Active substanceAzithromycinAzithromycin
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  • Dosage form: & nbspfilm coated tablets
    Composition:

    On 1 film coated tablet:

    active substance: azithromycin dihydrate 524.11 mg (equivalent to 500 mg of azithromycin);

    Excipients: [microcrystalline cellulose, sodium lauryl sulfate, crospovidone, giprolose (hydroxypropylcellulose), magnesium stearate];

    auxiliary substances for the shell of Opadrai II (series 85): [Polyvinyl alcohol; macrogol (polyethylene glycol); talc; titanium dioxide; Aluminum lacquer based on indigo carmine dye; iron oxide yellow].

    Description:

    The tablets covered with a film membrane of light blue color, biconcave, oblong form, with a risk. On the cross-section, two layers are visible, the inner layer is white or almost white.

    Pharmacotherapeutic group:Antibiotic - azalide
    ATX: & nbsp

    J.01.F.A.10   Azithromycin

    Pharmacodynamics:

    Macrolide antibiotic of wide spectrum of action, azalide, acts bacteriostatically. Communicating with 50S - a 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 aerobic Gram-positive microorganisms: Staphylo­coccus aureus (methicillin-sensitive), Streptococcus pneumonia (penicillin-sensitive), Streptococcus pyogenes;

    aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophi­lus para influenza, Legionella pneumophila, Moraxella catarrhalis, Pasteuretta multocida, Neisseria gonorrhoeae;

    some anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyromonas spp.;

    as well as other pathogens: Chlamydia trachomatis, Chlamydia pneumoniae, Chla­mydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

    Moderately sensitive or insensitive aerobic Gram-positive microorganisms - Streptococcus pneumonia (moderately sensitive or resistant to penicillin).

    Not active against aerobic Gram-positive microorganisms - Entero­coccus faecalis, Staphylococcus spp. (methicillin-resistant); anaerobic group Bacteroides fragilis, Streptococcus pneumonia, beta-hemolytic Streptococcus spp. groups A, Enterococcus faecalis and Staphylococcus aureus (including methicillin-resistant strains), resistant to erythromycin and other macrolides and lincosamides, are also resistant to azithromycin.

    Pharmacokinetics:

    Azithromycin is rapidly absorbed from the gastrointestinal tract (GIT), which is due to its resistance to acidic environment and lipophilicity. Rapidly distributed throughout the body, while in tissues are reached high concentrations of antibiotic. After oral administration of 500 mg, the maximum concentration of azithromycin in blood plasma (CmOh) is achieved in 2.5 - 2.9 hours and is 0.4 mg / l. Bioavailability is 37.5%.

    Azithromycin well penetrates the respiratory tract, organs and tissues of the urogenital tract (in particular, into the prostate gland), the skin and soft tissues. High concentration in tissues (10-50 times higher than in plasma) and a long half-life (T1/2) are due to low binding of azithromycin to blood plasma proteins, as well as its ability to penetrate eukaryotic cells and to concentrate in a medium with a low pH surrounding the lysosome. This in turn determines a large apparent volume of distribution (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 in places of infection localization, 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. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which allowed the development of short (3-day and 5-day) treatment courses.

    In the liver demethylated, the metabolites formed are not active.

    Excretion of azithromycin from the blood plasma takes place in 2 stages: T./ з is 14-20 hours in the range from 8 up to 24 hours after taking the drug and 41 hours in the range of 24 to 72 hours, which allows the drug to be used once a day.

    The drug is produced mainly, with bile in the 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 (sinusitis, tonsillitis, pharyngitis, otitis media);

    Infections of the lower respiratory tract (bacterial, including those caused by atypical pathogens, pneumonia, exacerbation of chronic bronchitis);

    Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

    Urinary tract infections (gonorrheal and non-renal urethritis, cervicitis); the initial stage of Lyme disease (borreliosis) is migratory erythema.

    Contraindications:

    Hypersensitivity (including to other macrolides); severe hepatic and / or renal failure, lactation period, children up to 12 years with a body weight less than 45 kg, simultaneous reception with ergotamine and dihydroergotamine.

    Carefully:

    -arrhythmia (possible ventricular arrhythmias and lengthening of the interval QT);

    - Moderate dysfunction of the liver or kidney;

    -The joint use of terfenadine, warfarin, digoxin.

    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 it is necessary to prescribe the drug during lactation, breastfeeding should be stopped (it is excreted in breast milk).

