Azitromitsin-BHFZ

General characteristics. Structure:

Active ingredient: azithromycin; 1 capsule contains azithromycin in the form of dihydrate azithromycin (in terms of 100% anhydrous substance) – 250 mg; excipients: cellulose microcrystallic, magnesium stearate, sodium laurilsulfat.osnovny physical and chemical properties: solid capsules with the case white and a lid of yellow color. Contents of capsules – powder, granules or a column of white or almost white color.

Pharmacological properties:

Pharmacodynamics. Azithromycin is the representative of new subgroup of makrolidny antibiotics – azaleads. Possesses a wide range of antimicrobic action. The mechanism of action is caused by inhibition of biosynthesis of protein owing to linkng of azithromycin with 50S-subunit of a ribosome and oppression of a peptidiltranslokaza.

Azithromycin is active concerning gram-positive aerobic bacteria: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalacticae, Streptococcus viridans, streptococci of the groups C, F and G, Staphylococcus aureus, Staphylococcus epidermidis; some gram-positive anaerobic bacteria: Clostridium perfringens; gram-negative aerobic bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus ducreyi, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Neisseria gonorrhoeae, Neisseria meningitidis, Helicobacter pylori, Gardnerella vaginalis, Campylobacter jejuni.

Azithromycin is also active concerning intracellular and other microorganisms: Mycobacterium avium complex, Legionella pneumophila, Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum, Listeria monocitogenes, Borrelia burgdorferi, Treponema pallidum.

To azithromycin microorganisms, resistant are steady against erythromycin.

 

Pharmacokinetics. Azithromycin is quickly and well soaked up from a GIT that is caused by its stability in acid medium and lipophilicity. It is quickly distributed in an organism. Well gets into respiratory tracts, bodies and fabrics of an urogenital path, into skin and soft tissues. High concentration in fabrics and a long elimination half-life of an obuslovlovlena low linkng of azithromycin with serum proteins, and also its ability to get into eukaryotic cells and to concentrate in the environment with a low rn, a surrounding lysosome. It determines the large seeming distribution volume (31,1 l/kg) and high plasma clearance. Ability of drug to collect preferential in lysosomes is especially important for elimination of intracellular activators.

Phagocytes deliver azithromycin to places of an infection where release it in the course of phagocytosis. Already in 12 – 72 h in the place of an inflammation the high therapeutic concentration exceeding the minimum overwhelming concentration for contagiums are created.

The elimination half-life is long, out of fabrics it is brought slowly – 60 – 76 h. Azithromycin remains in bactericidal concentration in the inflammation centers within 5 – 7 days after reception of the last dose that defines a possibility of a single dose of drug in days and a short course of treatment (3 or 5 days).

Small part – with urine is removed generally with bile.

Indications to use:

Treatment of the infectious diseases caused by activators, sensitive to drug:

• infections of ENT organs, upper parts of respiratory tracts (sinusitis, average otitis, bacterial pharyngitis, tonsillitis);
• lower respiratory tract infections (bacterial bronchitis, pneumonia);
• scarlet fever;
• infections of skin and soft tissues (ugly face, impetigo, secondary pyodermatoses);
• infections of an urogenital path (gonorrheal and not gonorrheal urethritis and/or cervicitis);
• the infections of a stomach and duodenum caused by Helicobacter pylori (in complex therapy);
• disease Laima (borreliosis) in an initial stage.

Route of administration and doses:

Before purpose of drug it is desirable to define sensitivity of the microflora which caused a disease. Azitromitsin-BHFZ it is necessary to accept 1 time a day in 1 hour prior to food or in 2 hours later as the concomitant use with food reduces azithromycin absorption.

To adults and children 14 years at respiratory infections are more senior, infections of skin and soft tissues in the first day 500 mg once, and from 2 to 5 day - on 250 mg a day are appointed; or on 500 mg once a day within 3 days (a course dose – 1,5 g).

At acute infections of an urogenital path 1 g (4 capsules) is appointed once.

For treatment of an initial stage of a disease of Lyme (the chronic migrating erythema) 1 g (4 capsules) in the first day and on 500 mg daily from 2 to 5 day is appointed once (a course dose – 3 g).

At the infections of a stomach and duodenum caused by Helicobacter pylori – 1 g (4 capsules) a day once within 3 days.

Features of use:

It is necessary to apply with care at patients with the expressed disturbances of functions of a liver or kidneys, and also at the patients having disturbances of a cordial rhythm (arrhythmias and lengthening of an interval of QT on the cardiogram).

Ethanol substantially reduces azithromycin absorption therefore during treatment by drug it is necessary to abstain from the use of alcoholic drinks.

In case time of administration of drug was passed, it is necessary to accept the passed dose as soon as possible, and the subsequent – at an interval of 24 h.

Elderly people and patients with an impaired renal function have no need for correction of doses.

Ability to influence speed of response at control of motor transport or other mechanisms. Drug does not influence speed of response at control of motor transport or other mechanisms.

 

Use of drug during pregnancy. Use of drug during pregnancy is justified only in that case when the estimated advantage for mother exceeds potential risk for a fruit.

In case of drug use by the women nursing feeding should be stopped. 

Children. Azitromitsin-BHFZ in the form of capsules children are not recommended to appoint up to 14 years.

Side effects:

From digestive tract: nausea, vomiting, diarrhea, lock, loss of appetite, gastritis, reversible moderate increase in activity of hepatic transaminases, cholestatic jaundice, pseudomembranous colitis.

From an urinary system: nephrite.

From a reproductive system: vaginal candidiasis.

Co of the party of cardiovascular system: heart consciousness, thorax pains.

Allergic reactions: skin rashes, Quincke's edema, urticaria, conjunctivitis.

Dermatological reactions: photosensitization, itch.

From laboratory indicators: neutrophilia, eosinophilia. The changed indicators are returned to norm in 2 – 3 weeks after the end of treatment.

Interaction with other medicines:

Antiacid means (calciferous, aluminum, magnesium) slow down azithromycin absorption therefore it is necessary to observe a 2-hour interval between reception of Azitromitsina-BHFZ and these drugs.

Azithromycin, unlike other makrolidny antibiotics, does not contact isoenzymes of system _{of P450 cytochrome} therefore interaction with theophylline, terfenadiny, carbamazepine, triazolamy, digoxin is not observed.

In need of simultaneous use with warfarin it is recommended to carry out careful control of a prothrombin time.

At a concomitant use with ergotamine and dihydroergotamine manifestation of their toxic action (a heavy peripheral vasospasm, a dizesteziya) is possible. Use of this combination is contraindicated.

Linkozamida reduce, and tetracycline and chloramphenicol increase efficiency of azithromycin.

Contraindications:

• Hypersensitivity to azithromycin and other components of drug;
• hypersensitivity to antibiotics of group of macroleads;
• children's age up to 14 years.

Overdose:

It is shown by nausea, vomiting, diarrhea, a temporary hearing loss. Symptomatic treatment.

Storage conditions:

In the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 6 or 10 capsules in the blister, on 1 blister in a pack.