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

    One tablet, film-coated, contains:

    Dosage of 125 mg

    active substance: azithromycin dihydrate (in terms of azithromycin) - 125,000 mg;

    Excipients: cellulose microcrystalline - 9,000 mg; lactose monohydrate - 8.366 mg; povidone K-30 - 6,500 mg; crospovidone - 6,500 mg; sodium lauryl sulfate - 0.325 mg; silicon dioxide colloidal - 1,650 mg; magnesium stearate - 1,650 mg;

    film sheath: [hypromellose - 3,000 mg, talc - 1,000 mg, titanium dioxide 0.550 mg, macrogol 4000 (0.405 mg) 0.450 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) ( 9%)] - 5,000 mg.

    Dosage 500 mg

    active substance: azithromycin dihydrate (in terms of azithromycin) - 500,000 mg;

    Excipients: microcrystalline cellulose - 36,000 mg; lactose monohydrate - 33.464 mg; povidone K-30 - 26,000 mg; crospovidone - 26,000 mg; sodium lauryl sulfate - 1,300 mg; silicon dioxide colloidal - 6,600 mg; magnesium stearate - 6,600 mg;

    film sheath: [hypromellose - 12,000 mg, talc - 4,000 mg, titanium dioxide (2,200 mg, macrogol 4000 (polyethylene glycol 4000) - 1,800 mg] or [dry film-coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) ( 9%)] - 20,000 mg.

    Description:

    Round biconvex tablets covered with a film coat of white or almost white color. On the cross section, the nucleus is white or almost white in color.

    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-a subunit of the ribosome, inhibits peptidranslokase at the stage of translation and inhibits 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.

    Table №1. The sensitivity scale of microorganisms to azithromycin (minimal inhibitory concentration (MIC), mg / l):

    Microorganisms

    MIC, mg / l

    Staphylococcus

    <1

    >2

    Streptococcus A, B, C, G

    <0,25

    >0,5

    S. pneumoniae

    <0,25

    >0,5

    N. influenzae

    <0,12

    >4

    M. catarrhalis

    <0,5

    >0,5

    N. gonorrhoeae

    <0,25

    >0,5

    In most cases, azithromycin is sensitive:

    - aerobic Gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive), Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Streptococcus groups A, B, 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., Porphyromonas spp.;

    - other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Chlamydia psittaci, Mycoplasma pneumoniae, Mycoplasma hominis, Borrelia burgdorferi.

    Microorganisms that can develop 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:

    After oral administration azithromycin well absorbed and quickly distributed in the body. After a single dose of 500 mg bioavailability - 37% (the effect of "first passage"), the maximum concentration in the blood (0.4 mg / l) is created after 2-3 hours, the apparent volume of distribution is 31 l / kg, binding to blood plasma proteins inversely proportional to the concentration in the blood and is 7-50%. Penetrates through cell membranes (effective for infections caused by intracellular pathogens). It is transported by phagocytes to the site of infection, where it is released in the presence of bacteria. Easily passes the histohematological barriers and enters the tissues. Concentration in tissues and cells is 10-50 times higher than in plasma, and in the focus of infection - 24-34% more than in healthy tissues.

    In azithromycin, a very long half-life is 30-50 hours. The half-life of the tissues is much larger. The therapeutic concentration of azithromycin is maintained up to 5-7 days after the last dose. Azithromycin is excreted mostly unchanged in 50% of the intestine, 6% in the kidneys. In the liver, demethylated, losing activity.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms susceptible to azithromycin:

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

    - infection of the lower respiratory tract (acute bronchitis, exacerbation of chronic bronchitis);

    - Community-acquired pneumonia, incl. caused by atypical pathogens (see section "Special instructions");

    - infections of the skin and soft tissues (acne vulgaris of moderate severity, erysipelas, impetigo, secondarily infected dermatoses);

    - the initial stage of Lyme disease (borreliosis) - migrating erythema (erythema migrans);

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

    Contraindications:

    - increased sensitivity to azithromycin, erythromycin, other macrolides, ketolides or other components of the drug;

    - impaired hepatic function;

    - severe renal dysfunction (creatinine clearance (CK) less than 40 ml / min);

    - Children under 12 years of age with a body weight of less than 45 kg (for tablets 500 mg);

