Composition, structure and packing
Hard gelatin capsules, with the body and lid in white; content caps - white powder.
A capsule. azithromycin dihydrate (in terms of azithromycin) 250 mg.
Excipients: anhydrous lactose, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
Hard gelatin capsules, with the body and lid in white; content caps - white powder.
A capsule. azithromycin dihydrate (in terms of azithromycin) 500 mg.
Excipients: anhydrous lactose, corn starch, sodium lauryl sulphate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
Clinico-pharmacological group: Antibiotic macrolide - azalid.
Pharmacological action
Broad-spectrum antibiotic from the macrolide, a derivative azalida. When you create inflammation in high concentrations has a bactericidal effect.
It is active against Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Staphylococcus viridans, Staphylococcus aureus; Gram-bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Helicobacter pylori, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.; also active against other microorganisms: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Azithromycin is inactive against Gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
Absorption
Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After receiving Azitrala oral dose of 500 mg Cmax of azithromycin in plasma achieved after 2.5-2.96 h and is 0.4 mg / liter. Bioavailability is 37%.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (particularly in the prostate gland), in skin and soft tissue. The high concentration in tissues (10-50 times higher than in blood plasma) and a long T1 / 2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in an environment with low pH, environmental lysosomes. That, in turn, determines a large Vd = 31.1 L / kg and higher Plasma clearance.
The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens. Shown that phagocytes deliver azithromycin to the localization of infection sites, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissues (on average 24-34%) and correlated with severity of inflammatory edema. Despite the high concentration in phagocytes, azithromycin did not significantly affect their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after receiving the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
Metabolism
The liver demethylates with the formation of inactive metabolites.
Withdrawal
Derivation of azithromycin from plasma occurs in 2 stages: T1 / 2 is 14-20 h in the range from 8 hours to 24 hours after drug administration and 41 h - in the range from 24 h to 72 h, which allows you to use a drug once a day .
Statement
Infectious and inflammatory diseases caused by organisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);
Infection of lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
scarlet fever;
infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis);
urogenital tract infection (gonorrheal urethritis and / or cervicitis);
Lyme disease (borreliosis) - for treatment of early stage (erythema migrans);
gastric and duodenal ulcers associated with Helicobacter pylori (in a combination therapy).
Dosage regimen
Drugs are taken 1 time / day for 1 hour before meals or 2 hours after meals.
With infections of the upper and lower respiratory tract adult appoint 500 mg / day in 1 reception for 3 days; course dose of 1.5 PM
When infections of skin and soft tissues of adult appoint 1 g in 1 day to 1 admission; further - 500 mg in 1 receive daily from 2 to 5 th day; course dose is 3 g.
In uncomplicated urethritis and / or cervicitis designate single 1 g in 1 reception.
When Lyme disease (borrelia) for the treatment of early stages (erythema migrans) appoint 1 g in 1-day and 500 mg in 1 reception daily from 2 to 5 th day (course dose - 3 g).
In gastric ulcer and duodenal ulcer associated with Helicobacter pylori, a drug prescribed to 1 g / day for 3 days in a combination therapy of H. pylori.
Children of drug prescribed rate of 10 mg / kg 1 time / day for 3 days or 1 day - 10 mg / kg followed in 3 days - at 5-10 mg / kg / day (course dose is determined rate of 30 mg / kg).
In the treatment of erythema migrans dose is 20 mg / kg in 1-day and 10 mg / kg from 2 to 5 th day.
Side effect
On the part of the digestive system: nausea (3%), diarrhea (5%), abdominal pain (3%), indigestion, vomiting, flatulence, melena, cholestatic jaundice, increase in liver transaminases (1% or less). The children - constipation, anorexia, gastritis.
Since the cardiovascular system: heart, chest pain (1% or less).
From the side of the central nervous system: headache, dizziness, drowsiness; in children - a headache (for the treatment of otitis media), hyperkinesia, Anxiety, neurosis, sleep disorder (1% or less).
On the part of the urogenital system: jade, vaginal candidiasis (1% or less).
Allergic reactions: rash, photosensitivity, edema Quincke.
Other: fatigue, kandidomikoz oral cavity in children - conjunctivitis, pruritus, urticaria.
Contraindications
renal failure;
hepatic impairment;
Lactation (breastfeeding);
Children age 12 months;
Hypersensitivity to azithromycin and other macrolide antibiotics.
