Active substanceCefazolinCefazolin
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    The active substance is cefazolin (in the form of cefazolin sodium) 0.5 g or 1.0 g, respectively.
    Description:Powder of color from white to slightly yellowish.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.B.04   Cefazolin

    Pharmacodynamics:

    Cefazolin is a semisynthetic cephalosporin antibiotic of the first generation for parenteral administration. Like all other beta-lactam antibiotics, it has a bactericidal action, affecting synthesis of cell walls of microorganisms. Has a wide range of activities, active in a relationship

    Gram-positive aerobes: Staphylococcus spp. (sensitive to methicillin), Streptococcus spp., Streptococcus pneumoniae,

    Gram-negative aerobes: Branhamella catarrhalis, Citrobacter koseri, Escherichia coii, Haemophilus influenzae, Klebsiella spp., Neisseria gonorrhoeae, Proteus mirabilis

    anaerobes: Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Prevotella spp., Propionibacterium acnes, Veilonella spp.

    Microorganisms with intermediate sensitivity: anaerobes. Eubacterium spp.

    Ineffective in a relationship

    Gram-positive aerobes: Enterococci spp., Staphylococcus spp. (methicillin-resistant), Listeria monocytogenes

    Gram-negative aerobes: Acinetobacter baumanii, Aeromonas spp, Alcaligenes denitrificans, Bordetella spp., Campylobacter spp., Citrobacter freundii, Enterobacter spp., Legionella spp., Morganella morganii, Proteus vulgaris, Providencia spp., Pseudomonas spp., Serratia spp., Vibrio spp., Yersinia enterocolitica

    anaerobes: Bacteroides spp., Clostridium difficile,

    a also: Chlamydia spp., Mycobacterium spp., Mycoplasma spp., Rickettsia spp. Resistant to penicillin Streptococcus pneumoniae have cross-resistance to cephalosporins, such as cefazolin.

    Pharmacokinetics:

    Cefazolin is used parenterally. After intramuscular injection, the maximum serum concentrations are reached after 30-75 minutes.

    Concentrations (μg / ml) in serum after intramuscular injection:

    Dose 30 minutes 1 hour 2 hours 4 hours 6 hours 8 hours

    500 mg 36.2 36.8 37.9 15.5 6.3 3

    1 g 60,1 63,8 54, З 29,3 13,2 7,1

    Concentrations (μg / ml) in serum after intravenous administration 1 g:

    5 minutes 15 minutes 30 minutes 1 hour 2 hours 4 hours

    188,4 135,8 106,8 73,7 45,6 16,5

    About 65 - 92% of cefazolin binds to plasma proteins. Cefazolin very well penetrates into tissues, including skeletal muscles, myocardium, bone tissue, bile and the tissues of the gallbladder, endometrium and vagina. Cefazolin penetrates the placenta and is found in breast milk. In small amounts, it penetrates into the cerebrospinal fluid and intraocular fluid.

    Cefazolin is not metabolized. Most of the administered dose is subjected to glomerular filtration and is excreted in the urine in a microbiologically active form. A small part is excreted with bile. The plasma half-life is about 2 hours; in patients with impaired renal function, the half-life can be longer.

    Indications:
    Cefazolin is indicated for the treatment of infections caused by microorganisms sensitive to cefazolin:
    - Bacterial infections of the upper and lower respiratory tract;
    - urinary tract infection (including acute pyelonephritis);
    - infections of the skin and soft tissues, incl. wound and burn infections;
    - endocarditis;
    - septicemia;
    - infections of the abdominal cavity and biliary tract;
    - infections of bone and connective tissues (including osteomyelitis);
    - syphilis;
    - gonorrhea;
    - mastitis;
    - prevention of infection during surgical interventions.
    Contraindications:
    Hypersensitivity to cefazolin or other cephalosporin antibiotics;
    neonates up to 1 month (safety of use of the drug is not established).

    Carefully:Renal failure, intestinal diseases (including colitis).
    Pregnancy and lactation:The appointment of cefazolin in pregnancy is permissible only if the expected benefit for the mother exceeds the potential risk to the fetus. Cefazolin in small amounts is excreted in breast milk. If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be resolved.
    Dosing and Administration:

    Cefazolin Sandoz is intended for intravenous (including in the form of infusion) and intramuscular injection.

