Azithromycin

General characteristics. Structure:

Active ingredient: 250 mg of azithromycin.

Excipients: a mannitol, sodium lauryl sulfate, calcium stearate, starch corn - enough up to the mass of contents of the capsule of 330.0 mg.

Structure of a cover of the capsule: gelatin, glycerin (E-422), the water purified titanium dioxide (E-171), sodium лаурисульфат (E-487), quinolinic yellow (E-104), a sunset (E-110).

Makrolidny antibiotic with the expressed bacteriostatic action.

Pharmacological properties:

Pharmacodynamics. Azithromycin (9-деоксо-9а-аза-9а-метил-9а-гомоэритромицин A) possesses antibacterial (bacteriostatic) action. Communicates with 50S in subunit of ribosomes, oppresses to a peptidtranslokaz at a stage of broadcasting and suppresses protein biosynthesis, slowing down growth and reproduction of bacteria, at high concentration the bactericidal effect is possible.

Range of antimicrobic effect of azithromycin wide, it includes gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalctiae, Streptococcus pneumoniae, Streptococcus pyogenes, streptococci of the groups C, F, G, Streptococcus viridans), except steady against erythromycin, and gram-negative (Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Campylobacter jejuni, Legionella pneumophila, Neisseria gonorrhoeae, Gardnerella vaginalis) microorganisms, anaerobe bacterias (Bacteroides bivius, Peptostreptococcus spp., Peptococcus, Clostridium perfringens), chlamydias (Chlamydia trachomatis, Chlamydia pneumoniae), mycobacteria (Mycobacteria avium complex), mycoplasma (Mycoplasma pneumoniae), ureaplasma (Ureaplasma urealyticum), spirochete (Treponema pallidum).

Pharmacokinetics. It is steady in acid medium, липофилен. It is quickly soaked up in a GIT. After a single dose of 500 mg bioavailability makes 37%, the maximum concentration in blood (0,4 mg/l) is reached in 2-3 hours. Meal and alcohol reduces the speed and completeness of absorption. In case of administration of drug soon after meal the maximum concentration in blood (With max) decreases approximately by 50%. The seeming volume of distribution makes 31,1 l/kg, linkng with proteins in inverse proportion to concentration in blood and makes 7-50%. The elimination half-life of T1/2 makes 68 hours. Stable level in plasma is reached in 5-7 days.

Azithromycin easily passes gistogematichesky barriers and comes to fabrics. It is transported also by phagocytes, polymorphonuclear leukocytes and macrophages to the place of an infection where it is released in the presence of bacteria. Gets through membranes of cells (it is effective at the infections caused by intracellular activators). Than in plasma, and in the infection center – for 2 4-34% it is more concentration in fabrics and cells 10-50 times higher, than in healthy fabrics. High level of concentration remains in fabrics within 5-7 days after the last introduction. In a liver azithromycin demetilirutsya, the formed metabolites are inactive. Plasma clearance – 630 ml/min. About 50% of the accepted dose of azithromycin are removed with bile in not changed look, 6% - with urine. At elderly men (65-85 years) parameters of pharmacokinetics do not change, at elderly women – increases With max (by 30-50%). At children at the age of 1-5 years are reduced, in comparison with adults, the maximum concentration in blood, an elimination half-life and an indicator of AUC.

Indications to use:

Infections upper (bacterial pharyngitis and tonsillitis) and lower (a bacterial exacerbation of chronic obstructive pneumonia, intersticial and alveolar pneumonia, bacterial bronchitis) airways, ENT organs (quinsy, average otitis, laryngitis and sinusitis), urinogenital system (an urethritis and/or a cervicitis), skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis), a chronic stage of the migrating erythema (an initial stage of a disease of Lyme), the diseases of a stomach and a 12-perstny gut associated with Helicobacter pylori.

Route of administration and doses:

Accept 1 time a day inside in 1 hour prior to food or in 2 hours after food. In the first day of treatment by the adult appoint in a dose 0,5 g/days, from 2 to 5 day — 0,25 g/days. A course dose — 1,5 g.

At urogenital diseases — 1 g once, at Lyme's disease — 1 g in the first day, from 2 to 5 day — on 0,5 g (a course dose — 3 g).

At the diseases of a stomach and a 12-perstny gut associated with Helicobacter pylori accept 1 g/days within 3 days as a part of a combination therapy.

To children 12 months in the first day of therapy — 10 mg/kg of body weight of 1 times a day, then for 4 days of therapy — on 5 mg/kg/days or on 10 mg/kg/days within 3 days are more senior (a course dose — 30 mg/kg of body weight).

At Lyme's disease — in the first day of 20 mg/kg/days, from 2 to 5 day — on 10 mg/kg/days. 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 subsequent — with breaks at 24 o'clock.

Features of use:

Elderly persons and at patients with an impaired renal function have no need to change a dosage.

Side effects:

Nausea, vomiting, diarrhea, lock, meteorism, abdominal pain, melena, cholestatic jaundice, stethalgia, weakness, heartbeat, headache, dizziness, drowsiness, sleeplessness, conjunctivitis, nephrite, vaginitis, neutropenia or neutrophilia, reversible moderate increase in activity of liver enzymes, pseudomembranous colitis, candidiasis, photosensitization, skin rash, Quincke's disease, eosinophilia, at children, besides — a hyperkinesia.

Interaction with other medicines:

Antacids reduce azithromycin absorption (the break between receptions is recommended not less than 2 hours).

In spite of the fact that azithromycin is weaker, than erythromycin, inhibits P 450 cytochrome, careful control of a condition of patients at co-administration of the drugs which are metabolized in a liver is required.

Azithromycin strengthens effect of alkaloids of an ergot, dihydroergotamine.

Slows down secretion, increases concentration in plasma and toxicity of Cycloserinum, indirect anticoagulants, Methylprednisolonum, felodipin, the medicines which are exposed to a microsomal oxidation (carbamazepine, ergot alkaloids, valproic acid, hexobarbital, Phenytoinum, Disopyramidum, Bromocriptinum, theophylline, etc. ksantinovy derivatives, peroral hypoglycemic medicines).

Linkozamida weaken efficiency, tetracycline and chloramphenicol — strengthen. Pharmaceutical it is incompatible with heparin.

It is dangerous to combine azithromycin with the drugs extending QT interval on an ECG.

Contraindications:

Hypersensitivity (including to other macroleads), heavy abnormal liver functions, pregnancy, a lactation (for the period of treatment stop breastfeeding).

With care appoint at the expressed renal failures, abnormal liver functions (especially to children), at cardiac arrhythmias (ventricular arrhythmias and lengthening of an interval of QT are possible). After cancellation of treatment of reaction of hypersensitivity at some patients can remain, in this case specific therapy under observation of the doctor is necessary.

Overdose:

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

Treatment: symptomatic (there is no specific antidote).

Storage conditions:

To store drug in protected from moisture, light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg in a blister strip packaging No. 6, No. 10.