Azithromycin

General characteristics. Structure:

Active ingredient: 250 mg of azithromycin a dihydrate (in terms of azithromycin).

Excipients: cellulose microcrystallic, povidone (поливинилпироллидон low-molecular medical), magnesium stearate, sodium lauryl sulfate, lactose (sugar milk).

Gelatinous solid capsules: gelatin, the water purified methylparahydroxybenzoate (нипагин), пропилпарагидроксибензоат (нипазол), titanium dioxide (titanium dioxide).

Antibiotic of a broad spectrum of activity. Is the representative of subgroup of makrolidny antibiotics of azaleads, works bacteriostatically. During creation in the center of an inflammation of high concentration has bactericidal effect.

Pharmacological properties:

Pharmacodynamics. Works on out of - and intracellular activators. Gram-positive microorganisms are sensitive to azithromycin: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalaciae, streptococci of the groups C, F and G, Staphylococcus aureus, Streptococcus viridans; gram-negative microorganisms: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducrei, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptocoiccus spp; and also Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdorferi. Azithromycin 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. 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%. Azithromycin well gets into respiratory tracts, bodies and fabrics of an urogenital path (in particular in a prostate), in 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 correlate with degree of inflammatory hypostasis. Despite high concentration in phagocytes, azithromycin has no significant effect on their function. 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 a day.

50% are removed with bile in an invariable look, 6% — 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 (including caused by atypical activators);
- infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis);
- infections of an urogenital path (uncomplicated urethritis and/or cervicitis);
- a disease Laima (borreliosis), for treatment of an initial stage (erythema migrans);
- the diseases of a stomach and a duodenum associated with Heliobacter 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 — 500 mg/days for 1 reception within 3 days (a course dose - 1,5 g).

At infections of skin and soft tissues - 1000 mg/days in the first day for 1 reception, further on 500 mg/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 1000 mg.

At a disease Laima (borreliosis) for treatment of the I stage (erythema migrans) — 1000 mg in the first day and on 500 mg 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 are more senior (with the body weight of 50 kg and more) at infections of upper and lower respiratory tracts, skin and soft tissues - 500 mg of 1 times a day within 3 days.

At treatment of erythema migrans at children a dose — 1000 mg in the first day and on 500 mg daily from 2 to 5 day.

Features of use:

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 the 24th hour.

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.

Use at pregnancy and in the period of a lactation. It can be applied during pregnancy when the advantage of its use considerably exceeds the risk existing always when using any drug during pregnancy.

In need of purpose of drug in the period of a lactation, it is necessary to resolve an issue of the breastfeeding termination.

Side effects:

From digestive tract: diarrhea (5%); nausea (3%); abdominal pains (3%); 1% and less — dyspepsia (a meteorism, vomiting), a melena, cholestatic jaundice, increase in activity of "hepatic" transaminases; children have locks, anorexia, gastritis; taste change, candidiasis of a mucous membrane of an oral cavity (1% and less).

From cardiovascular system: heartbeat, thorax pain (1% and less).

From a nervous system: dizziness, headache, drowsiness; children have a headache (at therapy of average otitis), a hyperkinesia, uneasiness, neurosis, a sleep disorder (1% and less).

From urinogenital system: vaginal candidiasis, nephrite (1% and less).

Allergic reactions: rash, Quincke's edema, skin itch, small tortoiseshell; children have a conjunctivitis, an itch, urticaria.

Others: increased fatigue, photosensitization.

Interaction with other medicines:

Antacids (aluminum and magnesium containing), ethanol and food slow down and reduce 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 macroleads and warfarin strengthening of anti-coagulative effect is possible, careful control of a prothrombin time is necessary for patients.

Digoxin: increase in 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, Bromocriptinum, Phenytoinum, peroral hypoglycemic means, theophylline and other ksantinovy derivatives) — at the expense of inhibition of a microsomal oxidation in hepatocytes azithromycin.

Linkozamina weaken efficiency, tetracycline and chloramphenicol — strengthen.

Contraindications:

Hypersensitivity (including to other macroleads); hepatic and/or renal insufficiency; lactation period; children's age up to 12 years.

With care — during pregnancy; at arrhythmia; to children with abnormal liver functions and/or kidneys.

Overdose:

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

Treatment: immediate gastric lavage and symptomatic treatment.

Storage conditions:

List B. In the dry, protected from light place at a temperature not over 25 ºС. To store in the place, unavailable to children. Period of validity 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Capsules on 250 mg. On 6 or 10 capsules in a blister strip packaging. On 6 capsules in banks polymeric. Each planimetric packaging or to bank together with the application instruction is placed in a pack from a cardboard.