Active substanceAmoxicillin + Clavulanic acidAmoxicillin + Clavulanic acid
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  • Dosage form: & nbsppowder for solution for intravenous administration
    Composition:

    Active substances: Amoxicillin sodium in terms of amoxicillin - 0.5 g, 1.0 g; potassium clavulanate in terms of clavulanic acid - 0.1 g; 0.2 g

    Description:Powder from white to white with a yellowish hue of color.
    Pharmacotherapeutic group:Antibiotic - penicillin semisynthetic + beta-lactamase inhibitor
    ATX: & nbsp

    J.01.C.R.02   Amoxicillin in combination with enzyme inhibitors

    Pharmacodynamics:

    The drug is a combination of semisynthetic penicillin amoxicillin and beta-lactamase inhibitor-clavulanic acid. It acts bactericidal, inhibits the synthesis of the bacterial wall.

    Active in relation to:

    aerobic Gram-positive bacteria (including strains producing beta-lactamases): Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Enterococcus spp, Corynebacterium spp., Listeria monocytogenes;

    anaerobic Gram-positive bacteria: Clostridium spp., Peptococcus spp., Peptostreptococcus spp.;

    aerobic Gram-negative bacteria (including strains producing beta-lactamases): Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Moraxella catarrhalis, Haemophilus influenzae, Haemophilus ducreyi, Yersinia multocida (before Pasteurella), Campylobacter jejuni;

    anaerobic gram-negative bacteria (including strains, producing beta-lactamase): Bacteroides spp., including Bacteroides fragilis.

    Clavulanum acid suppresses II, III, IV and V types beta-lactamase, inactive at relations­the beta-lactamase I type, produced Enterobacter spp., Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp.

    Clavulanic acid has high affinity for penicillinases, thereby forming a stable complex with the enzyme, thus preventing the enzymatic degradation of amoxicillin under the influence of beta-lactamase.

    Pharmacokinetics:

    After intravenous administration of the drug at doses of 1.2 and 0.6 g, the average values ​​of the maximum concentration in the blood plasma (Cmah) amoxicillin is 105.4 and 32.2 μg / ml, clavulanic acid is 28.5 and 10.5 μg / ml, respectively. Both components are characterized by a good distribution in the fluids and tissues of the body (lungs, middle ear, pleural and peritoneal fluids, uterus, ovaries). Amoxicillin permeates also in the synovial fluid, liver, prostate, palatine tonsils, muscle tissue, gall bladder, the secret of the paranasal sinuses, bronchial secretion. Amoxicillin and clavulanic acid do not penetrate the blood-brain barrier in non-inflamed meninges.

    Active substances penetrate the placental barrier and in trace concentrations are excreted in breast milk.

    Binding to plasma proteins is 17-20% for amoxicillin, 22-30% for clavulanic acid.

    Metabolised both components in the liver. Amoxicillin partially metabolized-10% of the administered dose, clavulanic acid undergoes intensive metabolism-50% of the administered dose.

    After intravenous administration of amoxicillin + clavulanic acid at doses of 1.2 and 0.6 g, the elimination half-life (T1 / 2) for amoxicillin is 0.9 and 1.07 hours for clavulanic acid 0.9 and 1.12 parts.

    Amoxicillin is excreted by the kidneys (50-78% of the administered dose) practically unchanged through tubular secretion and glomerular filtration. Clavulanic acid is excreted by the kidneys by glomerular filtration in an unchanged form, partly in the form of metabolites (25-40% of the administered dose) within 6 hours after taking the drug. Small amounts can be excreted through the intestines and lungs.

    In patients with severe renal failure, the elimination half-life increases to 7.5 hours for amoxicillin and up to 4.5 hours for clavulanic acid.

    Both components are removed by hemodialysis and minor amounts by peritoneal dialysis.

    Indications:

    Infectious-inflammatory diseases caused by sensitive strains of microorganisms:

    - endocarditis, meningitis, sepsis, peritonitis;

    - infections of the upper respiratory tract (including ENT organs): acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis;

    - infections of the lower respiratory tract: acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia;

    - infections of the genitourinary system: pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, mild chancroid, gonorrhea;

    - infection in gynecology: cervicitis, salpingitis, salpingoophoritis, tubo-ovarian abscess, endometritis, bacterial vaginitis, septic abortion;

    - skin and soft tissue infections: erysipelas, impetigo, secondary-infected dermatoses, abscess, phlegmon, wound infection;

    - infections of bone and connective tissues:

    - infections of the biliary tract: cholecystitis, cholangitis;

    - odontogenic infections

    - prevention of infections in surgery.

    Contraindications:

    Individual intolerance of the components that make up the drug, increased sensitivity to antibacterial drugs of the cephalosporin group and other beta-lactam antibiotics, infectious mononucleosis (including with the appearance of a crustacean rash).

    Carefully:

    Pregnancy, lactation, severe hepatic insufficiency, diseases of the gastrointestinal tract (including colitis in the anamnesis associated with the use of penicillins), chronic renal failure.

    Pregnancy and lactation:

    The drug may be administered during pregnancy only in those cases where the intended benefit to the mother exceeds the potential risk to the fetus.

    Amoxicillin and clavulanic acid penetrate into breast milk in small amounts, so if you need to use the drug during lactation, you should decide whether to stop breastfeeding.

    Dosing and Administration:

    The drug is administered intravenously. The dosage regimen is set individually, depending on the severity of the course, the localization of the infection and the sensitivity of the pathogen.

    Adults and children over 12 years of age: the drug is prescribed in a dose of 1.2 g every 8 hours (3 times a day), in the case of a severe course of infection - every 6 hours (4 times a day).

    The maximum daily dose is 6 g.

