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

    1 tablet, film-coated, contains:

    active substance: clarithromycin 500 mg;

    Excipients: croscarmellose sodium, pregelatinized starch, colloidal silicon dioxide, povidone, stearic acid, magnesium stearate, talc, microcrystalline cellulose;

    film sheath: opada yellow OY-S-32924, (hypromellose, titanium dioxide, propylene glycol, giprolose, polysorbate 80, lacquer aluminum based on quinoline yellow dye, sorbic acid, vanillin), macrogol.

    Description:

    Smooth yellow elliptical forms biconvex tablets, covered with a film membrane.

    Pharmacotherapeutic group:antibiotic-macrolide
    ATX: & nbsp

    J.01.F.A.09   Clarithromycin

    Pharmacodynamics:

    Clarithromycin is a semi-synthetic macrolide antibiotic with a broad spectrum of action. Antibacterial effect of clarithromycin carried out by suppressing protein synthesis due to binding to 50sa subunit of bacterial ribosomes. Clarithromycin has a pronounced activity against a wide range of aerobic and anaerobic Gram-positive and Gram-negative organisms. The minimum inhibitory concentration of clarithromycin (MIC) is half that of erythromycin for most microorganisms.

    14-hydroxy-metabolite clarithromycin also has antimicrobial activity. The minimum inhibitory concentrations of this metabolite are equal to or higher than the MIC of clarithromycin; in a relationship N.influenzae 14-hydroxy-metabolite is twice as active as clarithromycin.

    Clarithromycin shows activity in vitro in respect of the following organisms:

    - gramp-positive aerobic bacteria: Staphylococcus aureus (sensitive clarithromycin), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Listeria monocytogenes;

    - Gram-negative aerobic bacteria: Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae, Legionella pneumophila, Bordetella pertussis, Helicobacter pylori, Campylobacter jejuni;

    - predominantly intracellular microorganisms: Mycoplasma pneumoniae, Ureaplasma urealyticum. Chlamydia trachomatis, Chlamydia pneumoniae, Mycobacterium avium, Mycobacterium leprae, M. kansaii, M. chelonae. M. marinum, M. fortitum;

    - anaerobic microorganisms: Bacteroides fragilis, Clostridium perfringens, Propionibacterium acnes, Peptococcus species.

    In addition, the drug is active in relation to Toxoplasma species.

    Bactericidal activity clarithromycin possesses in relation to some bacterial strains: Haemophilus influenzae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Moraxella (Branhamella) catarrhalis, Neisseria gonorrhoeae, H. pylori and Campylobacter spp.

    Pharmacokinetics:

    Clarithromycin is rapidly and well absorbed from the gastrointestinal tract after ingestion. The microbiologically active metabolite of 14-hydroxyclarithromycin is formed after the "first passage" through the liver. Food intake does not affect the bioavailability of clarithromycin, but somewhat slows the onset of absorption of clarithromycin and the formation of 14-hydroxy metabolite. The pharmacokinetics of clarithromycin is non-linear in nature: the equilibrium concentration is achieved 2 days after the start of the drug.

    Clarithromycin is excreted by the kidneys, as well as through the intestines. When taking 500 mg twice daily, the excretion of the drug by the kidneys is about 36%. 14-hydroxyclarithromycin, the main metabolite found in urine, accounts for about 10-15% of it.

    When taking 500 mg of clarithromycin three times a day, the concentration of clarithromycin in the plasma is higher than when taking this dose twice a day.

    The content of clarithromycin in tissues, including glandular and pulmonary tissue, is several times higher than in the circulating blood. In therapeutic concentrations clarithromycin 80% bound to plasma proteins.

    Clarithromycin penetrates into gastric mucus. The level of clarithromycin in mucus and tissues The stomach rises with combined therapy with omeprazole. Clarithromycin penetrates into breast milk.
    Indications:

    Infections caused by microorganisms sensitive to clarithromycin:

    - infections of the lower respiratory tract (including acute and chronic bronchitis, pneumonia);

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

    - skin and soft tissue infections;

    - peptic ulcer of the duodenum for eradication N. pylori (as part of complex therapy with proton pump inhibitors).

    Contraindications:

    - Hypersensitivity to antibiotics of macrolides;

    - simultaneous appointment with ergot derivatives;

    - simultaneous administration of the following drugs: cisapride, pimozide, terfenadine;

    - children's age till 12 years;

    - impaired renal function (creatinine clearance <30 mL / min)

    - pregnancy and lactation.

    Carefully:

    Ppatients with violations of the liver and kidneys (creatinine clearance> 30 ml / min).

    Pregnancy and lactation:

    Safety of clarithromycin during pregnancy and lactation not studied.

    The drug penetrates into breast milk. If necessary, use during lactation should stop breastfeeding.

    Dosing and Administration:

    Inside.

    Adults: by 500 mg 2 times a day for 7 days; with severe course of infection course treatment is increased to 14 days.

    Children over 12 years old: dosing regimen, both for adults.

    For treatment duodenal ulcers caused by H. pylori (adults):

    Scheme of triple therapy (7-14 days): clarithromycin 500 mg 2 times a day, lansoprazole 30 mg 2 times a day, amoxicillin 1000 mg 2 times a day.

    Scheme of triple therapy (7 days): clarithromycin 500 mg 2 times a day, lansoprazole 30 mg 2 times a day, metronidazole 400 mg 2 times a day.

    The scheme triple therapy (7 days): tolarithromycin 500 mg 2 times a day, omeprazole 40 mg per day, amoxicillin 1000 mg 2 times a day or metronidazole 400 mg 2 times a day.

    The scheme of triple therapy (10 days): clarithromycin 500 mg 2 times a day is prescribed with amoxicillin 100 mg 2 times a day and omeprazole 20 mg per day.

