Composition, structure and packing
Capsules are white capsules contents - powder white or white with a yellowish tint.
A capsule. azithromycin (in the form of dihydrate) 250 mg.
Excipients: mannitol (mannitol), corn starch, magnesium stearate, sodium lauryl sulfate.
The composition of the shell and operculum capsules: titanium dioxide (E171), gelatin medicine.
Hard gelatin capsules, with the body white and yellow cap, the contents of capsules - powder white or white with a yellowish tint.
A capsule. azithromycin (in the form of dihydrate) 500 mg.
Excipients: mannitol (mannitol), corn starch, magnesium stearate and sodium lauryl sulphate.
The composition of the capsule shell: titanium dioxide (E171), quinoline yellow (E104), sunset yellow dye (E110), gelatin medicine.
Clinico-pharmacological group: Antibiotic macrolide - azalid.
Pharmacological action
Broad-spectrum antibiotic, a representative subgroup of macrolide antibiotics - azalidov. Communicating with the 50S subunit of ribosomes, inhibits peptidtranslokazu at the stage of translation, inhibits protein synthesis and slows the growth and multiplication of bacteria. Valid bacteriostatic, in high concentrations has a bactericidal effect. Operates on extra-and intracellular pathogens.
It is active against Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Staphylococcus aureus, Streptococcus viridans; 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, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Azithromycin is not active against gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
Absorption
After taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After oral administration of 500 mg of azithromycin Cmax in plasma is achieved through 2.5-3 h and is 0.4 mg / liter.
Bioavailability - 37%. Acceptance of the drug along with diet slows down and reduces the absorption of azithromycin.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (in particular, 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. This, in turn, defines a large apparent Vd (31.1 L / kg) and high 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 the degree 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
In the liver azithromycin demethylates formed metabolites are inactive.
Withdrawal
Withdrawal of azithromycin from plasma takes place in 2 stages: T1 / 2 is 14-20 hours in the range of 8 to 24 hours after taking the drug and 41 hours - in the range of 24 to 72 hours to allow the 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 (including tonsillitis, sinusitis, tonsillitis, otitis media);
scarlet fever;
Infection of lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
urogenital tract infections (including urethritis and / or cervicitis);
Lyme disease (Lyme disease) in the early stages (erythema migrans);
gastric and duodenal ulcers, associated to Helicobacter pylori (in the combined therapy).
Dosage regimen
Azitroks ingest 1 time / day for 1 hour before or 2 hours after meals.
Adults with infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days (course dose - 1.5 g).
With infections of the skin and soft tissue administered in a dose of 1 g / day for 1 admission on the first day, then - 500 mg / day every day from 2 to 5 days. Heading dose - 3 PM
In uncomplicated urethritis and / or cervicitis designate single 1 in a complicated, protracted urethritis / cervicitis caused by Chlamydia trachomatis, and 1 g 3 times with an interval of 7 days (taking the drug in the treatment of the day 07/01/1914). Heading dose of 3 g.
When Lyme disease (borrelia) for the treatment of stage I (erythema migrans) appoint 1 g in 1-day and 500 mg daily from 2 to 5 th day. Heading dose - 3 PM
For gastric ulcers and duodenal ulcers associated with Helicobacter pylori, appoint 1 g / day for 3 days in a combination therapy of H. pylori.
For children weighing over 45 kg with infections of the upper and lower respiratory tract, skin and soft tissue, scarlet fever medication prescribed at 500 mg (1 capsule). 1 reception for 3 days.
Children over 12 years of drug (kaps. 250 mg) designate a rate of 10 mg / kg 1 time / day for 3 days or the first day - 10 mg / kg followed by 4 days - on 5-10 mg / kg / day 3 days. Heading dose - 30 mg / kg.
In the treatment of erythema migrans in children dose of the drug (Table 500 mg) is 1 g at 1 day and 500 mg daily from 2 to 5 th day. Heading dose - 3 years Apply Azitroks in the form of tablets of 250 mg should dose - 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: diarrhea (5%), nausea (3%), abdominal pain (3%), 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increase in liver transaminases; children - constipation , anorexia, gastritis. Chance kandidomikoz oral mucosa.
Since the cardiovascular system: a feeling of palpitations, chest pain (≤ 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headaches (for the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disturbances (≤ 1%).
On the part of the reproductive system: ≤ 1% - vaginal candidiasis.
From the urinary system: ≤ 1% - jade. Dermatological reactions: in some cases, rash, photosensitivity.
Allergic reactions: rash, itching, Quincke's edema, urticaria, conjunctivitis.
Other: fatigue.
