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 light yellow tint of color.
    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 strain of group B), Enterococcus faecalis, many other strains of beta-hemolytic Streptococcus spp .;
    Gram-negative microorganisms Escherichia coli, Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Citrobacter 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 organisms - Gram-positive and Gram-negative cocci (including Peptococcus spp, Peptostreptococcus spp and Veillonella spp...), Gram positive asporogenous sporo- and anaerobes (Clostridium spp, Eubacterium spp, Lactobacillus spp...) and gram-negative rods (including Fusobacterium spp,. many strains of Bacteroides spp. including Bacteroides fragilis).
    Stable, in relation to plasmid beta-lactam wide-spectrum azemes (TEM-1-2, SHV-1), however, it is destroyed under the influence of broad-spectrum enzymes (TEM-3-2, SHV-2-5). Causes disulfiramoid-like effect
    Pharmacokinetics:
    The connection with plasma proteins is 82-93%. The time required to reach the maximum concentration after intramuscular injection is -1-2 h, after intravenous administration - at the end of the infusion. The maximum concentration in the blood after intramuscular injection is 1 and 2 g 65-75 and 97 μg / ml, respectively; after a single intravenous injection of 1, 2, 3 and 4 g, the maximum concentration in the blood is 153, 252, 340 and 506 μg / ml, respectively. The maximum concentration in the urine after intramuscular and intravenous administration is 2 g - 1 and more than 2.2 mg / ml, respectively.
    Cefoperazone achieves therapeutic concentrations in such tissues and body fluids as peritoneal, ascitic fluid and cerebrospinal fluid (with meningitis), urine, bile, gallbladder walls, lungs, sputum, palatine tonsils and sinus mucosa, atria, kidneys, ureters, prostate, testicles, uterus, fallopian tubes, bones, cord blood and amniotic fluid.
    The volume of distribution is 0.14-2 l / kg. The half-life is 1.6-2.4 hours, regardless of the mode of administration, 2.8-4.2 hours for hemodialysis, 2.2 hours for newborns and children from 2 months. up to 11 years. It is excreted with bile - 70-80%, kidneys - 20-30% unchanged.In patients with impaired liver function and bile duct obstruction, the elimination half-life increases to 3-7 hours, the excretion by the kidneys is 90% or more. Even with severe liver damage, therapeutic concentrations are achieved in the bile, and the half-life is only 2-4 times longer.
    In patients with renal-hepatic insufficiency cefoperazone can cumulate.
    Indications:
    Infectious and inflammatory diseases caused by microorganisms sensitive to cefoperazone: bacterial infections of the 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, infections small pelvis organs, gonorrhea.
    Prevention of infectious complications after abdominal, gynecological and orthopedic operations, as well as in cardiovascular surgery.
    Contraindications:Hypersensitivity to cefoperazon (including antibiotics group cephalosporins, penicillins and other beta-lactam antibiotics).
    Carefully:Renal and hepatic insufficiency, colitis in the anamnesis.
    Pregnancy and lactation:
    When pregnancy is used only if the intended benefit for the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation, breastfeeding should be discontinued.
    Dosing and Administration:
    Intravenous, intramuscular.
    Doses and duration of treatment are determined by the nature and severity of the course: infections and are set individually. It is recommended to monitor the concentration of cefoperazone in the blood serum (assuming that the daily dose is more than 2 g) with a combined disturbance of liver and kidney function and, if necessary, adjust the dose.
    Adults - in an average daily dose of 2 - 4 g, divided into 2 doses. In severe infections, the daily dose can be increased to 12 g and administered 2 to 4 g every 8 hours or 3 to 6 g every 12 h. Treatment with the drug can be started before the results of a study of the sensitivity of microorganisms.
    With uncomplicated gonococcal urethritis, a single intramuscular injection of 0.5 g of the drug is recommended.
    In the treatment of infections caused by Streptococcus pyogenes in adults and children, the duration of therapy should be at least 10 days.
    For the prevention of postoperative complications - intravenously for 1 g or 2 g for 30-90 min before the operation. The dose can be repeated every 12 hours (in most cases for no more than 24 hours). For operations with an increased risk of infection (for example, operations in the colorectal area) or if the infection is dangerous (for example, in open-heart surgery or joint replacement), the prophylactic use of the drug may continue for 72 hours after the operation is completed.
    Patients with a violation of liver function dose adjustment may be required with severe obstruction of the bile duct, severe liver disease or with concomitant renal dysfunction. The daily dose should not exceed 2 g, while there is no need to monitor the concentration of cefoperazone in the blood serum.

    Because the cefoperazone is mainly excreted not through the kidneys, when applied in therapeutic doses (2-4 g / day) in patients with impaired renal function, dose adjustment is not required. Patients who have a glomerular filtration rate below 18 ml / min or a serum creatinine level above 3.5 mg / dL should not exceed a daily dose of 4 g.

    When hemodialysis, the half-life of cefoperazone from the blood serum decreases slightly, so the drug should be administered after the end of dialysis.

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

    Newborns (less than 8 days) - daily dose is 50-200 mg / kg body weight; the drug should be injected every 12 hours.

