Active substanceCefazolinCefazolin
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:Active substance: Cefazolin sodium in terms of cefazolin - 1.0 g.
    Description:The powder is white or almost white.
    Pharmacotherapeutic group:Antibiotic-cephalosporin
    ATX: & nbsp

    J.01.D.B.04   Cefazolin

    Pharmacodynamics:
    Cefazolin is a generation I cephalosporin antibiotic for parenteral use; has a broad spectrum of antimicrobial action; acts bactericidal, disrupting the synthesis of the components of the cell wall of microorganisms by blocking the enzymes involved in the synthesis of the mucopeptide, which is part of the cell membrane.
    In vitro cefazolin is active against gram-positive microorganisms: Staphylococcus aureus (both producing and not producing penicillinase), Staphylococcus epidermidis; Most strains of Streptococcus spp., including Streptococcus pneumoniae and beta-hemolytic streptococci in group A; Gram-negative microorganisms: Salmonella spp., Escherichia coli, Shigella spp., Proteus mirabilis, Klebsiella spp., Haemophilus influenzae, Neisseria gonorrhoeae, Enterobacter aerogenes, Treponema spp.
    Cefazolin is ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp. (including Proteus vulgaris), Providencia rettgeri, Enterobacter cloacae, Morganella morganii, Serratia spp., strains of Staphylococcus spp., methicillin resistant, many strains of Enterococcus spp.
    Pharmacokinetics:

    The maximum concentration (CmOh) after intramuscular injection, 1 g of cefazolin is observed after 1 hour and is about 64 μg / ml; FROMmOh after intravenous administration is observed after 5 minutes and is about 188 μg / ml.

    Cefazolin quickly penetrates most tissues and body fluids (bones, joints, heart and vascular tissue, the abdominal cavity, kidneys and urinary tracts, the middle ear, the respiratory tract, skin and soft tissues, as well as into synovial, peritoneal and pericardial fluids, pleural exudate, in bile, sputum and urine), reaching a therapeutic concentration in them; passes through the placenta and in small amounts is excreted in breast milk.

    The volume of distribution is 0.12 l / kg.

    The connection with plasma proteins is 85%.

    Cefazolin is not metabolized.

    It is excreted mainly by the kidneys in unchanged form (during the first 24 hours - about 80%), as well as with bile.

    Half-life with normal kidney function is about 1.8-2.0 h.

    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to cefazolin:
    - upper and lower respiratory tract;
    - LOP-organs, including otitis media;
    - urinary tract and small gas;
    - bile ducts;
    - skin and soft tissues, including wound and burn infections;
    - bones and joints, including osteomyelitis;
    - sepsis;
    - peritonitis;
    - mastitis;
    - syphilis, gonorrhea;
    - endocarditis.
    Preventive maintenance of surgical infections in the pre- and postoperative period.
    Contraindications:Hypersensitivity to antibiotics of the cephalosporin series and other beta-lactam antibiotics; pregnancy; children up to 1 month.
    Carefully:
    In case of kidney failure and intestinal diseases, including colitis in the anamnesis; during lactation; in children under 1 year.

    Dosing and Administration:

    Enter intramuscularly or intravenously (struino or drip).

    Adults

    Recommended doses for adults, depending on the nature of the infection, are listed in Table 1.

    Table 1

    Nature of infection

    Single dose

    Frequency of administration

    Infections of medium gravity and severe

    0.5-1 g

    Every 6-8 hours

    An easy form of infection caused by sensitive Gram-positive cocci

    0.25-0.5 g

    Every 8 hours

    Acute uncomplicated urinary tract infection

    1 g

    Every 12 hours

    Pneumococcal pneumonia

    0.5 g

    Every 12 hours

    Severe, life-threatening infections (eg, sepsis, endocarditis)

    1-1.5 g

    Every 6 hours

    The maximum daily dose is -6 g.

    The average duration of treatment is 7-10 days.

    Prevention of surgical infections

    Enter 1 g for 0.5-1 h before surgery. At long operations - 0,5-1 g during the operation. If necessary, inject 0.5-1 g every 6-8 hours during the first day after the operation.

    Adults with impaired renal function

    A change in the dosing regimen is required in accordance with the creatinine clearance value (Table 2) after the initial dose, which should correspond to the nature and severity of the infection (see Table 1).

    table 2

    Creatinine clearance, ml / min

    Concentration of creatinine in plasma, mg%

    % daily dose

    Interval between administrations, hour

    55 and more

    1.5 and less

    100

    6-8

    35-54

    1,6-3,0

    100

    8

    11-34

    3,1-4,5

    50

    12

    10 or less

    4.6 and more

    50

    18-24

    Children

    The average daily dose for children (over the month) is 25-50 mg / kg; In severe infection, the dose can be increased to 100 mg / kg / day. Multiplicity of administration - 3-4 times a day.

    Children with impaired renal function

    Correction of the dosing regimen is performed depending on the values ​​of creatinine clearance (Table 3).All recommended doses are administered after the initial dose, which should match the nature and severity of the infection (see Table 1).