    Doses depend on the sensitivity of the pathogens, which caused infection, and severity course of the disease.

    Adults

    Standard doses used to treat adults:


    Dose

    Frequency of introductions

    Daily dose

    Infections of mild degree

    500 mg

    every 8 hours

    1.5 g

    gravity

    1 g

    every 12 hours

    2 grams

    Uncomplicated infections

    urinary tract

    1 g

    every 12 hours

    2 grams

    Infections of moderate severity and severe infections

    1 g

    every 6-8 hours

    3-4 grams

    Life-threatening infections

    From 1 g to 1.5 g

    every 6 hours

    4 - 6 g

    In rare cases, doses up to 12 g were used.

    Recommendations for dosing regimens adult patients with renal insufficiency:

    Creatinine clearance (ml / min / 1.73 m2)

    Serum creatinine (mg / 100 mL)

    Daily dose

    Interval between administrations

    >55

    <1,5

    Usual Dose

    Without changes

    35-54

    1,6-3,0

    Usual Dose

    With an interval of 12 hours

    11-34

    3,1-4,5

    50% of the usual dose

    With an interval of 12 hours

    < 10

    >4,6

    25% of the usual dose

    With an interval of 24 hours

    Prevention of postoperative infection.

    For 30 minutes - 1 hour before the operation, intravenous or intramuscular injection of the initial dose of 1 to 2 g.

    In long-term operations (2 hours and longer), another 500 mg-1 g during the operation is administered intravenously or intramuscularly. The dose and time of administration depend on the type and duration of the operation.

    After the operation, 500 mg - 1 g intravenously or intramuscularly with an interval of 6-8 hours is administered within 24 hours.

    If potential infections pose a great danger to the patient (eg, after heart surgery or a serious orthopedic operation, such as complete joint replacement), it is recommended to continue the postoperative injection of the drug for 24-48 hours.

    For elderly patients correction of doses is not required.

    Children aged 1 month and older.

    The daily dose for the treatment of infections of mild and moderate severity is 25 - 50 mg / kg body weight, is administered in 3-4 doses.

    In cases of severe infection, the daily dose may be increased to the maximum recommended dose of 100 mg / kg body weight.

    Recommendations on the dosage regimen in the treatment of children with renal insufficiency

    Creatinine clearance (ml / min / 1.73 m2)

    The dose of cefazolin (mg / kg)

    Dosing interval (h)

    >50

    7 (up to 500 mg per administration)

    6 to 8

    25-50

    7

    12

    10-25

    7

    24 to 36

    < 10

    7

    48 to 72

    At the beginning of treatment for children who undergo hemodialysis, the drug is administered at a dose of 7 mg / kg body weight. Since during the dialysis, serum cefazolin level is reduced by 35-65%, a dose of 3-4 mg / kg body weight is introduced between the dialysis procedures (the interval between dialysis procedures is 72 hours).

    Duration of treatment depends on the course of the disease. In accordance with the principles of antibiotic therapy, treatment with cefazolin is recommended to continue for at least 2-3 days after the disappearance of the febrile condition and / or obtaining confirmation of the eradication of the pathogen.

    Preparation of solutions for intramuscular injection.

    For intramuscular administration of Cefazolin Sandoz 1 g of the drug is dissolved in 4 ml, 0.5 g - in 2 ml of a 0.5% solution of lidocaine or water for injection.

    The maximum dose for intramuscular injection is 1 g, is injected deep into the muscle.

    When treating children under the age of 1 year should not be dissolved cefazolin in solutions of lidocaine.

    Preparation of solutions for intravenous administration.

    Solutions cefazolina with lidocaine should not be used for intravenous administration.

    For intravenous administration, Cefazolin Sandoz is dissolved in water for injection or a 0.9% solution of sodium chloride (at least 4 ml of solution is required to dissolve each gram of the powder). By slow intravenous injection (3-5 min), up to 1 g of cefazolin can be administered.

    To administer higher daily doses (4 to 6 g in 2 to 3 doses), intravenous infusion is used.

    To prepare a solution for intravenous infusion the drug is dissolved in 50-100 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose, injected for 20-30 minutes.

    During the dilution, vials should be vigorously shaken until the drug is completely dissolved. Only transparent and colorless solutions are used.

