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

    1 tablet contains:

    active substance: clarithromycin 250 mg or 500 mg;

    ExcipientsCroscarmellose sodium, sodium lauryl sulfate, microcrystalline cellulose, povidone (polyvinyl pyrrolidone low molecular weight medical), magnesium stearate, silicon dioxide colloid (aerosil), hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol 6000), titanium dioxide, giprolose (hydroxypropyl cellulose), quinoline yellow , vanillin.

    Description:

    The tablets covered with a film membrane of yellow color, biconvex form, oblong with rounded edges, with a risk.

    On the cross-section, two layers are visible, the inner layer is white or almost white.

    Pharmacotherapeutic group:antibiotic-macrolide
    ATX: & nbsp

    J.01.F.A.09   Clarithromycin

    Pharmacodynamics:

    Clarithromycin is a bacteriostatic second-generation antibiotic from the group of macrolides of a wide spectrum of action. Disrupts the synthesis of the protein of microorganisms (binds to 50S subunit of the ribosome membrane of a microbial cell). It acts on extracorporeal and intracellular pathogens. Active in relation to:Streptococcus agalactiae (Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae), Haemophilus influenzae (parainfluenzae), Haemophilus ducreyi, Neisseria gonorrhoeae, Neisseria meningitides, Listeria monocytogenes, Legionella pneumophila, Mycoplasma pneumoniae, Helicobacter pylori (Campylobacter), Campylobacter jejuni, Chlamydia pneumoniae, Moraxella catarrhalis, Bordetella pertussis, Propionibacterium acne, Mycobacterium avium, Mycobacterium leprae, Mycobacterium kansasii, Mycobacterium marinum, Staphylococcus aureus, Ureaplasma urealyticum, Toxoplasma gondii, Corynebacterium spp., Borrelia burgdorferi, Pasteurella multocida, some anaerobes (Eubacterium spp., Peptococcus spp. Propionibacterium spp., Clostridium perfringens, Bacteroides melaninogenicus), is less active with respect to Mycobacterium tuberculosis.

    Pharmacokinetics:

    Absorption is fast. Food slows down absorption, without significantly affecting bioavailability. The connection with plasma proteins is more than 90%. After a single dose, 2 peaks of the maximum concentration of the drug in the blood plasma are recorded. The second peak is due to the ability of the drug to concentrate in the gallbladder, followed by a gradual or rapid intake into the intestine and absorption. Time to reach the maximum concentration of the drug in blood plasma for oral administration of 250 mg - 1-3 hours.

    After oral administration, 20% of the dose is rapidly hydroxylated in the liver by cytochrome enzymes CYP3A4, CYP3A5 and CYP3A7 with the formation of the main metabolite - 14-hydroxyclarithromycin, which has a pronounced antimicrobial activity against Haemophilus influenzae. Is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7. With a regular intake of 250 mg / day, the equilibrium concentrations of the unchanged drug and its main metabolite are 1 and 0.6 μg / ml, respectively; the half-life is 3-4 hours and 5-6 hours, respectively. When the dose is increased to 500 mg / day, the equilibrium concentration of the unchanged drug and its metabolite in plasma is 2.7-2.9 and 0.83-0.88 μg / ml, respectively; the half-life is 4.8-5 hours and 6.9-8.7 hours, respectively. In therapeutic concentrations, it accumulates in the lungs, skin and soft tissues (concentrations 10 times higher than serum levels). Excreted by the kidneys and intestines (20-30% - in unchanged form, the rest - in the form of metabolites). With a single intake of 250 mg and 1200 mg, kidneys are allocated 37.9 and 46%, intestines - 40.2 and 29.1%, respectively.

    Indications:

    - Infections of the lower respiratory tract (including bronchitis, pneumonia);

    - infections of the upper respiratory tract (including pharyngitis, sinusitis);

    - infections of the skin and soft tissues (including folliculitis, erysipelas);

    - mycobacterial infections caused by Mycobacterium avium and Mycobacterium intracellulare;

    - localized infections caused by Mucobacteriuna-fortuitum and Mycobacterium kansasii;

    - prevention of the spread of infection caused by the complex Mycobacterium avium (MAC infection) in HIV-infected patients with an amount Cd4 lymphocytes not more than 100 / μL;

    - eradication Helicobacter pylori with the purpose of reducing the frequency of recurrences of peptic ulcer of the stomach and duodenum;

    - odontogenic infections.

    Contraindications:

    - Hypersensitivity to drugs of the macrolide group;

    - simultaneous reception of clarithromycin with the following drugs: astemizole, cisapride, pimozide and terfenadine;

    - porphyria;

    - pregnancy (I trimester);

    - lactation period;

    - children under 12 years.

    Carefully:

    Renal and / or hepatic insufficiency. Against the background of taking medicines metabolized by the liver, it is recommended to measure their concentration in the blood.

