Active substanceCefoperazoneCefoperazone
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    Active substance: of cefoperazone sodium (in terms of the content of cefoperazone) - 1 g.

    Description:
    White or light yellow crystalline powder. Hygroscopic.

    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.

    Active in a relationship Gram-positive microorganisms - Staphylococcus aureus and Staphylococcus epidermidis (strains producing and not producing penicillinase), Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic strain of the 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 rettgeri (formerly Proteus rettgeri), Providencia spp., Serratia spp. (incl. Serratia marcescens), Salmonella spp., Shigella spp., many strains Pseudomonas aeruginosa and Pseudomonas other species, some strains 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. and Veillonella spp.), Gram-positive sporo- and nonspore-forming anaerobes (Clostridium spp., Eubacter spp., Lactobacillus spp.) and gram-negative (including Fusobacterium spp., many strains Bacteroides fragilis spp., Prevotella spp. and other representatives of strains Bacteroides spp.). Stable in relation to broad-spectrum plasmid beta-lactamases (TEM-1-2, SHV-1), but is destroyed under the influence of extended-spectrum enzymes (TEM-3-2, SHV-2-5). Causes a teturus-like effect.

    Pharmacokinetics:Cefoperazone binds to plasma proteins by 82-93%. After intramuscular injection, the time to reach the maximum concentration of the drug is 1-2 hours, after intravenous administration - at the end of the infusion. The maximum concentration (Cmax) after intramuscular administration of 1 and 2 g is 65-75 and 97 μg / ml, respectively; after a single intravenous injection of 1, 2, 3 and 4 g (Cmax) - 153, 252, 340 and 506 μg / ml, respectively.
    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, testes, uterus, fallopian tubes, bones, cord blood and amniotic fluid. The secretion of the drug in breast milk occurs in very small quantities. The drug does not displace bilirubin from the compound with plasma proteins.
    The volume of distribution of the drug is 0.14-2 l / kg.The half-life (T1 / 2), regardless of the route of administration, is 1.6-2.4 h; with hemodialysis - 2.8-4.2 h; in newborns and children from 2 months. up to 11 years - 2.2 hours. cefoperazone in unchanged form mainly with bile (70-80%) and kidneys (20-30%). In patients with impaired liver function and bile duct obstruction, the elimination half-life is 3-7 hours, kidney removal is 90% or more. Even with severe liver damage, therapeutic concentrations are achieved in bile, and T1 / 2 is only 2-4 times longer. In patients with renal-hepatic insufficiency can cumulate.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

    - bacterial infections of the upper and lower respiratory tract (including bronchitis, pneumonia, empyema of the pleura and lung abscess);

    - infections of the kidneys and urinary tract (including pyelonephritis and cystitis);

    - infections of the abdominal cavity (including peritonitis, cholecystitis, cholangitis);

    - sepsis, meningitis;

    - infections of the skin and soft tissues;

    - infection of bones and joints;

    - infectious and inflammatory diseases of the pelvic organs (including endometritis, gonorrhea and other infections of the genital tract).

    Prevention of infectious complications after abdominal, gynecological and orthopedic operations, as well as in cardiovascular surgery.
    Contraindications:Hypersensitivity to cephalosporin and other beta-lactam antibiotics.
    Carefully:Renal and hepatic insufficiency, colitis in the anamnesis.
    Pregnancy and lactation:The use of cefoperazone during pregnancy is only permissible if the intended benefit to the mother exceeds the potential risk to the fetus. If necessary, the appointment in the lactation period should resolve the issue of stopping breastfeeding.
    Dosing and Administration:

    Cefoperazone is administered intravenously (by drip and jet) and intramuscularly.

    Adults: average daily dose of 2-4 g of cefoperazone, administered in equal portions every 12 hours. In severe infections, the daily dose may be increased to 8 grams, also administered in equal portions every 12 hours. There was no evidence of any complications cefoperazone when administered at a daily dose of 12 g and even 16 g divided into equal doses every 8 hours. Treatment can be started before the results of a study of the sensitivity of microorganisms.

    With uncomplicated gonococcal urethritis, a one-time intramuscular injection of 500 mg of the drug is recommended.

    For the prevention of postoperative complications - 1 g or 2 g IV for 30-90 min before the operation. The dose can be repeated every 12 hours, however, in most cases within no more than 24 hours.

    In cases of operations with an increased risk of infection (for example, colorectal area), or if the infection is particularly dangerous (for example, in open-heart surgery or joint prosthetics), prophylactic use can continue for 72 hours after the operation is completed.

