Composition, form of production and packaging
Capsules hard gelatinous, size в„–00, with a white casing and an orange lid; the contents of the capsules are white to white powder with a yellowish hue of color.
1 caps.
azithromycin 500 mg
Excipients: microcrystalline cellulose, magnesium stearate.
Composition of the shell: gelatin, titanium dioxide, yellow "sunset sunset."
3 pcs. - packings of cellular contour (1) - 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 2012.
PHARMACHOLOGIC EFFECT
Antibiotic group of macrolides, a representative of the subgroup of azalides. Has a wide spectrum of antimicrobial action. When creating a high inflammation in the focus of inflammation has a bactericidal effect.
The drug is active against Gram-positive cocci : Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Streptococcus viridans, Staphylococcus aureus; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Campylobacter jejuni, Neisseria gonorrhoeae, Gardnerella vaginalis; anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp.
It is also active against: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Zitrolide В® forte is not active against gram-positive bacteria, resistant to erythromycin.
PHARMACOKINETICS
Suction
When ingestion azithromycin is rapidly absorbed from the digestive tract, which is due to its resistance in acidic medium and lipophilicity. After taking the drug inside at a dose of 500 mg C max azithromycin in the blood plasma is achieved through 2.5-2.96 h and is 0.4 mg / l. Bioavailability is 37%.
Distribution
Azithromycin well penetrates 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 the large 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 severity of the inflammatory process. 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 demethylated in the liver with the formation of inactive metabolites.
Excretion
Excretion of azithromycin from the blood plasma occurs 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 after taking the drug, which allows it to be taken 1 time / day.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract and ENT organs (angina, pharyngitis, sinusitis, tonsillitis, otitis media);
- infections of the lower respiratory tract (bacterial and atypical pneumonia, bronchitis);
scarlet fever;
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- infection of the genitourinary system (uncomplicated urethritis and / or cervicitis);
- Lyme disease (borreliosis) - for treatment of 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 meals or 2 hours after eating.
Adults with infections of the upper and lower respiratory tract appoint 500 mg / day for 3 days; the course dose is 1.5 g.
For infections of the skin and soft tissues, 1 g is prescribed on day 1 and 500 mg daily from day 2 to day 5 (course dose 3 g).
In acute infections of the genitourinary system (uncomplicated urethritis or cervicitis), appoint only 1 g.
In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), 1 g is prescribed on day 1 and 500 mg daily from day 2 to day 5 (course dose 3 g).
With gastric ulcer and duodenal ulcer associated with Helicobacter pylori , the drug is prescribed for 1 g / day for 3 days as part of a combination therapy.
For children, the drug is prescribed at the rate of 10 mg / kg body weight 1 time / day for 3 days or on the 1st day - 10 mg / kg, then for 4 days - 5-10 mg / kg / day (course dose - 30 mg / kg).
In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), children are prescribed at a dose of 20 mg / kg on day 1 and 10 mg / kg on day 2 to day 5.
SIDE EFFECT
On the part of the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases; in children - constipation, anorexia, gastritis.
From the cardiovascular system: palpitation, pain in the chest (? 1%).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance (? 1%).
From the genitourinary system: vaginal candidiasis, nephritis (? 1%).
Allergic reactions: rash, photosensitivity, Quincke's edema; children - conjunctivitis, itching, hives.
Other: increased fatigue.
CONTRAINDICATIONS
severe hepatic impairment;
- severe renal failure;
- the period of breastfeeding;
- children's age till 12 years;
- hypersensitivity to the components of the drug;
- hypersensitivity to other macrolides.
With caution apply the drug in pregnancy, arrhythmia (possibly the development of ventricular arrhythmias, prolongation of the QT interval), in children with severe impaired liver or kidney function.
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.
The drug is contraindicated for use during breastfeeding. If it is necessary to use Zitrolide forte during lactation, the question of stopping breastfeeding should be resolved.
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in children with severe renal dysfunction.
The drug is contraindicated in patients with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Caution should be used in children with severe impairment of liver function.
The drug is contraindicated in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
For children, the drug is prescribed at the rate of 10 mg / kg body weight 1 time / day for 3 days or on the 1st day - 10 mg / kg, then for 4 days - 5-10 mg / kg / day (course dose - 30 mg / kg).
In Lyme disease (borreliosis) for the treatment of stage I (erythema migrans), children are prescribed at a dose of 20 mg / kg on day 1 and 10 mg / kg on day 2 to day 5.
SPECIAL INSTRUCTIONS
It is necessary to observe a break of 2 hours with the simultaneous use of azithromycin with antacids.
After the drug is discontinued, hypersensitivity reactions may persist in some patients, which requires specific therapy under the supervision of a physician.
OVERDOSE
Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.
DRUG INTERACTION
Antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin.
With the simultaneous administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, but considering that the interaction of macrolides and warfarin may enhance the anticoagulant effect, patients need careful monitoring of prothrombin time.
With the simultaneous use of azithromycin with digoxin, the concentration of the latter increases.
With the simultaneous use of azithromycin with ergotamine and dihydroergotamine, the toxic effect of the latter (vasospasm, dysesthesia) is enhanced.
With the simultaneous use of azithromycin with triazolam, clearance decreases and the pharmacological action of the latter increases.
Azithromycin slows down the excretion and increases plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, and drugs undergoing microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic agents , xanthine derivatives, including theophylline) due to the azithromycin inhibition of microsomal oxidation in hepatocytes.
Lincosamines weaken the effectiveness of azithromycin.
Tetracycline and chloramphenicol increase the effectiveness of azithromycin.
Azithromycin is pharmaceutically incompatible with heparin.
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 - 3 years.
