Azitrus

General characteristics. Structure:

Active agent: azithromycin a dihydrate in terms of azithromycin – 50 mg, 100 mg, 200 mg, 400 mg, 800 mg, 1200 mg Excipients: sodium citrate (sodium citrate trisubstituted), fragrance food orange, sodium saccharinate (saccharin soluble), коллидон CL-M (кросповидон), sugar (sucrose).

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 (bacterial and atypical 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. 
Route of administration and doses
Inside for 1 h to or in 2 h after food of 1 times a day.
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 1 g.
At a disease Laima (borreliosis) for treatment of the I stage (erythema migrans) – 1 g in the first day and 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 at infections of upper and lower respiratory tracts, skin and soft tissues appoint at the rate of 10 mg/kg of body weight of 1 times a day within 3 days (a course dose – 30 mg/kg of body weight) or within 5 days: in the first day – 10 mg/kg of body weight, then on 5-10 mg/kg of body weight of 1 times a day within 4 days.
Depending on the body weight of the child the following schemes of a dosage are recommended:

Body weight            release Form                      Average daily (one-time) dose
 
    5 kg             powder for preparation                    of 2,5 ml (50 mg)
    6 kg                 of suspension of 100 mg / 5 ml                         of 3 ml (60 mg)
    7                                                                           kg 3,5 ml (70 mg)
    8                                                                            kg 4 ml (80 mg)
    9                                                                           kg 4,5 ml (90 mg)
 10-14                                                                           kg 5 ml (100 mg)
 
 15-24 kg          powder for preparation                   of 5 ml (200 mg) 
  25-34 kg           of suspension of 200 mg / 5 ml                          of 7,5 ml (300 mg)
 35-44                                                                          kg 10 ml (400 mg) 
  > 45 kg                                                                      appoint doses for adults (500-1000 mg)

At treatment of erythema migrans at children drug is appointed 1 time a day within 5 days: 20 mg/kg of body weight in the first day and on 10 mg/kg of body weight from 2 to 5 day.

Suspension preparation.
One-dose package. In a pure glass pour a small amount of prokipyachenny and chilled water, then pour out contents of one package and mix before receiving homogeneous suspension.
After reception to wash out a glass water, to dry up and store in the dry and pure place.
Bank. In bank, containing 400 mg or 800 mg of azithromycin, by means of the doser of polymeric compound add 12 ml of prokipyachenny and chilled water or the distilled water; in bank, containing 1200 mg of azithromycin – 18 ml. Suspension before the use is shaken up. 
Dose suspension a bilateral spoon: the big spoon contains 5 ml of suspension, small – 2,5 ml; or the spoon having two marks: lower corresponds to 2,5 ml of suspension and upper – 5 ml; or doser polymeric compound.
After use to wash out a spoon and the doser water, to dry up and store in the dry and pure place.

Features of use:

Not to accept with food. In case of the admission of reception, passed doses it is necessary to accept 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 reactions: rash, urticaria, skin itch, Quincke's disease; children have a conjunctivitis, an itch, urticaria. Other: adynamy, photosensitization.

Interaction with other medicines:

Use 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 macroleads 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); hepatic and/or renal nedostatoch-a nost, the lactation period, children's age up to 6 months (efficiency and safety is not established).

Overdose:

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

Storage conditions:

List B. In the dry, protected from light place at a temperature from 15 to 25 °C. Water suspension is stored at a temperature from 15 to 25 °C no more than 5 days or in the refrigerator no more than 14 days. To store in the places unavailable to children. 
Period of validity 2 years. To use drug before the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of suspension for intake of 100 mg / 5 ml; bank (jar) of dark glass of 17 g with a dosing spoon (spoon), a pack cardboard 1.