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

    Composition per one tablet:

    Core:

    Active substance: azithromycin dihydrate (in terms of azithromycin) 132.489 mg (125 mg), 264.978 mg (250 mg), 529.956 mg (500 mg).

    Excipients: calcium hydrophosphate (calcium phosphate disubstituted anhydrous) 16.301 mg, 32.602 mg, 65.204 mg; hypromellose (HPMC 15 cps) 1,500 mg, 3,000 mg, 6,000 mg; cellulose microcrystalline 8,400 mg, 16,800 mg, 33,600 mg; corn starch 5,050 mg, 10,100 mg, 20,200 mg; pregelatinized starch 17,100 mg, 34,200 mg, 68,400 mg; sodium lauryl sulfate 0.610 mg, 1.220 mg, 2.440 mg; sodium croscarmellose 5,700 mg, 11,400 mg, 22,800 mg; silicon dioxide colloid (aerosil) 0.950 mg, 1.900 mg, 3.800 mg; magnesium stearate 1,900 mg, 3,800 mg, 7,600 mg.

    Sheath:

    Excipients: hypromellose (HPMC 6 cps) 3,400 mg, 6,800 mg, 13,600 mg; titanium dioxide 0.660 mg, 1.320 mg, 2.640 mg; polysorbate-80 0.140 mg, 0.280 mg, 0.560 mg; talc 2,800 mg, 5,600 mg, 11,200 mg.

    Description:Round biconvex tablets covered with a film coat of white or almost white color, on the transverse section the nucleus is almost white.
    Pharmacotherapeutic group:Antibiotic - azalide
    ATX: & nbsp

    J.01.F.A.10   Azithromycin

    Pharmacodynamics:

    Antibiotic of a wide spectrum of action. Is a representative of a subgroup of macrolide antibiotics - azalides. Communicating with 50S subunit of ribosomes, inhibits peptidranslokase at the stage of translation, inhibits protein synthesis, slows the growth and multiplication of bacteria, acts bacteriostatically, bactericidal effect at high concentrations. Effects on extracorporeal and intracellular pathogens. It is active against Gram-positive aerobic microorganisms: Streptococcus spp. (groups A, B, C, G), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Staphylococcus aureus (methicillin-sensitive); Gram-negative aerobic microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Legionella pneumophila, Neisseria gonorrhoeae, Pasteurella multocida; some anaerobic microorganisms: Prevotella spp., Clostridium perfringens, Fusobacterium spp., Porphyriomonas spp.; and Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

    Microorganisms that can develop resistance to azithromycin: gram-positive aerobes (Streptococcus pneumoniae (penicillin-resistant). Initially, resistant microorganisms: gram-positive aerobes (Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides), Gram-positive bacteria resistant to erythromycin); anaerobes (Bacteroides fragilis).

    Pharmacokinetics:

    Azithromycin is rapidly absorbed from the gastrointestinal tract, which is due to its stability in an acidic environment and lipophilicity. After oral administration of 500 mg, the maximum concentration of azithromycin in the blood plasma is achieved in 2 to 3 hours and is 0.4 mg / l. Bioavailability is 37 %.

    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 a long half-life 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 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 outbreaks 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 have a significant effect on their function. Azithromycin remains in bactericidal concentrations in the inflammatory focus within 5-7 days after the last dose, which allowed to develop 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: the half-life period is 14-20 hours in the interval from 8 to 24 hours after the drug administration and 41 hours in the interval from 24 to 72 hours, which allows using the drug once a day.

    Azithromycin is excreted mainly in unchanged form - 50% of the intestine, 6% of the kidneys.

    Indications:

    Infectious and inflammatory diseases caused by microorganisms sensitive to the preparation, including:

    - infections of the upper respiratory tract and ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media);

    - infection of the lower respiratory tract (pneumonia, including caused by atypical pathogens, bronchitis, including acute, exacerbation of chronic);

    - urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis);

    - infection of the skin and soft tissues (Lyme disease (initial stage - erythema migrans), rye, impetigo, secondary pyodermatosis, acne vulgaris (acne) of moderate severity).

