2010/06/24

Azithrus

Composition, structure and packing

Gelatine capsules, yellow; content caps - white granules or nearly white.

A capsule. azithromycin (in the form of dihydrate) 250 mg.

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

The composition of gelatin capsules: titanium dioxide, metilgidroksibenzoat, propilgidroksibenzoat, acetic acid, gelatin. Powder for suspension for oral use white or nearly white, with orange odor; preparation of the suspension - a homogeneous, white with a yellowish tinge.

Clinico-pharmacological group: Antibiotic macrolide - azalid.

Pharmacological action

Broad-spectrum antibiotic of macrolides, azalid.

Valid bacteriostatic. Communicating with the 50S-subunit of ribosomes, inhibits protein synthesis and slows the growth and multiplication of bacteria. In high concentrations, has a bactericidal effect. Operates on extra-and intracellular pathogens.

It is active against Gram-positive microorganisms: Streptococcus spp. (Groups C, F and G, except for resistance to 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, Campylobacter jejuni, Neisseria gonorrhoeae and Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp., as well as intracellular pathogens: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma pneumoniae, Mycobacterium avium complex, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.

Azithromycin is not active against gram-positive bacteria resistant to erythromycin.

Pharmacokinetics

Absorption

After taking the drug inside azithromycin is rapidly absorbed from the gastrointestinal tract, due to its stability in acidic medium and lipophilicity. After receiving the oral dose of 500 mg Cmax in the plasma is achieved through 2.5-2.9 h and is 0.4 mg / liter. Bioavailability - 37.5%.

Distribution

Azithromycin is quickly distributed throughout the body, while in the tissues reached high concentrations of antibiotic. Well into the respiratory tract, organs and tissues of the urogenital tract (in particular, in the prostate gland), in skin and soft tissue. The high concentration in tissues (10-50 times higher than in blood plasma) and a long T1 / 2 due to low binding of azithromycin from plasma proteins, as well as its ability to penetrate into eukaryotic cells and concentrate in an environment with low pH, environmental lysosomes. This, in turn, defines a large apparent Vd (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. Shown that phagocytes deliver azithromycin to the localization of infection sites, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection was significantly higher than in healthy tissues (on average 24-34%) and correlated with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin did not significantly affect their function. Azithromycin remains in bactericidal concentrations of inflammation within 5-7 days after receiving the last dose, which allowed the development of short (3-day and 5-day) courses of treatment.

Metabolism

Azithromycin is metabolized in the liver by demethylation with the formation of inactive metabolites.

Withdrawal

Withdrawal of azithromycin from plasma takes place in two stages: T1 / 2 was 14-20 h in the range of 8 to 24 h after drug administration and 41 h - in the range of 24 to 72 hours, which allows to use a drug once a day. Derive mainly from the bile in unchanged form, a small part is displayed by the kidneys.

Statement

Infectious and inflammatory diseases caused by organisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (including tonsillitis, sinusitis, tonsillitis, pharyngitis, otitis media);
Infection of lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
urinary tract infection (gonorrheal urethritis and negonoreyny);
infections of the reproductive system (including cervicitis);
scarlet fever;
Lyme disease (Lyme disease) in the early stages (erythema migrans);
gastric and duodenal ulcers, associated to Helicobacter pylori (in the combined therapy).

Dosage regimen

Drugs are taken by mouth 1 time / day for 1 hour before or 2 hours after meals.

Adults

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

With infections of the skin and soft tissue appoint 1 g / day in 1 day, then 500 mg daily from 2 to 5-day (course dose - 3 g).

In uncomplicated urethritis and / or cervicitis appoint a single city

When Lyme disease (borrelia) for the treatment of early stages (erythema migrans) appoint 1 g in 1-day and 500 mg daily, from 2 to 5 days (course dose - 3 g).

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

Children

The drug in capsule form prescribed for children over 3 years and / or body weight over 25 kg in infections of the upper and lower respiratory tract, skin and soft tissue at the rate of 10 mg / kg 1 time / day for 3 days (course dose - 30 mg / kg), or 1 day - 10 mg / kg, then 4 days - at 5-10 mg / kg / day.

