Composition, form of production and packaging
Capsules of white color в„–0; the contents of the capsules are white or white powder with a yellowish hue.
1 caps.
azithromycin (in the form of dihydrate) 250 mg
Excipients: mannitol (mannitol), corn starch, magnesium stearate, sodium lauryl sulfate.
Composition of the body and cap capsules: titanium dioxide (E171), gelatin medical.
6 pcs. - packings of cellular contour (1) - packs cardboard.
Capsules hard gelatinous, в„–00, with the case of white color and a lid of yellow color; the contents of the capsules are white or white powder with a yellowish hue.
1 caps.
azithromycin (in the form of dihydrate) 500 mg
Excipients: mannitol (mannitol), corn starch, magnesium stearate, sodium lauryl sulfate.
The composition of the capsule shell: titanium dioxide (E171), quinoline yellow (E104) dye, sunset yellow sunset (E110), gelatin medical.
3 pcs. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antibiotic of a wide spectrum of action, the representative of a subgroup of macrolide antibiotics - azalides. Linking to the 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, inhibits protein synthesis, slows the growth and multiplication of bacteria. It acts bacteriostatically, in high concentrations has a bactericidal effect. Effects on extracorporeal and intracellular pathogens.
It is active against gram-positive cocci : Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, 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, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Azithromycin is not active against Gram-positive bacteria, resistant to erythromycin.
PHARMACOKINETICS
Suction
After taking the drug inside, azithromycin is rapidly absorbed from the digestive tract, which is due to its stability in acidic medium and lipophilicity. After oral administration, 500 mg of azithromycin C max in plasma is achieved after 2.5-3 h and is 0.4 mg / l. Bioavailability is 37%.
Taking the drug simultaneously with food slows down and reduces the absorption of azithromycin.
Distribution
Azithromycin well penetrates the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), into the skin and soft tissues. High concentrations in tissues (10-50 times higher than in plasma) and long T 1/2 are due to low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a medium with a low pH surrounding the lysosome . This, in turn, determines a large apparent V d (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is especially important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the site of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (an average of 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function.
Azithromycin is retained in bactericidal concentrations in the inflammatory focus within 5-7 days after administration of the last dose, which allowed the development of short (3-day and 5-day) treatment courses.
Metabolism
In the liver, azithromycin is demethylated, the metabolites formed are inactive.
Excretion
Excretion of azithromycin from the blood plasma takes place in 2 stages: T 1/2 is 14-20 hours in the interval from 8 to 24 hours after taking the drug and 41 hours in the interval from 24 to 72 hours, which allows using the drug once a day.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract and ENT organs (including angina, sinusitis, tonsillitis, otitis media);
scarlet fever;
- infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
- skin and soft tissue infections (including erysipelas, impetigo, secondarily infected dermatoses);
- infections of the urogenital tract (including urethritis and / or cervicitis);
- Lyme disease (borreliosis) in the initial stage (erythema migrans);
- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in combination therapy).
DOSING MODE
Azithrox В® is taken orally 1 time / day for 1 hour before or 2 hours after a meal.
Adults with infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days (exchange dose - 1.5 g).
When skin and soft tissue infections are prescribed at a dose of 1 g / day for 1 reception on the first day, then - 500 mg / day daily from 2 to 5 days. The course dose is 3 g.
With uncomplicated urethritis and / or cervicitis, appoint only 1 g.
With complicated, long-term urethritis / cervicitis caused by Chlamydia trachomatis, 1 g 3 times at intervals of 7 days (taking the drug at 1-7-14 days of treatment). The course dose is 3 g.
In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on day 1 and 500 mg daily from day 2 to day 5. The course dose is 3 g.
With gastric ulcer and duodenal ulcer associated with Helicobacter pylori , appoint 1 g / day for 3 days as a combination of anti-Helicobacter therapy.
Children with a body weight of more than 45 kg with infections of the upper and lower respiratory tract, skin and soft tissues, scarlet fever, the drug is prescribed at 500 mg / day (1 caps.) For 1 reception for 3 days.
Children over 12 years of age (250 mg capsule) are prescribed at the rate of 10 mg / kg 1 time / day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day within 3 days. The course dose is 30 mg / kg.
In the treatment of erythema migrans in children, the dose of the drug (capsule 500 mg) is 1 g in day 1 and 500 mg daily from day 2 to day 5. The course dose is 3 g. Use Azitrox В® in the form of 250 mg capsules should be given at a dose of 20 mg / kg on the first day and 10 mg / kg on the 2nd to the 5th day.
SIDE EFFECT
On the part of the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases; in children - constipation, anorexia, gastritis. Possible kandidomikoz mucous membrane of the mouth.
From the cardiovascular system: a feeling of heartbeat, pain in the chest (? 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disturbances (? 1%).
On the part of the reproductive system :? 1% - vaginal candidiasis.
From the urinary system :? 1% - nephritis.
Dermatological reactions: in some cases - a rash, photosensitivity.
Allergic reactions: rash, itching, Quincke's edema, hives, conjunctivitis.
Other: increased fatigue.
CONTRAINDICATIONS
- liver failure;
- kidney failure;
- Children weighing less than 45 kg (for capsules 500 mg);
- children's age till 12 years;
- hypersensitivity to antibiotics of macrolides.
Caution should be used during arrhythmia (possible ventricular arrhythmias, prolongation of the QT interval), in children with severe impairment of liver or kidney function.
PREGNANCY AND LACTATION
The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.
If you need to use the drug during lactation, you should decide whether to stop breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated in severe violations of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in severe violations of liver function.
APPLICATION FOR CHILDREN
Contraindicated: children under 12 years.
SPECIAL INSTRUCTIONS
Azithrox В® should not be taken with food.
In case of missing the next dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at an interval of 24 hours.
It is necessary to observe a break of at least 2 h between taking Azitrox and antacid preparations.
After the withdrawal of treatment, hypersensitivity reactions in some patients may persist, which requires specific therapy under the supervision of a physician.
OVERDOSE
Symptoms: when using the drug in high doses, it is possible to increase the side effect - severe nausea, temporary hearing loss, vomiting, diarrhea.
Treatment: gastric lavage, the appointment of activated charcoal, the conduct of symptomatic therapy.
DRUG INTERACTION
Antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin.
Azithromycin does not bind to the isoenzymes of the cytochrome P450 system. Unlike most macrolides, at present no interaction of azithromycin with theophylline, terfenadine, carbamazepine, triazolam, digoxin has been observed.
Macrolides (with the exception of azalides) slow down excretion and increase the plasma concentration and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and also drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline), by inhibiting microsomal oxidation in hepatocytes, while when applied azalides such interaction to date have been noted.
With the simultaneous use of azithromycin with digoxin, an increase in the concentration of the latter is observed.
With the simultaneous administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, but considering that the interaction of macrolides and warfarin may enhance the anticoagulant effect, patients need careful monitoring of prothrombin time.
With the simultaneous use of azithromycin with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) is enhanced.
With the simultaneous use of azithromycin with triazolam, clearance decreases and the pharmacological action of triazolam is enhanced.
Lincosamines reduce the effectiveness of azithromycin.
Tetracycline and chloramphenicol increase the effectiveness of azithromycin.
Pharmaceutical incompatibility
Azithromycin is pharmaceutically incompatible with heparin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of 15 В° to 25 В° C. Shelf life - 2 years.