    Contraindications:

    Hypersensitivity to azithromycin and other macrolides; hypersensitivity to other components of the drug; increased sensitivity to erythromycin, ketolides; a severe liver function disorder: more than 9 on the Child-Pugh scale; impairment of renal function of severe degree: creatinine clearance (CC) less than 40 ml / min; children under 3 years (for tablets 125 mg), children under 12 years of age with a body weight of up to 45 kg (for tablets 250 and 500 mg); simultaneous reception of ergotamine and dihydroergotamine.

    Carefully:

    If the liver function is mild (5-6 points on the Child-Pugh scale) and average (7-9 on the Child-Pugh scale), severity; violation of the function of the nights is mild (creatinine clearance (CC) 60-89 ml / min) and average (SC more than 40 ml / min) severity; in patients with proarrhythmogenic factors (especially in elderly patients): in patients with congenital or acquired lengthening of the interval QT, in patients with risk factors for lengthening the interval QT (receiving antiarrhythmic drugs classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, with concurrent administration of terfenadine, warfarin, digoxin, antipsychotics (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), cyclosporine: with disturbances of water-electrolyte balance, especially in case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure); with myasthenia gravis; pregnancy.

    Pregnancy and lactation:

    The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

    If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

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

    Adults and children over 12 years of age with a body weight of more than 45 kg (tablets Azithromycin 250 and 500 mg):

    In infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues (with the exception of the initial stage of Lyme disease (erythema migrans) and acne of moderate severity) - 500 mg per day for 1 reception for 3 days (exchange dose - 1.5 g).

    At the initial stage of Lyme disease (erythema migrans) - 1000 mg per day on the first day at a time, then 500 mg per day daily from 2 to 5 days (course dose - 3 g).

    With indication of acne vulgaris (acne) of moderate severity at 1. 2 and 3 days of treatment take 500 mg once a day, then take a break from the fourth and seventh day, from the eighth day of treatment take 500 mg once a week for 9 weeks. The course dose is 6.0 g.

    In cases of urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis) for the treatment of uncomplicated urethritis / cervicitis is prescribed in a dose of 1000 mg once.

    Children from 3 to 12 years with a body weight of up to 45 kg (tablets Azithromycin 125 mg): When infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - at the rate of 10 mg / kg body weight 1 time per day for 3 days.For convenience of dosing, it is suggested to use Table 1.

    Table 1. Calculation of the dose of the drug Azithromycin for children with a body weight of less than 45 kg.

    Weight

    bodies

    The dose of azithromycin (the number of tablets 125 mg)

    18-30 kt

    250 mg azithromycin (2 tablets)

    31-44 kg

    375 mg of azithromycin


    (3 tablets)

    More than 45 kg

    Apply doses recommended for adults

    With pharyngitis / tonsillitis caused by Streptococcus pyogenes - 20 mg / kg once a day for 3 days (exchange dose of 60 mg / kg). The maximum daily dose is 500 mg.

    When treating the initial stage of Lyme disease (erythema migrans) - 20 mg / kg once a day on the first day, then at the rate of 10 mg / kg once a day from 2 to 5 days (exchange dose of 60 mg / kg).

    In case of impaired renal function.

    When used in patients with mild-to-moderate dysfunction, correction of the dose is not required.

    When the liver function is impaired.

    When used in patients with impaired liver function of mild and moderate severity, dose adjustment is not required.

    Elderly patients.

    When used in elderly patients, dose adjustment is not required.

    Side effects:

    Most of the reported adverse reactions are reversible after the end of the course of treatment or discontinuation of the drug.

    Classification of the incidence of adverse events (WHO): very often (with a frequency of more than 1/10), often (with a frequency of at least 1/100 but less than 1/10), infrequently (at a frequency of at least 1/1000 but less than 1 / 100), rarely (with frequency is not less than 1/10000, but less than 1/1000), very rarely (with a frequency of less than 1/10 000), including individual messages.

    From the blood and lymphatic systems: often - lymphocytopenia, eosinophilia; infrequently - leukopenia, neutropenia; rarely - thrombocytopenia, hemolytic anemia.

    From the central nervous system: often - dizziness, headache, paresthesia, impaired perception of taste, anorexia; infrequently - anxiety, nervousness, hyposthenia, insomnia, drowsiness; rarely - agitation, delirium, hallucinations; very rarely - fainting, convulsions, psychomotor hyperactivity, aggression, anosmia, loss of taste sensations, parosmia, myasthenia gravis exacerbation, perversion of smell.