With caution is prescribed for arrhythmias (ventricular fibrillation and possible prolongation of the interval QT), pregnancy, and in children with severe disorders of the liver or kidneys.
Pregnancy and lactation
During pregnancy Azitral can be applied, when the intended use of such therapy substantially outweigh the risks existing in the application of drugs during pregnancy. In the appointment during lactation breastfeeding should be suspended at the time of treatment.
Application for violations of liver function
The drug is contraindicated in hepatic failure.
Application for violations of renal function
The drug is contraindicated in renal impairment.
Cautions
In the case of missed the missed dose should be taken as early as possible, and follow - with an interval of 24 h. Note that after the withdrawal of the drug allergic reactions in some patients may persist, requiring appropriate treatment and medical supervision. Among the methods Azitrala and antacid drugs should be observed by a break of at least 2 hours
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: the holding of symptomatic therapy.
Drug Interactions
Antacids (aluminum and magnesium), ethanol, food slow and reduce the absorption of azithromycin.
When combined warfarin and Azitrala changes in recommended doses prothrombin time is not revealed, however, given that the interaction of macrolides and warfarin may be increased anticoagulant effect requires monitoring prothrombin time.
When the joint application of azithromycin increases the concentration of digoxin.
With simultaneous application of azithromycin increases the toxic effect of ergotamine and dihydroergotamine (vasospasm and dysesthesia).
When the joint application of azithromycin slows excretion and enhances the pharmacological effects triazolama.
With the combined application of azithromycin slows excretion, increases the concentration in blood plasma and increases the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina. Azithromycin, inhibition of microsomal oxidation in rat hepatocytes, slow elimination, increases the concentration in the serum and enhances the toxicity of carbamazepine, terfenadina, cyclosporine, geksobarbitala, ergot alkaloids, valproic acid, phenytoin, dizopiramid, bromocriptine, theophylline (and other xanthine derivatives), oral hypoglycemic tools .
When the joint application linkozaminy weaken the effectiveness of azithromycin and tetracycline and chloramphenicol increase.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry place at temperatures not above 25 ° C.
Shelf life - 3 years.
Hard gelatin capsules, with the body and lid in white; content caps - white powder.
A capsule. azithromycin dihydrate (in terms of azithromycin) 250 mg.
Excipients: anhydrous lactose, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
Hard gelatin capsules, with the body and lid in white; content caps - white powder.
A capsule. azithromycin dihydrate (in terms of azithromycin) 500 mg.
Excipients: anhydrous lactose, corn starch, sodium lauryl sulphate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
Clinico-pharmacological group: Antibiotic macrolide - azalid.
Pharmacological action
Broad-spectrum antibiotic from the macrolide, a derivative azalida. When you create inflammation in high concentrations has a bactericidal effect.
It is active against Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Staphylococcus viridans, Staphylococcus aureus; Gram-bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Helicobacter pylori, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.; also active against other microorganisms: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Azithromycin is inactive against Gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
Absorption
Azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After receiving Azitrala oral dose of 500 mg Cmax of azithromycin in plasma achieved after 2.5-2.96 h and is 0.4 mg / liter. Bioavailability is 37%.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (particularly in the prostate gland), in skin and soft tissue. The high concentration in tissues (10-50 times higher than in blood plasma) and a long T1 / 2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in an environment with low pH, environmental lysosomes. That, in turn, determines a large Vd = 31.1 L / kg and higher Plasma clearance.
The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens. Shown that phagocytes deliver azithromycin to the localization of infection sites, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissues (on average 24-34%) and correlated with severity of inflammatory edema. Despite the high concentration in phagocytes, azithromycin did not significantly affect their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after receiving the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.
Metabolism
The liver demethylates with the formation of inactive metabolites.
Withdrawal
Derivation of azithromycin from plasma occurs in 2 stages: T1 / 2 is 14-20 h in the range from 8 hours to 24 hours after drug administration and 41 h - in the range from 24 h to 72 h, which allows you to use a drug once a day .
Statement
Infectious and inflammatory diseases caused by organisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);
Infection of lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
scarlet fever;
infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatitis);
urogenital tract infection (gonorrheal urethritis and / or cervicitis);
Lyme disease (borreliosis) - for treatment of early stage (erythema migrans);
gastric and duodenal ulcers associated with Helicobacter pylori (in a combination therapy).
