Composition, form of production and packaging
Capsules hard gelatinous, size в„–0, with a body and a lid of white color; the contents of the capsules are white powder.
1 caps.
azithromycin dihydrate (in terms of azithromycin) 250 mg
Excipients: lactose anhydrous, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
6 pcs. - blisters (1) - packs of cardboard.
6 pcs. - blisters (2) - packs of cardboard.
6 pcs. - blisters (3) - packs of cardboard.
6 pcs. - blisters (4) - packs of cardboard.
Capsules hard gelatinous, size в„–0, with a body and a lid of white color; the contents of the capsules are white powder.
1 caps.
azithromycin dihydrate (in terms of azithromycin) 500 mg
Excipients: lactose anhydrous, corn starch, sodium lauryl sulfate, magnesium stearate, titanium dioxide, purified water, methylparaben, propylparaben, gelatin.
3 pcs. - blisters (1) - packs of cardboard.
3 pcs. - blisters (2) - packs of cardboard.
3 pcs. - blisters (3) - packs of cardboard.
3 pcs. - blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
A broad-spectrum antibiotic from the macrolide group, a derivative of azalide. When creating a high inflammation in the focus of inflammation has a bactericidal effect.
It is active against gram-positive cocci: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus groups C, F and G, Staphylococcus viridans, Staphylococcus aureus; Gram-negative bacteria: Haemophilus influenzae, Moraxella catarrhalis, Bordetella pertussis, Bordetella parapertussis, Legionella pneumophila, Haemophilus ducreyi, Campylobacter jejuni, Helicobacter pylori, Neisseria gonorrhoeae, Gardnerella vaginalis; some anaerobic microorganisms: Bacteroides bivius, Clostridium perfringens, Peptostreptococcus spp .; is also active against other microorganisms: Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.
PHARMACOKINETICS
Suction
Azithromycin is rapidly absorbed from the digestive tract, which is due to its stability in acidic environment and lipophilicity. After taking Azitram inwards at a dose of 500 mg C max of azithromycin in 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 (particularly the prostate gland), 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 severity 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
In the liver, it is demethylated 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 range from 8 hours to 24 hours after taking the drug and 41 hours in the range from 24 hours to 72 hours, which allows the drug to be applied once / day.
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);
- 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 urogenital tract (gonorrheal urethritis and / or cervicitis);
- Lyme disease (borreliosis) - for treatment of the initial stage (erythema migrans);
- Stomach ulcer and duodenal ulcer associated with Helicobacter pylori (as part of combination therapy).
DOSING MODE
The drug is taken 1 time / day for 1 hour before meals or 2 hours after meals.
In infections of the upper and lower respiratory tract, adults are prescribed 500 mg / day in 1 dose for 3 days; the course dose is 1.5 g.
For infections of the skin and soft tissues, adults are prescribed 1 g in the first day in a single dose; further - on 500 mg in 1 reception daily from 2nd on 5th days; the course dose is 3 g.
With uncomplicated urethritis and / or cervicitis, appoint 1 g once in a single dose.
In Lyme disease (borreliosis) for the treatment of the initial stage (erythema migrans), 1 g is prescribed on the first day and 500 mg in 1 dose every day from the 2nd to the 5th day (the course dose is 3 g).
With gastric ulcer and duodenal ulcer associated with Helicobacter pylori , the drug is prescribed for 1 g / day for 3 days as a combination of anti-Helicobacter therapy.
For children, the drug is prescribed at the rate of 10 mg / kg of body weight 1 time / day for 3 days or on the 1st day - 10 mg / kg, then for 3 days - 5-10 mg / kg / day (the exchange dose is determined at the rate of 30 mg / kg). In the treatment of erythema migrans, the dose is 20 mg / kg on day 1 and 10 mg / kg from day 2 to day 5.
SIDE EFFECT
On the part of the digestive system: nausea (3%), diarrhea (5%), abdominal pain (3%); dyspepsia, vomiting, flatulence, melena, cholestatic jaundice, increased activity of hepatic transaminases (1% or less). Children - constipation, anorexia, gastritis.
From the cardiovascular system: palpitation, chest pain (1% or less).
From the side of the central nervous system: headache, dizziness, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance (1% or less).
From the genitourinary system: nephritis, vaginal candidiasis (1% or less).
Allergic reactions: rash, photosensitivity, Quincke's edema.
Other: increased fatigue, candidomycosis of the oral cavity; children - conjunctivitis, itching, hives.
CONTRAINDICATIONS
- kidney failure;
- liver failure;
- lactation period (breastfeeding);
- Children's age up to 12 months;
- hypersensitivity to azithromycin and other antibiotics of the macrolide group.
Be wary when arrhythmia (possible ventricular arrhythmia and lengthening of the QT interval), pregnancy, as well as children with severe impaired liver or kidney function.
PREGNANCY AND LACTATION
In pregnancy, Azitral can be used when the intended benefit of such therapy is significantly greater than the risk that exists when using medicines during pregnancy.
When prescribing the drug during lactation, breastfeeding should be suspended for the duration of treatment.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated for use in renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated for use in liver failure.
APPLICATION FOR CHILDREN
Contraindication: children under 12 months.
SPECIAL INSTRUCTIONS
If missed, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at 24-hour intervals.
It should be borne in mind that after the withdrawal of the drug allergic reactions in some patients may persist, which requires appropriate therapy and medical supervision.
Between the administration of Azitral and antacid preparations it is recommended to observe a break of at least 2 h.
OVERDOSE
Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.
Treatment: symptomatic therapy.
DRUG INTERACTION
Antacids (aluminum and magnesium-containing), ethanol, food slow down and reduce the absorption of azithromycin.
With the combined use of warfarin and Azitral in recommended doses, no changes in prothrombin time have been detected, however, considering that the interaction of macrolides and warfarin may increase the anticoagulant effect, prothrombin time control is necessary.
When combined, azithromycin increases the concentration of digoxin.
With the simultaneous use of azithromycin increases the toxic effect of ergotamine and dihydroergotamine (vasospasm and dysesthesia).
When combined, azithromycin slows the excretion and enhances the pharmacological effects of triazolam.
When combined, azithromycin slows the excretion, increases the concentration in the blood plasma and increases the toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine.
Azithromycin, by inhibiting microsomal oxidation in hepatocytes, slows down excretion, increases serum concentrations and increases the toxicity of carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, phenytoin, disopyramide, bromocriptine, theophylline (and other xanthine derivatives), oral hypoglycemic agents .
When combined, lincosamines weaken the effectiveness of azithromycin, and tetracyclines and chloramphenicol are enhanced.
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 place at a temperature of no higher than 25 В° C. Shelf life - 3 years.
