jaundice, dark urine, bleeding tendency or hepatic encephalopathy.
Ergotamine: in patients taking ergot alkaloid derivatives in parallel with some macrolides, there have been cases of ergot toxicity. It has not been proven that Azithromycin, when taken together with ergot alkaloid derivatives, causes ergotoxicity, however, these drugs should not be prescribed together.
Secondary infection: as with other antibiotics, monitoring for signs of secondary infections with non-susceptible organisms, including fungi, is recommended.
Clostridium Difficile-associated diarrhea: diarrhea associated with organisms Clostridium difficile, has been observed with almost all antibacterial drugs, including azithromycin. The severity can vary from mild diarrhea to acute colitis. Antibacterial therapy alters the normal intestinal microflora and leads to overgrowth of the body C. difficile.
Impaired kidney function: in patients with severe renal insufficiency (GFR<10 мл/мин) системное воздействие азитромицина увеличивается на 33 %.
Prolongation of repolarization and QT interval myocardial infarction, which carries the risk of developing cardiac arrhythmia and torsades de pointes, have been reported in the treatment of other macrolides. A similar effect cannot be completely excluded when using azithromycin in patients who are at increased risk of prolonged myocardial repolarization, so special care is needed when treating patients with:
hereditary or documented prolongation of the QT interval;
concomitant use of other drugs known to prolong the QT interval, such as class IA and III antiarrhythmics, tizapride and terfenadine;
electrolyte imbalance, especially in the case of the development of hypokalemia and hypomagnesemia;
clinically significant bradycardia, cardiac arrhythmias, or severe heart failure.
Exacerbation of symptoms of myasthenia gravis or new myasthenic syndrome has been reported in patients treated with azithromycin.
Streptococcal infections: penicillin is generally the drug of choice in the treatment of pharyngitis/tonsillitis caused by Streptococcus pyogenes, and as a prophylaxis of acute rheumatic fever. Azithromycin is generally effective in the treatment of acute pharyngitis, but there is no evidence of efficacy in the prevention of acute rheumatic fever.