Active substanceCefoperazoneCefoperazone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:active substance - cefoperazone sodium in terms of cefoperazone-1.0 g.
    Description:The powder is white or white with a yellowish hue.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.12   Cefoperazone

    Pharmacodynamics:

    Semisynthetic cephalosporin antibiotic III generation for parenteral administration only. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms.

    Cefoperazone is active in vitro for a large number of different clinically relevant microorganisms. Resistant to the action of many beta-lactamases. Active in relation to:

    - Gram-positive microorganisms: Staphylococcus aureus (strains producing and non-producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic group streptococcus A), Streptococcus agalactiae, (beta-hemolytic streptococcus group B), Streptococcus faecalis;

    - Gram-negative microorganisms: Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrobacter spp., Haemophilus influenzae, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia spp. (including Providencia rettgeri), Serratia spp. (at t. h. Serratia marcescens), Salmonella spp., Shigella spp., Pseudomonas spp. (at t.h. Pseudomonas aeruginosa), some strains Acinetobacter spp., Neisseria gonorrhoeae (strains, producing and non-reducing beta-lactamase), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica;

    -anaerobic microorganisms: gram positive cocci (including Peptococcus spp., Peptostreptococcus spp.), Clostridium spp., Eubacterium spp., Fusobacterium spp., Bacteroides fragilis, others strains Bacteroides spp.

    Pharmacokinetics:
    Relationship with plasma proteins - 82 - 93%. The time to reach the maximum concentration in plasma (TCmax) after intramuscular injection (in / m) -1-2 h, after intravenous administration (in / in) - at the end of infusion.
    Achieves therapeutic concentrations in such tissues and body fluids as peritoneal, ascitic and spinal (with meningitis), urine, bile, gallbladder walls, lungs, sputum, palatine tonsils and sinus mucosa, atria, kidneys, ureters, prostate, testes, uterus, fallopian tubes, bones, cord blood and amniotic fluid.
    The volume of distribution is 0.14-2 l / kg. The half-life period (T1 / 2) is 1.6-2.4 hours, independently of the mode of administration, 2.8-4.2 hours for hemodialysis, 2.2 hours for newborns and children from 2 months to 11 years. It is excreted with bile - 70-80%, kidneys - 20-30% unchanged. In patients with impaired liver function and obstruction of biliary tract T1 / 2 - 3 - 7 hours, excretion by the kidneys - 90% or more. Even with severe liver damage, therapeutic concentrations are achieved in bile, and T1 / 2 is only 2 to 4 times longer. In patients with renal-hepatic insufficiency can cumulate.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to cefoperazone:
    - infections of the lower and upper respiratory tract;
    - urinary tract infections;
    - infections of the abdominal cavity organs (cholangitis, cholecystitis, peritonitis);
    - meningitis;
    - septicemia;
    - infection of bones and joints;
    - infections of the skin and soft tissues;
    - infection of the pelvic organs (endometritis, genital tract infections);
    - uncomplicated gonococcal urethritis.

