Azithromycin

General characteristics. Structure:

Active ingredient: 250 mg or 500 mg of azithromycin.

Excipients: sodium glikolit starch, microcrystallic cellulose, corn starch, Natrium benzoicum, talc, sodium a lauryl sulfate, magnesium stearate. Structure of a cover: polyethylene glycol, is sawn through glycol, Tabcoat Pink dye (a gidroksipropilmetiltsellyuloz, polyethyleneglycol, titanium dioxide, E 127 erythrosine, talc).

Antibiotic of a makrolidny number of a wide range of antimicrobic action.

Pharmacological properties:

Pharmacodynamics. An antibiotic of group of macroleads - an azalead. Possesses a wide range of antimicrobic action. Communicating with 50S-cybjedinitsey ribosomes, suppresses biosynthesis of proteins of a microorganism. In high concentration renders bactericidal effect. It is active concerning a number of gram-positive bacteria: Streptococcus pneumoniae, S. pyogenes, S. agalactiae, S. viridans, streptococci of group C, F and G, Staphylococcus aureus, S. epidermidis. He has effect on the gram-positive bacteria steady against erythromycin. It is effective concerning gram-negative microorganisms: Haemophilus influenzae, H. parainfluenzae and N. of ducreyi, Moraxella catar-rhalis, Bordetella pertussis and V. of parapertussis, Neisseria gonorrhoeae and N. meningitidis, Brucella melitensis, Helicobacter pylori, Gardnerella vaginalis.

It is active concerning Campylobacter jejuni, some anaerobic microorganisms: Clostridium perfringens, and also Micobacteria avium complex, Besides, is effective concerning intracellular and other microorganisms, including: Legionella pneumophila, Chlamydia trachomatis and S. of pneumoniae, Mycoplasma pneumoniae, Ureaplasma urealyticum, Listeria monocitogenes, Borrelia burgdorferi, Treponema pallidum.

Pharmacokinetics. At intake Azithromycin is well soaked up and bystroraspredelyatsya on all organism. Gets in cells, including phagocytes which migrate in the inflammation center, promoting creation of therapeutic concentration of drug in the place of an infection. In 12-72 hours in the place of an inflammation high therapeutic concentration (1-9 mg/kg) exceeding the minimum overwhelming concentration for contagiums are created. Possesses a long elimination half-life and it is slowly brought out of fabrics (on average 60–76 hours). The specified properties define a possibility of a single dose of drug in days and the short mode of dosing (3 days) providing a 7-10-dnevny course of treatment.

It is metabolized generally in a liver, metabolites are not active.

Drug generally with bile in not changed look is emitted, a small part is removed by kidneys.

Indications to use:

- upper respiratory tract infections (bacterial pharyngitis / tonsillitis, sinusitis, average otitis);
- lower respiratory tract infections (bacterial bronchitis, intersticial and alveolar pneumonia, exacerbation of chronic bronchitis);
- infections of skin and soft tissues (the chronic migrating erythema - an initial stage of a disease of Lyme, an ugly face, impetigo, secondary pyodermatoses);
- infections, sexually transmitted (urethritis, cervicitis);
- the diseases of a stomach and a 12-perstny gut associated with Helicobacter pylori.

Route of administration and doses:

Inside, 1 time a day. Bioavailability of tablets does not depend on meal.

- at an infection of upper and lower respiratory tracts, skin and soft tissues (except for the chronic migrating erythema): to adults and children 12 years are more senior: 500 mg once a day within 3 days (a course dose of 1,5 g), to children are from 6 to 12 years: from calculation 10mg/kg body weights once a day within 3 days (a course dose of 30 mg/kg).

- at chronic migrating eriteme:vzrosly and to children 12 years are more senior: 1 time a day within 5 days: the 1st day – 1,0 g (2 tablets on 500 mg), then from the 2nd to the 5th day - on 500 mg (a course dose of 3,0 g), children is from 6 to 12 years: in the 1st day - in a dose of 20 mg/kg of body weight and then from 2 to the 5th day - daily in a dose of 10 mg/kg of body weight (a course dose of 30 mg/kg).

- at the diseases of a stomach and a 12-perstny gut associated with Helicobacter pylori: 1 g (2 tablets on 500 mg) in days within 3 days in combination with anti-secretory means and other medicines.

- at the infections transmitted sexual a putem:neoslozhnenny urethritis / cervicitis – 1 g once complicated it is long the proceeding urethritis/cervicitis caused by Chlamydia trachomatis - on 1 g three times at an interval of 7 days (1-7-14). Course dose of 3 g.

Features of use:

In case of the admission of reception of one dose of drug - it is necessary to accept the passed dose as soon as possible, and the subsequent - with breaks at 24 o'clock.

Precautionary measures at azithromycin use. It is necessary to observe a break of 2 h at simultaneous use of antacids.

With care apply at the expressed abnormal liver functions, kidneys, 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 that demands specific therapy under observation of the doctor.

Side effects:

Meet seldom (in 1% of cases less):

From digestive tract: melena, cholestatic jaundice, swelling, nausea, vomiting, diarrhea, lock, loss of appetite, gastritis.

Allergic reactions: skin rashes; photosensitization, Quincke's edema.

From urinogenital system: vaginal candidiasis, nephrite.

From cardiovascular system: heartbeat, thorax pain.

From a nervous system: dizziness, a headache, вертиго, drowsiness, children have a headache (at therapy of average otitis), a hyperkinesia, uneasiness, neurosis, sleep disorders.

Others: reversible moderate increase in activity of liver enzymes, increased fatigue, itch, small tortoiseshell, conjunctivitis.

In extremely rare sluchayakhneytrofiliya and eosinophilia. The changed indicators are returned to limits of norm in 2-3 weeks after the treatment termination.

It is necessary to inform the attending physician on emergence of any side effect.

Interaction with other medicines:

The antiacid means (containing aluminum, magnesium) substantially reduce azithromycin absorption therefore drug should be accepted, at least, in one hour prior to or in two hours after reception of these drugs.

Does not contact enzymes of a complex of R-450 cytochrome and unlike makrolidny antibiotics, interaction with theophylline, terfenadiny, carbamazepine, triazolamy, digoxin so far is noted.

Macroleads at a concomitant use with Cycloserinum, indirect anticoagulants, Methylprednisolonum, felodipiny and the drugs which are exposed to a microsomal oxidation (cyclosporine, hexobarbital, ergot alkaloids, valproic acid, Disopyramidum, бромкриптин, Phenytoinum, peroral hypoglycemic means) slow down removal, increase concentration and toxicity of the specified drugs; while at use of azaleads of such interaction it was not noted so far.

In need of joint reception with warfarin it is recommended to carry out careful control of a prothrombin time.

At a concomitant use of macroleads with ergotamine and dihydroergotamine manifestation of their toxic action (a vasospasm, a dizesteziya) is possible.

Linkozamina weaken, and tetracycline and chloramphenicol increase efficiency of azithromycin.

Pharmaceutical it is incompatible with heparin.

Contraindications:

- Hypersensitivity to antibiotics of group of macroleads;

- Heavy abnormal liver functions and kidneys;

- Pregnancy;

- Feeding by a breast (for the period of treatment stop).

Overdose:

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

Treatment: symptomatic.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above 25 °C. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 6 tablets in the blister, on 1 blister in a cardboard pack.