Active substanceAzithromycinAzithromycin
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  • Dosage form: & nbspcapsules
    Composition:

    1 capsule contains the active substance - azithromycin (in the form of azithromycin dihydrate - 262.03 mg) - 250 mg.

    Excipients: lactose anhydrous - 163,60 mg * (151,57 mg), corn starch - 47,00 mg, sodium lauryl sulfate - 0,94 mg, magnesium stearate - 8,46 mg,

    composition shell capsules: titanium dioxide E 171 - 1.44 mg, the dye patented blue V E 131 - 0.0164 mg, gelatin - up to 96 mg.

    * The amount of lactose anhydrous depends on the activity of the active substance.

    Description:Hard gelatin capsule of light blue color. Contents of the capsules: white powder.

    Pharmacotherapeutic group:Antibiotic-azalide
    ATX: & nbsp

    J.01.F.A.10   Azithromycin

    Pharmacodynamics:

    Azithromycin is a bacteriostatic broad-spectrum antibiotic from the group of macrolides-azalides. It has a wide spectrum of antimicrobial action. The mechanism of action of azithromycin is associated with the suppression of protein synthesis of a microbial cell. Communicating with 50S- subunit of the ribosome, inhibits peptidranslokase at the stage of translation and suppresses protein synthesis, slowing the growth and multiplication of bacteria. In high concentrations has a bactericidal effect.

    It has activity against a number of gram-positive, gram-negative, anaerobic, intracellular and other microorganisms.

    Microorganisms may initially be resistant to the action of the antibiotic or may acquire resistance to it.

    Scale sensitivity microorganisms to azithromycin:

    Microorganism

    Y

    MIC *, mg / l

    Sensitive

    Sustainable

    Staphylococcus

    <1

    >2

    Streptococcus A, AT, C, G

    <0,25

    >0,5

    Streptococcus

    pneumoniae

    <0,25

    >0,5

    Haemophilus

    influenzae

    <0,12

    >4

    Moraxella

    catarrhalis

    <0,5

    >0,5

    Neisseria

    gonorrhoeae

    <0,25

    >0,5

    * Minimum inhibitory concentration

    In most cases, azithromycin is sensitive:

    Aerobic Gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Streptococcus agalactiae, streptococcus groups C, G;

    aerobic gram-negative microorganisms: Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae;

    anaerobic microorganisms: Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp., Peptostreptococcus spp.;

    other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci. Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi. Microorganisms with acquired resistance to azithromycin: Streptococcus pneumoniae (penicillin-resistant).

    Microorganisms, initially resistant:

    aerobic Gram-positive microorganisms: Enterococcus faecalis, Staphylococcus spp. (methicillin-resistant staphylococci with very high frequency have acquired 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 after 2.5 - 2.96 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 concentration in tissues (in 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 to 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 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 have a significant effect on their function. Azithromycin remains in bactericidal concentrations for 5-7 days after the last dose, which allowed to develop short (3-day and 5-day) treatment courses.

    The liver is demethylated. the metabolites formed are not active.

    In azithromycin, a very long half-life is 35-50 hours. The half-life of the tissues is significantly more.

    The drug is produced mainly with bile in the unchanged form, a small part of the kidneys.

    Indications:

    Infectious-inflammatory diseases caused by susceptible azithromycin by microorganisms:

    - 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, acute bronchitis, exacerbation of chronic bronchitis);

    - infections of the skin and soft tissues (acne vulgar mild, rye, impetigo, secondarily infected dermatoses);

    - urogenital tract infections (urethritis and / or cervicitis) caused by Chlamydia trachomatis;

    - Lyme disease (borreliosis), for the treatment of the initial stage (erythema migrans).

    Contraindications:

    - hypersensitivity to azithromycin or other components of the drug;

    - increased sensitivity to erythromycin, other macrolides, ketolides;

    - violations of liver function of a serious degree;

    - impaired renal function of severe degree (creatinine clearance less than 40 ml / min);

    - simultaneous reception with ergotamine, dihydpoepgotamin;

    - the period of breastfeeding;

    - Children under 12 years old with a body weight of up to 45 kg;

    - Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the preparation contains lactose).

    Carefully:Myasthenia gravis, liver function disorders of mild and moderate severity, dysfunction of mild to moderate light nights (creatinine clearance more than 40 ml / min),in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired lengthening of the interval QT, in patients receiving antiarrhythmic drug therapy classes IA (quinidine, procainamide) and III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin and levofloxacin), with disturbances of water-electrolysis balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia or severe heart failure; simultaneous use of digoxin, warfarin, cyclosporine; pregnancy.
    Pregnancy and lactation:

    In pregnancy, it can be used when the benefits of using it significantly exceed the risk that exists always when using any drug during pregnancy. If you need to use the drug during lactation, breastfeeding is suspended.

    Dosing and Administration:

    Azithromycin should be taken 1 hour before meals or 2 hours after meals. The drug is taken 1 time / day.

