Active substanceCefoperazoneCefoperazone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    Each vial contains an active substance:

    Cefoperazone sodium 0.5 g 1.0 g 2.0 g

    equivalent to cefoperazone
    Description:
    White or white with a yellowish tint powder.

    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.12   Cefoperazone

    Pharmacodynamics:

    Cephalosporin semisynthetic antibiotic III generation of a wide range of activities. Has a bactericidal effect by inhibiting the synthesis of the cell wall of microorganisms: acetylates membrane-bound transpeptidases, thereby violating the cross-linking of peptidoglycans necessary to ensure the strength and rigidity of the cell wall. 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: Esherichia coli, Klebsiella spp. (including Kleb­siella pneumonia), Enterobacter spp., Citrobacter spp., Haemophilus influenzae (strains producing and non-producing beta-lactamases), Proteus mirabilis, Proteus vulgaris, Morganella morganii, Providencia rettgeri, Providcncia stuartii, Serratia marcescens, Salmonella spp. and Shigella spp., Pseudomonas spp., including Pseudomonas aeruginosa, some strains Acinetobacter spp., Neisseria gonorrhoeae (strains producing and not producing beta-lactamases) and Neisseria meningitidis, Bordetella pertussis, Yersinia enterocolitica;

    anaerobic microorganisms: Gram-positive cocci (including Peptococcus spp., Peptostreptococcus spp.), Gram-positive sporo- and nonspore-forming anaerobes (Clostridium difficile, Eubacterium spp., Lactobacillus spp.) and gram-negative rods (including Fusobacterium spp., some strains Bacteroides fragilis, and others you- teroides spp.).

    Pharmacokinetics:
    The time to reach the maximum concentration (TCmax) after intramuscular injection is 1-2 hours; after intravenous administration - at the end of the infusion. The maximum concentration (C max) in the blood serum after intramuscular injection of 0.25 g and 0.5 g of cefoperazone is 22 μg / ml and 33 μg / ml, respectively. Cmax for intravenous administration of 1 g and 2 g of the drug is 153 μg / ml and 252 μg / ml, respectively.
    The connection with plasma proteins is 82-93%.
    Cefoperazone reaches therapeutic concentrations in the tissues and body fluids: ascitic, peritoneal, synovial fluid, urine, bile and gallbladder walls, lungs, sputum, palatine tonsils, sinus mucosa, atria, kidneys, ureters, prostate, testicles, uterus, fallopian tubes, bones, cord blood, amniotic fluid, as well as in cerebrospinal fluid (with meningitis). In small concentrations cefoperazone can be found in breast milk.
    The volume of distribution is 0.14 - 2 l / kg. The half-life (T1 / 2) is an average of 2 hours, regardless of the mode of administration, 2.8 to 4.2 hours for hemodialysis,2.2 hours for newborns and children from 2 months to 11 years. It is output in active form (meta-bolziruetsya less than 1%) 70-80% with bile, 20-30% - kidneys. 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 the bile, and T 1/2 is prolonged only 2 to 4 times. In patients with renal-hepatic insufficiency can cumulate.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

    - infections of the upper and lower respiratory tract;

    - urinary tract infections;

    - infections of the skin and soft tissues;

    - infection of bones and joints;

    - Infectious inflammatory diseases of the pelvic organs (endometritis, gonorrhea);

    - abdominal infections (peritonitis, cholecystitis, cholangitis);

    - sepsis;

    - meningitis.

    Prevention of infectious complications in abdominal, gynecological and traumatological operations, as well as in cardiovascular surgery.
    Contraindications:Hypersensitivity to cephalosporins and other beta-lactam antibiotics.
    Carefully:Renal and hepatic insufficiency, colitis in the anamnesis.
    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. When appointing cefoperazona during lactation it is necessary to stop breastfeeding.
    Dosing and Administration:
    Intravenous (drip, jet), intramuscularly.
    Adults: an average daily dose of cefoperazone 2- 4 g, administered in equal parts every 12 hours. In severe infections, the daily dose can be increased to 8 g, administered also in equal parts every 12 hours. There were no complications in the administration of cefoperazone in the daily dose of 12 g and even 16 g divided into equal doses every 8 h. Treatment can be initiated 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 for no more than 24 hours.
    In case of operations with an increased risk of infection (for example, operations in the rectal area), or if the infection is especially dangerous (for example, in open-heart surgery or joint replacement), preventive 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 a serum creatinine level above 3.5 mg / dL should not exceed a daily dose of 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.Newborns (<8 days) receive 50-200 mg / kg of body weight per day in equal parts every 12 hours. Daily doses up to 300 mg / kg were applied without complications in young children and children with severe infections, including bacterial meningitis. Efficacy and safety of use in children has not been established to date.

