Active substanceCefepimCefepim
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.

    Composition:

    Cefepime is a sterile mixture of cefepime hydrochloride monohydrate and L - arginine. Contents of 1 bottle:

    Active substance: cefepime hydrochloride monohydrate (in terms of cefepime) 1000 mg;

    Excipient: L - arginine from 615 to 820 mg.

    Description:White or white with a yellowish tint powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.E.01   Cefepim

    Pharmacodynamics:
    Antibacterial agent from the group of cephalosporins of the IV generation. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide ^ a spectrum of action against gram-positive and gram-negative bacteria, strains resistant to aminoglycosides and / or cephalosporin antibiotics of the third generation.Highly resistant to hydrolysis by most beta-lactamases and rapidly penetrates into gram-negative bacterial cells. Inside the bacterial cell, the molecular target is penicillin-binding proteins (PSB). It is active in vivo and in vitro for gram-positive aerobes: Staphylococcus aureus (only methicillin-sensitive strains), Streptococcus pneumoniae, Streptococcus pyogenes (group A), Streptococcus spp of the viridans group; Gram-negative aerobes: Enterobacter spp., Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa.
    In vitro is active against gram-positive aerobes: Staphylococcus epidermidis (methicillin-sensitive strains only), Staphylococcus saprophyticus, Streptococcus agalactiae (group B); Gram-negative aerobes: Acinetobacter Iwoffii, Citrobacter diversus, Citrobacter freundii, Enterobacter agglomerans, Haemophilus influenzae (including strains producing beta-lactamase), Hafnia alvei, Klebsiella oxytoca, Moraxella catarrhalis (including strains producing beta-lactamases), Morganella morganii, Proteus vulgaris , Providencia rettgeri, Providencia stuartii, Serratia marcescens.
    Most strains of Enterococcus, incl. Enterococcus faecalis, Streptococcus spp (methicillin-resistant) staphylococci, Stenotrophomonas maltophilia (formerly known as Xanthomonas maltophilia), Clostridium difficile are not sensitive to cefepime. Bacteroides fragilis are not sensitive to cefepime.
    Pharmacokinetics:Bioavailability of 100%. TCmax (the time to reach the maximum concentration) after intravenous (iv) and intramuscular (IM) administration at a dose of 1 g is achieved by the end of infusion and after 1-2 hours, respectively. C max (maximum concentration) with a / m dose of 1 g - 30 mcg / ml; with iv injection in a dose of 1 g - 82μg / ml; time to reach the average therapeutic concentration in plasma - 12 h; the average therapeutic concentration at the m / m injection is 0.2 mcg / ml, with the w / v - 0.7 mcg / ml. High concentrations are determined in urine, bile, peritoneal fluid, blister exudate, bronchial mucus secretion, sputum, prostate gland, appendix and gallbladder. The volume of distribution is 0.25 l / kg, in children from 2 months to 16 years - 0.33 l / kg. The connection with plasma proteins is 20%. Metabolized in the liver and kidneys by 15%. (half-life) -2 hours, total clearance - 120 ml / min, renal clearance - 110 ml / min. It is excreted by the kidneys (by glomerular filtration in unchanged form - 85%), with breast milk. T1 / 2 -13 hr hemodialysis, continuous peritoneal dialysis at -19 h.
    Indications:
    - Infectious-inflammatory diseases caused by microorganisms sensitive to cefepime.
    - Pneumonia (moderate to severe) caused by Streptococcus pneumoniae (including concomitant bacteremia), Pseudomonas aeruginosa, Klebsiella pneumoniae or Enterobacter spp.
    - Febrile neutropenia (empirical therapy).
    - Complicated and uncomplicated urinary tract infections (including pyelonephritis) caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis.
    - Uncomplicated skin and soft tissue infections caused by Staphylococcus aureus (methicillin-sensitive strains only), Streptococcus pyogenes.
    - Complicated intra-abdominal infections (in combination with metronidazole) caused by Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Enterobacter spp ..
    - Prevention of infections in the conduct of cavitary surgery.
    Contraindications:
    - Hypersensitivity to cefepime or L-arginine, as well as to cephalosporin antibiotics, penicillins or other beta-lactam antibiotics;
    - Children up to 2 months. (for the intravenous route of administration);
    - Children under 12 years of age (for intramuscular route of administration);
    Carefully:Diseases of the gastrointestinal tract (including in the anamnesis): pseudomembranous colitis, ulcerative colitis, regional enteritis or antibiotic-associated colitis, chronic renal failure.
    Pregnancy and lactation:Use in pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.
    Dosing and Administration:

    Intravenously (IV) infusion (for at least 30 minutes) or intramuscularly (IM) (only with complicated or uncomplicated urinary tract infections of mild and moderate severity caused by E. coli).