    Pregnancy and lactation:

    The use of the drug during pregnancy (II and III trimesters) is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

    Clarithromycin excreted in breast milk, so if you need to prescribe the drug during lactation, breastfeeding should stop.

    Dosing and Administration:

    Inside, adults and children over 12 years - 250-500 mg 2 times a day. Duration of treatment is 6-14 days.

    In the treatment of infections caused by Mycobacterium avium, appoint or nominate inside on 500 mg 2 times a day. Duration of treatment - 6 months or more.

    For eradication Helicobacter pylori in patients with peptic ulcer and duodenal ulcer, clarithromycin prescribe 250-500 mg twice a day as part of a combination therapy. Duration of treatment for 7-14 days.

    In patients with chronic renal insufficiency (creatinine clearance less than 30 ml / min or serum creatinine concentration more than 3.3 mg / 100 ml) - 250 mg / day (single dose), in severe infections - 250 mg twice a day. The maximum duration of treatment for patients in this group is 14 days.

    Side effects:

    From the nervous system: headache, dizziness, anxiety, fear, insomnia, "nightmarish" dreams; rarely - disorientation, hallucinations, psychosis, depersonalization, confusion.

    From the digestive system: nausea, vomiting, gastralgia, diarrhea, stomatitis, glossitis, increased activity of "liver" transaminases, cholestatic jaundice, rarely - pseudomembranous enterocolitis.

    From the sense organs: noise in the ears, change in taste (dysgeusia); in isolated cases - hearing loss, which occurs after the drug is discontinued.

    On the part of the organs of hematopoiesis and the system of hemostasis: rarely - thrombocytopenia (unusual bleeding, hemorrhage).

    Allergic reactions: skin rash, itching, malignant exudative erythema (Stevens-Johnson syndrome), anaphylactoid reactions.

    Other: development of resistance of microorganisms.

    Overdose:

    Symptoms: nausea, vomiting, diarrhea, headache, confusion.

    Treatment: gastric lavage and symptomatic treatment. Hemodialysis and peritoneal dialysis do not lead to a significant change in the concentration of clarithromycin in the blood serum.

    Interaction:

    Contraindicated the simultaneous use of clarithromycin with cisapride, pimozide, terfenadine, astemizole, as this leads to an increase in the concentration of these drugs in blood plasma by 2-3 times, which can cause lengthening of the interval QT, disturbance of the rhythm of the heart, including ventricular tachycardia, ventricular fibrillation.

    At simultaneous reception clarithromycin increases the concentration in the blood of drugs metabolized in the liver with the help of cytochrome P450 enzymes: indirect anticoagulants, carbamazepine, theophylline, triazolam, midazolam, cyclosporine, vinblastine, disopyramide, phenytoin, rifabutin, simvastatin,lovastatin, digoxin, alprazolam, valproic acid, cilostazol, methylprednisolone, omeprazole, quinidine, ergot alkaloids, sildenafil, tacrolimus.

    At simultaneous reception of clarithromycin and zidovudine in HIV-infected patients there was a decrease in the value of the equilibrium concentration of zidovudine (between the use of drugs, an interval of at least 4 hours is required).

    With the simultaneous use of ritonavir (200 mg every 8 hours) and clarithromycin (500 mg every 12 hours), the metabolism of clarithromycin slows down (Cmax clarithromycin increased by 31%, Cmin - by 182%, AUC - on77%). There was a significant delay in the formation of 14-hydroxyclarithromycin. When taking ritonavir, do not simultaneously prescribe clarithromycin in a dose of more than 1 g per day. In this case, in patients without renal dysfunction, there is no need to correct the dose of clarithromycin. This is of great importance in the case of using this combination in patients with impaired renal function: for patients with creatinine clearance from 30 to 60 ml / min, the dose of clarithromycin is reduced by 50% (up to 500 mg once a day).

    It is possible to develop cross-resistance between clarithromycin, lincomycin and clindamycin.
    Special instructions:

    In the presence of chronic liver diseases it is necessary to carry out regular monitoring of serum enzymes.

    Caution is prescribed against the background of drugs metabolized by the liver (it is recommended to measure their concentration in the blood).

    In the case of co-administration with warfarin or other indirect anticoagulants, prothrombin time should be monitored. It is necessary to pay attention to the possibility of cross-resistance between clarithromycin and other antibiotics from the macrolide group, as well as lincomycin and clindamycin.

    With prolonged or repeated use of the drug, it is possible to develop superinfection (growth of insensitive bacteria and fungi).

    Form release / dosage:

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

    Packaging:

    For 7 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 2 or 3 contour squares, together with the instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 20 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006777/09
    Date of registration:25.08.2009
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia
    Information update date: & nbsp25.07.2011
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