    Adults and children over 12 years of age with a body weight of over 45 kg: for upper and lower respiratory infections, ENT-organs prescribe but 500 mg / day (2 capsules) 1 time per day for 3 days (course dose - 1.5 g).

    With infections of rut and soft tissue prescribe 500 mg (2 capsules) 1 time per day for 3 days (the course dose is 1.5 g).

    With acne vulgaris of moderate severity: on days 1, 2 and 3 of treatment take 500 mg (2 capsules, 250 mg) once a day, then take a break from the fourth to the seventh day, from the eighth day of treatment take 500 mg once a week (with an interval of 7 days) for 9 weeks. The course dose is 6 g.

    When uncomplicated urethritis and / or cervicitis, caused by Chlamydia trachomatis appoint once 1 g (4 caps, 250 mg each).

    When Lyme disease (borreliosis / for treatment of the initial stage (erythema migrans) appoint 1 g (4 caps, 250 mg) on ​​the first day and 500 mg daily from the 2nd to the 5th day (the course dose is 3 g).

    If you miss a dose of 1 dose, the missed dose should be taken as soon as possible, and the subsequent dose - with a break of 24 hours.

    Patients with impaired renal function

    When used in patients with impaired renal function of mild and moderate severity (creatinine clearance > 40 ml / min) dose adjustment is not required.

    Patients with impaired hepatic function

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

    Elderly patients

    In elderly patients, dose adjustment is not required.

    Side effects:

    The frequency of side effects is classified according to the recommendations of the World Health Organization: very often - no less than 10%, often less than 1%, but less than 10%, infrequently - not less than 0.1%, but less than 1%, rarely - not less than 0.01%, but less than 0.1%, very rarely - less than 0.01%; The unknown frequency can not be estimated from the available data.

    Infectious diseases: infrequently - candidiasis, including mucous membranes of the oral cavity and genitals, pneumonia, pharyngitis, gastroenteritis, respiratory diseases, rhinitis; an unknown frequency is pseudomembranous colitis.

    From the side of the blood and lymphatic system: infrequently - leukopenia, neutropenia, eosinophilia; very rarely - thrombocytopenia, hemolytic anemia.

    From the side of metabolism and nutrition: infrequently - anorexia.

    Allergic reactions: infrequently angioedema, hypersensitivity reaction; an unknown frequency is an anaphylactic reaction.

    From the nervous system: often - headache; infrequently - dizziness, dyspnoea, paresthesia, drowsiness, insomnia, nervousness; rarely - agitation; unknown frequency - hypesthesia, anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell, perversion of smell, loss of taste sensations, myasthenia gravis, delirium, hallucinations.

    From the side of the organ of vision: infrequently - impaired vision.

    From the side of the hearing organ and labyrinthine disorders: infrequently - hearing disorder, vertigo; unknown frequency - hearing impairment, including deafness and / or tinnitus.

    From the cardiovascular system: infrequently - a feeling of palpitations, "tides" of blood to the face; unknown frequency - lowering blood pressure, increasing the interval QT on an electrocardiogram, arrhythmia such as "pirouette", ventricular tachycardia.

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

    From the side gastrointestinal tract: very often diarrhea; often - nausea, vomiting, abdominal pain; infrequent - meteorism, dyspepsia, constipation, gastritis, dysphagia, bloating, dryness of the oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands; very rarely - a discoloration of the tongue, pancreatitis.

    From the liver and bile ducts: infrequently - hepatitis; rarely a violation of the liver, cholestatic jaundice; unknown frequency - hepatic insufficiency (in rare cases with a legal outcome mainly against a background of severe impairment of liver function); liver necrosis, fulminant hepatitis.

    From the skin and subcutaneous tissues: infrequently - skin rash, itching, hives, dermatitis, dry skin, sweating; rarely - the reaction of photosensitization; unknown frequency - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme.

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

    From the side of the kidneys and urinary tract: infrequently - dysuria, pain in the kidney; unknown frequency - interstitial nephritis, acute renal failure.

    From the genitals and breast: infrequently - metrorrhagia, dysfunction of testicles.

    Other: infrequently - asthenia, malaise, fatigue, face swelling, chest pain, fever, peripheral edema.

    Laboratory data: often a decrease in the number of lymphocytes,increasing the number of eosinophils, basophils increase amount, increasing the number of monocytes, increased neutrophil count, reduced bicarbonate concentration in the blood plasma; infrequently - increased activity aspartate aminotransferase, alanine aminotransferase, increasing the concentration of bilirubin in blood plasma, increasing concentrations of urea in the blood plasma, increased plasma concentrations of creatinine, the change of potassium content in the blood plasma, increased alkaline phosphatase activity in plasma, increasing chlorine content in the blood plasma, increased glucose concentration in blood, an increase in the number of platelets, increase of hematocrit, increase of bicarbonate concentration in blood plasma, change of sodium content in blood plasma.

    Overdose:

    Symptoms: severe nausea, temporary loss of hearing, vomiting, diarrhea.

    Treatment: gastric lavage, symptomatic treatment.

