Active substanceCefazolinCefazolin
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.

    Composition:
    Each vial contains cefazolin sodium (USP) in an amount equivalent to 0.5 g or 1 g of cefazolin (USP).

    Description:
    One vial contains cefazolin 0.5 g or 1.0 g as cefazolin sodium salt.

    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.B.04   Cefazolin

    Pharmacodynamics:
    Cephalosporin antibiotic of the first generation for parenteral use. It acts bactericidal, disrupting the synthesis of the cell wall of microorganisms. Has a wide spectrum of action, is active against Gram-positive (Staphylococcus spp., Staphylococcus aureus (not producing and producing penicillinase, including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp. , Salmonella spp., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) microorganisms. It is active against Haemophilus influenzae, some strains of Enterobacter and Enterococcus.
    Ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.
    Pharmacokinetics:
    The time to reach the maximum concentration (Tmax) with intramuscular (in / m) administration at a dose of 500 and 1000 mg, respectively - 2 and 1 h; The maximum concentration (C max) is 38 and 64 μg / ml; after intravenous (iv) administration of TCmax - at the end of infusion, after iv administration of 1000 mg of Stax - 180 μg / ml. Penetrates into joints, tissues of the cardiovascular system, into the abdominal cavity, kidneys and urinary tract, placenta, middle ear, respiratory tract, skin and soft tissues. In small amounts excreted in breast milk. Concentration in the tissue of the gallbladder and bile is much higher than in the serum. With obstruction of the gallbladder, the concentration in the bile is less than in the plasma. The volume of distribution is 0.12 l / kg. The connection with plasma proteins is 85%. The half-life period (T1 / 2) with v / m introduction is 1.8 h, with iv injection -2 hours. If the renal function T1 / 2 is disturbed, 20-40 h.
    It is excreted mainly by the kidneys in an unchanged form: within the first 6 hours, 60-90%, after 24 hours, 70-95%. Stamens in the urine are 1000 μg / ml and 4000 μg / ml after the / m administration and doses of 500 mg and 1000 m, respectively.

    Indications:Bacterial infections of the upper and lower respiratory tract, urinary and biliary tract, pelvic organs, skin and soft tissues, bones and joints; endocarditis, sepsis, peritonitis, otitis media, osteomyelitis, mastitis; wound, burn and postoperative infections; syphilis, gonorrhea and other diseases caused by microorganisms sensitive to cefazolin. Preventive maintenance of surgical infections in the pre- and postoperative period.
    Contraindications:
    Hypersensitivity to cephalosporins and other beta-lactam antibiotics.
    Pregnancy and lactation. If necessary, breast-feeding is stopped.
    Do not appoint a newborn (up to 1 month).
    Carefully:Renal / hepatic insufficiency, pseudomembranous enterocolitis.
    Dosing and Administration:
    Intramuscularly, intravenously (struino or drip).
    The average daily intake for adults is 1 g; the frequency of administration is 2 times a day. The maximum daily dose is 6 g, the frequency of administration can be increased up to 3-4 times a day.
    The average duration of treatment with Cesolin is 7-10 days.For the prevention of postoperative infection - 1 g for 30 min before the operation, 0.5-1 g - for the operation time and for 0.5-1 g - every 6-8 h within 24 hours after the operation.
    Patients with impaired renal function require a change in the dosing regimen, in accordance with the values ​​of creatinine clearance (CK). With SC 55 ml / min or more, or with a plasma creatinine content of 1.5 mg% or less, a full dose can be administered. With SC 54-35 ml / min, or with a creatinine content of 3-1.6 mg% in the plasma, a full dose can be given, but the intervals between injections can be increased to 8 hours. With QA 34-11 ml / min or creatinine in plasma 4, 5-3.1 mg% - 1/2 dose at 12 hour intervals. Patients with CC 10 ml / min or less, or with a plasma creatinine content of 4.6 mg% or more - 1/2 of the average dose every 18-24 h. All recommended doses are administered after the initial shock dose.
    The average daily dose for children is 20-50 mg / kg; In severe infection, the dose can be increased to 100 mg / kg / day. Multiplicity of administration - 3-4 times a day. In children with impaired renal function, correction of the dosing regimen is performed depending on the values ​​of the CC. With CC 70-40 ml / min - 60% of the average daily dose and injected after 12 hours. At KK 40-20 ml / min - 25% of the average daily dose with an interval of 12 hours. Children with KK 5-20 ml / min - 10% of the average daily dose every 24 hours.All recommended doses are given after the initial shock dose.
    Preparation of solutions.
    For intramuscular injection, the drug is dissolved in 2-3 ml of water for injection, isotonic sodium chloride solution or 0.25-0.5% solution of novocaine and injected deep into the muscle.
    For intravenous drip, the drug is dissolved in 100-250 ml of isotonic sodium chloride solution or 5% glucose solution; infusion is carried out for 20-30 minutes (rate of administration of 60-80 drops per minute).
    For intravenous fluid administration, a single dose of the drug is diluted in 10 ml of isotonic sodium chloride solution and injected slowly for 3-5 minutes.
    During the dilution, the vials are vigorously shaken until the powder is completely dissolved.
    Side effects:
    Allergic reactions: hyperthermia, skin rash, urticaria, skin itching, bronchospasm, eosinophilia, Quincke's edema, arthralgia, anaphylactic shock, erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome).
    From the nervous system: convulsions.
    From the side of the urinary system: in patients with kidney disease in the treatment of large doses (6 g) - renal dysfunction (in these cases, the dose is reduced and treatment is controlled by the dynamics of urea nitrogen and creatinine in the blood).
    From the digestive system: nausea, vomiting, diarrhea, abdominal pain, pseudomembranous enterocolitis, rarely - cholestatice jaundice, hepatitis.
    From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia.
    With long-term treatment - dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidiasis stomatitis).
    Laboratory indicators: positive Coombs reaction, increased activity of "liver" transaminases, hypercreatininaemia, increased prothrombin time.
    Local reactions: with the / m introduction - soreness (at the injection site), with / in the introduction - phlebitis.
    Interaction:
    It is not recommended simultaneous reception with anticoagulants and diuretics. With the simultaneous use of cefazolin and "loop diuretics", a blockade of its tubular secretion occurs.
    Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).
    Drugs that block tubular secretion, increase concentration in the blood, slow down excretion and increase the risk of developing toxic reactions.
    Probenecid disrupts the excretion of cefazolin.
    Simultaneous administration with ethanol can cause disulfiram-like reactions.
    Special instructions:
    Patients who had a history of allergic reactions to penicillins and carbapenems may have increased sensitivity to cephalosporin antibiotics.
    During treatment with cefazolin, positive direct and indirect Coombs probes can be obtained, as well as a false positive urine reaction to sugar.
    When prescribing the drug, the exacerbation of GIT diseases, especially colitis, is possible.
    Patients using the drug should refrain from drinking alcohol.
    Safety of use in preterm infants and children of the first year of life is not established.
    Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection.
    Packaging:0.5 g or 1.0 g of active substance is placed in a vial of colorless glass, sealed with a rubber stopper, rolled up with an aluminum cap and closed with a plastic lid. Each vial with the instruction for use is placed in a cardboard box.
    Storage conditions:List B. In a dry place at a temperature of no higher than 30 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N016211 / 01
    Date of registration:05.05.2010
    The owner of the registration certificate:Lupine Co., Ltd.Lupine Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspLUPIN LIMITEDLUPIN LIMITED
    Information update date: & nbsp14.10.2015
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