AZITROKS

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, J03, J15, J15.7, J16.0, J20, J32, J35.0, J42, K25, K26, L01, L30.3, N34, N72
Manufacturer: OAO Pharmstandard-Leksredstva (Russia)

Pharmaceutical form, composition and packaging

Capsules White # 0; contents of capsules – powder white or white with a yellowish Sheen color.

Excipients: mannitol (mannyt), corn starch, magnesium stearate, sodium lauryl.

The composition of the body and cap of the capsule: Titanium dioxide (E171), Medicinal gelatine.

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

Capsules hard gelatin, # 0000, with a corps of white and yellow Cap; contents of capsules – powder white or white with a yellowish Sheen color.

Excipients: mannitol (mannyt), corn starch, magnesium stearate, sodium lauryl.

Ingredients of the capsule shell: Titanium dioxide (E171), quinoline yellow dye (E104), colorant sunset yellow (E110), Medicinal gelatine.

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

Pharmacological action

Broad-spectrum antibiotic, a representative subgroup of macrolide antibiotics - azalides. Communicating with the 50S subjedinica ribosom, oppressing peptidtranslokazu being broadcast, Suppresses protein synthesis, slowing the growth and reproduction of bacteria. Bacteriostatic, in high concentrations has a bactericidal effect. Acts on the outside- and intracellular pathogens.

It is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus Group C, F and G, Streptococcus viridans, 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 also Chlamydia trachomatis, Mycoplasma pneumoniae, 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. Once inside 500 mg azithromycin (C)_max plasma achieved through 2.5-3 h and is 0.4 mg / l. Bioavailability – 37%.

At the same time taking the drug with food slows down and reduces absorption of azithromycin.

Distribution

Azithromycin well into the respiratory tract, 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

In the liver of azithromycin demetiliruetsa, metabolites formed are inactive.

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.

Testimony

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

- Infections of the upper respiratory tract and ENT (in t. no. sore throat, sinusitis, tonsillitis, otitis media);

- Scarlet fever;

- Infections of the lower respiratory tract (in t. no. bacterial and atypical pneumonia, bronchitis);

- Infections of the skin and soft tissues (in t. no. mug, impetigo, secondarily infected dermatitis);

- Urogenitalynogo tract infections (incl. urethritis and/or zerwitzit);

- 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

Azitroks^® is inwards 1 time / day for 1 hours before or after 2 hours after meals.

Adults 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 administered at a dose of 1 g/day for 1 reception on the first day, further – by 500 mg/day every day with 2 by 5 days. Kursovaya dose – 3 g.

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

At complicated, long-term ongoing urethritis/cervicitis, caused by Chlamydia trachomatis, by 1 g 3 times at intervals of 7 days (taking drugs 1-7-14 day treatment). Kursovaya dose 3 g.

At Lyme disease (ʙorrelioze) for the treatment of stage I (Erythema migrans) appointed 1 g in 1 day and 500 mg daily from 2-5 days. 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 weighing more 45 kg at infections of the upper and lower respiratory tract infections, skin and soft tissue, scarlet fever the drug is prescribed for 500 mg / day (1 caps.) for 1 Reception for 3 days.

Children over 12 years preparation (caps. by 250 mg) appoint at 10 mg / kg 1 times / day for 3 days or the first day of – 10 mg / kg, then 4 day – by 5-10 mg / kg / day for 3 days. Kursovaya dose – 30 mg / kg.

At treatment of erythema migrans in children dose (tab. 500 mg) is 1 g in 1 day and 500 mg daily from 2-5 days. Kursovaya dose – 3 g. Use Azitroks^® in the form of tablets 250 mg dose should be – 20 mg / kg on day 1 and 10 mg / kg from the 2nd to the 5th day.

Side effect

From the digestive system: diarrhea (5%), nausea (3%), stomach ache (3%); 1% and less-dyspepsia, flatulence, vomiting, ground, cholestatic jaundice, increase in liver transaminases; children – constipation, anorexia, gastritis. Possible candidiasis mucous membranes of the oral cavity.

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

CNS: dizziness, headache, drowsiness; children – headache (for the treatment of otitis media), giperkineziya, anxiety, neurosis, sleep disorders (≤1%).

On the part of the reproductive system: ≤1% – vaginal candidiasis.

From the urinary system: ≤1% – jade.

Dermatological reactions: in some cases the rash, photosensitivity.

Allergic reactions: rash, itch, angioedema, hives, conjunctivitis.

Other: fatigue.

Contraindications

- Liver failure;

- Renal failure;

children weighing less than 45 kg (Capsule 500 mg);

- Children up to age 12 years;

- Hypersensitivity to macrolide antibiotics.

FROM caution the drug should be used with arrhythmia (possible jeludockove adults, QT prolongation), in children with acute disabilities liver or kidney disease.

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 decide the issue of termination of breastfeeding.

Cautions

Azitroks^® should not be taken with food.

If you skip the regular reception of the missed dose should be taken as soon as possible, and subsequent – intervals 24 no.

It is necessary to observe a break of at least 2 h between admission Azitroksa^® and antacid drugs.

After the treatment of hypersensitivity reactions in some patients may persist, which require a specific therapy under the supervision of a physician.

Overdose

Symptoms: in applying the drug in high doses may increase side effects – severe nausea, temporary hearing loss, vomiting, diarrhea.

Treatment: gastric lavage, appointment of activated carbon, symptomatic therapy.

Drug Interactions

Antacids (aluminum- and magnesium-), ethanol and food slows down and reduces the absorption of azithromycin.

Azithromycin is not associated with the izofermentami zitohroma P450. Unlike the majority of macrolides, Currently, no interactions of azithromycin with theophylline, terfenadine, karʙamazepinom, triazolamom, digoksinom.

Makrolidы (except azalidov) slow down and increase concentration in plasma and toxicity zikloserina, 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), through inhibition of mikrosomalnogo oxidation in gepatocitah, While in the application azalidov such interactions to date not stated.

Together with the use of azithromycin with digoxin concentrations rise last.

When concomitant administration of warfarin and azithromycin (at conventional doses) changes in prothrombin time is not revealed, However, given the, that the interaction of macrolides and warfarin may increase the anticoagulant effect, Patients should be closely monitored prothrombin time.

Together with the use of azithromycin with ergotaminom and digidroergotaminom amplified their toxic effect (vasospasm, dysesthesia).

Together with the use of azithromycin with triazolam reduced clearance and enhanced drugs triazolama.

Linkozaminy reduce efficacy of azithromycin.

Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

Pharmaceutical incompatibility

Azithromycin pharmaceutically incompatible with heparin.

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 of 15 ° to 25 ° C. Shelf life - 2 year.