    Double therapy scheme (14 days): clarithromycin 500 mg 3 times a day, omeprazole inside 40 mg 1 time at day.

    When defeat function kidneys

    When creatinine clearance is> 30 ml / min, no dose adjustment is usually required.

    At simultaneous taking ritonavir for patients with impaired function kidneys a dose adjustment according to the following scheme is recommended: for patients with a creatinine clearance of 30-60 ml / min, the dose of clarithromycin should be reduced by 50%.

    Side effects:

    Usually clarithromycin well tolerated by patients.

    Co hand gastrointestinal tract: tnausea, vomiting, indigestion, diarrhea, abdominal pain, stomatitis, glossitis, pancreatitis, oral cavity candidiasis, discoloration of the tongue and teeth; rarely - pseudomembranous enterocolitis. The discoloration of the teeth is reversible and is usually restored by a special treatment in the dental clinic. As with the administration of other antibiotics from the macrolide group, liver function abnormalities are possible, incl. an increase in hepatic enzyme activity, hepatic and / or cholestatic hepatitis with or without jaundice. These violations of the liver can be severe, but usually they are reversible. Very few cases of hepatic insufficiency and death were observed, mainly on the background of severe co-morbidities and / or concomitant drug therapy.

    On the part of the blood system: at exceptional cases - leukopenia and thrombocytopenia; increased serum creatinine levels.

    Co hand central and peripheral nervous system: Parrest, headache, smell disorders, change in taste, dizziness, agitation, insomnia, nightmares, feelings of fear, ringing in the ears, confusion, disorientation, hallucinations, psychosis, depersonalization, reversible hearing loss, convulsions.

    From the side of the cardiovascular system: toAs with other macrolides, lengthening interval QT, ventricular tachycardia, polymorphic ventricular tachyarrhythmia (torsades de pointes).

    From the side supportingly-powerful systems: aangrialgia, myalgia.

    From the urinary system: isolated cases of increased plasma creatinine, interstitial nephritis, renal failure.

    Allergic reactions: tourticaria, angioedema, anaphylactic shock, in rare cases - Stevens-Johnson syndrome, toxic epidermal necrolysis.

    Other: Rcaustically - hypoglycemia in patients taking oral hypoglycemic drugs or insulin.

    Overdose:

    Symptoms: symptoms from the gastrointestinal tract. One of the patients receiving 8 g of clarithromycin had cases of mental disorders, paranoid behavior, hypoglycemia, hypoxemia.

    Treatment: gastric lavage, maintenance therapy. Hemodialysis or peritoneal dialysis is ineffective, as for other macrolides.

    Interaction:

    With the simultaneous administration of clarithromycin with cisapride, pimozide and terfenadine in plasma, elevated concentrations of these drugs are observed, which may cause lengthening of the interval QT and heart rhythm disturbances, including ventricular tachycardia, ventricular fibrillation, arrhythmia, and torsade de pointes; Similar effects are observed with simultaneous administration of astemizole and other macrolides.

    Clarithromycin does not interact with oral contraceptives.

    As with other macrolide antibiotics, the simultaneous administration of clarithromycin and other drugs metabolized with the participation of cytochrome P450 (warfarin, ergot alkaloids, triazolam, midazolam, disopyramide, lovastatin, rifabutin, phenytoin, ciclosporin and tacrolimus) may be accompanied by an increase in the concentration of these drugs in the blood serum.

    With the simultaneous use of clarithromycin and inhibitors HMG-KoA-reductase (lovastatin, simvastatin) it is possible to develop rhabdomyolysis.

    With the simultaneous administration of clarithromycin and theophylline, the concentration of theophylline in the blood serum and its toxicity increase.

    Simultaneous administration of clarithromycin and warfarin or digoxin may be accompanied by an increase in the severity of their effects.

    With the simultaneous administration of clarithromycin and carbamazepine, the effect of carbamazepine may be enhanced due to a decrease in the rate of carbamazepine excretion.

    With concurrent administration of clarithromycin and zidovudine (inside), HIV-infected adults may be able to reduce the equilibrium concentration of zidovudine. This can be largely avoided by increasing the interval between the use of clarithromycin and zidovudine up to 1-2 hours. For children this interaction was not noted.

    With the simultaneous administration of ritonavir and clarithromycin for the latter, the values ​​of pharmacokinetic parameters increase: the area under

    the pharmacokinetic curve (AUC), the maximum concentration in the blood plasma (CmOh), the minimum concentration in the blood plasma (Cmin). For patients with normal renal function, dose adjustment is usually not required due to the wide therapeutic range of doses of clarithromycin.

    With the simultaneous use of clarithromycin and omeprazole, clarithromycin and lansoprazole, as well as clarithromycin and ranitidine, an increase in the concentration of drugs in the blood plasma is possible, but usually no dose adjustment is required.

    With the simultaneous use of clarithromycin and hypoglycemic agents, including insulin, in rare cases, the development of hypoglycemia is possible.

    Special instructions:

    The use of clarithromycin tablets in children younger than 12 years is not recommended.

    With the simultaneous administration of clarithromycin and warfarin should be regularly to monitor prothrombin time.

    When concurrent administration of clarithromycin and digoxin should be carried out monitoring the level of serum digoxin concentration.

    Form release / dosage:

    Tablets, film-coated, 500 mg.

    Packaging:

    For 7 tablets in a blister of PVC / aluminum foil.

    2 blisters (7 tablets each), along with instructions for use in a cardboard box.

    Storage conditions:

    In a dry, the dark place 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:LSR-009023/09
    Date of registration:10.11.2009
    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: & nbsp03.09.2012
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