Azitsin, capsules on 0,25 g No. 6

General characteristics. Structure:

Active ingredient: azithromycin;
1 capsule contains azithromycin in terms of 100% anhydrous substance of 250 mg; excipients: lactoses monohydrate, sodium lauryl sulfate, povidone, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Azithromycin – the representative of new subgroup of makrolidny antibiotics – azaleads. Contacts subunit 50S of a ribosome 70S of sensitive microorganisms, oppressing RNA-dependent synthesis of protein, slows down growth and reproduction of bacteria, at high concentration the bactericidal effect is possible.

Has a wide range of antimicrobic action. Gram-positive cocci – Streptococcus pneumoniae are sensitive to drug, S.pyogenes, S.agalactiae, streptococci of groups C, F and G, S.viridans; Staphylococcus aureus; gram-negative bacteria – Haemophilus influenzae, N. of parainfluenzae, Moraxella catarrhalis, Bordatella pertussis, B.parapertussis, Legionella pneumophila, H.ducrei, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms – Bacteroides bivius, Clostridium perfringens, Peptostreptococcus species, and also Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi. Does not influence the gram-positive microorganisms resistant to erythromycin.

Pharmacokinetics. After intake azithromycin is quickly soaked up from the digestive channel. Bioavailability makes about 37% (effect of "the first passing"). At intake of 500 mg of azithromycin the maximum concentration in blood serum is reached in 2,5–3 h and makes 0,4 mg/l. Drug well gets into respiratory tracts, bodies and fabrics of an urogenital path, in particular, in a prostate, in skin and soft tissues. Concentration of drug in fabrics and cells 10-100 times higher, than in blood serum. Stable level in plasma is reached in 5–7 days. Drug in a large number collects in the phagocytes transporting it to places of an infection and an inflammation where gradually release in the course of phagocytosis.

Contacts proteins in inverse proportion to concentration in blood (7–50% of drug). About 35% are metabolized in a liver by demethylation, losing activity.

More than 50% of a dose are removed with bile in not changed look, about 4,5% – with urine for 72 h.

Plasma elimination half-life makes 14–20 h (in the range of 8–24 h after administration of drug) and 41 h (in the range of 24–72 h). Meal considerably changes pharmacokinetics.

With age parameters of pharmacokinetics do not change at men (65–85 years), at women the maximum concentration (Cmax) increases by 30–50%.

Pharmaceutical characteristics.

Main physical and chemical properties: the solid capsules with a lid and the case of white color containing powder or granules of white color.

Incompatibility. Pharmaceutical it is incompatible with heparin.

Indications to use:

The infections caused by the microorganisms sensitive to azithromycin:
- infections of ENT organs (bacterial pharyngitis / tonsillitis, sinusitis, average otitis);
- respiratory infections (bacterial bronchitis, intersticial and alveolar pneumonia);
- infections of skin and soft tissues: the chronic migrating erythema (an initial stage of a disease of Lyme), an ugly face, impetigo, secondary pyodermatoses;
- infections which are transmitted sexually: uncomplicated urethritis / cervicitis;
- the infections of a stomach and a duodenum caused by Helicobacter pylori.

Route of administration and doses:

Apply to adults and children with body weight more than 45 kg. Азицин® apply inside, 1 time a day for an hour to food or in two hours after food as the concomitant use breaks azithromycin absorption.

At infections of ENT organs and respiratory tracts, skin and soft tissues (except the chronic migrating erythema): 500 mg (2 capsules once) in days for 3 days.

At the chronic migrating erythema: 1 time a day for 5 days, the 1st day – 1 g (4 capsules on 250 mg), then – on 500 mg (2 capsules) from the 2nd to the 5th day.

At infections which are transmitted sexually: 1 g once.

At a peptic ulcer of a stomach and duodenum, associated with Helicobacter pylori: 1 g a day for 3 days as a part of complex therapy.

In case of the admission of reception of 1 dose of drug it is necessary to accept the passed dose as soon as possible, and the following – bucketed in 24 h.

People of advanced age and patients with renal failures have no need to change a dosage.

Features of use:

It is necessary to use with care drug at patients who have disturbance of a cordial rhythm (arrhythmias and lengthening of an interval of QT on the cardiogram).

Considering that drug is metabolized in a liver and is excreted with bile, patients should not appoint it with heavy hepatic pathology. When developing a heavy liver failure treatment by azithromycin has to be stopped.

In case of the admission of reception of a dose it is necessary to accept the passed dose as soon as possible, and the subsequent – at an interval of 24 h.

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

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

During treatment it is necessary to refrain by drug from the use of alcoholic drinks.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

During treatment it is necessary to abstain from driving of motor transport and from the occupations requiring special attention and speed of mental and motor reactions.

Side effects:

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

From urinogenital system: nephrite, vaginal candidiasis.

From cardiovascular system: heart consciousness, thorax pain.

Allergic reactions: skin rashes, Quincke's disease, small tortoiseshell, conjunctivitis, multiformny erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis.

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.

From the central nervous system: dizziness, headache, вертиго, drowsiness; hyperkinesia, uneasiness, neurosis, sleep disorder (1% and less).

Others: hyperpotassemia, arthralgia, deterioration in hearing.

Interaction with other medicines:

Antiacid means slow down azithromycin absorption. It is recommended to adhere to an interval not less than 2 h between administration of drug and an antacid. It is necessary to pay attention to a concomitant use of drug with theophylline, terfenadiny, warfarin, carbamazepine, Phenytoinum, triazolamy, digoxin, ergotamine, cyclosporine as makrolidny antibiotics can strengthen effect of above-mentioned drugs.

Unlike the majority of macroleads, azithromycin does not contact P450 cytochrome complex enzymes.

Linkozamida weaken, and tetracycline and chloramphenicol increase efficiency of azithromycin. Pharmaceutical it is incompatible with heparin.

Contraindications:

Hypersensitivity to makrolidny antibiotics or other components of drug. Heavy abnormal liver functions. Children with body weight it is less than 45 kg (for this dosage form).

Use during pregnancy or feeding by a breast.

It is not recommended to appoint drug during pregnancy, except for cases when use is necessary according to vital indications.

In case of use of drug in the period of a lactation feeding by a breast needs to be stopped.

Children.

Азицин® appoint to children with body weight from 45 kg.

Overdose:

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

Treatment: symptomatic therapy; probe gastric lavage.

Storage conditions:

Period of validity. 2 years. To store in the place, unavailable to children, in original packaging, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 6 capsules in a blister strip packaging, on 1 blister strip packaging in a pack.