    From the sense organs: infrequently - hearing disorders, vertigo, impaired vision; unknown frequency - hearing impairment, including deafness and / or tinnitus.

    From the respiratory system and JIOP- bodies: infrequently - shortness of breath, nosebleed.

    From the cardiovascular system: infrequently - a feeling of palpitations, "tides" of blood to the face; very rarely - lowering blood pressure, arrhythmia, ventricular tachycardia, increasing the interval QT, arrhythmia of the "pirouette" type.

    Infectious diseases: infrequently - rhinitis, respiratory diseases, pharyngitis, pneumonia, candidiasis, including mucous membranes of the oral cavity and genitals, gastroenteritis.

    From the digestive system: very often - nausea, diarrhea, abdominal pain, flatulence (bloating), often - vomiting; infrequent - eructations, dysphagia, gastritis, constipation, dryness of the oral mucosa, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - a discoloration of the tongue, pseudomembranous colitis, pancreatitis.

    From the liver and bile ducts: infrequently - hepatitis, hyperbilirubinemia, increased activity of "liver" transaminases; very rarely - cholestatic jaundice, hepatic insufficiency (in rare cases, fatal, mainly on the background of a violation of liver function), fulminant hepatitis, liver necrosis.

    Allergic reactions: often - itching, rash; infrequently - Stevens-Johnson syndrome, photosensitivity,hives; rarely anaphylactic reactions (including angioedema) in rare cases with fatal outcome, toxic epidermal necrolysis. erythema multiforme.

    From the skin and subcutaneous tissues: dry skin, dermatitis, sweating.

    From the musculoskeletal system: often - arthralgia; infrequently - osteoarthritis, myalgia, pain in the neck, back pain.

    From the genitourinary system: infrequently - increased residual urea nitrogen and creatinine concentration in the blood plasma, dysuria, pain in the kidney, metrorrhagia. dysfunction of testicles; very rarely - interstitial nephritis, acute renal failure.

    Other: often - weakness; infrequently - chest pain, peripheral edema, asthenia (malaise, fatigue sensation); infrequently - swelling of the face, fever.

    Laboratory data: often - an increase in the number of basophils, monocytes, neutrophils, a decrease in the concentration of bicarbonates in the blood plasma; infrequently, an increase in the activity of alkaline phosphatase, an increase in the chlorine content, an increase in the glucose concentration, an increase in the concentration of bicarbonates in the blood plasma, an increase in the number of platelets, an increase in hematocrit, a change in the sodium content in the blood plasma, and a change in the potassium concentration in the blood plasma.

    The occurrence of any side effect should be reported to the doctor in charge.

    Overdose:

    When taking high doses of the drug, there may be an increase in side effects: temporary loss of hearing, nausea, vomiting, diarrhea. In this case, gastric lavage is shown, symptomatic therapy is performed.

    Interaction:

    Antacids (aluminum and magnesium-containing) do not affect the bioavailability of azithromycin, but reduce its maximum concentration in the blood by 30%, so the drug should be taken, but at least one hour before or two hours after taking these drugs. When combined with anticoagulants indirect effect of the coumarin series (warfarin) and azithromycin (in usual doses) patients need careful monitoring of prothrombin time. At simultaneous reception fluconazole reduces the maximum concentration of azithromycin in the blood by 18%, h that has no clinical significance.

    When used simultaneously with cyclosporine, correction of the dose of cyclosporin and monitoring of its concentration in the blood are necessary.

    With the joint administration of digoxin and azithromycin, it is necessary to control the concentration of digoxin in the blood,since many macrolides increase absorption of digoxin in the intestine, thereby increasing its maximum concentration in the blood.

    With the simultaneous administration of macrolides with ergotamine and dihydroergotamine possible manifestation of their toxic effects (vasospasm, dysesthesia) - concomitant use is contraindicated. Caution should be exercised in the joint administration of terfenadine and azithromycin, since it was found that the simultaneous use of terfenadine or cisapride and antibiotics of the macrolide class causes arrhythmia and lengthening of the interval QT. Proceeding from this, it is impossible to exclude the aforementioned complications in the joint administration of terfenadine and azithromycin. With the simultaneous administration of azithromycin and rifabutin in rare cases, the development of neutropenia, the development mechanism of which, as well as the presence of a causal relationship with the administration of the drug are not established.

