Composition, form of production and packaging
Capsules of gelatinous, yellow color, в„–0; the contents of the capsules are granules of white or almost white color.
1 caps.
azithromycin (in the form of dihydrate) 250 mg
Excipients: povidone (polyvinylpyrrolidone), calcium stearate, microcrystalline cellulose.
The composition of gelatin capsules: titanium dioxide, methylhydroxybenzoate, propylhydroxybenzoate, acetic acid, gelatin.
6 pcs. - packings of cellular contour (1) - packs cardboard.
Powder for the preparation of a suspension for ingestion of white or almost white, with an orange smell; The prepared suspension is homogeneous, white with a yellowish tinge.
1 pack.
azithromycin (in the form of dihydrate) 50 mg
- "- 100 mg
- "- 200 mg
Excipients: sodium citrate (sodium citric acid trisubstituted), orange flavored food, sodium saccharinate, collidone CL-M (crospovidone), sucrose.
4.2 g - single dose packages (3) - cardboard packs.
4.2 g - packs of single-dose (6) - packs of cardboard.
4.2 g - single dose packages (3) complete with a glass - packs of cardboard.
4.2 g - single dose packages (6) complete with a glass - packs of cardboard.
AzitRus В® forte
The tablets covered with a film membrane white or white with a yellowish shade of color, are oval.
1 tab.
azithromycin (in the form of dihydrate) 500 mg
Excipients: calcium stearate, starch 1500, potato starch, crospovidone (clolidon CL-M), povidone (polyvinylpyrrolidone), lactose, talc, microcrystalline cellulose.
Sheath composition: hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene oxide 4000, polyethylene glycol 4000), titanium dioxide (titanium dioxide).
3 pcs. - packings of cellular contour (1) - packs cardboard.
3 pcs. - packings cellular planimetric (2) - packs cardboard.
6 pcs. - packings of cellular contour (1) - packs cardboard.
3 pcs. - polymer cans (1) - packs of cardboard.
6 pcs. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
A broad-spectrum antibiotic of the macrolide group, azalide. It acts bacteriostatically. Linking to the 50S-subunit of the ribosome, suppresses protein synthesis, slows the growth and multiplication of bacteria. In high concentrations has a bactericidal effect. Effects on extracorporeal and intracellular pathogens.
It is active against gram-positive microorganisms : Streptococcus spp. (groups C, F and G, other than erythromycin-resistant), 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 asintracellular 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
Suction
After taking the drug inside, azithromycin is rapidly absorbed from the digestive tract, which is due to its stability in acidic medium and lipophilicity. After oral administration at a dose of 500 mg C max in plasma is achieved through 2.5-2.9 hours and is 0.4 mg / l. Bioavailability is 37.5%.
Distribution
Azithromycin is rapidly distributed throughout the body, with high concentrations of antibiotic in tissues. It penetrates well into the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), into the skin and soft tissues. High concentrations in tissues (10-50 times higher than in plasma) and long T 1/2 are due to low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and concentrate in a medium with a low pH surrounding the lysosome . This, in turn, determines a large apparent V d (31.1 l / kg) and high plasma clearance. The ability of azithromycin to accumulate mainly in lysosomes is especially important for the elimination of intracellular pathogens. It is proved that phagocytes deliver azithromycin to the site of infection, where it is released during phagocytosis. The concentration of azithromycin in the foci of infection is significantly higher than in healthy tissues (an average of 24-34%) and correlates with the degree of inflammatory edema. Despite the high concentration in phagocytes, azithromycin does not significantly affect their function.
Azithromycin is retained in bactericidal concentrations in the inflammatory focus within 5-7 days after administration of the last dose, which allowed the development of short (3-day and 5-day) treatment courses.
Metabolism
Azithromycin is metabolized in the liver by demethylation with the formation of inactive metabolites.
Excretion
Excretion of azithromycin from the blood plasma takes place in 2 stages: T 1/2 is 14-20 hours in the interval from 8 to 24 hours after taking the drug and 41 hours in the interval from 24 to 72 hours, which allows using the drug once a day.
It is excreted mainly with bile in unchanged form, a small part is excreted by the kidneys.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);
scarlet fever;
- Infections of the lower respiratory tract (bacterial, including those caused by atypical pathogens of pneumonia, exacerbation of chronic pneumonia, bronchitis);
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- urinary tract infections (gonorrheal and non-renal urethritis);
- infection of female genital organs (cervicitis);
- Lyme disease (borreliosis) in the initial stage (erythema migrans);
- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in combination therapy).
DOSING MODE
The drug is taken orally 1 time / day for 1 hour before or 2 hours after a meal.
Adults
When infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days (exchange dose - 1.5 g).
For skin and soft tissue infections , 1 g / day is prescribed on the first day, then 500 mg daily from day 2 to day 5 (course dose 3 g).
With uncomplicated urethritis and / or cervicitis, appoint only 1 g.
In Lyme disease (borreliosis) for the treatment of the initial stage (erythema migrans) appoint 1 g in the first day and 500 mg daily from day 2 to day 5 (course dose - 3 g).
With gastric ulcer and duodenal ulcer associated with Helicobacter pylori , appoint 1 g / day for 3 days as a combination of anti-Helicobacter therapy.