    Pneumonia (moderate to severe) caused by Streptococcus pneumoniae (including with concomitant bacteremia), Pseudomonas aeruginosa, Klebsiella pneumoniae or Enterobacter spp.: in / in 1-2 g every 12 hours for 10 days.

    Febrile neutropenia (empirical therapy): iv 2 g every 8 hours for 7 days or until neutropenia is resolved.

    Complicated or uncomplicated urinary tract infections of mild and moderate severity caused by E. coli, Klebsiella pneumoniae, Proteus mirabilis: in / in or in / m (only for infections caused by E. coli) for 0.5-1 g every 12 hours for 7-10 days. Severe complicated or uncomplicated urinary tract infections (including pyelonephritis) caused by E. coli or Klebsiella pneumoniae: in / in 2 g every 12 hours for 10 days.

    Severe and severe infections of the skin and soft tissues caused by Staphylococcus aureus (only methicillin-sensitive strains), Streptococcus pyogenes: in / in 2 g every 12 hours for 10 days.

    Complicated intra-abdominal infections (in combination with metronidazole) caused by Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Enterobacter spp., Bacteroides fragilis: in / in 2 g every 12 hours for 7-10 days.

    To prevent infection during surgical interventions on the abdominal organs: 60 minutes before the start of the surgical operation, 2 g of the drug is injected intravenously for 30 minutes. At the end of the infusion, add an additional 500 mg of metronidazole intravenously. Metronidazole solutions should not be administered concomitantly with cefepime. Infusion system before the introduction of metronidazole should be washed.During long (more than 12 hours) surgical operations 12 hours after the first dose, it is recommended to re-administer 2 g of the drug intravenously for 30 minutes with followed by administration of 500 mg of metronidazole.

    In children from 2 months and with body weight up to 40 kg recommended dosing regimen for all indications (excluding febrile neutropenia) - 50 mg / kg every 12 h in / in; with febrile neutropenia - 50 mg / kg every 8 h. Duration of treatment as in adults. The maximum dose for children should not exceed the recommended dose for adults.

    Have patients with impaired renal function (creatinine clearance [CK] <30 ml / min), the dose of the drug should be adjusted. The initial dose of cefepime should be the same as for patients with normal renal function. The recommended maintenance doses of the drug are shown in the table.

    Creatinine clearance (CK) (ml / min)

    Recommended maintenance doses


    >50

    2 g every 8 hours (usual dose,

    2 g every 12 hours (usual dose,

    1 g every 12 hours (usual dose,

    500 mg every 12 hours (normal



    adjustment is not required)

    adjustment is not required)

    adjustment is not required)

    dose,

    adjustment is not required)

    30-50

    2 g every 8 hours

    2 g every 12 h

    1 g every 12 h

    500 mg every 12 hours

    11-29

    1 g every 12 h

    1 g every 24 h

    500 mg every 24 hours

    500 mg every 24 hours

    <10

    1 g every 24 h

    500 mg every 24 hours

    250 mg every 24 hours

    250 mg every 24 hours








    Patients on hemodialysis, on the 1st day, 1 g, then 0.5 g every 24 hours for all infections and 1 g every 24 hours for the treatment of febrile neutropenia. On the day of hemodialysis, the drug is administered after the end of the hemodialysis session; it is desirable to enter cefepime every day at the same time.

    Data on the use of the drug in children with concomitant chronic renal failure (CRF) However, given the similarity of pharmacokinetics in children and adults, the dosage regimen (dose reduction or increase in the interval between administrations) in children with CRF is similar to the dosing regimen in adults.

    To prepare a solution for intravenous administration the preparation is dissolved in 10 ml (1.0 g) of sterile water for injection, 5% dextrose solution or 0.9% sodium chloride solution. Intravenously injected intravenously for 3-5 minutes. For intravenous infusion, the prepared solution is combined with other solutions for intravenous infusions (0.9% sodium chloride solution, 5% or 10% dextrose solution, Ringer's lactate solution and 5% dextrose solution, maximum concentration 40 mg / ml) and injected within less than 30 minutes.

    For the preparation of solution for the / m introduction the drug is dissolved in sterile water for injection, 0.9% solution of sodium chloride, bacteriostatic water for injection with paraben or benzyl alcohol, in 0.5% and 1% solution of lidocaine hydrochloride (1.0 g in 2.4 ml).

