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

    1 one tablet, film-coated, contains active substance: azithromycin dihydrate in terms of azithromycin 500 mg;

    Excipients: pregelatinized starch 40.00 mg, low-substituted giprolose (LHPC 21) 70.00 mg, sodium lauryl sulfate 5.00 mg, croscarmellose sodium, 9.00 mg, calcium hydrophosphate dihydrate 135.50 mg, silicon dioxide colloid 0.50 mg, lactose anhydrous 96.00 mg, magnesium stearate 20.00 mg; film coating: a coating material for tablets Sepyphylm 752 white (hypromellose (E464) 35-45%, microcrystalline cellulose- (E460) 27-37%, macrogol-40 stearate 5-10%, titanium dioxide (E171) 15-25%) .

    Description:Tablets are white oval-shaped, film-coated, with a risk on one side.
    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. Has activity against a number. 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.

    The sensitivity scale of microorganisms to azithromycin (Minimum inhibitory concentration (MIC), mg / l):

    Microorganisms

    MIC, mg / l

    Sensitive

    Sustainable

    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, sensitive microorganisms

    Gram-positive aerobes

    Staphylococcus aureus methicillin-sensitive, Streptococcus pneumoniae penicillin-sensitive, Streptococcus pyogenes

    Gram-negative aerobes

    Haemophilus influenzae, Haemophilus parainfluenzae, Legionella pneumophila, Moraxella catarrhalis, Pasteurella multocida, Neisseria gonorrhoeae

    Anaerobes

    Clostridium perfringens, Fusobacterium spp., Prevotella spp., Porphyriomonas spp.

    Other microorganisms

    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, Staphylococci (methicillin-resistant staphylococci exhibit a very high degree of resistance to macrolides), Gram-positive bacteria resistant to erythromycin.

    Anaerobes: Bacteroides ffagilis.

    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 (0.4 mg / l) in the blood is created after 2-3 hours, apparent, the volume of distribution is 31.1 l / kg, binding to proteins is 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. Concentrations in tissues and cells are 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 35-50 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 output, basically, in the unchanged form - 50% of the intestine, 6% of the kidneys. In the liver, demethylated, losing activity.

    Indications:

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

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

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

    - urinary tract infection (gonorrheal and non-gonorrheal urethritis, cervicitis);

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

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

    Contraindications:

    - hypersensitivity to antibiotics of the macrolide group;

    - hypersensitivity, to the active substance or ancillary components;

    - severe violations of the liver and kidneys;

    - breast-feeding;

    - children under 12 years of age with a body weight of less than 45 kg;

    - simultaneous administration with ergotamine and dihydroergotamine;

    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption (due to the presence of lactose in the composition).

    Carefully:

    - moderate violations of the liver and kidneys;

    - arrhythmia, incl. predisposition to arrhythmia and lengthening of the interval Q-T (risk of ventricular arrhythmia and lengthening of the interval Q-T);

    - myasthenia gravis, simultaneous reception of terfenadine, warfarin, digoxin.

    Pregnancy and lactation:

    Azithromycin is used in pregnancy only if the benefit to the mother exceeds the possible risk to the fetus. During treatment with Zitnob®, breastfeeding is suspended.

    Dosing and Administration:

    Inside, 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 over 45 kg:

    Infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues

    500 mg once a day for 3 days

    Urinary tract infections

    1 g once

    Acne vulgaris

    500 mg once a day for 3 days, then 500 mg once a week for 9 weeks. The first weekly tablet should be taken 7 days after the first daily tablet (8 days from the start of treatment),the subsequent 8 weekly tablets-with an interval of 7 days.

    With migratory erythema

    1 time per day for 5 days: 1st day - 1g (2 tablets), then from 2nd to 5th day - 500 mg (course dose 3g)

    The appointment of patients with impaired renal function - for patients with moderate impairment of kidney function (creatinine clearance> 40ml / min) dose adjustment is not needed.

    Side effects:

    Classification of adverse reactions according to the frequency of development:

    Frequently -> 1/100 and <1/10,

    Infrequently -> 1/1000 and <1/100,

    Rarely -> 1/10000 and <1/1000,

    Very rarely - <1/10000.

    From the blood and lymphatic systems:

    Rarely - thrombocytopenia, neutropenia, eosinophilia, lymphopenia, hemolytic anemia, and leukopenia.

    From the digestive system:

    Often - diarrhea, nausea, vomiting, abdominal pain / spasms, dyspepsia. Infrequently - loose stools, flatulence, digestive disorders, anorexia. Rarely - constipation, discoloration of the tongue, pseudomembranous colitis, cholestatic jaundice, hepatitis, changes in laboratory parameters of liver function, hyperbilirubinemia, pancreatitis. Very rarely - liver dysfunction, liver necrosis (possibly fatal).

    From the cardiovascular system:

    Rarely - lowering blood pressure, increasing the interval Q-T, arrhythmia such as "pirouette", ventricular tachycardia, palpitation.

