Active substanceCefoperazoneCefoperazone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    1 bottle contains:

    Active substance:

    Cefoperazone sodium is equivalent to cefoperazone ........... 1,000 g
    Description:White or white with a yellowish tint powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.12   Cefoperazone

    Pharmacodynamics:
    Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide range of action.
    It is active against gram-positive microorganisms - Staphylococcus aureus and Staphylococcus epidermidis (strains producing and not producing penicillinase), Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic strain of group A), Streptococcus agalactiae (beta-hemolytic streptococcus group; B), Enterococcus faecalis, many other strains of beta-hemolytic Streptococcus spp .; Gram-negative microorganisms - Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrabacter spp, Haemophilus influenzae (strains producing and not producing beta-lactamases), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia spp. (including Providencia rettgeri), Serratia spp. (including Serratia marcescens), Salmonella spp., Shigella spp., Pseudomonas spp. (including many strains of Pseudomonas aeruginosa), some strains of Acinetobacter spp., Neisseria gonorrhoeae (strains producing and not producing beta-lactamases), Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica;
    anaerobic microorganisms - Gram-positive and Gram-negative cocci (including Peptococcus spp., Peptostreptococcus spp.), Gram-positive spore-forming and spore-forming anaerobes (Clostridium spp., Eubacter spp., Lactobacillus spp.) and Gram-negative bacilli (including Veillonella spp., Fusobacterium spp., Bacteroides spp. including Bacteroides fragilis).
    Stable against broad spectrum plasmid beta-lactamases (TEM-1-2, SHV-1), but it is destroyed under the influence of broad-spectrum enzymes (TEM-3-2, SHV-2-5). Causes a disulfiram-like effect.
    Pharmacokinetics:
    The connection with plasma proteins is 82-93%. TCmax (the time to reach the maximum concentration) after intramuscular (IM) administration - 1-2 hours, after intravenous (IV) -in the end of infusion, Cmax (maximum concentration) after IM im injection 1 and 2 g - 65- 75 and 97 μg / ml, respectively; after a single intravenous injection of 1, 2, 3 and 4 g of Cmax - 153, 252, 340 and 506 μg / ml, respectively. Stam in the urine after IM and in / in the introduction of 2 g - 1 and more than 2.2 mg / ml, respectively.
    Achieves therapeutic concentrations in such tissues and body fluids as peritoneal, ascitic fluid and cerebrospinal fluid (with meningitis), urine, bile, gall bladder 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. T1 / 2 (half-life) - 1.6-2.4 h, regardless of the mode of administration, 2.8-4.2 h - with hemodialysis, 2.2 h - in 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 bile duct obstruction T1 / 2 -3-7 h, excretion with the kidneys - 90% or more.Even with severe liver damage, therapeutic concentrations are achieved in the bile, and T1 / 2 is only 2-4 times lengthened: In patients with renal-hepatic insufficiency, it can accumulate.
    Indications:
    Infectious and inflammatory diseases caused by sensitive microorganisms: upper and lower respiratory tract, kidney and urinary tract, abdominal infections (peritonitis, cholecystitis, cholangitis), sepsis, meningitis, skin and soft tissue infections, infections of bones and joints, pelvic infection, gonorrhea.
    Prevention of infectious complications after abdominal, gynecological and orthopedic operations, as well as in cardiovascular surgery.
    Contraindications:Hypersensitivity (including, to other beta-lactam antibiotics).
    Carefully:Renal-hepatic insufficiency, colitis in the anamnesis, children's age.
    Pregnancy and lactation:
    The purpose of the drug during pregnancy is possible only in cases where the intended use for 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:Intravenous (intravenously), intramuscularly (in / m). Adults - in an average daily dose of 2-4 g, divided into 2 doses. In severe infections, the dose can be increased to 12 g / day: 2-4 g every 8 h or 3-6 g every 12 h. Treatment can be initiated 1 before the results of a study of the sensitivity of microorganisms. With uncomplicated gonococcal urethritis - once, in / m, 500 mg. For the prevention of postoperative complications - IV, 1 g or 2 g for 30-60 min before the start of the operation, with repeated every 12 hours (in most cases within 24 hours). In operations with an increased risk of infection (eg, operations in the colorectal area), or if the infection is dangerous (for example, when operations on the open heart or joint prosthetics), preventive use of the drug can continue for 72 hours after the operation is completed.

    Children the drug should be prescribed in daily doses at a rate of 50 to 200 mg per 1 kg of body weight; the drug should be injected every 8-12 hours. The maximum daily dose is 12 g.

    With intravenous infusion of slow injection, the maximum single dose is 50 mg / kg of body weight; duration of administration - at least 3-5 minutes.

    Newborns (Less than 8 days) the daily dose is from 50 to 200 mg / kg; the drug should be injected every 12 hours.

    When abnormal liver function Dose adjustment may be required when severe severe obstruction of the bile duct, or severe liver disease with concomitant renal dysfunction. The daily dose should not exceed 2 g, with no need to control the concentration of cefoperazone in serum.

