Азитро®

General characteristics. Structure:

Active agent - dihydrate azithromycin (in terms of azithromycin) 250.0 mg.

Excipients: lactoses monohydrate, potato starch, polysorbate-80, calcium stearate.

Structure of a gelatin capsule: gelatin, titanium dioxide (Е 171), methylparahydroxybenzoate, пропилпарагидроксибензоат.

Pharmacological properties:

Pharmacokinetics. At intake azithromycin is quickly soaked up from digestive tract that is caused by its stability in acid medium and lipophilicity and distribution on all organism. Meal reduces azithromycin absorption. The maximum concentration in plasma is reached in 2-3 hours. Azithromycin well gets into respiratory tracts, bodies and fabrics of an urogenital path, a prostate, into skin and soft tissues. High concentration in fabrics (is 50 times higher, than concentration in plasma) and long half-life is caused by low linkng of azithromycin with proteins of a blood plasma, and also its ability to get into eukaryotic cells and to concentrate in the environment with a low rn, a surrounding lysosome. Ability of azithromycin to collect in lysosomes is especially important for elimination of intracellular activators. Phagocytes deliver azithromycin to places of localization of an infection where it is released in the course of phagocytosis. But despite high concentration in phagocytes, azithromycin does not exert impact on their function. Azithromycin remains in bactericidal concentration in the inflammation center within 5-7 days after reception of the last dose that allowed to develop short (3-day and 5-day) courses of treatment. Removal of azithromycin from a blood plasma happens in 2 stages: the elimination half-life (T1/2) makes 14-20 h in the range from 8 h to 24 h after administration of drug and 41 h – in the range from 24 h to 72 h that allows to use drug of 1 times/days. About 50% are removed in not changed look, other 50% - in the form of 10 inactive metabolites. Drug, generally with bile in not changed look is emitted, a small part (about 6%) is removed by kidneys.

Pharmacodynamics. Азитро® is an antibiotic of a broad spectrum of activity, the first representative of new subgroup of makrolidny antibiotics – azaleads. Possesses bacteriostatic action, but during creation in the center of an inflammation of high concentration causes bactericidal effect. Connecting 50S a ribosome subunit, азитро suppresses synthesis of protein in sensitive microorganisms.

It is active concerning aerobic gram-positive bacteria: Streptococcus pneumoniae, S. pyogenes, S. agalactiae, S. viridans, streptococci of the groups C, F and G, Staphylococcus aureus, S. еpidermidis. It is effective concerning aerobic gram-negative bacteria: Haemophilus influenzae, H. Рarainfluenzae and H. ducreyi, Moraxella catarrhalis, Bordetella pertussis, B. parapertussis, Neisseria gonorrhoeae and N. meningitidis, Helicobacter pylori, Legionella pneumophila, Campylobacter jejuni, Gardnerella vaginalis. It is active concerning some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp. Besides, C. pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum, Listeria monocytogenes, Treponema pallidum, Borrelia burgdorferi is effective concerning Chlamydia trachomatis. To drug gram-positive bacteria, resistant are steady against erythromycin.

Indications to use:

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

- quinsy, pharyngitis, sinusitis, tonsillitis, average otitis;

- chronic bronchitis in an aggravation stage, extra hospital or hospital pneumonia;

- the ugly face, impetigo for the second time infected a dermatosis;

- Lyme's disease (for treatment of an initial stage);

- the diseases of a stomach and a duodenum associated with Helicobacter pylori (as a part of a combination therapy);

- diseases, sexually transmitted (including the urethritis, tservitit, genital and extragenital clamidiosis).

Route of administration and doses:

Drug is used inside, for 1 h to food or in 2 h after food, 1 times a day.

Adult: quinsy, pharyngitis, sinusitis, tonsillitis, average otitis, chronic bronchitis in an aggravation stage, pneumonia, an ugly face, impetigo for the second time infected a dermatosis - appoint 500 mg in the 1st day, then on 250 mg with 2nd for the 5th days or on 500 mg/days within 3 days (a course dose - 1,5 g). 

The urethritis, cervicitis, clamidiosis - appoint once 1 g (4 capsules on 250 mg).