    Intravenous administration
    A 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. 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 administration of droplets to facilitate dissolution, it is recommended to use 5 ml of solvent per 1 g of cefoperazone. The resulting solution is added to the infusion solution (Ringer's lactate solution, 5% dextrose solution, 0.9% sodium chloride solution) 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.

    Intramuscular injection

    For the preparation of solutions intended for intravenous injections, sterile water for injection or 0.9% solution of sodium chloride. 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, 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 dilution method is recommended: first add the required amount of sterile water for injection and shake until cefoperazone powder completely dissolves, 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).

    Side effects:

    Allergic reactions: urticaria, maculopapular rash, fever, eosinophilia, erythema multiforme, itching, malignant exudative erythema (Stevens-Johnson syndrome), rarely Quincke's edema, anaphylactic shock.

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

    Laboratory indicators: hypoprothrombinemia, increased prothrombin time, increased activity of "liver" transaminases and alkaline phosphatase, transient hypercreatininaemia, transient eosinophilia, decrease in hematocrit, positive Coombs reaction.

    From the hematopoiesis: anemia, reversible neutropenia (with prolonged use), bleeding.

    Local reactions: phlebitis (with intravenous administration), soreness at the injection site (with intramuscular injection).

    Other: candidiasis

    Overdose:
    Symptoms: epileptic seizure.

    Treatment: diazepam administration, symptomatic therapy.
    Interaction:
    Do not mix the solution of cefoperazone in one syringe with aminoglycosides due to the chemical-physical incompatibility (if necessary, combined therapy with these drugs cefoperazone and the aminoglycoside is administered as a sequential fractional intravenous administration, using two separate intravenous catheters).
    Non-steroidal anti-inflammatory drugs (diclofenac, ibuprofen, indomethacin, ketorolac and others), indirect anticoagulants, heparin, thrombolytics and antiagregnants (dipyridamole, alprostadil and others) increase the frequency of hypoprothrombinemia, increase the risk of bleeding.
    Aminoglycosides and looped diuretics increase the risk of developing nephrotoxicity, especially in people with kidney failure.
    With the co-administration of cefoperazone with ethanol, or if the interval between their administration is less than 5 days, a disulfiram-like reaction may occur in the form of hyperemia, nausea, vomiting, headache, dyspnea, tachycardia, lowering of blood pressure, abdominal cramps.
    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.
    Patients with hypersensitivity to penicillins may have cross-allergic reactions to cephalosporin antibiotics, including, cefoperazone.
    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 with cefoperazonom and within 5 days after it is completed, you should refrain from taking ethanol, because it is possible to develop a disulfiram-like reaction.
    Patients with a malabsorption of food (for example, suffering from muco-viscidosis), as well as patients who have been on parenteral nutrition for a long time, may have vitamin K deficiency. Such patients should be monitored for prothrombin time and, if necessary, shows the appointment of exogenous vitamin K.
    Long-term use can lead to the development of resistance of the pathogen. In the case of obstruction of the bile duct, severe liver disease or concomitant renal dysfunction,it may be necessary to change the dosage regimen.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular injection.
    Packaging:
    Powder for the preparation of a solution for intravenous and intramuscular injection of 0.5 g of cefoperazone in bottles with a capacity of 10 ml. For 1.0 and 2.0 g of cefoperazone in bottles with a capacity of 20 ml of colorless, clear glass, hermetically sealed with rubber stoppers, crimped aluminum caps with a protective plastic lid.
    One bottle with instructions for use is placed in a cardboard box.
    For hospitals: 50 bottles together with instructions for use are placed in a cardboard box.
    Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° 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-004597/09
    Date of registration:09.06.2009
    The owner of the registration certificate:Karnataka Antibiotics & Pharmaceuticals LimitedKarnataka Antibiotics & Pharmaceuticals Limited India
    Manufacturer: & nbsp
    Information update date: & nbsp28.10.2015
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