Dosage regimen
Drugs are taken 1 time / day for 1 hour before meals or 2 hours after meals.
With infections of the upper and lower respiratory tract adult appoint 500 mg / day in 1 reception for 3 days; course dose of 1.5 PM
When infections of skin and soft tissues of adult appoint 1 g in 1 day to 1 admission; further - 500 mg in 1 receive daily from 2 to 5 th day; course dose is 3 g.
In uncomplicated urethritis and / or cervicitis designate single 1 g in 1 reception.
When Lyme disease (borrelia) for the treatment of early stages (erythema migrans) appoint 1 g in 1-day and 500 mg in 1 reception daily from 2 to 5 th day (course dose - 3 g).
In gastric ulcer and duodenal ulcer associated with Helicobacter pylori, a drug prescribed to 1 g / day for 3 days in a combination therapy of H. pylori.
Children of drug prescribed rate of 10 mg / kg 1 time / day for 3 days or 1 day - 10 mg / kg followed in 3 days - at 5-10 mg / kg / day (course dose is determined rate of 30 mg / kg).
In the treatment of erythema migrans dose is 20 mg / kg in 1-day and 10 mg / kg from 2 to 5 th day.
Side effect
On the part of the digestive system: nausea (3%), diarrhea (5%), abdominal pain (3%), indigestion, vomiting, flatulence, melena, cholestatic jaundice, increase in liver transaminases (1% or less). The children - constipation, anorexia, gastritis.
Since the cardiovascular system: heart, chest pain (1% or less).
From the side of the central nervous system: headache, dizziness, drowsiness; in children - a headache (for the treatment of otitis media), hyperkinesia, Anxiety, neurosis, sleep disorder (1% or less).
On the part of the urogenital system: jade, vaginal candidiasis (1% or less).
Allergic reactions: rash, photosensitivity, edema Quincke.
Other: fatigue, kandidomikoz oral cavity in children - conjunctivitis, pruritus, urticaria.
Contraindications
renal failure;
hepatic impairment;
Lactation (breastfeeding);
Children age 12 months;
Hypersensitivity to azithromycin and other macrolide antibiotics.
With caution is prescribed for arrhythmias (ventricular fibrillation and possible prolongation of the interval QT), pregnancy, and in children with severe disorders of the liver or kidneys.
Pregnancy and lactation
During pregnancy Azitral can be applied, when the intended use of such therapy substantially outweigh the risks existing in the application of drugs during pregnancy. In the appointment during lactation breastfeeding should be suspended at the time of treatment.
Application for violations of liver function
The drug is contraindicated in hepatic failure.
Application for violations of renal function
The drug is contraindicated in renal impairment.
Cautions
In the case of missed the missed dose should be taken as early as possible, and follow - with an interval of 24 h. Note that after the withdrawal of the drug allergic reactions in some patients may persist, requiring appropriate treatment and medical supervision. Among the methods Azitrala and antacid drugs should be observed by a break of at least 2 hours
Overdose
Symptoms: severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: the holding of symptomatic therapy.
Drug Interactions
Antacids (aluminum and magnesium), ethanol, food slow and reduce the absorption of azithromycin.
When combined warfarin and Azitrala changes in recommended doses prothrombin time is not revealed, however, given that the interaction of macrolides and warfarin may be increased anticoagulant effect requires monitoring prothrombin time.
When the joint application of azithromycin increases the concentration of digoxin.
With simultaneous application of azithromycin increases the toxic effect of ergotamine and dihydroergotamine (vasospasm and dysesthesia).
When the joint application of azithromycin slows excretion and enhances the pharmacological effects triazolama.
With the combined application of azithromycin slows excretion, increases the concentration in blood plasma and increases the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina. Azithromycin, inhibition of microsomal oxidation in rat hepatocytes, slow elimination, increases the concentration in the serum and enhances the toxicity of carbamazepine, terfenadina, cyclosporine, geksobarbitala, ergot alkaloids, valproic acid, phenytoin, dizopiramid, bromocriptine, theophylline (and other xanthine derivatives), oral hypoglycemic tools .
When the joint application linkozaminy weaken the effectiveness of azithromycin and tetracycline and chloramphenicol increase.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry place at temperatures not above 25 ° C.
Shelf life - 3 years.
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