    Children up to 3 months old: premature and in the perinatal period - in a dose of 30 mg / kg (based on the entire drug) 2 times a day, in the postperinatal period - in a dose of 30 mg / kg (calculated on the whole drug) 3 times a day.

    Children aged 3 months to 12 years: in a dose of 30 mg / kg (based on the whole drug) 3 times a day; in case of severe infection - 4 times a day.

    Duration of treatment is from 5 to 14 days.

    For the prevention of postoperative infections in operations lasting less than 1 hour during introductory anesthesia is administered at a dose of 1.2 g. For longer operations, 1.2 g, every 6 hours during the day. With a high risk of infection, administration can be continued for several days.

    For patients with renal insufficiency the dose and / or the interval between drug administrations should be adjusted depending on the degree of insufficiency: when creatinine clearance is greater than 30 ml / min, dose reduction is not required; with a creatinine clearance of 10-30 ml / min, treatment starts with the introduction of 1.2 g, then 0.6 g every 12 hours; when the creatinine clearance is less than 10 ml / min - 1.2 g, then 0.6 g / day.

    For children, the dose and multiplicity of administration should be reduced in the same way.

    Since 85% of the drug is removed by hemodialysis, at the end of each hemodialysis procedure it is necessary to administer the usual dose of the drug.

    With peritoneal dialysis, dose adjustments are not required.

    Rules for the preparation and administration of solutions for intravenous injection:

    Dissolve the contents of the 600 mg (500 mg + 100 mg) vial in 10 ml of water for injection or 1.2 g (1000 mg + 200 mg) in 20 ml of water for injection.

    In / in slowly (within 3-4 minutes)

    Rules for the preparation and administration of solutions for intravenous infusion:

    For infusion administration of the drug, further dilution is necessary: ​​the prepared solutions containing 600 mg (500 mg + 100 mg) or 1.2 g (1000 mg + 200 mg) of the drug should be diluted in 50 ml or 100 ml of the infusion solution, respectively. Duration of infusion 30-40 minutes.

    As a solvent for intravenous infusion, the following infusion solutions can be used: isotonic sodium chloride solution, Ringer's solution, potassium chloride solution.

    Side effects:

    From the gastrointestinal tract: loss of appetite, nausea, vomiting, diarrhea; rarely - a violation of liver function, increased activity of alanine aminotransferase (ALT) or asparagine aminotransferase (ACT); in isolated cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.

    Allergic reactions: itching, hives, erythematous rashes; rarely - multi-form exudative erythema, angioedema, anaphylactic shock; in isolated cases - exfoliative dermatitis, Stevens-Johnson syndrome.

    From the hematopoietic system: reversible increase in prothrombin time, leukopenia, reversible agranulocytosis and hemolytic anemia.

    From the central nervous system: dizziness, headache, reversible hyperactivity and convulsions.

    From the side of the kidneys and urinary tract: interstitial nephritis, crystalluria.

    Other: Candidiasis and other types of superinfection.

    Local Reactions: in some cases, phlebitis at the site of intravenous administration.
    Overdose:

    In most cases, overdose symptoms include disorders of the gastrointestinal tract (abdominal pain, diarrhea, vomiting), anxiety can also occur, insomnia, dizziness, in isolated cases - convulsive seizures.

    In case of an overdose, the patient should be under the supervision of a physician, treatment - symptomatic. Amoxicillin + clavulanic acid is removed by hemodialysis.

    Interaction:

    Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect; bacteriostatic medicinal products (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

    The drug improves the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). With the simultaneous administration of the drug with anticoagulants, it is necessary to monitor blood coagulability.

    Amoxicillin + clavulanic acid reduces the effectiveness of oral contraceptives. With the simultaneous use of the drug with ethinyl estradiol or with drugs, during the metabolism of which parahaminobenzoic acid (PABA) is formed, there is a risk of bleeding "breakthrough".

    Diuretics, allopurinol, phenylbutazone, NSAIDs (non-steroidal anti-inflammatory drugs) and other drugs that block tubular secretion, increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

    Allopurinol increases the risk of skin rash.

    With the simultaneous use of the drug with methotrexate, the toxicity of the drug increases.

    Do not use concomitantly with disulfiram.

    Pharmaceutically incompatible with solutions containing blood, proteins, lipids, glucose, dextran, bicarbonate. Do not mix in a syringe or infusion bottle with other medicines. Incompatible with aminoglycosides.

    Special instructions:

    In course treatment it is necessary to monitor the status of the function of the organs of hematopoiesis, liver, kidneys.

    Patients with severe renal dysfunction require adequate dose adjustment or an increase in the intervals between dosing.

    Lab tests: high concentrations of amoxicillin give a false positive urine reaction to glucose when using a Benedict reagent or Fehling solution. It is recommended to use enzymatic reactions with glucosidase.

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

    Data on the adverse effects of the drug in the recommended doses on the ability to drive or work with machines there.

    Form release / dosage:Powder for solution for intravenous administration 0.5 g + 0.1 g, 1.0 g + 0.2 g.
    Packaging:

    For 0.5 g + 0.1 g, 1.0 g + 0.2 g of active substances in bottles with a capacity of 10 ml.

    1 bottle with instructions for use in a pack of cardboard.

    10 bottles with instructions for use in a cardboard box.

    For hospital:

    - 50 bottles and 5 instructions for use in a cardboard box;

    - 1 bottle with instructions for use (from 1 to 50 bottles with an equal number of instructions for use) in a cardboard box.

    Storage conditions:

    In the dark place at a temperature of no higher than 15 ° C.

    Keep out of the reach of children.

    After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001490/08
    Date of registration:14.03.2008 / 11.09.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp19.08.2017
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