    Dosing and Administration:

    Inside, 1 hour before or 2 hours after meals 1 time per day.

    Adults and children over 12 years with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 0.5 g / day for 1 reception for 3 days (exchange dose - 1.5 g).

    With infections of the urogenital tract (uncomplicated urethritis or cervicitis) - once 1in

    With Lyme disease (borreliosis) for treatment of stage I (Erythema migrans) - 1 g on the first day and 0.5 g daily from 2 to 5 days (course dose - 3 g).

    Side effects:

    The incidence of adverse reactions with azithromycin is given below in accordance with the generally accepted classification:

    Often (1/10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), including individual messages.

    From the digestive tract: often - diarrhea, nausea, vomiting, pain or cramps in the abdomen; infrequently - flatulence, unformed stool, digestive disorders, anorexia; rarely - constipation, discoloration of the tongue, pseudomembranous colitis, hepatitis, cholestatic jaundice, impaired functional liver tests (increased activity of "liver" transaminases), liver necrosis and hepatic insufficiency (up to a lethal outcome).

    From the side of the nervous system, infrequently - dizziness, vertigo, drowsiness, headache, convulsions, perversion of taste and smell; rarely - paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, anxiety, nervousness.

    From the genitourinary system: infrequently - vaginitis; rarely - interstitial nephritis, acute renal failure.

    From the musculoskeletal system: infrequently - arthralgia.

    Allergic reactions: infrequent - rash, hives, itching of the skin; rarely - angioedema, anaphylactic reactions, Stevens-Johnson syndrome.

    From the sense organs: rarely - hearing loss, deafness, ringing in the ears.

    From the cardiovascular system (SSS): rarely - a feeling of heartbeat, arrhythmia (including ventricular tachycardia, pirouette tachycardia), lengthening of the interval Q-T.

    From the skin: rarely - photosensitization, erythema multiforme, toxic epidermal necrolysis.

    From the hematopoiesis: rarely - thrombocytopenia, very rarely - transient neutropenia.

    Other: rarely - candidiasis.

    Overdose:

    Symptoms of an overdose: deafness, nausea, vomiting, diarrhea.

    Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy.

    Interaction:

    Antacids (aluminum and magnesium-containing), ethanol and food slow down and reduce the absorption of azithromycin, so azithromycin should be taken 1 hour before or 2 hours after taking antacids.

    When used simultaneously with cyclosporine, the concentration in the blood should be monitored and the dose of the latter should be corrected.

    With the co-administration of warfarin and azithromycin (in usual doses), no changes in prothrombin time have been detected, however, given the interaction of macrolides and warfarin, an anticoagulant effect may increase, patients need to carefully monitor prothrombin time and the international normalized ratio (INR).

    Increases the concentration of digoxin.

    Ergotamine and dihydroergotamine: increased toxic effect (ergotism - vasospasm, dysesthesia). Simultaneous use is contraindicated.

    Triazolam: reduced clearance and increased pharmacological action of triazolam.

    Azithromycin slows down excretion and increases plasma concentrations and toxicity of cycloserine, indirect anticoagulants, methylprednisolone, felodipine, as well as drugs (LS) undergoing microsomal oxidation (carbamazepine, terfenadine, ciclosporin, hexobarbital, ergot alkaloids, valproic acid, disopyramide, bromocriptine, phenytoin, oral hypoglycemic drugs, theophylline and other xanthine derivatives), by inhibiting microsomal oxidation in hepatocytes with azithromycin.

    Lincosamines weaken, and tetracycline and chloramphenicol increase the effectiveness of azithromycin.

    Simultaneous use with rifabutin can lead to neutropenia.

    Special instructions:

    Do not take with food.

    In case of missing the dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours.

    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.

    With pharyngitis and tonsillitis caused by Streptococcus pyogenes, antibiotics of choice are penicillins. The effectiveness of azithromycin for the prevention of rheumatic fever is unknown.

    With the use of azithromycin, as well as with the use of other antibiotics, it is possible to develop superinfection (including fungal).

    Effect on the ability to drive transp. cf. and fur:

    It is necessary to refrain from activities associated with the need for high concentration of attention and rapid psychomotor reactions (including fromdriving) in the treatment Azithromycin Fort-OBL.

    Form release / dosage:Tablets, film-coated, 500 mg.
    Packaging:

    For 2, 3 or 6 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 2, 3, 4, 5 or 6 contour squares, together with the instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009004/10
    Date of registration:31.08.2010 / 11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp22.06.2017
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