Composition, form of production and packaging
The tablets covered with a cover of light pink color, oblong, biconcave; On the cross-section, two layers are visible: the inner layer is white or almost white.
1 tab.
azithromycin (in the form of dihydrate) 500 mg
Excipients: calcium phosphate dihydrate - 77.2 mg, sodium lauryl sulfate - 1.3 mg, povidone (polyvinylpyrrolidone) - 39 mg, crospovidone (polyplasdone X-El-10) - 19.5 mg, magnesium stearate - 13 mg.
Sheath composition: hypromellose (hydroxypropylmethylcellulose) 4.33 mg, titanium dioxide 0.94 mg, povidone (polyvinylpyrrolidone) 2.6776 mg, talc 1.11 mg, polysorbate 80 (twin 80) 0.94 mg, dye azorubin (carmoazine) 0.0024 mg .
3 pcs. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Antibiotic of broad spectrum of action of the group of azalides. When creating a high inflammation in the focus of inflammation has a bactericidal effect.
Gram-positive cocci are sensitive to azithromycin : Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, group C, F and G streptococci, Staphylococcus aureus, Staphylococcus viridans; 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. It is active against Chlamydia trachomatis, Mycoplasma pneumoniae, Ureaplasma urealyticum, Treponema pallidum, Borrelia burgdoferi.
Azithromycin is inactive against gram-positive bacteria resistant to erythromycin.
PHARMACOKINETICS
Suction
After oral administration, azithromycin is rapidly absorbed from the digestive tract, which is due to its resistance to acidic environment and lipophilicity. After taking 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 (10-15 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
In the liver demethylated, the metabolites formed are active.
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.
INDICATIONS
Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:
- infection of the urogenital tract (uncomplicated urethritis and / or cervicitis);
- infections of the upper respiratory tract and ENT organs (sore throat, sinusitis, tonsillitis, pharyngitis, otitis media);
scarlet fever;
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans);
- Diseases of the stomach and duodenum, associated with Helicobacter pylori (in combination therapy).
DOSING MODE
Inside for 1 hour or 2 hours after eating 1 time / day.
Adults with infections of the upper and lower respiratory tract - 500 mg / day for 1 reception for 3 days (exchange dose - 1.5 g).
With infections of the skin and soft tissues - 1 g / day on the first day for 1 reception, then 500 mg / day daily from the 2nd to the 5th day (the course dose is 3 g).
In acute infections of the urogenital organs (uncomplicated urethritis or cervicitis) once 1 g.
With Lyme disease (borreliosis) for the treatment of the initial stage (erythema migrans) - 1 g on 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 , 1 g / day for 3 days as a combination of anti-Helicobacter therapy.
Children are prescribed at the rate of 10 mg / kg 1 time / day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day for 3 days (exchange dose - 30 mg / kg).
In the treatment of erythema migrans in children, the dose is 20 mg / kg on the first day and 10 mg / kg from day 2 to day 5.
SIDE EFFECT
On the part of the digestive system: diarrhea (5%), nausea (3%), abdominal pain (3%); 1% or less - dyspepsia, flatulence, vomiting, melena, cholestatic jaundice, increased activity of hepatic transaminases; in children - constipation, anorexia, gastritis.
From the cardiovascular system: palpitation, chest pain (1% or less).
From the side of the central nervous system: dizziness, headache, drowsiness; children - headache (with medication otitis media), hyperkinesia, anxiety, neurosis, sleep disturbance (1% or less).
From the genitourinary system: vaginal candidiasis, nephritis (1% or less).
Allergic reactions: rash, photosensitivity, Quincke's edema.
Other: increased fatigue; children - conjunctivitis, itching, hives.
CONTRAINDICATIONS
- liver failure;
- kidney failure;
- Lactation period (for the duration of treatment, they are suspended);
- Children's age up to 12 months;
- Hypersensitivity to azithromycin or other macrolides.
Carefully
- Pregnancy (can be used when the benefit from its use significantly exceeds the risk that exists always when using any drug during pregnancy);
- Arrhythmia (ventricular arrhythmias and QT interval prolongation are possible);
- marked violations of the liver or kidney in children.
PREGNANCY AND LACTATION
In pregnancy, azithromycin 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).
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated in renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in case of liver failure.
APPLICATION FOR CHILDREN
The drug is contraindicated in children under 12 months.
With caution, use the drug for children with severe impaired liver or kidney function.
Children are prescribed at the rate of 10 mg / kg 1 time / day for 3 days or on the first day - 10 mg / kg, then 4 days - 5-10 mg / kg / day for 3 days (exchange dose - 30 mg / kg).
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.
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 moderate doses), no changes in prothrombin time have been detected, however, considering that the interaction of macrolides and warfarin may enhance 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, toxic action (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 that undergo microsomal oxidation (carbamazepine, terfenadine, cyclosporine, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic means, xanthine derivatives, including theophylline) due to the azithromycin inhibition of microsomal oxidation in hepatocytes.
Lincosamides 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
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 3 years.
Do not use after the expiration date.