    From the nervous system:

    Infrequent - dizziness / vertigo, headache, drowsiness. Rarely - paresthesia, asthenia, insomnia, hyperactivity, aggressiveness, anxiety, nervousness.

    From the sense organs:

    Rarely, noise in the ears, reversible hearing impairment down to deafness (when taking high doses for a long time), a violation of the perception of taste and smell.

    From the genitourinary system:

    Rarely - increased residual urea nitrogen and creatinine concentration in blood plasma, interstitial nephritis, acute renal failure.

    Allergic reactions:

    Infrequent - itching, skin rashes. Rarely, angioedema, hives, photosensitivity, anaphylactic reaction, including edema (in rare cases, fatal), erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

    Other:

    Infrequently - arthralgia. Rarely - weakness, peripheral edema, malaise, hyperglycemia.

    Overdose:

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

    Treatment: symptomatic.

    Interaction:

    Antacids (aluminum and magnesium-containing) do not affect bioavailability, but reduce the concentration of azithromycin in the blood by 30%, so the interval between their intake should be 1 hour before or 2 hours after taking these drugs.

    With simultaneous use with derivatives of ergotamine and dihydroergotamine, toxic effects (vasospasm, dysesthesia) of the latter are possible.

    When combined with anticoagulants indirect effect of the coumarin series (warfarin) and azithromycin (in usual doses) patients need careful monitoring of prothrombin time.

    Caution should be exercised in the joint administration of terfenadine and azithromycin, since it has been established that simultaneous reception of terfenadine and macrolides causes arrhythmia and lengthening Q-T interval. Proceeding from this, it is impossible to exclude the aforementioned complications in the joint administration of terfenadine and azithromycin.

    When used simultaneously with cyclosporine, the concentration of cyclosporin in the blood should be monitored.

    With simultaneous use with digoxin is necessary, monitoring the concentration of digoxin in the blood (possibly increasing absorption of digoxin in the intestine).

    At simultaneous application with nelfinavir it is possible to increase the incidence of adverse reactions of azithromycin (decrease in hearing, increase of activity of "liver" transaminases).

    When combined with zidovudine azithromycin does not affect the pharmacokinetic parameters of zidovudine in blood plasma or on the excretion of his and his metabolite glucuronide by the kidneys, but the concentration of the active metabolite of phosphorylated zidovudine in mononuclear cells of peripheral vessels increases. The clinical significance of this fact is not determined. The possibility of inhibiting the isoenzyme should be considered CYP3A4 azithromycin with simultaneous application with cyclosporine, terfenadine, ergot alkaloids, cisapride, pimozide, quinidine, astemizole and other drugs, the metabolism of which occurs with the participation of this enzyme.

    Azithromycin does not affect the concentration of carbamazepine, cimetidine, didanosine, efavirenz, fluconazole, indinavir, midazolam, theophylline, triazolam, trimethoprim / sulfamethoxazole, cetirizine,sildenafil, atorvastatin, rifabutin and methylprednisolone in the blood with simultaneous application.

    Special instructions:

    In case of missed dose, the missed dose should be taken as soon as possible, and the subsequent dose should be taken at intervals of 24 hours. Zitnob® should be taken 1 hour before or 2 hours after taking antacid medicines. Take with caution patients with moderate hepatic impairment because of the possibility of developing fulminant hepatitis and severe hepatic insufficiency in such patients. In the presence of symptoms of liver dysfunction (rapidly increasing asthenia, jaundice, darkening of the urine, a tendency to bleeding, hepatic encephalopathy) therapy with azithromycin should be discontinued and an examination of the functional state of the liver should be carried out. With moderate renal failure (CC greater than 40 ml / min), azithromycin should be administered under the control of kidney function. Contraindicated simultaneous administration of azithromycin with derivatives of ergotamine and dihydroergotamine because of the possible development of ergotism. When using the drug, both on the background of taking and 2-3 weeks after discontinuation 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 of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole is indicated. Do not use drugs that inhibit the intestinal motility. Since it is possible to extend the interval Q-T in patients receiving macrolides, including azithromycin, with the use of azithromycin, caution should be exercised in patients with known risk factors for lengthening the interval Q-T: elderly age; violation of electrolyte balance (hypokalemia, hypomagnesemia); syndrome of congenital lengthening of the interval, Q-T; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous reception of drugs that can lengthen the interval Q-T (including antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics; fluoroquinolones). With the use of azithromycin, the development of myasthenic syndrome or myasthenia exacerbation is possible.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
    Form release / dosage:

    Tablets, film-coated 500 mg.

    Packaging:

    3 tablets per blister of aluminum foil and PVC / PE / PVDC. 1 blister in a cardboard box, along with instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:2 years. Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001048
    Date of registration:21.10.2011
    The owner of the registration certificate:Nobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh. Turkey
    Manufacturer: & nbsp
    Representation: & nbspNobel Ilach Sanayi Ve Tidjaret A.Sh.Nobel Ilach Sanayi Ve Tidjaret A.Sh.Russia
    Information update date: & nbsp19.08.2015
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