    - children under 3 years (for tablets 125 mg);

    - the period of breastfeeding;

    - simultaneous administration with ergotamine and dihydroergotamine;

    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

    Carefully:

    Pregnancy; myasthenia gravis; violations of liver function of mild and moderate severity; renal dysfunction of mild and moderate severity (QC more than 40 ml / min); elderly patients; 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 (moxifloxacin, levofloxacin), with a violation of the water-electrolyte 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 and lactation:

    Azithromycin is used in pregnancy only in cases where the benefit to the mother exceeds the possible risk to the fetus.During treatment with azithromycin, breastfeeding is suspended.

    Dosing and Administration:

    Inside, not liquid, at least 1 hour before or 2 hours after meals, once a day.

    Adults and children over 12 years of age with a body weight of more than 45 kg

    With infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues: 1 tablet (500 mg) once a day for 3 days (course dose of 1.5 g).

    With acne vulgaris of moderate severity: 1 tablet (500 mg) 1 time per day for 3 days, then 1 tablet (500 mg) 1 time per week for 9 weeks (course dose 6.0 g). The first weekly tablet should be taken 7 days after taking the first daily tablet (the 8th day from the start of treatment), the subsequent 8 weekly tablets - with an interval of 7 days.

    With Lyme disease (the initial stage of borreliosis) - migratory erythema (erythema migrans): 1 time per day for 5 days: 1st day - 1.0 g (2 tablets of 500 mg), then from the 2nd to the 5th day - 0.5 g (1 tablet of 500 mg) (course dose of 3 , 0 g).

    In cases of urinary tract infections caused by Chlamydia trachomatis (urethritis, cervicitis): uncomplicated urethritis / cervicitis - 1.0 g (2 tablets of 500 mg) once.

    Children aged 3 to 12 years with a body weight of less than 45 kg

    With 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 (course dose 30 mg / kg). For the convenience of dosing, table No. 2 is recommended.

    Table 2. Calculation of the dose of the drug Azithromycin for children weighing less than 45 kg:

    Body mass

    Amount of azithromycin in tablets

    18-30 kg

    2 tablets of 125 mg (250 mg of azithromycin)

    31-44 kg

    3 tablets of 125 mg (375 mg of azithromycin)

    not less than 45 kg

    appoint doses recommended for adults

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

    With Lyme disease (the initial stage of borreliosis) - migratory erythema (erythema migrans): 20 mg / kg once a day on the first day, then at the rate of 10 mg / kg of body weight 1 time per day from 2 to 5 days. The course dose is 60 mg / kg.

    Patients with impaired renal function

    In patients with impaired renal function of mild and moderate severity (CK> 40 ml / min), dose adjustment is not required.

    Patients with impaired hepatic function

    If the liver function is mild and moderate, dosage adjustment is not required.

    Elderly patients

    Correction of the dose is not required. Since older patients may have ongoing pro-rhythmogenic conditions, caution should be exercised when using the drug Azithromycin, due to the high risk of developing cardiac arrhythmias, including arrhythmias such as "pirouette."

    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not 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% (including isolated cases).

    Infectious diseases:

    infrequently - Candidiasis, including the mucous membrane of the mouth and genitals;

    rarely - pseudomembranous colitis.

    From the side of metabolism and nutrition: often anorexia.

    Allergic reactions:

    often - skin itching, skin rash;

    infrequently - hypersensitivity reactions, photosensitization reaction, urticaria, Stevens-Johnson syndrome, angioedema;

    rarely - Anaphylactic reaction, erythema multiforme, toxic epidermal necrolysis.

    From the side of blood and lymphatic system:

    often - eosinophilia, lymphopenia;

    infrequently - leukopenia, neutropenia;

    rarely - thrombocytopenia, hemolytic anemia.

    From the respiratory system:

    infrequently - pneumonia, pharyngitis, respiratory diseases, rhinitis, shortness of breath, nosebleeds.

    From the nervous system:

    often - headache, dizziness, paresthesia, a violation of taste; infrequently - hypoesthesia, drowsiness, insomnia, nervousness;

    rarely - agitation;

    rarely - anxiety, aggression, fainting, convulsions, psychomotor hyperactivity, loss of smell (or anosmia) and taste sensations, myasthenia gravis, anxiety;

    frequency unknown - perversion of smell, delirium, hallucinations.