Contraindications
hepatic impairment;
renal failure;
children weighing less than 45 kg (for capsules 500 mg);
Children under 12 years
Hypersensitivity to macrolide antibiotics.
With care use in patients with arrhythmias (ventricular arrhythmias may be, the elongation range QT), in children with severe disorders of the liver or kidneys.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. When necessary use during lactation should resolve the issue of termination of breastfeeding.
Application for violations of liver function
The drug is contraindicated in severe liver problems.
Application for violations of renal function
The drug is contraindicated in severe renal dysfunction.
Cautions
Azitroks should not be taken with food. In the case of missing next meal missed dose should be taken as quickly as possible, and follow - with an interval of 24 h.
Must comply with a break of at least 2 hours between doses Azitroksa and antacid drugs. After discontinuation of treatment hypersensitivity reactions in some patients may persist, which requires specific therapy under medical supervision.
Overdose
Symptoms: when using the drug in high doses may be increased side effects - severe nausea, temporary hearing loss, vomiting, diarrhea. Treatment: gastric lavage, the appointment of activated carbon, conducting symptomatic therapy.
Drug Interactions
Antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin. With simultaneous use of azithromycin with digoxin observed an increased concentration of the latter. In case of simultaneous appointment of warfarin and azithromycin (at normal doses) changes prothrombin time is not revealed, but given that the interaction of macrolides and warfarin may be increased anticoagulation effect, patients need careful monitoring prothrombin time. With the simultaneous use of azithromycin with ergotamine and dihydroergotamine increasing their toxicity (vasospasm, dysesthesia).
With simultaneous use of azithromycin with triazolamom decreases clearance and increases the pharmacological effect triazolama.
Azithromycin inhibits microsomal oxidation in hepatocytes and therefore slows the excretion and increases plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina, as well as preparations exposed to microsomal oxidation (carbamazepine, terfenadin, cyclosporine, geksobarbital, ergot alkaloids, valproic acid, dizopiramid, bromocriptine, phenytoin, oral hypoglycemic funds, xanthine derivatives, including theophylline). Linkozaminy reduce the effectiveness of azithromycin. Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.
Pharmaceutical incompatibilities
Azithromycin pharmaceutically incompatible with heparin.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C. Shelf life - 2 years.
Capsules are white capsules contents - powder white or white with a yellowish tint.
A capsule. azithromycin (in the form of dihydrate) 250 mg.
Excipients: mannitol (mannitol), corn starch, magnesium stearate, sodium lauryl sulfate.
The composition of the shell and operculum capsules: titanium dioxide (E171), gelatin medicine.
Hard gelatin capsules, with the body white and yellow cap, the contents of capsules - powder white or white with a yellowish tint.
A capsule. azithromycin (in the form of dihydrate) 500 mg.
Excipients: mannitol (mannitol), corn starch, magnesium stearate and sodium lauryl sulphate.
The composition of the capsule shell: titanium dioxide (E171), quinoline yellow (E104), sunset yellow dye (E110), gelatin medicine.
Clinico-pharmacological group: Antibiotic macrolide - azalid.
Pharmacological action
Broad-spectrum antibiotic, a representative subgroup of macrolide antibiotics - azalidov. Communicating with the 50S subunit of ribosomes, inhibits peptidtranslokazu at the stage of translation, inhibits protein synthesis and slows the growth and multiplication of bacteria. Valid bacteriostatic, in high concentrations has a bactericidal effect. Operates on extra-and intracellular pathogens.
It is active against Gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, streptococci of groups C, F and G, Staphylococcus aureus, Streptococcus viridans; 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, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Azithromycin is not active against gram-positive bacteria resistant to erythromycin.
Pharmacokinetics
Absorption
After taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After oral administration of 500 mg of azithromycin Cmax in plasma is achieved through 2.5-3 h and is 0.4 mg / liter.
Bioavailability - 37%. Acceptance of the drug along with diet slows down and reduces the absorption of azithromycin.
Distribution
Azithromycin well into the respiratory tract, organs and tissues of the urogenital tract (in particular, 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. This, in turn, defines a large apparent Vd (31.1 L / kg) and high 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 the degree 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
In the liver azithromycin demethylates formed metabolites are inactive.
Withdrawal
Withdrawal of azithromycin from plasma takes place in 2 stages: T1 / 2 is 14-20 hours in the range of 8 to 24 hours after taking the drug and 41 hours - in the range of 24 to 72 hours to allow the 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 (including tonsillitis, sinusitis, tonsillitis, otitis media);
scarlet fever;
Infection of lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
urogenital tract infections (including urethritis and / or cervicitis);
Lyme disease (Lyme disease) in the early stages (erythema migrans);
gastric and duodenal ulcers, associated to Helicobacter pylori (in the combined therapy).