    Interaction:

    Antacids (aluminum and magnesium-containing) do not affect bioavailability of azithromycin, but reduce its maximum blood concentration of approximately 25%, so the drug should be taken at least one hour before or two hours after taking these drugs. Food slows down and reduces absorption.

    When combined with anticoagulants indirect effect of the coumarin series (warfarin) may increase the anticoagulant effect; patients need careful monitoring of prothrombin time.

    Digoxin: possible increase digoxin concentration; is necessary to control the concentration of digoxin in the blood.

    Ergotamine and dihydroergotamine: increased toxic effects (vasospasm, dysesthesia); joint application is not recommended.

    Simultaneous use of terfenadine and antibiotics of the macrolide class causes arrhythmia and lengthening QT interval. It is necessary to take into account these data in the joint use of terfenadine and azithromycin.

    With simultaneous application fluconazole reduces the maximum concentration of azithromycin in the blood by 18%, which has no clinical significance. Separate reports of cases of rhabdomyolysis in patients concomitantly receiving azithromycin and statins.

    With simultaneous application azithromycin and rifabutin, neutropenia was sometimes observed. Despite the fact that neutropenia was associated with the use of rifabutin, a causal relationship between the use of a combination of azithromycin and rifabutin and neutropenia has not been established.

    With the simultaneous use of azithromycin and cyclosporine, it is necessary to monitor the concentration of cyclosporine in the blood plasma and adjust the dose accordingly.

    When combined with zidovudine azithromycin has an insignificant effect on the pharmacokinetics, including kidney excretion, zidovudine and its glucuronide metabolite, but the concentration of the active metabolite-phosphorylated zidovudine in mononuclear cells of peripheral blood is increasing (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 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.

    In pharmacokinetic studies of the effect of a single dose of cimetidine on the pharmacokinetics of azithromycin, no changes in the pharmacokinetics of azithromycin have been observed, provided cimetidine is administered 2 hours before azithromycin. Azithromycin does not affect the concentration in the blood plasma of carbamazepine, efavirenz, didanosine, fluconazole, indinavir, cetirizine, midazolam, theophylline, triazolam, nelfinavir, trimethoprim / sulfamethoxazole, sildenafil, atorvastatin, methylprednisolone while simultaneous use.

    Special instructions:

    If you miss one dose of the drug - the missed dose should be taken as soon as possible, and the next - with interruptions of 24 hours.

    Azithromycin should be taken at least one hour before or two hours after taking antacid preparations. Azithromycin should be used with caution in patients with mild and moderate impairment of liver function due to the possibility of developing fulminant hepatitis and severe hepatic insufficiency.

    In the presence of symptoms of impaired liver function, such as fast increasing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy, drug therapy should be discontinued and a study of the functional state of the liver should be carried out.

    For mild and moderate renal dysfunction (CC greater than 40 mL / min), azithromycin therapy should be performed with caution under the control of the kidney function.

    As with the use of other antibacterial drugs, patients with azithromycin should regularly be examined for susceptible microorganisms and signs of development of superinfections, including fungal ones.

    The drug should not be used for longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosing regimen.

    There is no data on the possible interaction between azithromycin and derivatives of ergotamine and dihydroergotamine, but because of the development of ergotism with the simultaneous use of macrolides with derivatives of ergotamine and dihydroergotamine, this combination is not recommended.

    With prolonged use of azithromycin, the development of pseudomembranous colitis caused by Clostridium difficile, both in the form of mild diarrhea, and severe colitis. In the development of antibiotic-associated diarrhea against the background of taking the drug, and also after 2 months after the end of therapy, clostridial pseudomembranouscolitis.

    When treating macrolides, including azithromycin, prolonged cardiac repolarization and interval QT, increasing the risk of developing cardiac arrhythmias, including arrhythmias such as pirouettes.

    Care should be taken when using the drug in patients with proarrhythmogenic factors (especially in elderly patients): with congenital or acquired lengthening of the interval QT, in patients receiving antiarrhythmic drug therapy classes IA (quinidine, procainamide), III (dofetilide, amiodarone and sotalol), cisapride, terfenadine, antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones and (moxifloxacin and levofloxacin), with disturbances of the water-electrolyte balance, especially in the case of hypokalemia or hypomagnesemia, with clinically significant bradycardia, cardiac arrhythmia, or severe heart failure. The use of azithromycin may provoke the development of a myasthenic syndrome or cause an exacerbation of myasthenia gravis.

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

    In connection with the possible development against the background of treatment of unwanted reactions from the central nervous system,caution should be exercised when driving vehicles and performing other activities that require increased attention and speed of psychomotor reactions.

    Form release / dosage:Capsules 250 mg.
    Packaging:

    6 capsules per blister of PVC / AL. 1 blister with instructions for use in a pack of cardboard.

    Storage conditions:In a dry, dark place at a temperature of 15 to 25 ° C. Keep out of the reach of children.
    Shelf life:3 years

    Do not use after expiration of the expiration date stated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013856 / 01
    Date of registration:15.10.2007
    The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia
    Manufacturer: & nbsp
    Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia
    Information update date: & nbsp26.10.2015
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