Active substanceCefoperazoneCefoperazone
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:
    Cefoperazone sodium (in terms of cefoperazone) - 1000 mg.
    Description:
    Crystalline powder white or white with a yellowish hue.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.

    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 others 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. (including Serratia marcescens), Salmonella spp., Shigella spp., many strains of Pseudomonas aeruginosa and Pseudomonas of other species, some strains of Acinetobacter spp., Neisseria gonorrhoeae (strains producing and not producing beta-lactamases), Neisseria meningitidis , Bordetella pertussis, Yersinia enterocolitica; -grampolozhitelnye anaerobes and Gram negative cocci (including Peptococcus, Peptostreptococcus and Veilloneilla spp.), Gram positive asporogenous sporo- and anaerobes (Clostridium spp., Eubacterium spp., Lactobacillus spp.) and gram (including Fusobacterium spp., many strains of Bacteroides fragilis spp ., Prevotella spp., And others.representatives of strains of Bacteroides spp.).

    Pharmacokinetics:

    The connection with plasma proteins is 82-93%. The time to reach the maximum concentration (Tmax) after the / m administration is 1 -2 hours, after the IV, at the end of the infusion, the maximum concentration (Cmax) after the IM of 1000 mg, 2000 mg is 65-75 μg / 97 μg / ml, respectively; after a single intravenous administration of 1000, 2000, 3000 and 4000 mg of Cmax-153, 252, 340, 506 μg / ml, respectively. Stam in the urine after IM and in / in the administration of 2000 mg - 1000 and more than 2200 μg / ml, respectively.

    Achieves therapeutic concentrations in body tissues and fluids: peritoneal, ascitic fluid and spinal 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 volume of distribution is 0.14-2 l / kg. The half-life period (T1 / 2) 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 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, urinary excretion -90% and 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:

    Bacterial infections of the upper and lower respiratory tract, urinary tract, abdominal infections (peritonitis, cholecystitis, cholangitis, etc.), sepsis, meningitis, skin and soft tissue infections, infections of bones and joints, infectious and inflammatory diseases of the pelvic organs (endometritis, gonorrhea and other infections of the genital tract).

    Prevention of infectious complications after abdominal, gynecological, cardiovascular and orthopedic operations.

    Contraindications:Hypersensitivity (including to other beta-lactam antibiotics).
    Carefully:Renal and hepatic insufficiency, pregnancy, lactation, colitis in the anamnesis.
    Dosing and Administration:

    Intravenous and intramuscular.

    Adults - in an average daily dose of 2000-4000 mg, 2 times a day. In severe infections, the dose can be increased to 12000 mg / day: 2000-4000 mg every 8 hours, or 3000-6000 mg every 12 hours. Treatment can be started before receiving the results of the sensitivity study of microorganisms. With uncomplicated gonococcal urethritis - once, intramuscularly, 500 mg.

    For antibacterial prophylaxis of postoperative complications-IV, 1000 mg or 2000 mg 30-60 minutes before the beginning of the operation, with repeated every 12 hours (in most cases within 24 hours). In case of operations with an increased risk of infection (for example, operations in the colorectal area), or if the infection can be particularly harmful (for example, in open-heart surgery or joint prosthetics), the prophylactic use of the drug may continue for 72 hours after the operation is completed.

    In patients with renal-hepatic insufficiency - not more than 2000 mg / day. Patients with a glomerular filtration rate below 18 ml / min, or creatinine above 3.5 mg / ml - not more than 4000 mg / day. With isolated liver failure, no dose reduction is required if the patient does not receive the maximum dose, compensatory increases in renal excretion of the drug to 90% or more.

    Children - daily doses from 50 to 200 mg per 1 kg of body weight; in 2 admission (every 12 hours) or more, if necessary. Newborns (less than 8 days), every 12 hours. Daily doses, up to 300 mg / kg, are used without complications in young children and children with severe infections, including bacterial meningitis.

    Intramuscular injection

    For the preparation of solutions for intramuscular administration, the following solvents can be used:

    -styrene water for injections;

    -0.9% solution of sodium chloride;

    -0.5% solution of lidocaine hydrochloride,

    which are added to 1000 mg of cefoperazone in a volume of 3 ml. With intramuscular injection, the drug is injected deep into the gluteus muscle Freshly prepared solutions of cefoperazone are stored for no longer than 24 hours at a temperature of 5 to 25 ° C.

    Intravenous administration.

    With direct (jet) intravenous injection, the maximum single dose of cefoperazone for adults is 2000 mg, for children 50 mg / kg of body weight, while the duration of administration should be at least 3-5 minutes. A solution for intravenous administration is prepared ex tempore. The following solvents can be used:

    dextrose 5%;

    -0.9% solution of sodium chloride;

    Ringer's lactate solution;

    -styrene water for injections.

    For intravenous administration of 1000 mg of cefoperazone is dissolved in 5 ml of sterile water for injection, the resulting solution is added to the infusion solution to a concentration of 20-100 mg / ml. The duration of administration, depending on the volume of the solution, can be 10 to 30 minutes or more.

    Side effects:

    Allergic reactions: urticaria, maculopapular rash, fever, eosinophilia, erythema multiforme, incl. malignant exudative erythema (Stevens-Johnson syndrome), Coombs positive reaction.

    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 "liver" transaminases and alkaline phosphatase, hypercreatininaemia, anemia, neutropenia.

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

    Overdose:An epileptic fit. Treatment: sedation with diazepam.
    Interaction:

    Pharmaceutically incompatible with aminoglycosides (if necessary combined therapy with cefoperazone and aminoglycoside is prescribed in the form of sequential fractional intravenous administration of the drugs, using 2 separate intravenous catheters).

    With ethanol, disulfiram-like reactions.

    Indirect anticoagulants, heparin, thrombolytics increase the risk of hypoprothrombinemia, bleeding.

    Aminoglycosides and looped diuretics increase 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.

    Patients with hypersensitivity to penicillin should be prescribed with great care.

    In cases of obstruction of the bile duct, severe liver disease or concomitant renal dysfunction, it may be necessary to change the dosage regimen (see section "Method of administration and dose").

    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).

    When appointing during lactation it is necessary to stop breastfeeding.

    Patients who adhere to inadequate diet or with malabsorption of food (eg, cystic fibrosis), as well as patients who are in for a long time on parenteral nutrition, monitoring of prothrombin time may be deficient in vitamin K. Such patients should be carried out, and if necessary, they the purpose of exogenous vitamin K.

    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.
    Packaging:

    In a bottle transparent colorless glass type I with a butyl rubber cap and rubber stopper combined aluminum and plastic.

    10 bottles were placed in a cardboard box, together with instructions for use.

    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.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002223/07
    Date of registration:15.08.2007
    Expiration Date:Unlimited
    The owner of the registration certificate:Yucea Pharmaceutical Group Co., Ltd.Yucea Pharmaceutical Group Co., Ltd. China
    Manufacturer: & nbsp
    Representation: & nbspInstitute of Health CJSCInstitute of Health CJSC
    Information update date: & nbsp10.06.2018
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