Dosage regimen
Azitroks ingest 1 time / day for 1 hour before or 2 hours after meals.
Adults with infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days (course dose - 1.5 g).
With infections of the skin and soft tissue administered in a dose of 1 g / day for 1 admission on the first day, then - 500 mg / day every day from 2 to 5 days. Heading dose - 3 PM
In uncomplicated urethritis and / or cervicitis designate single 1 in a complicated, protracted urethritis / cervicitis caused by Chlamydia trachomatis, and 1 g 3 times with an interval of 7 days (taking the drug in the treatment of the day 07/01/1914). Heading dose of 3 g.
When Lyme disease (borrelia) for the treatment of stage I (erythema migrans) appoint 1 g in 1-day and 500 mg daily from 2 to 5 th day. Heading dose - 3 PM
For gastric ulcers and duodenal ulcers associated with Helicobacter pylori, appoint 1 g / day for 3 days in a combination therapy of H. pylori.
For children weighing over 45 kg with infections of the upper and lower respiratory tract, skin and soft tissue, scarlet fever medication prescribed at 500 mg (1 capsule). 1 reception for 3 days.
Children over 12 years of drug (kaps. 250 mg) designate a rate of 10 mg / kg 1 time / day for 3 days or the first day - 10 mg / kg followed by 4 days - on 5-10 mg / kg / day 3 days. Heading dose - 30 mg / kg.
In the treatment of erythema migrans in children dose of the drug (Table 500 mg) is 1 g at 1 day and 500 mg daily from 2 to 5 th day. Heading dose - 3 years Apply Azitroks in the form of tablets of 250 mg should dose - 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: diarrhea (5%), nausea (3%), abdominal pain (3%), 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increase in liver transaminases; children - constipation , anorexia, gastritis. Chance kandidomikoz oral mucosa.
Since the cardiovascular system: a feeling of palpitations, chest pain (≤ 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headaches (for the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disturbances (≤ 1%).
On the part of the reproductive system: ≤ 1% - vaginal candidiasis.
From the urinary system: ≤ 1% - jade. Dermatological reactions: in some cases, rash, photosensitivity.
Allergic reactions: rash, itching, Quincke's edema, urticaria, conjunctivitis.
Other: fatigue.
Contraindications
hepatic impairment;
renal failure;
children weighing less than 45 kg (for capsules 500 mg);
Children under 12 years
Hypersensitivity to macrolide antibiotics.
With care use in patients with arrhythmias (ventricular arrhythmias may be, the elongation range QT), in children with severe disorders of the liver or kidneys.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. When necessary use during lactation should resolve the issue of termination of breastfeeding.
Application for violations of liver function
The drug is contraindicated in severe liver problems.
Application for violations of renal function
The drug is contraindicated in severe renal dysfunction.
Cautions
Azitroks should not be taken with food. In the case of missing next meal missed dose should be taken as quickly as possible, and follow - with an interval of 24 h.
Must comply with a break of at least 2 hours between doses Azitroksa and antacid drugs. After discontinuation of treatment hypersensitivity reactions in some patients may persist, which requires specific therapy under medical supervision.
Overdose
Symptoms: when using the drug in high doses may be increased side effects - severe nausea, temporary hearing loss, vomiting, diarrhea. Treatment: gastric lavage, the appointment of activated carbon, conducting symptomatic therapy.
Drug Interactions
Antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin. With simultaneous use of azithromycin with digoxin observed an increased concentration of the latter. In case of simultaneous appointment of warfarin and azithromycin (at normal doses) changes prothrombin time is not revealed, but given that the interaction of macrolides and warfarin may be increased anticoagulation effect, patients need careful monitoring prothrombin time. With the simultaneous use of azithromycin with ergotamine and dihydroergotamine increasing their toxicity (vasospasm, dysesthesia).
With simultaneous use of azithromycin with triazolamom decreases clearance and increases the pharmacological effect triazolama.
Azithromycin inhibits microsomal oxidation in hepatocytes and therefore slows the excretion and increases plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina, as well as preparations exposed to microsomal oxidation (carbamazepine, terfenadin, cyclosporine, geksobarbital, ergot alkaloids, valproic acid, dizopiramid, bromocriptine, phenytoin, oral hypoglycemic funds, xanthine derivatives, including theophylline). Linkozaminy reduce the effectiveness of azithromycin. Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.
Pharmaceutical incompatibilities
Azithromycin pharmaceutically incompatible with heparin.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C. Shelf life - 2 years.
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