    Patients with impaired renal function are given a usual daily dose (2-4 g). Patients who have a glomerular filtration rate below 18 ml / min or serum creatinine above 3.5 mg / ml, daily dose should not exceed 4 g.

    In patients with severe impairment of liver function, expressed by obstruction of the bile ducts, the daily dose of the drug should not exceed 2 g.

    In patients with renal-hepatic insufficiency, the concentration of cefoperazone in the blood should be monitored and, if necessary, the dose should be adjusted.

    Use in children

    In children, the daily dose of cefoperazone is 50-200 mg / kg body weight, administered in equal portions in two divided doses every 12 hours or more if necessary. The maximum daily dose is 12 g.

    For IV injections, the maximum single dose for children is 50 mg / kg, the duration of administration is at least 3-5 minutes. Newborn (<8 days) is administered a 50- 200 mg / kg body weight per day in equal parts every 12 hours. Daily doses up to

    up to 300 mg / kg were used without complications in young children and children with severe infections, including bacterial meningitis.

    Intravenous administration

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

    To prepare a solution for intravenous administration, 1 g of cefoperazone should be dissolved in 10 ml of sterile water for injection or another compatible solution and administered 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 the solution for intravenous drip, 1 g of cefoperazone is dissolved in 5 ml of sterile water for injection, the resulting solution is added to the infusion solution (Ringer's lactate solution, 5% dextrose solution,isotonic sodium chloride solution) to a concentration of 20-100 mg / ml. The duration of administration depending on the volume of the solution can be from 10-30 minutes or more.

    Intramuscular injection

    For the preparation of solutions intended for w / o Injection, may be used sterile water for injections or isotonic sodium chloride solution. To dilute 0.5 g of the drug should be used 2 ml of solvent, 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, a solution of lidocaine is recommended to prepare the solution (in case the patient does not have a 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 dilution method is recommended: first add the required amount of sterile water for injection and shake until cefoperazone powder completely dissolves,then add the required 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).

    Side effects:

    Allergic reactions: urticaria, itchy skin, maculopapular rash, fever, eosinophilia, multiform exudative erythema (including Stevens-Johnson syndrome), rarely anaphylactic shock.

    From the gastrointestinal tract: nausea, vomiting, diarrhea, pseudomembranous colitis.

    On the part of the organs of hematopoiesis and the system of hemostasis: bleeding (vitamin K deficiency), anemia, reversible neutropenia (with prolonged use). Laboratory indicators: hypoprothrombinemia, increased prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, Coombs positive reaction.

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

    Overdose:
    Symptoms: epileptic seizure.
    Treatment: sedative therapy with diazepam.
    Interaction:
    Pharmaceutically incompatible with aminoglycosides (if necessary combined therapy with cefoperazone and aminoglycoside drugs are prescribed as a sequential fractional intravenous drug administration using 2 separate intravenous catheters).
    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.
    It is not compatible with ethanol, it is possible to develop disulfiram-like reactions in the form of hyperemia, nausea, vomiting, headache, dyspnea, tachycardia, lowering blood pressure, abdominal cramps.
    Special instructions:
    Can be used with combination therapy in combination with other antibiotics.
    In cases of bile duct obstruction, severe liver disease or concomitant renal dysfunction, there may be a need to change the dosing regimen. In patients with impaired liver function and with concomitant renal damage, it is necessary to monitor the concentration of the drug in the blood serum. If the concentration of the drug is not measured in the serum, then in these cases the dose should not exceed 2 g / day.
    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 impaired food intake (eg, those suffering from cystic fibrosis), as well as patients who have been on parenteral nutrition for a long time, may there is a deficiency of vitamin K.In such patients, prothrombin time should be monitored and, if necessary, the purpose of vitamin K is indicated. When using cefoperazone (as well as other antibiotics), superinfection may develop, which requires the withdrawal of the drug and the appointment of appropriate treatment.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 1 g.


    Packaging:1 g of active substance in a hermetically sealed vial of colorless clear glass. The bottle is sealed with a rubber stopper, crimped with an aluminum cap. The aluminum cap is supplied with a plastic cap to control the first opening. Each vial with the instruction for use is placed in a cardboard box.
    Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C. The prepared solution is stable for 7 days when stored in a refrigerator (2-8 ° C). Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002589/09
    Date of registration:02.04.2009
    The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp31.10.2015
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