Active substanceAzithromycinAzithromycin
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  • Dosage form: & nbspcapsules
    Composition:

    Composition per one capsule

    Active substance: azithromycin dihydrate in terms of azithromycin 250 mg.

    Excipients: Mannitol (mannitol) - 54.58 mg, corn starch - 13.10 mg, magnesium stearate - 2.0 mg, sodium lauryl sulfate -0.32 mg;

    Capsules, hard gelatin: capsule composition: body and cap - titanium dioxide (E 171), gelatin (gelatin medical).

    Description:Capsules of white color №0. The contents of the capsules are white powder or white with a yellowish hue.
    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.; a also 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, stable 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 after 2.5 - 3.0 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 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 persists in bactericidal concentrations in the inflammatory focus within 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: 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, basically, in unchanged form - 50% of the intestine, 12% of the kidneys.

    Indications:

    Infectious-inflammatory diseases caused by microorganisms sensitive to azithromycin, including:

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

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

    - infection of the urogenital tract (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 (including other macrolides), components of the drug; severe hepatic insufficiency: more than 9 points on a scaleChild-Pugh (no data on effectiveness and safety); severe renal failure: creatinine clearance (CC) less than 40 ml / min (no data on efficacy and safety); children under the age of 12 years with a body weight of less than 45 kg (for this dosage form); simultaneous reception of ergotamine and dihydroergotamine.

    Carefully:

    With a moderate violation of liver function (7-9 points on the scale Child-Pugh); chronic renal failure (CC more than 40 ml / min); arrhythmias or predisposition to arrhythmia and lengthening of the Q-T interval; with simultaneous administration of terfenadine, warfarin, digoxin; with myasthenia gravis; during 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.

    Descriptions of individual cases and observational studies have shown that the use of azithromycin during pregnancy does not lead to an increase in the incidence of adverse pregnancy outcomes and is not associated with the occurrence of any specific developmental defects in the child. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

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

    Adults with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues (except for the initial stage of Lyme disease (erythema migrans) and acne of medium severity) -500 mg (2 capsules) per day for 1 reception for 3 days (the course dose is 1.5 g).

    At the initial stage of Lyme disease (erythema migrans) - 1000 mg (4 capsules) per day on the first day at a time, then 500 mg (2 capsules) per day every day from 2 to 5 days (course dose - 3 g).

    At the indication of acne ordinary (acne) of moderate severity at 1, 2 and 3 day of treatment take 500 mg (2 capsules) 1 time per day, then take a break from the fourth to the seventh day, from the eighth day of treatment take 500 mg (2 capsule) once a week for 9 weeks (course dose of 6 g).

    When infections of the urogenital tract (urethritis, cervicitis) for the treatment of uncomplicated urethritis or cervicitis caused by Chlamydia trachomatis, take once 1000 mg (4 capsules).

    Children with a body weight of more than 45 kg with infections of the upper and lower respiratory tract, ENT organs, skin and soft tissues - 500 mg (2 capsules) per day for 1 reception for 3 days; when treating the initial stage of Lyme disease (erythema migrans) -1000 mg (4 capsules) on the first day and 500 mg (2 capsules) daily from 2 to 5 days (course dose - 3 g).

    For patients with impaired renal function (creatinine clearance more than 40 ml / min), correction of the dosing regimen 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 a frequency of at least 1/10000, but less than 1/1000), very rarely (with a frequency of less than 1/10000), (including individual messages).

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

    From the side of the central nervous system: often - dizziness, headache, paresthesia, a violation of perception of taste sensations; infrequently - anxiety, nervousness, hyposthenia, insomnia, drowsiness; rarely - agitation; very rarely - fainting, convulsions, psychomotor hyperactivity, anosmia, loss of taste, parosmia, exacerbation myasthenia gravis.

    From the sense organs: infrequent - a decrease in the severity of hearing, tinnitus; rarely - Vertigo, reduced visual acuity, deafness.

    From the cardiovascular system: infrequent - a feeling of heartbeat; rarely - lowering blood pressure; very rare - arrhythmia, including: ventricular tachycardia, increased interval Q-T, arrhythmia such as "pirouette."

    From the digestive system: very often - nausea, diarrhea, abdominal pain, flatulence; often - vomiting; infrequently - gastritis, constipation, melena, anorexia; 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, liver failure (in rare cases with a fatal outcome, mainly on the background of a violation of liver function), fulminant hepatitis, liver necrosis.

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

    From the musculoskeletal system:: often - arthralgia.

    From the genitourinary system: infrequent increase of residual urea nitrogen and creatinine concentration in blood plasma; very rarely - interstitial nephritis, acute renal failure.

    Other: often - weakness; infrequently - pain in the chest, peripheral edema, asthenia, hyperglycemia, conjunctivitis.

    Infections and infestations: infrequently - vaginitis, candidiasis of various localizations.

    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, severe nausea, vomiting, diarrhea. In this case, gastric lavage, the appointment of activated charcoal, and symptomatic therapy are indicated.

    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 interval between their intake should be at least 1 hour before or 2 hours after taking these drugs. With the simultaneous administration of ergotamine and dihydroergotamine derivatives, it is possible to intensify their toxic effects (vasospasm, dysesthesia).

    When combined with anticoagulants indirect effect of the coumarin series (warfarin) and azithromycin (in usual doses) patients need careful monitoring of prothrombin time. Care should be taken when co-prescribing terfenadine and azithromycin, since it has been established that simultaneous administration of terfenadine and macrolides may cause 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, it is necessary to monitor the concentration of cyclosporine in the blood.

    With the joint administration of digoxin and azithromycin, it is necessary to control the concentration of digoxin in the blood, since many macrolides increase the 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).

    With the joint administration of azithromycin and zidovudine, azithromycin does not affect the pharmacokinetic parameters of zidovudine in the blood plasma or on the excretion by the kidneys of its and its metabolite glucuronide,but the concentration of the active metabolite - phosphorylated zidovudine - increases in mononuclear cells of peripheral blood. The clinical significance of this fact is not determined.

    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.

    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 together.

    The possibility of inhibiting the isoenzyme should be considered CYP3A4 preparations of the group of macrolides 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, however, this type of interaction was not observed with the use of azithromycin.Special studies to study the interaction with these drugs have not been conducted.

    Special instructions:

    If you miss a 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 moderate impaired hepatic 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.

    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 stopping 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. Do not use drugs that inhibit the intestinal motility.

    Since it is possible to prolong the Q-T interval in patients receiving macrolides, including azithromycin, with the use of azithromycin, caution should be used in patients with known risk factors for prolonging the Q-T interval: the elderly; violation of electrolyte balance (hypokalemia, hypomagnesemia); syndrome of congenital extension of the Q-T interval; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous administration of drugs capable of extending the Q-T interval (including antiarrhythmics of 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.

    The WHO European Office recommends azithromycin as a drug of choice in the treatment of chlamydial infection in pregnant women. Azithromycin on the risk of use in pregnant women, according to the FDA classification, is classified in Category B (animal reproduction studies have not identified fetal damage due to the administration of azithromycin, but no controlled studies have been conducted in pregnant women).

    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:Capsules 250 mg.
    Packaging:6 or 10 capsules in the outline package. 1, 2, 6 or 12 contour mesh packages with instructions for use in a pack of cardboard.
    Storage conditions:Store at a temperature not exceeding 25 ° C.
    Keep out of the reach of children.
    Shelf life:3 years.Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001157 / 01
    Date of registration:02.06.2010
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp22.08.2015
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