    Daily doses up to 300 mg / kg were applied without complications in children "of early age and children with severe infections, including bacterial meningitis.

    Preparation of solutions for injection:

    For intramuscular injection - To 1.0 g of cefoperazone 4.0 ml of solvent is added to obtain a final concentration of cefoperazone 250 mg / ml. The following solutions can be used as solvents:

    - water for injections;

    - 0.9% solution of sodium chloride.

    To reduce the pain with intramuscular injections in cases where a solution with a concentration of 250 mg / ml or more is supposed to be introduced, it is recommended to use a solution 2% lidocaine solution (in case the patient does not have a hypersensitivity reaction to lidocaine).This solution can be prepared using water for injection in combination with 2% lidocaine solution.

    The following two-step dilution method is recommended: first add the required amount of water for injections and shake until cefoperazone powder completely dissolves, then add the necessary amount of 2% lidocaine solution and mix.

    The final concentration of cefoperazone

    Stage 1

    The volume of water for injection

    2 stage

    Volume of 2% lidocaine solution

    Bottle of 1.0 g

    250 mg / ml

    2.6 ml

    0.9 ml

    Bottle of 1.0 g

    333 mg / ml

    1.8 ml

    0.6 ml

    Intramuscular injection is done deep into the large muscle (the gluteus maximus muscle or the anterior thigh surface).

    For intravenous fluid administration - 1.0 g of the preparation is dissolved in 10 ml of solvent. The following solutions can be used as solvents:

    - water for injections;

    - 0.9% solution of sodium chloride;

    - 5% dextrose solution;

    With intravenous jet injection, the maximum single dose of the drug for adults is 2.0 g, for children - 50 mg / kg body weight. The duration of administration is at least 3-5 minutes.

    For intravenous drip - 1.0 g of the drug is dissolved in 5 ml of water for injection. The resulting solution is added to 20-100 ml of an infusion solution (0.9% sodium chloride solution, 5% dextrose solution, Ringer's lactate solution).

    The duration of intravenous drip introduction, depending on the volume of the solution can be from 10-30 minutes or more.

    When used as a solvent for sterile water for injection, its volume should not exceed 20 ml.

    Side effects:

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

    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, increased activity of "hepatic" transaminases and alkaline phosphatase, hypercreatininaemia, anemia, neutropenia, eosinophilia, Coombs positive reaction.

    Local Reactions: with intravenous injection - phlebitis; when intramuscular introduction - soreness in the injection site.

    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 in the form of sequential fractional intravenous administration of drugs using two separate intravenous catheters. Cefoperazone should be administered before the administration of the aminoglycoside.
    When co-administered with ethanol, disulfiram-like reactions may develop.
    Indirect anticoagulants, heparin, thrombolytics, antiaggregants, non-steroidal anti-inflammatory drugs 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 treatment it is necessary to 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. Cefoperazone is largely excreted with bile. In patients with liver disease or obstruction of the biliary tract, the half-life of cefoperazone from the blood plasma is usually prolonged, and the excretion of the drug by the kidneys increases. Nevertheless, even with severe violations of liver function in the bile
    therapeutic concentrations of cefoperazone are achieved, and the half-life is only 2-4 times longer.
    In cases of obstruction of the bile duct, severe liver disease or concomitant renal dysfunction, it may be necessary to change the dosage regimen.
    Can be used with combination therapy in combination with other antibiotics.
    With prolonged therapy, it is recommended to periodically monitor the kidneys, liver and hematopoiesis.This is especially important for newborns, especially premature and small children.
    Long-term use can lead to the development of resistance of the pathogen.
    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 Clostridium difficile, producing toxins A and B, which lead to the development of Clostridium 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 and 2-3 weeks after cessation of treatment should be considered as suspicious for the development of Clostridium difficile associated diarrhea. In mild cases, it is sufficient to discontinue treatment and apply ion-exchange resins (colestramine, Colestipol). In severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin, bacitracin or metronidazole is indicated.Do not use drugs that inhibit the intestinal motility.
    If it is necessary to use the drug in newborns, including preterm infants, the expected positive effects of therapy and the possible risk associated with treatment should be taken into account. In newborns with nuclear jaundice cefoperazone Do not displace bilirubin from the connection with plasma proteins.
    During the period of application of the drug, a false positive reaction to glucose in the urine can take place when using solutions of Benedict or Feling.
    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 malabsorption of food (for example, suffering from cystic fibrosis), as well as patients who have been on parenteral nutrition for a long time, may have vitamin K deficiency. These patients should be monitored for prothrombin time, and if necessary the purpose of vitamin K.
    Effect on the ability to drive transp. cf. and fur:
    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require - increased concentration and speed of psychomotor reactions.

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 1.0 g

    Packaging:For 1.0 g of the drug in bottles with a capacity of 10 ml, hermetically sealed with rubber stoppers, crimped with aluminum or combined caps. 1 bottle with instruction for use is placed in an individual pack of 50 bottles with an equal number of instructions for use placed in a cardboard box (for hospitals).
    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-001608
    Date of registration:23.03.2012
    Date of cancellation:2017-03-23
    The owner of the registration certificate:Company DEKO, LLC Company DEKO, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.10.2015
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