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

    From the side of the hearing organ and labyrinthine disorders:

    often - deafness;

    infrequently - Tinnitus, hearing disorder;

    rarely - Vertigo.

    From the cardiovascular system:

    infrequently - sensation of the heartbeat, "tides" of blood to the skin of the face;

    rarely - lowering blood pressure, increasing the interval QT, arrhythmia such as "pirouette", ventricular tachycardia.

    From the gastrointestinal tract:

    Often - nausea, flatulence, abdominal pain, diarrhea;

    often - dyspepsia, vomiting;

    infrequently - constipation, gastritis, gastroenteritis, dysphagia, bloating, dryness of the oral mucosa, belching, ulcers of the oral mucosa, increased secretion of the salivary glands;

    rarely - changing the color of the tongue, pancreatitis.

    From the liver and bile ducts:

    infrequently - increased activity of "hepatic" transaminases, increased concentration bilirubin, hepatitis;

    rarely - abnormal liver function;

    rarely - cholestatic jaundice, hepatic insufficiency (in rare cases with a fatal outcome mainly on the background of severe violations of the liver function), liver necrosis, fulminant hepatitis.

    From the skin:

    infrequently - dermatitis, dry skin, increased sweating.

    From the osteomuscular system and connective tissue:

    often - arthralgia;

    infrequently - osteoarthritis, myalgia, back pain, neck pain.

    From the genitourinary system:

    infrequently - an increase in the concentration of urea and creatinine in the blood plasma, dysuria, pain in the kidney, metrorrhagia, dysfunction of the testicles;

    rarely - interstitial nephritis, acute renal failure. Laboratory indicators:

    often - a decrease in the concentration of bicarbonates in the blood plasma, an increase in the number of: basophils, monocytes, neutrophils;

    infrequently - increase in the number of platelets, increase in hematocrit; an increase in the activity of alkaline phosphatase, an increase in the chlorine content, an increase in the concentration of glucose in the blood plasma, an increase in the concentration of bicarbonates in the blood plasma, a change in the sodium content in the blood plasma, a change in the potassium concentration.

    Other:

    often - weakness;

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

    Overdose:

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

    Treatment: symptomatic.

    Interaction:

    Antacids do not affect the bioavailability of azithromycin, but reduce the maximum concentration in the blood by 30%, so azithromycin should be taken at least one hour before or two hours after taking these drugs or food.

    Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir,midazolam, triazolama, trimethoprim / sulfamethoxazole, cetirizine, sildenafil and methylprednisolone in blood plasma with simultaneous application. Simultaneous use of atorvastatin (10 mg daily) and azithromycin (500 mg daily) did not cause a change in the concentration of atorvastatin in the blood plasma (based on the inhibition of GMK-CoA reductase). However, in the post-marketing period, separate reports were received on cases of rhabdomyolysis in patients receiving concomitantly azithromycin and statins.

    Simultaneous use of azithromycin and rifabutin does not affect the concentration of each drug in the blood plasma. With the simultaneous use of 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.

    In a pharmacokinetic study involving healthy volunteers who were ingested for three days azithromycin (500 mg / day once), and then ciclosporin (10 mg / kg / day once), a significant increase in the maximum plasma concentration and area under the "concentration-time" curve of cyclosporine was detected. Care should be taken when using these drugs at the same time. In case of simultaneous use of these drugs, it is necessary to monitor the concentration of cyclosporine in the blood plasma and, accordingly, adjust the dose.

    With the simultaneous use of digoxin and azithromycin, it is necessary to monitor the concentration of digoxin in the blood plasma, many macrolides increase absorption of digoxin in the intestine.

    If it is necessary to use simultaneously with anticoagulant means of indirect action (such as warfarin, other anticoagulants of the coumarin type) it is recommended to carry out a thorough prothrombin time control.

    It was found that the simultaneous use of terfenadine 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 with concurrent administration of terfenadine and azithromycin.

    Simultaneous use of azithromycin (1200 mg) and nelfinavir (750 mg 3 times a day) causes an increase in the equilibrium concentrations of azithromycin in the blood plasma. Clinically significant side effects were not observed and dose adjustment of azithromycin when it is used simultaneously with nelfinavir is not required.

