AZITRUS FORTE

Active material: Azithromycin
When ATH: J01FA10
CCF: Macrolide antibiotics – azalid
ICD-10 codes (testimony): A31.0, A38, A46, A48.1, A56.0, A56.1, A56.4, A69.2, B96.0, H66, J01, J02, J03, J15, J15.7, J16.0, J20, J32, J35.0, J42, K25, K26, L01, L30.3, N34, N72
Manufacturer: Synthesis of (Russia)

Pharmaceutical form, composition and packaging

Capsules gelatin, yellow color, №0; contents of capsules – granules white or nearly white.

Excipients: povidone (polyvinylpyrrolidone), calcium stearate, microcrystalline cellulose.

Composition of gelatin capsules: Titanium dioxide, metilgidroksiʙenzoat, propyl, acetic acid, gelatin.

6 PC. – packings Valium planimetric (1) – packs cardboard.

Powder for oral suspension white or nearly white, with orange scent; приготовленная суспензия – uniform, white with a yellowish tinge.

Excipients: sodium citrate (натрий лимоннокислый трехзамещенный), ароматизатор пищевой апельсиновый, sodium saccharin, kollidon CL-M (krospovydon), sucrose.

4.2 g – adjust the packages (3) – packs cardboard.
4.2 g – adjust the packages (6) – packs cardboard.
4.2 g – adjust the packages (3) в комплекте со стаканчиком – packs cardboard.
4.2 g – adjust the packages (6) в комплекте со стаканчиком – packs cardboard.

АзитРус^® forte

Pills, Film-coated white or white with a yellowish tint, Oval.

Excipients: calcium stearate, starch 1500, potato starch, krospovydon (kollidon CL-M), povidone (polyvinylpyrrolidone), lactose, talc, microcrystalline cellulose.

The composition of the shell: gipromelloza (hydroxypropylmethylcellulose), macrogol (polyethylene oxide 4000, polyethylene glycol 4000), Titanium dioxide (титана двуокись).

3 PC. – packings Valium planimetric (1) – packs cardboard.
3 PC. – packings Valium planimetric (2) – packs cardboard.
6 PC. – packings Valium planimetric (1) – packs cardboard.
3 PC. – plastic jars (1) – packs cardboard.
6 PC. – plastic jars (1) – packs cardboard.

Pharmacological action

Антибиотик широкого спектра действия группы макролидов, azalid. Bacteriostatic. Communicating with the 50S subjedinica ribosoma-, Suppresses protein synthesis, slowing the growth and reproduction of bacteria. В высоких концентрациях оказывает бактерицидный эффект. Acts on the outside- and intracellular pathogens.

Active against grampolaugitionah microorganisms: Streptococcus spp. (Group C, F and G, кроме устойчивых к эритромицину), 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, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; Some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp., and intracellular pathogens: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pale, Borrelia burgdorferi.

Azithromycin are not active against Gram-positive bacteria, erythromycin resistant.

Pharmacokinetics

Absorption

After taking the drug inside azithromycin is rapidly absorbed from the digestive tract, due to its stability in an acidic medium and lipophilicity. After oral dose 500 mg C_max plasma achieved through 2.5-2.9 h and is 0.4 mg / l. Bioavailability – 37.5%.

Distribution

Азитромицин быстро распределяется по всему организму, при этом в тканях достигаются высокие концентрации антибиотика. Хорошо проникает в дыхательные пути, organs and tissues of the urogenital tract (in particular, in prostate), in skin and soft tissue. High concentrations in tissues (in 10-50 times higher, than in blood plasma) and a long T_1/2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrated in a low pH environment, environmental lysosomes. It, in turn, It defines a large apparent V_d (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is particularly important for elimination of intracellular pathogens. Proved, that phagocytes deliver azithromycin to the localization of infection, where it is released in the process of phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher, than in healthy tissues (on average 24-34%) and correlate with the degree of inflammatory edema. Despite the high concentration in phagocytes, Azithromycin has no significant effect on their function.

Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatments.

Metabolism

Азитромицин метаболизируется в печени путем деметилирования с образованием неактивных метаболитов.

Deduction

Derivation of azithromycin in plasma passes 2 Phase: T_1/2 is 14-20 hours, ranging from 8 to 24 hours after dosing and 41 h - in the range of 24 to 72 no, allowing you to use the drug 1 time / day.

Выводится в основном с желчью в неизмененном виде, небольшая часть выводится почками.

Testimony

Infectious-inflammatory diseases, caused by susceptible to malaria infections:

- Infections of the upper respiratory tract and ENT (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);

- Scarlet fever;

- Infections of the lower respiratory tract (Bacterial, incl. вызванные атипичными возбудителями пневмонии, обострение хронической пневмонии, bronchitis);

- Infections of the skin and soft tissues (mug, impetigo, secondarily infected dermatitis);

- Urinary tract infections (гонорейный и негонорейный уретрит);

— инфекции женских половых органов (cervicitis);

- Lyme disease (ʙorrelioz) in the initial stage (Erythema migrans);

- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in a combination therapy).

Dosage regimen

The drug is taken orally 1 time / day for 1 hours before or after 2 hours after meals.

Adult

At infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days (dose rate- 1.5 g).

At infections of skin and soft tissue appoint 1 g / day Day 1, then 500 mg daily from the 2nd to the 5th day (dose rate- 3 g).

At uncomplicated uretrite and/or cervicitis administered once 1 g.

