Azitrus

General characteristics. Structure:

Active agent: dihydrate azithromycin (in terms of azithromycin) –500 mg; 
Excipients:

Structure of a kernel: calcium stearate - 7,6 mg; starch of 1500 - 30,4 mg, starch of potato 33,0 mg, кросповидон (коллидон CL-M) (type B) - 22,8 mg, povidone (polyvinylpirrolidone low-molecular medical 12600 ± 2700, пласдон K-17) - 10,7 mg; lactoses monohydrate (sugar milk) - 51,7 mg; talc - 22,8 mg; cellulose microcrystallic - 81,0 mg.

Structure of a cover: a gipromelloz (oksipropilmetiltsellyuloz) - 35,4 mg; a macrogoal 4000 (poly(ethylene oxide) 4000, polyethyleneglycol 4000) - 1,84 mg; titanium dioxide (titanium dioxide) - 2,76 mg.

Pharmacological properties:

Pharmacodynamics. The antibiotic of a broad spectrum of activity, an azalead, works bacteriostatically. Communicating with 50S – ribosome subunit, suppresses protein synthesis, slows down growth and reproduction of bacteria. In high concentration renders bactericidal effect. Works on out of - and intracellular activators. It is active concerning gram-positive microorganisms: Streptococcus spp. (groups C, F and G, except steady against erythromycin), Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Staphylococcus epidermidis, Staphylococcus aureus; gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Helicobacter pylori, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.; and also intracellular activators: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. It is inactive concerning the gram-positive bacteria steady against erythromycin.

Pharmacokinetics. Azithromycin is quickly soaked up from digestive tract that is caused by its stability in acid medium and lipophilicity. It is quickly distributed on all organism, at the same time in fabrics high concentration of an antibiotic are reached. After intake of 500 mg the maximum concentration of azithromycin in a blood plasma is reached in 2,5 – 2,9 h and makes 0,4 mg/l. Bioavailability makes 37,5%. Azithromycin well gets into respiratory tracts, bodies and fabrics of an urogenital path (in particular, into a prostate), into skin and soft tissues. High concentration in fabrics (is 10-50 times higher, than in a blood plasma) and a long elimination half-life are 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. It, in turn, determines the large seeming distribution volume (31,1 l/kg) and high plasma clearance. Ability of azithromycin to collect preferential in lysosomes, is especially important for elimination of intracellular activators. It is proved that phagocytes deliver azithromycin to places of localization of an infection where it is released in the course of phagocytosis. Concentration of azithromycin in the centers of an infection it is reliable above, than in healthy fabrics (on average for 24-34%) and correlates with degree of inflammatory hypostasis. Azithromycin remains in bactericidal concentration within 5-7 days after reception of the last dose that allowed to develop short (3-day and 5-day) courses of treatment. In a liver it demetilirutsya, the formed metabolites are not active. Removal of azithromycin from a blood plasma takes place in 2 stages: the elimination half-life makes 14-20 h in the range from 8 to 24 h after administration of drug and 41 h – in the range from 24 to 72 h that allows to use drug of 1 times/days. Drug generally with bile in an invariable look is removed, a small part is removed by kidneys.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug;
Infections of upper parts of respiratory tracts and ENT organs (quinsy, sinusitis, tonsillitis, pharyngitis, average otitis);
Scarlet fever;
Infections of lower parts of respiratory tracts (the bacterial, including caused by atypical activators pneumonia, exacerbation of chronic pneumonia, bronchitis);
Infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis);
Infections of urinary tract (gonorrheal and not gonorrheal urethritis, cervicitis);
Disease Laima (borreliosis), for treatment of an initial stage (erythema migrans);
The diseases of a stomach and duodenum associated with Helicobacter pylori (as a part of a combination therapy).

Route of administration and doses:

Inside, for 1 h to or in 2 h after food of 1 times a day. 
The adult at infections of upper and lower parts of respiratory tracts - 0.5 g/days for 1 reception within 3 days (a course dose - 1.5 g).
At infections of skin and soft tissues - 1 g/days in the first day for 1 reception, further on 0.5 g/days daily from 2 to 5 day (a course dose - 3 g).
At acute infections of urinogenital bodies (an uncomplicated urethritis or a cervicitis) - once 1 g.
At a disease Laima (borreliosis) for treatment of the I stage (erythema migrans) - 1 g in the first day and 0.5 g daily from 2 to 5 day (a course dose - 3 g).
At a peptic ulcer of a stomach and the duodenum associated with Helicobacter pylori – 1 g/days within 3 days as a part of the combined antikhelikobakterny therapy.
To children 12 years and/or with body weight more than 50 kg are more senior at infections of upper and lower respiratory tracts, skin and soft tissues appoint 0.5 g of 1 times a day within 3 days (a course dose - 1.5 g).
At treatment of erythema migrans at children (12 years and/or weighing more than 50 kg are more senior) drug is appointed by 1 g/days in the first day for 1 reception and 0.5 g daily from 2 to 5 day (a course dose - 3 g).

Features of use:

Not to accept with food. 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 in 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.

Side effects:

From digestive tract: diarrhea (5%), nausea (3%), an abdominal pain (3%), 1% and less – a meteorism, vomiting, a melena, cholestatic jaundice, increase in activity of "hepatic" transaminases, at children is locks, a loss of appetite, gastritis; candidiasis of a mucous membrane of an oral cavity, taste change (1% and less).
From cardiovascular system: heartbeat, thorax pain (1% and less).
From a nervous system: headache, dizziness, drowsiness; children have a headache (at therapy of average otitis), a hyperkinesia, uneasiness, neurosis, sleep disorders (1% and less).
From urinogenital system: vaginal candidiasis, nephrite (1% and less).
Allergic реакции:сыпь, urticaria, skin itch, Quincke's disease; children have a conjunctivitis, an itch, urticaria. Other: adynamy, photosensitization.

Interaction with other medicines:

Antacids (aluminum and magniysoderzhashchy), ethanol and food slow down and reduce azithromycin absorption. At joint purpose of warfarin and azithromycin (in usual doses) changes of a prothrombin time it is not revealed, however, considering that at interaction of mokrolid and warfarin strengthening of anti-coagulative effect is possible, careful control of a prothrombin time is necessary for patients. Increases concentration of digoxin. Ergotamine and dihydroergotamine: strengthening of toxic action (vasospasm, dizesteziya). To triazoles: decrease in clearance and increase in pharmacological action of a triazolam. Slows down removal and increases concentration in 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, бромокрипин, Phenytoinum, peroral hypoglycemic medicines, theophylline, etc. ksantinovy derivatives), at the expense of inhibition of a microsomal oxidation in hepatocytes azithromycin. Linkozamina weaken, and tetracycline and chloramphenicol increase efficiency of azithromycin.

Contraindications:

Hypersensitivity (including to other macroleads); a liver and/or renal failure, the lactation period, to children up to 12 years and/or with body weight less than 50 kg. 
Use at pregnancy Use of drug at pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit. In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

Overdose:

Symptoms: nausea, temporary hearing loss, vomiting, diarrhea. Treatment: therapy is symptomatic; gastric lavage.

Storage conditions:

In the place protected from light at a temperature not over 25 ºС. To store in the places unavailable to children. Period of validity 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

3 pieces - planimetric strip packagings (1) - packs cardboard.
3 pieces - planimetric strip packagings (2) - packs cardboard.
6 pieces - planimetric strip packagings (1) - packs cardboard.