    Side effects:

    Allergic reactions: hyperthermia, urticaria, skin itching, rash, angioedema; rarely - exudative erythema multiforme (including Stevens-Johnson syndrome), Lyell's syndrome, bronchospasm, anaphylactic shock.

    Gastrointestinal tract:

    loss of appetite, diarrhea, abdominal pain, nausea and vomiting (in most cases, these symptoms are mild and disappear during or after treatment), dysbiosis; rare-transient hepatitis, cholestatic jaundice, pseudomembranous enterocolitis;

    transient increase in the level of "hepatic" transaminases, bilirubin and / or lactate dehydrogenase and alkaline phosphatase.

    Urinary system: transient increase in the level of blood urea nitrogen (AMC) and serum creatinine, rarely - renal dysfunction (when treated in large doses).

    Central nervous system: dizziness, general malaise, fatigue, nightmares, nervousness or anxiety, insomnia, drowsiness, weakness, sensation of "heat," changes in perception of color and confusion; encephalopathy and epileptiform seizures (in patients with renal insufficiency), aseptic meningitis.

    Local reactions: phlebitis at the site of intravenous injection, soreness at the injection site with intramuscular injection.

    Laboratory indicators: transitional - leukocytosis, granulocytosis, monocytosis, lymphocytopenia, basophilia, eosinophilia, granulocytopenia, neutropenia, leukopenia,thrombocytopenia, increased prothrombin time; rarely - reduction of hemoglobin and / or hematocrit, anemia, agranulocytosis, aplastic anemia, pancytopenia, hemolytic anemia.

    Other: pain in the chest, effusion to the pleural cavity, cough, rhinitis, hypoglycemia, hyperglycemia, vaginitis, thrombophlebitis, superinfection, candidiasis.

    Overdose:

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

    Laboratory indicators: elevated 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.

    Therapy: 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:
    Do not use cefazolin together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, erythromycin, chloramphenicol), since in vitro studies have shown that antagonism exists between them.
    It is not recommended joint use with probenecid (with concomitant use of probenecid, renal clearance of cefazolin decreases).
    With the simultaneous use of oral anticoagulants or high doses of heparin, control of blood clotting parameters is necessary.
    Pharmaceutically incompatible with aminoglycosides (mutual inactivation).
    At simultaneous application with aminoglycosides and diuretics the risk of development of toxic reactions increases (the control of parameters of function of kidneys is necessary).
    Special instructions:
    When appointing Cefazolin Sandoz, it is necessary to consider the possibility of developing a cross-allergy with other cephalosporins and occasionally encountering cross-allergic reactions to penicillins (especially in patients with allergic diathesis, bronchial asthma or pollinosis).
    In the presence of severe persistent diarrhea, it is necessary to consider the likelihood of developing pseudomembranous colitis associated with antibiotic therapy.Since this condition may pose a threat to the life of the patient, cefazolin should be discontinued immediately and appropriate treatment should be prescribed. The use of drugs that affect peristalsis is contraindicated. When treating patients with hypertension and heart failure, remember the sodium content in injectable solutions (48 mg per 1 g of cefazolin). Athletes need to take into account that if a solution of cefazolin with lidocaine was applied during treatment, doping tests can give positive results. Lab tests. If a urinalysis test for glucose is performed using Benedict's solution, Fehling's solution or Klinitest® tablets, the results may be false-positive, although cefazolin does not affect the results of a urine test for glucose content using the enzyme method.
    Both indirect and direct Coombs reaction can be false positive, including in newborns whose mothers received cephalosporins.
    Effect on the ability to drive transp. cf. and fur:The drug does not affect the ability to drive and other mechanisms.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g or 1.0 g.
    Packaging:
    Powder for solution for intravenous and intramuscular injection 0.5 g or 1.0 g in a vial, 1 bottle with instructions for medical use in a pack of cardboard.
    Packaging for hospitals: 10, 25, 50 or 100 bottles with instructions for medical use in a cardboard box.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C.
    Ready solutions - no more than 24 hours in a dark place at a temperature of 2-8 ° C.
    Keep out of the reach of children.
    Shelf life:
    3 years.
    Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N014844 / 01
    Date of registration:07.09.2007
    The owner of the registration certificate:Sandoz GmbHSandoz GmbH Austria
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp15.10.2015
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