In the treatment of early stages (erythema migrans) Lyme disease (borreliosis), a drug administered in a dose of 20 mg / kg / day 1, followed by 10 mg / kg from 2 to 5 day.

The drug in the form of a suspension for oral designate children older than 6 months with infections of the upper and lower respiratory tract, skin and soft tissue at the rate of 10 mg / kg 1 time / day for 3 days (course dose - 30 mg / kg) or within 5 days: 1 day - 10 mg / kg, then for 4 days - by 5-10 mg / kg / day.

In the treatment of early stages (erythema migrans) Lyme disease (borreliosis), a drug administered in a dose of 20 mg / kg / day 1, followed by 10 mg / kg from 2 to 5 th day.

Terms of preparing a suspension for oral

Single-dose packet. In a clean glass pour a small amount of boiled and cooled water, then pour the contents of one packet and mix until a homogeneous suspension. When you receive the glass should be rinsed with water, dried and stored in a dry and clean place.

Side effect
On the part of the digestive system: - diarrhea (5%), nausea (3%), abdominal pain (3%); ≤ 1% - flatulence, vomiting, melena, cholestatic jaundice, increase in liver transaminases; children - constipation loss of appetite, gastritis, candidiasis of the oral mucosa, changes in taste (≤ 1%).
Since the cardiovascular system: heart, chest pain (≤ 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; in children - a headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disturbances (≤ 1%).
From the urinary system: Jade (≤ 1%).
On the part of the reproductive system: vaginal candidiasis.
Allergic reactions: rash, urticaria, pruritus, angioedema; children - conjunctivitis, pruritus, urticaria.
Other: asthenia, photosensitivity.

Contraindications
renal failure;
hepatic impairment;
lactation (breastfeeding);
Children younger than 6 months (for suspension);
Children aged 3 years and / or body weight less than 25 kg (for capsules);
Hypersensitivity to the drug's components.

With care prescribers to patients with cardiac arrhythmias (ventricular arrhythmias are possible, lengthening the interval QT), children with severe disorders of the kidneys or liver, when pregnant.

Pregnancy and lactation

Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. When necessary use during lactation should resolve the issue of termination of breastfeeding.

Application for violations of liver function

The drug is contraindicated in severe liver problems.

Application for violations of renal function

The drug is contraindicated for use with severely impaired renal function.

Cautions

The drug is not taken during the meal. In the case of missing acceptance, should take the missed dose as soon as possible, and follow - with an interval of 24 hours is necessary to observe a break of at least 2 hours between taking the drug AzitRus and antacid drugs. After discontinuation of the drug hypersensitivity reactions in some patients may persist in such cases it is recommended the appointment of a specific therapy under medical supervision.

Overdose

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

Treatment: gastric lavage, the holding of symptomatic therapy.

Drug Interactions

With simultaneous use of antacids (aluminum and magnesium), ethanol and food slow down and reduce the absorption of azithromycin.

When the joint application AzitRus at therapeutic doses with warfarin prothrombin time change is not mentioned, but considering that the interaction of macrolides with warfarin may be increased anticoagulation effect when assigning patients to this combination requires careful monitoring prothrombin time.

With the simultaneous application of increasing concentrations of digoxin in the blood plasma.

With simultaneous application of enhanced toxicity (vasospasm, dysesthesia), ergotamine and dihydroergotamine.

With simultaneous application of decreasing clearance and increasing the pharmacological effect triazolama. Azithromycin inhibits microsomal oxidation in hepatocytes, which leads to slower excretion and increase of plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipina, as well as preparations exposed to microsomal oxidation (carbamazepine, terfenadin, cyclosporine, geksobarbital, ergot alkaloids, valproic acid, dizopiramid, bromocriptine, phenytoin, oral hypoglycemic means, xanthine derivatives, including theophylline). Linkozaminy reduce the effectiveness of azithromycin. Tetracycline and chloramphenicol enhance the effectiveness of azithromycin.

Terms and Conditions of storage

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 years.