    Preventive maintenance of infectious complications at abdominal, gynecological, cardiovascular and orthopedic operations.
    Contraindications:Hypersensitivity to cephalosporins and other beta-lactam antibiotics.
    Carefully:Renal and hepatic insufficiency, colitis in the anamnesis, children's age till 1 year.
    Pregnancy and lactation:Cefoperazone can be used during pregnancy if the intended benefit to the mother is greater than the potential risk to the fetus. If you need to use cefoperazona during lactation should stop breastfeeding.
    Dosing and Administration:
    In / m and / in (slowly streaming or drip). The drug is injected deep in the / m into the large gluteus muscle or the anterior surface of the thigh. For intravenous administration of slow jet injection, the maximum single dose is 2 g; duration of administration - at least 3-5 minutes. The duration of IV infusion is 15-60 minutes. Doses and duration of treatment are determined by the nature and severity of the infection and are set individually.
    The dose for adults is -2-4 g / day, divided into 2 injections (every 12 hours).In severe infections, the dose can be increased to 8 g / day, divided into 2 injections (every 12 hours). Treatment with the drug can begin before the results of a study of the sensitivity of microorganisms.
    With uncomplicated gonococcal urethritis - once in / m in a dose of 500 mg. Prevention of postoperative complications: 1 g or 2 g IV for 30-90 min before the start of operations, followed by repeated administration every 12 hours (in most cases for no more than 24 hours). In operations with an increased risk of infection (for example, operations in the colorectal area), in open-heart surgery or joint replacement, prophylactic use can continue for 72 hours after the operation is completed.
    Dose correction may be required in cases of severe bile duct obstruction, severe liver disease, or concomitant liver and kidney dysfunction. In this case, the daily dose should not exceed 2 g.
    Because the cefoperazone is mainly excreted with bile, then dose adjustments for violation of kidney function when used in recommended doses (2-4 g / day) is not required. At a glomerular filtration rate of less than 18 ml / min or a serum creatinine concentration greater than 3.5 mg / dl, the daily dose should not exceed 4 g.When hemodialysis, the drug should be administered after the end of the dialysis session. It is recommended to monitor the concentration of cefoperazone in the blood serum (provided that the daily dose exceeds 2 g) with a combined violation of liver function and kidney, and if necessary adjust the dose.

    The dose for children is 50-200 mg / kg / day, divided into equal parts, administered every 8-12 hours. The maximum dose is 12 g / day. With IV slow injection, the maximum single dose is 50 mg / kg; duration of administration - not less than 3-5 min. Newborns - (aged less than 8 days) - 50-200 mg / kg / day in equal parts every 12 hours.

    In the treatment of infections caused by Streptococcus pyogenes, in adults and children, the duration of therapy should be at least 10 days.

    Preparation of solutions:

    Intramuscular injection:

    To prepare solutions, sterile water for injection is used. If it is necessary to prepare a solution with a concentration of 250 mg / ml or more, a lidocaine solution is recommended as a solvent, which is prepared by diluting a 2% solution of lidocaine in sterile water for injection (approximate concentration of lidocaine hydrochloride in the resulting solution is 0.5%).It is recommended to dilute the drug in two stages:

    1) the necessary amount of sterile water for injection is first added and shaken until the powder is completely dissolved;

    - then add the necessary amount of 2% lidocaine solution and mix.

    The ultimate

    Stage 1

    2 stage


    concentration

    The volume is sterile

    Volume of 2% solution

    Entered volume *

    cefoperazone

    water for injection

    lidocaine

    250 mg / ml

    2.6 ml

    0,9 ml

    4.0 ml

    333 mg / ml

    1.8 ml

    0.6 ml

    3,0 ml

    [1] - Excess volume allows to completely fill the syringe of the specified volume.

    IV introduction.

    The contents of the vial are first dissolved in one of the following compatible solutions for intravenous administration (at a rate of at least 2.8 ml per 1 g of cefoperazone): 5% dextrose injection, 10% solution of dextrose for injection, 5% dextrose solution in 0.9% solution of sodium chloride for injection, 0.9% solution of sodium chloride for injection, 5% dextrose solution in 0.2% solution of sodium chloride for injection, sterile water for injections. To facilitate dissolution, it is recommended to use 5 ml of solvent per 1 g of cefoperazone.

    Then the resulting solution is further diluted in one of the above solvents.

    Intravenous drip introduction

    The contents of the vial are dissolved in 20 to 100 ml of a compatible intravenous solution of the above. When used as a solvent for sterile water for injection, its volume should not exceed 20 ml. Infusion is carried out for 15 minutes up to 1 hour;

    Intravenous jet slow introduction

    The maximum dose of cefoperazone should not exceed 2 g per administration in adults and 50 mg / kg of body weight in children. The drug is dissolved in a suitable solvent (final concentration of 100 mg / ml) and injected for 3-5 minutes.

