Azithromycin

General characteristics. Structure:

Active agent: dihydrate azithromycin — 265,3 mg in terms of active agent (azithromycin) — 250 mg.

Excipients: cellulose microcrystallic, starch corn, povidone low-molecular, magnesium stearate.

Structure of the capsule: titanium dioxide, patent blue, gelatin.

Pharmacological properties:

Pharmacodynamics. Antibacterial agent of a broad spectrum of activity, an azalead, works bacteriostatically. Communicating with 50S in subunit of ribosomes, oppresses to a peptidtranspokaz at a broadcasting stage, 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. Absorption — high, кислотоустойчив, липофилен. Bioavailability after a single dose of 0,5 g — 37% (effect of "the first passing" through a liver), the maximum concentration in a blood plasma after oral administration of 0,5 g — 0,4 mg/l, the period of achievement of the maximum concentration in a blood plasma — 2,5-2,9 h; in fabrics and cells concentration is 10-50 times higher, than in blood serum, distribution volume — 31,1 l/kg. Easily passes gistogematichesky barriers. Well gets into respiratory tracts, urinogenital bodies and fabrics, into a prostate, into skin and soft tissues; collects in the environment with a low rn, in lysosomes (that is especially important for an eradikation of intracellularly located activators). It is transported also by phagocytes, polymorphonuclear leukocytes and macrophages. Gets through membranes of cells and creates high concentration in them. Concentration in the centers of an infection it is reliable above (for 24-34%), than in healthy fabrics, and correlates with expressiveness of inflammatory hypostasis. Remains in effective concentration within 5-7 days after reception of the last dose. Communication with proteins of plasma — 7-50% (it is inversely proportional concentration in blood). In a liver it demetilirutsya, the formed metabolites are not active. Isoenzymes of CYP3A4, CYP3A5, CYP3A7 which inhibitor it is participate in metabolism of drug. Plasma clearance — 630 ml/min. The elimination half-life between 8 and 24 h after reception — 14-20 h, an elimination half-life in the range from 24 to 72 h — is removed with bile in not changed look, 6% 41 h 50% — kidneys. Meal significantly changes pharmacokinetics (depending on a dosage form): capsules — the maximum concentration in a blood plasma decreases (by 52%). At elderly men (65-85 years) pharmacokinetic parameters do not change, at women the maximum concentration in a blood plasma increases (by 30-50%), at children at the age of 1-5 years decrease the maximum contents in a blood plasma, an elimination half-life.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug: infections of upper parts of respiratory tracts and ENT organs (pharyngitis, tonsillitis, laryngitis, sinusitis, average otitis); scarlet fever; infections of lower parts of respiratory tracts (pneumonia (including caused by atypical activators), 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); Lyme's disease (an initial stage — erythema migrans), the peptic ulcer of a stomach and a 12-perstny gut 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 — 500 mg/days for 1 reception within 3 days (a course dose — 1500 mg). 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 — 3000 mg). 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) — 1000 mg in the first day and 500 mg daily from 2 to 5 day (a course dose — 3 g). At the peptic ulcer of a stomach and a 12-perstny gut associated with Helicobacter pylori — 1 g/days within 3 days as a part of the combined antikhelikobakterny therapy. To children 12 years (with body weight more than 45 kg) at infections of upper and lower respiratory tracts are more senior, than skin and soft tissues appoint 500 mg of 1 times a day within 3 days.
At treatment of erythema migrans at children (12 years are more senior) drug is appointed 1 time a day in a dose of 1000 mg in the first day and on 500 mg from 2 to 5 day.

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 of 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%), abdominal pain (3%); 1% and less — a meteorism, vomiting, a melena, cholestatic jaundice, increase in activity of "hepatic" transaminases; children have 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: dizziness, headache, 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 reactions: rash, urticaria, a skin itch, a Quincke's disease, children have a conjunctivitis.
- Other: adynamy, photosensitization.

Interaction with other medicines:

Antacids (aluminum - and magnesium - containing), 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 macroleads and warfarin strengthening of anti-coagulative effect is possible, careful control of a prothrombin time is necessary for patients.
Increases concentration of digoxin due to weakening of its inactivation an indestinal flora. 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 medicines, theophylline, etc. ksantinovy derivatives), at the expense of inhibition of a microsomal oxidation in hepatocytes azithromycin. Linkozamida weaken, and tetracycline and chloramphenicol increase efficiency of azithromycin.

Contraindications:

Hypersensitivity (including to other macroleads), a heavy liver/renal failure, the lactation period, children up to 12 years (with body weight less than 45 kg).

With CARE: arrhythmia (ventricular arrhythmias and lengthening of an interval of Q-T are possible), to children with abnormal liver functions or kidneys, pregnancy.

USE AT PREGNANCY And in the period of the LACTATION: it can be applied when the advantage of its use considerably exceeds the risk existing always when using any drug during pregnancy. If necessary purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

Overdose:

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

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules on 250 mg.
On 3, 6 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 3,6,12,18,24,30,36,42,48,54 or 60 capsules in a container polymeric for medicines or a bottle from glass melt with the screwed plastic covers. One container (bottle) or 1, 2, 3, 4, 5, 6, 7, 8,
9 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.
On 5, 10 or 20 containers (bottles) or on 20, 40, 60, 80 and 100 blister strip packagings together with the corresponding number of application instructions place in a box from a cardboard (for hospitals).