Children
The preparation in the form of capsules is prescribed for children older than 3 years and / or with a body weight of more than 25 kg with infections of the upper and lower divisions of the respiratory tract, skin and soft tissues at the rate of 10 mg / kg of body weight 1 time / day for 3 days (course dose - 30 mg / kg), or on the first day - 10 mg / kg, then for 4 days - 5-10 mg / kg / day.
In the treatment of the initial stage (erythema migrans) of Lyme disease (borreliosis), the drug is prescribed at a dose of 20 mg / kg on the first day, then 10 mg / kg on the 2nd to the 5th day.
The drug in the form of a suspension for ingestion is prescribed for children older than 6 months with infections of the upper and lower divisions of the respiratory tract, skin and soft tissues at the rate of 10 mg / kg of body weight 1 time / day for 3 days (exchange dose - 30 mg / kg) , or for 5 days: on the 1st day - 10 mg / kg, then for 4 days - 5-10 mg / kg / day.
The recommended dosage of the drug, depending on the weight of the child, is shown in the table.
Body weight Daily average (single) dose
Powder for the preparation of a suspension of 100 mg / 5 ml
5 kg 2.5 ml (50 mg)
6 kg 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)
Powder for the preparation of a suspension of 200 mg / 5 ml
15-24 kg 5 ml (200 mg)
25-34 kg 7.5 ml (300 mg)
35-44 kg 10 ml (400 mg)
> 45 kg prescribe doses for adults (500-1000 mg)
In the treatment of the initial stage (erythema migrans) of Lyme disease (borreliosis), the drug is prescribed at a dose of 20 mg / kg on the first day, then 10 mg / kg on the 2nd to the 5th day.
The preparation AzitRus В® forte (film-coated tablets) is prescribed for children older than 12 years and / or with a body weight of more than 50 kg for infections of the upper and lower respiratory tract, skin and soft tissues 500 mg 1 time / day for 3 days a dose of 1.5 g).
In the treatment of erythema migrans in children (over 12 years of age and / or with a body weight of more than 50 kg), AzithRus В® forte is prescribed 1 g / day on day 1 and 500 mg daily from day 2 to day 5 dose - 3 g).
Rules for the preparation of oral suspension
Single-dose package
A small amount of boiled and cooled water is poured into a clean glass, then the contents of one packet are poured and mixed until a homogeneous suspension is obtained. After the reception, the glass should be washed with water, dried and stored in a dry and clean place.
SIDE EFFECT
From the digestive system: possible - diarrhea (5%), nausea (3%), abdominal pain (3%); 1% - meteorism, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases; in children - constipation, decreased appetite, gastritis, candidiasis of the oral mucosa, a change in taste (? 1%).
From the cardiovascular system: palpitations, pain in the chest (? 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headache (in the treatment of otitis media), hyperkinesia, anxiety, neurosis, sleep disorders (? 1%).
From the urinary system: nephritis (? 1%).
On the part of the reproductive system: vaginal candidiasis.
Allergic reactions: rash, hives, itching, angioedema; children - conjunctivitis, itching, hives.
Other: asthenia, photosensitization.
CONTRAINDICATIONS
- kidney failure;
- liver failure;
- lactation (breastfeeding);
- Children's age up to 6 months (for suspension);
- Children under 3 years of age and / or body weight less than 25 kg (for capsules);
- Children under 12 years of age and / or body weight less than 50 kg (for film-coated tablets);
- Hypersensitivity to the components of the drug, as well as to other macrolides.
Caution is prescribed to patients with heart rhythm disorders (ventricular arrhythmias, prolongation of the QT interval), children with severe renal or hepatic impairment, during pregnancy.
PREGNANCY AND LACTATION
The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.
If you need to use the drug during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated for use in severe disorders of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated for use in severe violations of liver function.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 6 months (for suspension); in children under 3 years of age and / or with a body weight of less than 25 kg (for capsules); in children under 12 years of age and / or with a body weight of less than 50 kg (for film-coated tablets).
Caution is prescribed to children with severe impairment of kidney or liver function.
SPECIAL INSTRUCTIONS
The drug is not taken during meals.
In case of missed admission, the missed dose should be taken as soon as possible, and the subsequent dose at the 24 hour interval.
It is necessary to observe a break of at least 2 h between the administration of the drug AzitRus В® and antacid preparations.
After the drug has been withdrawn, hypersensitivity reactions may persist in some patients, in such cases it is recommended that specific therapy be administered under the supervision of a physician.
OVERDOSE
Symptoms: nausea, temporary loss of hearing, vomiting, diarrhea.
Treatment: gastric lavage, symptomatic therapy.
DRUG INTERACTION
With simultaneous use of antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin.
With joint use of azithromycin in therapeutic doses with warfarin, there was no change in prothrombin time, but considering that the interaction of macrolides with warfarin may enhance the anticoagulant effect, when this combination is prescribed, patients need careful monitoring of prothrombin time.
With simultaneous use, the concentration of digoxin in the blood plasma increases.
With simultaneous use, the toxic effect (vasospasm, dysesthesia) of ergotamine and dihydroergotamine is enhanced.
With simultaneous use, clearance decreases and the pharmacological action of triazolam is enhanced.
Azithromycin inhibits microsomal oxidation in hepatocytes, which leads to a delay in excretion and increase in plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and also drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents, xanthine derivatives, including theophylline).
Lincosamines reduce the effectiveness of azithromycin.
Tetracycline and chloramphenicol increase the effectiveness of azithromycin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 2 years. Shelf life of AzitrusВ® forte tablets is 3 years.