    Side effects:

    Allergic reactions: itching of the skin, maculopapular rash, urticaria, eosinophilia, fever, Stevens-Johnson syndrome, anaphylactoid reactions (including shock). The risk of developing allergic reactions is increased in patients with a tendency to allergic reactions (especially penicillin) in the anamnesis.

    From the hematopoiesis: reversible neutropenia (with prolonged treatment), false positive Coombs direct test, reduction of hemoglobin or hematocrit, eosinophilia and hypoprothrombinemia, bleeding.

    From the digestive system: nausea, vomiting, diarrhea, transient increase in activity of alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase, pseudomembranous colitis.

    Local reactions: phlebitis (with / in the introduction), soreness at the injection site (with the / m introduction).

    Overdose:
    Symptoms: neurological disorders; including convulsions.
    Treatment: symptomatic therapy. Hemodialysis is effective.
    Interaction:
    Pharmaceutically incompatible with aminoglycosides (if necessary combined therapy with cefoperazone and aminoglycoside is prescribed as a sequential fractional iv administration of drugs using 2 separate catheters).
    Incompatible with ethanol, it is possible to develop disulfiram-like reactions in the form of hyperemia, nausea, vomiting, headache, dyspnea, tachycardia, lowering of blood pressure, abdominal cramps.
    Indirect anticoagulants, heparin, thrombolytics increase the risk of hypoprothrombinemia, bleeding.
    Aminoglycosides and looped diuretics increase the risk of developing nephrotoxicity, especially in individuals with renal insufficiency.
    Drugs that reduce tubular secretion, increase the concentration of the drug in the blood and slow its elimination.

    Special instructions:
    Before the appointment of cefoperazone, you must collect a detailed allergological anamnesis in order to identify the patient's hypersensitivity to cephalosporins, penicillins and other medicines.
    If an allergic reaction occurs during treatment, cefoperazone should be discontinued and appropriate treatment initiated.
    In some patients, treatment with cefoperazone may lead to vitamin K deficiency in the body, which is due to the suppression of the intestinal flora that synthesizes this vitamin. The greatest risk is for patients with malabsorption syndrome (for example, in cystic fibrosis), as well as patients who adhere to a defective diet or who are for a long time on parenteral nutrition. In such patients during the treatment period, prothrombin time should be monitored and, if necessary, vitamin K.
    With prolonged therapy, it is recommended to periodically monitor the kidneys, liver and hematopoiesis. This is especially important for newborns, incl. preterm.
    Clostridium difficile associated diarrhea is observed against the background of almost all antibacterial drugs, including cefoperazone, and is manifested from mild forms of diarrhea to severe colitis with a fatal outcome. Treatment with antibacterial drugs leads to disruption of normal colon microflora, resulting in increased growth of Clostrifium difficile, producing toxins A and B, which lead to the development of Clostrifium difficile associated diarrhea. Hypertoxin-producing strains of Clostridium difficile lead to an increase in morbidity and mortality, as they may be resistant to ongoing antibiotic therapy. All cases of diarrhea in patients with antibiotic therapy should be considered as suspicious for the development of Clostridium difficile associated diarrhea.
    During treatment, a false positive reaction to glucose in the urine is possible, while conducting a study using solutions of Benedict or Felling. If it is necessary to use the drug in newborns, incl. premature, the expected positive effects of therapy and the possible risk associated with treatment should be considered. In newborns with nuclear jaundice cefoperazone Do not displace bilirubin from the binding sites of plasma proteins.
    Effect on the ability to drive transp. cf. and fur:use with caution.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 1.0 g.

    Packaging:
    By 1,0 g of active substance in a glass vial, hermetically sealed with a rubber stopper, followed by a cap of aluminum.
    1 bottle with instructions for use in a pack of cardboard.
    5 bottles 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 the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001650
    Date of registration:13.04.2012
    Date of cancellation:2017-04-13
    The owner of the registration certificate:LEKKO, ZAO LEKKO, ZAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp24.10.2015
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