    Azithromycin weakly interacts with isoenzymes of the cytochrome P450 system; 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.

    There was no interaction between azithromycin and theophylline.

    When combined with zidovudine azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or on the excretion of it and its metabolite glucuronide by the nights. Nevertheless, the concentration of the active metabolite of phosphorylated zidovudine in mononuclear cells of peripheral vessels increases. The clinical significance of this fact is not clear.

    With the simultaneous use of macrolides with ergotamine and dihydroergotamine, their toxic effect is possible.

    Given the theoretical possibility of ergotism, the simultaneous use of azithromycin derivatives of ergot alkaloids is not recommended.

    Special instructions:

    In case of missing one dose of the drug Azithromycin The missed dose should be taken as soon as possible, and the subsequent dose with interruptions of 24 hours. A drug Azithromycin should not be used for the treatment of pneumonia in patients for whom it is impossible to conduct oral therapy because of the severity of the disease and / or have the following risk factors: cystic fibrosis, bacteremia or suspicion of her condition that can change the body's response to the disease (immunodeficiency, functional asplenia and etc.), patients in need of hospitalization, elderly or weakened patients. A drug Azithromycin should be used with caution in patients with impaired liver function and mild to moderate severity due to the possibility of development of fulminant hepatitis and severe hepatic insufficiency.

    In the presence of liver disease symptoms, such as rapidly growing asthenia, jaundice, dark urine, a tendency to bleeding, hepatic encephalopathy,Therapy with Azithromycin should be discontinued and a study of the functional state of the liver should be carried out.

    When violations of the function of the kidneys of mild and moderate severity (CC more than 40 ml / min), therapy with Azithromycin should be performed with caution under the control of the state of kidney function. At the terminal stage of renal failure (CC less than 10 ml / min), the concentration of azithromycin in the blood plasma is increased by 33%.

    It is possible to develop resistance of microorganisms if the recommended duration of therapy is not observed. 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 Azithromycin do not use longer courses than indicated in the instructions, since the pharmacokinetic properties of azithromycin allow us to recommend a short and simple dosing regimen.

    It should be remembered that for the prevention of pharyngitis / tonsillitis caused by Streptococcus pyogenes, as well as for the prevention of acute rheumatic fever, the drug of choice is usually penicillin.

    With prolonged intake of the drug Azithromycin possibly the development of pseudomembranous colitis caused by Clostridium difficile, as in the form of mild diarrhea, and severe colitis. With the development of diarrhea against the background of taking the drug Azithromycin, and also 2 months after the end of therapy, clostridial pseudomembranous colitis should be excluded. The use of drugs that inhibit intestinal peristalsis is contraindicated. Syndrome of delayed repolarization of the ventricles - syndrome of lengthening the interval QT - increases the risk of arrhythmias, including arrhythmias such as "pirouette" against the background of taking macrolides, as well as azithromycin. Caution when using azithromycin should be observed in patients with lengthening interval QT, receiving antiarrhythmic drugs classes IA, III, cisapride, hypokalemia or hypomagnesemia, clinically significant bradycardia, arrhythmia or severe heart failure.

    Care should be taken when using the drug simultaneously Azithromycin and antipsychotic drugs (pimozide), antidepressants (citalopram), fluoroquinolones (moxifloxacin, levofloxacin), cyclosporine, as well as in elderly patients.

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

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

    With the development of undesirable effects from the nervous system and the organ of vision, care should be taken when performing actions requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets coated with a film coating, 125 mg and 500 mg.

    Packaging:

    3 or 6 tablets in a contour cell box made of a polyvinylchloride film and aluminum foil.

    6 tablets in a can of high-density polyethylene.

    For a dosage of 125 mg

    2 contour packs of 3 tablets, 1 contour squad package of 6 tablets or one pot along with instructions for medical use in a pack of cardboard.

    For a dosage of 500 mg

    1 or 2 contourcell packs of 3 tablets, 1 contour pack of 6 tablets or one bank, along with instructions for medical use in a pack of cardboard.

    Storage conditions:

    Store in a dark 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 expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002580
    Date of registration:14.08.2014
    The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp26.10.2015
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