    Table 3

    Creatinine clearance, ml / min

    % daily dose

    Interval between administrations, hour

    70-40

    60

    12

    39-20

    25

    12

    19-5

    10

    24

    Preparation of solution and method of administration

    Intramuscularly

    1 g of the drug is dissolved in 2.5 ml of water for injection or 0.9% solution of sodium chloride and injected deep into the muscle (for example, in the upper outer quadrant of the gluteus muscle). The approximate final volume and approximate final concentration of the resulting solution are indicated in Table 4.

    Table 4

    Dosage

    Volume of solvent

    Approximate final volume

    Approximate final concentration

    1 g

    2.5 ml

    3.0 ml

    330 mg / ml

    Intravenously

    Streaming: 1 g is dissolved in 10 ml of water for injection or 0.9% solution of sodium chloride; injected slowly for 3-5 minutes.

    Drip: 1 g is dissolved in 100-250 ml of 5% glucose solution (dextrose) or 0.9% sodium chloride solution; injected for 20-30 minutes at a rate of 60-80 drops per minute.

    During the dilution the vial must be vigorously shaken until the powder is completely dissolved.

    The color change of the solution to yellowish does not mean a loss of activity of the preparation.

    Side effects:

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

    From the nervous system: convulsions.

    From the urinary system: renal dysfunction in patients with kidney disease when treated with large doses (6 g / day); renal insufficiency.

    From the digestive system: nausea, vomiting, diarrhea, abdominal pain, anorexia, bleeding, glossitis, oral candidiasis, rarely - pseudomembranous colitis, hepatitis, cholestatic jaundice.

    From the hematopoiesis: leukopenia, neutropenia, thrombocytopaia, thrombocytosis, hemolytic anemia.

    Local reactions: rarely - tenderness at the injection site with intramuscular injection; with intravenous injection - phlebitis.

    Laboratory indicators: transient increase in the activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, increased prothrombin time, false positive reaction to glucose in the urine using Benedict's solution or Felling solution, positive direct and indirect Coombs test.

    Other: at long treatment - a dysbacteriosis, a superinfection; genital candidiasis, colpitis.

    Overdose:

    Symptoms: pain, inflammatory reactions and phlebitis at the site of administration; dizziness, headache, paresthesia, possibly the development of seizures (especially in patients with impaired renal function).

    Laboratory indicators: increased levels of creatinine, blood urea nitrogen, liver enzymes and bilirubin; a positive Coombs reaction; thrombocytosis and thrombocytopenia, eosinophilia, leukopenia, and an increase in prothrombin time.

    Treatment: immediately stop the introduction of the drug, carefully monitor the vital functions of the body and the relevant laboratory indicators; therapy is symptomatic. In severe cases, hemodialysis is possible. Peritoneal dialysis is not effective.

    Interaction:
    It is not recommended simultaneous reception with anticoagulants and diuretics. With the simultaneous use of cefazolin and "loop diuretics," there is a blockage of its kaNalsevoy secretion, which leads to an increase in the concentration of cefazolin in the blood.
    Drugs that block tubular secretion, increase the concentration of cefazolin in the blood,slow down its excretion and increase the risk of development of toxic reactions.
    Aminoglycosides increase the risk of kidney damage. Cefazolin is pharmaceutically incompatible with aminoglycosides (mutual inactivation).
    With simultaneous use with ethanol, disulfiram-like reactions can occur (spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).
    Do not use together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracycline, sulfonamides, erythromycin, chloramphenicol), since there is antagonism between them and cefazolin.
    A solution of cefazolin is not recommended to be mixed in one syringe with other antibiotics.
    Special instructions:
    When a patient appears during treatment for diarrhea, the diagnosis of pseudo-membranous colitis can not be ruled out; in the case of confirmation of this diagnosis, treatment is discontinued and therapy is prescribed in accordance with the severity of the complication.
    In patients with impaired renal or hepatic function, in patients with eating disorders, patients taking long-term antibiotics, and patients treated with anticoagulants should monitor prothrombin time.Such patients may require the introduction of vitamin K.
    The administration of the drug in the absence of a bacterial infection or with an unjustified prophylactic purpose increases the risk of developing resistant microorganisms.
    The safety of cefazolin in preterm infants and children of the first year of life has not been established.
    Effect on the ability to drive transp. cf. and fur:

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 1.0 g.
    Packaging:1 g of cefazolin in a bottle of colorless glass, corked with a rubber stopper and rolled up with an aluminum cap with a plastic lid. 1 bottle with instructions for use or 50 bottles with 3-5 instructions for use 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:2 years. Do not use after the time specified on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009318/08
    Date of registration:25.11.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.)Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.) India
    Manufacturer: & nbsp
    Representation: & nbspOrchid Chemicals and Pharmaceuticals Co., Ltd.Orchid Chemicals and Pharmaceuticals Co., Ltd.Russia
    Information update date: & nbsp12.06.2017
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