Composition, form of production and packaging
Capsules number 0, with a white body and an orange-yellow or yellow lid; the contents of the capsules are white to white powder with a creamy shade of color.
1 caps.
azithromycin 250 mg
Excipients: magnesium stearate, microcrystalline cellulose.
The composition of the capsule shell: gelatin, titanium dioxide, quinoline yellow, azorubin, ponso 4R.
6 pcs. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2008.
PHARMACHOLOGIC EFFECT
Antibiotic group of macrolides, is 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, Helicobacter pylori, Legionella pneumophila, Haemophilus ducreyi, 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 is not active against Gram-positive bacteria, resistant to erythromycin.
PHARMACOKINETICS
Suction
When administered orally, azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment 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 range 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 makes it possible to apply it 1 time / day.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infections of the upper respiratory tract and ENT organs (including angina, pharyngitis, sinusitis, tonsillitis, otitis media);
- infections of the lower respiratory tract (including bacterial and atypical pneumonia, bronchitis);
scarlet fever;
- infections of the skin and soft tissues (including erysipelas, impetigo, secondarily infected dermatoses);
- infections of the genitourinary system (including 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
Zitrolide and Citrolide Forte are 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.
Children Zitrolid and Zitrolid Forte are 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 in for 3 days (the course dose is 30 mg / kg).
With Lyme disease (borreliosis), the children are prescribed a dose of 20 mg / kg on day 1 and 10 mg / kg from day 2 to day 5 for treatment of the initial stage of erythema migrans .
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, a change in taste (? 1%).
From the cardiovascular system: a feeling of heartbeat, 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; in children (? 1%) - conjunctivitis, itching, urticaria.
CONTRAINDICATIONS
hepatic failure of severe degree;
- severe renal failure;
- lactation period (breastfeeding);
- children's age till 3 years;
- Hypersensitivity to azithromycin or other macrolides.
With caution apply the drug in pregnancy, arrhythmia (possibly the development of ventricular arrhythmias and prolongation of the QT interval), in children with severe impaired liver or kidney function.
PREGNANCY AND LACTATION
In pregnancy, Zitrolide and Sietrolide Forte should be used with caution and in cases where the expected benefit of therapy for the mother significantly exceeds the potential risk to the fetus.
The drug is contraindicated for use during lactation (breastfeeding). If it is necessary to use Zietrolide and Sietrolide Forte during lactation during treatment, breastfeeding should be suspended.
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.
SPECIAL INSTRUCTIONS
It is necessary to observe a break of 2 hours with the simultaneous use of antacids.
After the withdrawal of the treatment, hypersensitivity reactions in some patients may persist, which requires specific therapy under the supervision of a physician.
OVERDOSE
Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.
Treatment: withdrawal of the drug, symptomatic therapy.
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.
When combined with digoxin, the concentration of digoxin increases.
With simultaneous use with ergotamine and dihydroergotamine, their toxic effect (vasospasm, dysesthesia) is enhanced.
With simultaneous use with triazolam, clearance decreases and the pharmacological action of triazolam is enhanced.
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.
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. The expiration date of Zitrolid - 3 years, Zitrolida forte - 2 years.