At Lyme disease (ʙorrelioze) for the treatment of early stage (Erythema migrans) appoint 1 g in 1 day and 500 mg daily with 2 on the 5th day (dose rate- 3 g).

At gastric ulcer and duodenal ulcer, associated with Helicobacter pylori, appoint 1 g / day for 3 days in a combination therapy of H. pylori.

Children

Препарат в форме капсул назначают older children 3 лет и/или с массой тела более 25 kg at инфекциях верхних и lower respiratory tract infection, skin and soft tissue calculated 10 mg / kg body weight 1 times / day for 3 days (kursovaya dose – 30 mg / kg), или в 1-й день – 10 mg / kg , then for 4 days – by 5-10 mg / kg / day.

When treating начальной стадии (Erythema migrans) Lyme disease (боррелиоза) the drug is prescribed in a dose 20 мг/кг в 1-й день, then 10 mg / kg from the 2nd to the 5th day.

Препарат в форме суспензии для приема внутрь назначают older children 6 months at инфекциях верхних и lower respiratory tract infection, skin and soft tissue calculated 10 mg / kg body weight 1 times / day for 3 days (kursovaya dose – 30 mg / kg), or for 5 days: 1 day – 10 mg / kg, then for 4 days – by 5-10 mg / kg / day.

Рекомендуемые дозы препарата в зависимости от массы тела ребенка представлены в таблице.

When treating начальной стадии (Erythema migrans) Lyme disease (боррелиоза) the drug is prescribed in a dose 20 мг/кг в 1-й день, then 10 mg / kg at a 2 on the 5th day.

Rules suspension for oral administration

Odnodozovyj package

В чистый стаканчик наливают небольшое количество прокипяченой и охлажденной воды, then pour out the contents of one packet and mix before reception of a homogeneous slurry. После приема стаканчик следует промыть водой, высушить и хранить в сухом и чистом месте.

Препарат АзитРус^® forte (tablets, Film-coated) appointed older children 12 years и/или с массой тела более 50 kg at infections of the upper and lower respiratory tract infections, skin and soft tissue by 500 mg 1 times / day for 3 days (dose rate- 1.5 g).

At treatment of erythema migrans in children (senior 12 years и/или с массой тела более 50 kg) АзитРус^® форте назначают по 1 г/сут в 1-й день и по 500 mg daily with 2 on the 5th day (dose rate- 3 g).

Side effect

From the digestive system: possible – diarrhea (5%), nausea (3%), abdominal pain (3%); ≤ 1% - Flatulence, vomiting, ground, cholestatic jaundice, increase in liver transaminases; у детей — запоры, decreased appetite, gastritis, candidiasis of the oral mucosa, change in taste (≤ 1%).

Cardio-vascular system: heartbeat, chest pain (≤ 1%).

CNS: dizziness, headache, drowsiness; у детей — головная боль (при лечении среднего отита), giperkineziya, anxiety, neurosis, sleep disorders (≤ 1%).

From the urinary system: jade (≤ 1%).

On the part of the reproductive system: vaginal candidiasis.

Allergic reactions: rash, hives, itching, angioedema; children – conjunctivitis, itch, hives.

Other: asthenia, photosensitivity.

Contraindications

- Renal failure;

- Liver failure;

- Lactation (breast-feeding);

- Children up to age 6 months (for suspension);

- Children up to age 3 лет и/или масса тела менее 25 kg (Capsule);

- Children up to age 12 лет и/или масса тела менее 50 kg (Pill, film-coated);

- Hypersensitivity to the drug, а также к другим макролидам.

FROM caution назначают препарат пациентам с нарушениями сердечного ритма (possible jeludockove adults, QT prolongation), детям с выраженными нарушениями функции почек или печени, Pregnancy.

Pregnancy and lactation

Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.

If necessary, use during lactation should stop breastfeeding.

Cautions

Препарат не принимают во время приема пищи.

В случае пропуска приема, пропущенную дозу следует принять как можно раньше, and subsequent – intervals 24 no.

Необходимо соблюдать перерыв не менее 2 ч между приемами препарата АзитРус^® and antacid drugs.

После отмены препарата реакции гиперчувствительности у части пациентов могут сохраняться, в таких случаях рекомендуется назначение специфической терапии под наблюдением врача.

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Drug Interactions

При одновременном применении антациды (aluminum- and magnesium-), ethanol and food slows down and reduces the absorption of azithromycin.

При совместном применении азитромицина в терапевтических дозах с варфарином изменения протромбинового времени не отмечалось, However, given the, что при взаимодействии макролидов с варфарином возможно усиление антикоагулянтного эффекта, при назначении данной комбинации пациентам необходим тщательный контроль протромбинового времени.

При одновременном применении увеличивается концентрация дигоксина в плазме крови.

При одновременном применении усиливается токсическое действие (vasospasm, dysesthesia) ergotamine and dihydroergotamine.

При одновременном применении снижается клиренс и усиливается фармакологическое действие триазолама.

Азитромицин ингибирует микросомальное окисление в гепатоцитах, что приводит к замедлению выведения и повышению концентраций в плазме и токсичности циклосерина, anticoagulants, methylprednisolone, Felodipine, as well as preparations, undergoing microsomal oxidation (Carbamazepine, terfenadine, cyclosporine, geksoʙarʙital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemics, xanthine derivatives, incl. theophylline).

Linkozaminy reduce efficacy of azithromycin.

Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life - 2 year.