    Side effects:

    Allergic reactions: skin rash (including erythematous rashes), itching, fever, anaphylactoid reactions, false-positive Coombs reaction, eosinophilia, multiforme exudative erythema (including Stevens-Johnson syndrome), rarely toxic epidermal necrolysis (Lyell's syndrome).

    Local reactions: when in / in the introduction - phlebitis, with a / m - hyperemia and tenderness at the injection site.

    From the nervous system: headache, dizziness, insomnia, paresthesia, anxiety, confusion, convulsions, encephalopathy (in the absence of dose adjustment in patients with impaired renal function).

    From the genitourinary system: vaginitis.

    From the urinary system: impaired renal function.

    From the digestive system: diarrhea, nausea, vomiting, constipation, abdominal pain, dyspepsia, pseudomembranous colitis.

    On the part of the organs of hematopoiesis: anemia (incl.aplastic and hemolytic), thrombocytopenia, leukopenia, neutropenia, pancytopenia, bleeding.

    From the respiratory system: cough, chest pain.

    From the cardiovascular system: tachycardia, dyspnea, peripheral edema. Laboratory indicators: a decrease in hematocrit, an increase in prothrombin time, an increase in urea concentration, hypercreatininaemia, hypercalcemia, an increase in the activity of "hepatic" transaminases and alkaline phosphatase, and hyperbilirubinemia.

    Other: pain in the throat, thoracology, increased sweating, back pain, asthenia, development of superinfection, oropharyngeal candidiasis.

    Change in taste, anaphylactic shock, genital itching, urticaria, toxic oil, increased partial thromboplastin time.

    Overdose:
    Symptoms: convulsions, encephalopathy, neuromuscular excitation. More common in patients with CRF.
    Treatment: hemodialysis, maintenance, symptomatic therapy
    Interaction:
    Pharmaceutically incompatible with other antimicrobial drugs and heparin.
    Diuretics, aminoglycosides, polymyxin B reduce the tubular secretion of cefepime and increase its serum concentration, extend T1 / 2, increase nephrotoxicity (increases the risk of developing nephronecrosis). Cefepim increases the ototoxicity of aminoglycosides.
    Nonsteroidal anti-inflammatory drugs, slowing the excretion of cephalosporins, increase the risk of bleeding. When used simultaneously with bactericidal antibiotics (aminoglycosides), synergism is manifested, with bacteriostatic (macrolides, chloramphenicol, tetracyclines) - antagonism. Incompatible with the solution of metronidazole (before the administration of the solution of metronidazole for the prevention of infections during surgical interventions, the infusion system should be rinsed from the solution of cefepime). To avoid possible drug interactions with other drugs, cefepime solutions (like most other beta-lactam antibiotics) should not be administered concomitantly with solutions of vancomycin, gentamicin, tobramycin, netilmicin. When prescribing cefepime with the listed drugs, each antibiotic should be administered separately.
    Special instructions:
    When using cefepime, pseudomembranous colitis may occur.Therefore, it is important to bear this diagnosis in case of diarrhea during treatment with the drug. Mild forms of colitis do not require special treatment, it is sufficient to stop the introduction of the drug; mild or severe cases may require special treatment. Contraindicated the use of drugs that inhibit intestinal motility.
    There is a possibility of cross-over hypersensitivity in patients with allergic reactions to penicillins.
    With prolonged treatment, regular monitoring of peripheral blood, indicators of the functional state of the liver and kidneys is necessary.
    With a mixed aerobic-anaerobic infection before identifying pathogens, a combination with drugs active against anaerobes is appropriate. Patients who have a meningeal dissemination from a distant foci of infection, suspicions of meningitis or a diagnosis of meningitis are confirmed, an alternative antibiotic with confirmed clinical efficacy should be prescribed.
    It is possible to detect a positive Coombs test, a false positive test for glucose in the urine.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 1.0 g.

    Packaging:
    By 1.0 g of active substance in a vial of transparent glass with a label attached and sealed with a rubber stopper and an aluminum cap with a protective plastic cover. 1 bottle with instructions for use packed in a cardboard box.
    Storage conditions:In 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 the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001599
    Date of registration:22.03.2012
    Date of cancellation:2017-03-22
    The owner of the registration certificate:Harbin Pharmaceutical Group Co., Ltd. General Pharm. FactoryHarbin Pharmaceutical Group Co., Ltd. General Pharm. Factory China
    Manufacturer: & nbsp
    Representation: & nbspHarbin Pharmaceutical Group Co., Ltd.General Pharm. FactoryHarbin Pharmaceutical Group Co., Ltd. General Pharm. FactoryChina
    Information update date: & nbsp20.10.2015
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