    With the joint administration of azithromycin and zidovudine, azithromycin, has little effect on the pharmacokinetics, including kidney zidovudine or its glucuronide metabolite.The concentration of the active metabolite - phosphorylated zidovudine - increases in mononuclear cells of peripheral blood. The clinical significance of this fact is not determined.

    Simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentration of azithromycin in the blood plasma. Clinically significant side effects were not observed and correction of the dose of azithromycin with its simultaneous application with nelfinavir is not required. Azithromycin ns affects the concentration of carbamazepine, cimetidine (if cimetidine is used 2 hours before azithromycin). didanosine, efavirenz, indinavir, midazolam. theophylline, triazolam. trimethoprim / sulfamethoxazole. cetirizine, sildenafil, atorvastatin, rifabutin and methylprednisolone in the blood with simultaneous application.

    Separate reports of cases of rhabdomyolysis in patients concomitantly receiving azithromycin and statins.

    Azithromycin weakly interacts with cytochrome P450 isoenzymes. It was not revealed that azithromycin participates in pharmacokinetic interactions similar to erythromycin and other macrolides. Azithromycin It is not an inducer and inhibitor of cytochrome P450 isoenzymes.

    Special instructions:

    If you miss one dose of the drug - the missed dose should be taken as soon as possible, and the subsequent dose - at intervals of 24 hours.

    Azithromycin should be taken at least 1 hour before or 2 hours after taking antacid medicines.

    Azithromycin should be used with caution in patients with impaired hepatic and mild liver function due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency in such patients. In the presence of symptoms of impaired liver function (rapidly increasing asthenia, jaundice, darkening of the color of urine, a tendency to bleeding, hepatic encephalopathy) therapy with azithromycin should be discontinued and a study of the functional state of the liver.

    For renal insufficiency of mild and moderate severity, the use of azithromycin should be performed under the control of kidney function.

    Contraindicated simultaneous administration of azithromycin with derivatives of ergotamine and dihydroergotamine because of the possible development of ergotism.

    With the use of the drug, both on the background of taking and 2-3 weeks after the cessation of treatment, it is possible to develop diarrhea. caused by Clostridium difficile (pseudomembranous colitis). In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole.

    Drugs that inhibit the intestinal peristalsis are contraindicated. Since it is possible to extend the interval QT in patients receiving macrolides, including azithromycin, caution should be used with azithromycin in patients with known risk factors for lengthening the interval QT: heart disease (heart failure, myocardial infarction, bradycardia), advanced age, electrolyte imbalance (hypokalemia, hypomagnesemia), congenital lengthening interval syndrome QT, simultaneous reception of drugs that can lengthen the interval QT (including antiarrhythmics IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, fluoroquinolones).

    Azithromycin can provoke the development of myasthenic syndrome or cause an exacerbation of myasthenia gravis.

    As with the use of other antibacterial drugs, with drug therapy Azithromycin should regularly monitor patients for the presence of non-susceptible microorganisms and signs of development of superinfections, including fungal.

    A drug do not take longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple mode dosing.

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

    In the event of adverse reactions from the central nervous system, patients are advised to refrain from managing motor vehicles and practicing other potentially hazardous activities requiring increased concentration of attention, speed of psychomotor and motor reactions.

    Form release / dosage:

    Tablets, film-coated 125 mg, 250 mg and 500 mg.

    Packaging:

    For 6 tablets (for a dosage of 125 mg), for 3 or 6 tablets (for a dosage of 250 mg), 3 tablets (for a dosage of 500 mg) in a loop cell packaging made of a polyvinylchloride film and aluminum foil printed lacquer.

    1 contour cell pack of 6 tablets (for a dosage of 125 mg), 1 circuit cell pack of 3 tablets (for a dosage of 500 mg), or 1 circuit cell pack of 6 tablets or 2 contiguous cell packs of 3 tablets (for a dosage of 250 mg) together with instructions for medical use are placed in a pack of cardboard.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. At the end of the expiration date the drug should not be used.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002564
    Date of registration:06.08.2014
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp24.08.2015
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