    Patients with impaired renal function the drug can be administered in an average daily dose (2-4 g). Patients who have glomerular filtration rate below 18 ml / min, or serum creatinine above 3.5 mg / dL, the daily dose should not exceed 4 g In hemodialysis cefoperazone half-life from the blood serum decreases somewhat, and the drug should be administered after dialysis closure.

    Rules for the preparation and administration of a solution for intravenous administration

    For the preparation of solutions intended for w / o Injection, may be used sterile water for injection or 0.9% solution of sodium chloride. For breeding 1 g - 4 ml to obtain a final concentration of cefoperazone 250 mg / ml.To reduce pain with intramuscular injections, when a solution with a concentration of 250 mg / ml and more is intended to be administered, it is recommended to use a 2% lidocaine solution to prepare the solution (in case the patient has no hypersensitivity reaction to lidocaine). This solution can be prepared using sterile water for injection in combination with a 2% solution of lidocaine. The following two-step method of dilution is recommended: first add the required amount of sterile water for injection and shake until the powder cefoperazona completely dissolved, then add the necessary amount of 2% lidocaine and mix.

    The final concentration of cefoperazone

    Stage 1

    Sterile water volume

    2 stage

    Volume of 2% lidocaine

    Bottle 1 g

    250 mg / ml

    2.6 ml

    0.9 ml

    Bottle 1 g

    333 mg / ml

    1.8 ml

    0.6 ml

    In / m injection is made deep into the large muscle (the gluteus maximus muscle or the anterior surface of the thigh).

    Rules for the preparation and administration of a solution for intravenous administration Solution for intravenous administration is prepared ex tempore.

    As a solvent, 5% dextrose solution, 10% dextrose solution, 0.9% sodium chloride solution, sterile water for injection can be used.

    For cooking; solution for iv injection is necessary 1 g of cefoperazone dissolved in 10 ml of sterile water for injection or other compatible solution and injected for a minimum of 3-5 minutes. For intravenous administration, the maximum single dose of cefoperazone for adults is 2 g, for children - 50 mg / kg body weight.

    When preparing a solution for intravenous administration of droplets to facilitate dissolution, it is recommended to use 5 ml of solvent per g of cefoperazone. The resulting solution is added to the infusion solution (Ringer's lactate solution, 5% dextrose solution, 0.9% solution of sodium chloride) in a volume of 20-100 ml. The duration of administration, depending on the volume of the solution can be from 10-30 minutes or more.

    Side effects:

    Allergic reactions: urticaria, maculopapular rash, fever, multiforme exudative erythema (including Stevens-Johnson syndrome), itchy skin, Quincke's edema, anaphylactic shock.

    From the digestive system: nausea, vomiting, diarrhea, pseudomembranous colitis.

    On the part of the organs of hematopoiesis and the system of hemostasis: bleeding (vitamin K deficiency).

    Laboratory indicators: hypoprothrombinemia, increased prothrombin time, false-positive Coombs reaction, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, anemia, neutropenia, eosinophilia.

    Local reactions: with iv administration - phlebitis, thrombophlebitis; with the / m introduction, pain in the injection site, the formation of infiltrates and abscesses.

    Other: Candidiasis, including candidiasis stomatitis, candida colpitis.

    Overdose:
    Symptoms: neurological disorders, including convulsions.

    Treatment: symptomatic, sedative 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 intravenous catheters).
    When co-administered with ethanol, disulfiram-like reactions may develop.
    Antiaggregants, non-steroidal anti-inflammatory drugs, 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:
    Can be used with combination therapy in combination with other antibiotics. In cases of obstruction of the bile duct, severe liver disease or concomitant renal dysfunction, it may be necessary to change the dosage regimen.
    Long-term use can lead to the development of resistance of the pathogen. During the use of the drug, a false positive reaction to glucose in the urine with a solution of Benedict or Feling can take place.
    During treatment should be refrained from taking ethanol - there may be effects similar to the action of disulfiram (facial skin hyperemia, stomach and stomach spasms, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).
    Patients who adhere to a defective diet or who have a malnutrition (eg, those suffering from cystic fibrosis), as well as patients who have been on parenteral nutrition for a long time, may have vitamin K deficiency.In such patients, prothrombin time should be monitored and, if necessary, the purpose of vitamin K is indicated. The stability of the prepared solutions depends on their concentration and the nature of the solvent. Shelf life should not exceed 24 hours at room temperature; 5 days - when stored in the refrigerator at a temperature of 2 to 8 ° C. Solutions should be stored in glass or plastic syringes, glass or plastic bottles, designed to store solutions for parenteral administration.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 1g.


    Packaging:By 1.0 g of active substance in a clear glass bottle, sealed with a rubber stopper, crimped with an aluminum cap with a safety plastic lid. Each vial with instructions for use is placed in a cardboard box.
    Storage conditions:
    LIST OF B.
    Store in a 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 stated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004328/10
    Date of registration:17.05.2010
    The owner of the registration certificate:Agio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAgio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd.
    Information update date: & nbsp28.10.2015
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