Lyme's disease for treatment of an initial stage (erythema migrans) - is appointed on 1 g (4 capsules on 250 mg) in the 1st day and on 500 mg daily from the 2nd to the 5th day (a course dose – 3 g).

Diseases of a stomach and duodenum, ассоциированнех with Helicobacter pylori - appoint 1 g (4 capsules on 250 mg) in days within 3 days as a part of a combination therapy.

Children are 12 years old and are more senior.

Appoint tablets of 500 mg to children of 12 years and more than 45 kg 1 times/days within 3 days or in the first day on 10 mg/kg of body weight, then on 5 - 10 mg/kg of body weight a day within 3 days are more senior with body weight. At body weight less than 45 kg it is necessary to take other dosage form.

At treatment of the first stage of a disease of Lyme: the dose makes 20 mg/kg of body weight in the first day and on 10 mg/kg of body weight from 2 to 5 day.

At the admission of reception of 1 dose it is necessary to accept the passed dose as soon as possible, and the subsequent with a break of 24 h.

Elderly persons have no need to change a dosage.

Features of use:

To be careful at purpose of drug the patient with insufficiency of function of a liver and kidneys, disturbance of a cordial rhythm (ventricular arrhythmias and lengthening of an interval of QT are possible).

It is necessary to observe a break of 2 h at simultaneous use of antacids.

After cancellation of treatment of reaction of hypersensitivity at some patients can remain that demands purpose of specific therapy under observation of the doctor.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms.

Considering side effects of medicine, it is necessary to be careful at control of motor transport and potentially dangerous mechanisms.

Side effects:

Often:

- nausea, vomiting, diarrhea, abdominal pain.

Seldom:

- tromotsitopeniya;

- aggression, excitement, concern, nervousness, sleeplessness;

- paresthesias, adynamy;

- reversible decrease in hearing and sonitus;

- arrhythmias, lengthening of an interval of QT;

- appetite loss, meteorism, lock, pseudomembranous colitis;

- tranzitorny rise in level of aminotransferases of a liver, bilirubin, cholestatic jaundice, hepatitis;

- hypersensitivity reactions (reddening, skin rash, itch, Quincke's disease, photosensitivity), multiformny erythema, Stephen-Johnson's syndrome and toxic epidermal necrolysis, acute anaphylaxis;

- intersticial nephrite, acute renal failure.

Very seldom:

- fatigue, headache, dizziness, convulsions;

- change of taste and sense of smell;

- arthralgias;

- vaginita, candidiasis, superinfections.

Interaction with other medicines:

Antacids (aluminum and magniysoderzhashchy), ethanol and food slow down and reduce absorption of Azitro®.

At joint purpose of warfarin and Azitro® (in usual doses) changes of a prothrombin time it is not revealed, however, considering that at interaction of macroleads and warfarin strengthening of anti-coagulative effect is possible, careful control of a prothrombin time is necessary for patients.

Digoxin: Азитро® increases concentration of digoxin.

Ergotamine and dihydroergotamine: strengthening of toxic action (vasospasm, dizesteziya).

To triazoles: Азитро® causes decrease in clearance and strengthening of pharmacological action of a triazolan.

Азитро® slows down removal and increases concentration in a blood plasma and toxicity of Cycloserinum, indirect anticoagulants, Methylprednisolonum, felodipin, and also the medicines which are exposed to a microsomal oxidation (carbamazepine, терфенадин, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, Disopyramidum, Bromocriptinum, Phenytoinum, peroral hypoglycemic means, theophylline, etc. ksantinovy derivatives) - at the expense of inhibition of a microsomal oxidation in hepatocytes. Linkozamina weaken efficiency of Azitro®, tetracycline and chloramphenicol - strengthen.

Contraindications:

- hypersensitivity to azithromycin and antibiotics of group of macroleads;

- heavy abnormal liver functions;

- heavy renal failures;

- children's and teenage age up to 12 years;

- pregnancy and period of a lactation.

Overdose:

Symptoms: temporary hearing loss, nausea, vomiting and diarrhea.

Treatment - symptomatic.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C.

To store in the unavailable place of children!

Issue conditions:

According to the recipe

Packaging:

On 6 capsules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

On 1 blister strip packaging together with the approved instruction on a medical use in the state and Russian languages place in a pack from a cardboard.