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

    Composition:Cefazolin sodium (in terms of cefazolin) - 1.0 g.
    Description:
    The powder is white or white with a yellowish hue.

    Pharmacotherapeutic group:Antibiotic group cephalosporins.
    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. It has a wide spectrum of action, is active against grampolozhi-ing (Staphylococcus spp., Staphylococcus aureus (not producing and penicillinase), Streptococcus pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis) and gram (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp ., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) Of microorganisms. It is active against Haemophilus influenzae, some strains of Enterobacter spp. and Enterococcus spp.
    Ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin resistant strains of Staphylococcus spp.
    Pharmacokinetics:

    When taken orally cefazolin not absorbed. Cefazolin, administered intramuscularly or intravenously, creates high concentrations in the serum-

    With intramuscular (IM) administration cefazolin quickly absorbed from the injection site. After the / m administration, the concentrations in the blood are higher and last longer than after the administration of most other cephalosporins. Peak concentrations: after administration of 0.5 g and 1 g in the blood the following concentrations are achieved:

    Dose in / m

    Time after injection (in hours) and concentration in the blood (in μg / ml)

    1/2

    1.00

    2.00

    4.00

    6.00

    8.00

    10.00

    0.5 g

    32.20

    36.80

    37.90

    15.50

    6.30

    3.00

    1 g

    60.10

    63.80

    64.30

    29.80

    13.20

    7.10

    <4.1

    The duration of the half-life from the plasma is about two hours.

    After intravenous (iv) administration of 1 g, the maximum serum concentration in 188.4 μg / ml is reached after 5 minutes, decreasing after 4 hours to 16.5 μg / ml.

    Due to high and long levels in the blood cefazolin can be administered in a dose of 1 g with an interval of 12 hours, using a convenient scheme of two-fold administration per day.

    Approximately 70-90% of the administered dose binds to plasma proteins. Cefazolin easily penetrates into various tissues and organs, incl. and in the tonsils, gallbladder wall and appendix. Cefazolin also found in high concentrations in physiological fluids. In the absence of obstruction of the bile ducts 4 hours after injection, its concentrations in the bile are higher than those in the serum. Cefazolin reaches therapeutic concentrations in ascites and pleural fluid, inflammatory exudate, lungs, liver, skin and soft tissues, joints, heart and peritoneum, middle ear. Very high concentrations of cefazolin are created in the kidneys - after the administration of 1 g of cefazolin, its concentration in the urine is up to 4000 μg / ml. Cefazolin passes through the capillary membranes in the bones and reaches bactericidal concentrations in the fluid of the interstitial space of healthy and osteomelitic bone. In the absence of infection of meninges cefazolin is found in cerebrospinal fluid in extremely low concentrations, so we can assume that it does not pass through the blood-brain barrier. The concentration of cefazolin in the fetal blood flow is similar to that in the mother's bloodstream. Cefazolin is found in the milk of lactating women in very low concentrations.

    Cefazolin is not metabolized in the liver and is excreted unchanged.

    Cefazolin is excreted from the body mainly with urine due to glomerular filtration and tubular secretion. The amount of cefazolinum excreted in the urine is within the first 6h- 60-90%, after 24 hours - 70-95% of the administered dose. The excretion of cefazolin together with bile occurs only to a small extent.

    T1/2 from plasma is increased in patients with impaired renal function up to 20-40 hours.

    Indications:Bacterial infections caused by microorganisms sensitive to cefazolin: upper and lower respiratory tract, LOP organs (including otitis media), urinary and bile ducts, pelvic organs, skin and soft tissues, bones and joints (including osteomyelitis), endocarditis, sepsis, peritonitis, mastitis, wound, burn and postoperative infections, syphilis, gonorrhea.
    Preventive maintenance of surgical infections in the pre- and postoperative period.
    Contraindications:Hypersensitivity to drugs group cephalosporin and other (3-lactam antibiotics (including penicillins and carbapenems), the period of newborns (up to 1 month).It is not recommended simultaneous reception with anticoagulants and diuretics.
    Carefully:Renal failure, intestinal diseases (including colitis in the anamnesis), children's age from 1 to 12 months.
    Pregnancy and lactation:The drug is contraindicated in pregnancy. Breastfeeding should be discontinued if it is necessary to prescribe the drug during this period.
    Dosing and Administration:

    Cefazolin is intended only for parenteral administration - intramuscularly and intravenously (either jet or drip). Doses are set individually, taking into account the severity of the course and localization of the infection, the sensitivity of the pathogen.

    Preparation of solutions and application:

    Intramuscularly. A solution for intravenous injections is prepared by dissolving the dry matter in a 0.5% solution of lidocaine or in 2-3 ml of water for injection.

    For intravenous fluid administration, the powder is dissolved in 10 ml of sterile water for injection (at least 4 ml of solvent per 1 gram of dry matter).

    In both cases, after adding the solvent, the vial must be vigorously shaken to completely dissolve the powder.

    Doses up to 1 g of cefazolin can be administered as a slow intravenous infusion (in 3-5 minutes).If higher doses are used, infusion should be used (for a period longer than 20 and up to 30 minutes). For the preparation of the infusion solution, 100-150 ml of a 0.9% sodium chloride solution, 5% or 10% dextrose or dextrose solution with 0.9% sodium chloride solution, as well as a dextrose solution in Ringer's solution, 5% or a 10% solution of fructose in sterile water for injection, Ringer's injection solution and a 0.9% solution of sodium chloride, sodium bicarbonate. The drug is diluted in 50-100 ml of 5-10% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, 5% sodium bicarbonate solution.

    Use only freshly prepared and clear solutions. The possible yellowish color of the solution after dissolving the powder is not an indication of any change in the properties of the preparation or of differences in its therapeutic effectiveness.

    Dosing instructions for adults:

    Type of infection

    Dose

    Frequency of administration

    Infections of the lung course caused by sensitive Gram-positive cocci

    250-500 mg

    Every 8 hours

    Pneumococcal pneumonia

    0.5 g

    In 12 hours

    Acute uncomplicated urinary tract infections

    1 g

    In 12 hours

    Moderately heavy or heavy

    0.5-1 g

    After 6-8 hours

    Severe, life-threatening infections: endocarditis, septicemia

    1-1.5 g

    In 6 hours

    Use in children with normal renal function:

    Children from 1 month and older are prescribed - 25-50 mg / kg / day; the frequency of administration is 3-4 times a day. In severe infection, the dose can be increased to 100 mg / kg body weight.

    Use in patients with impaired renal function:

    Patients with impaired renal function require a change in the dosage regimen in accordance with the values ​​of CC: with a CC of 55 ml / min or more, or with a plasma creatinine concentration of 1.5 mg% or less, a full dose can be administered; with SC 54-35 ml / min or a plasma creatinine concentration of 3-1.6 mg%, a full dose can be administered, but the intervals between injections should be increased to 8 hours; with SC 34-11 ml / min or creatinine concentration in plasma 4.5-3.1 mg% - 1/2 dose at intervals of 12 hours; with CC 10 ml / min or less, or with a plasma creatinine concentration of 4.6 mg% or more - 1/2 of the usual dose every 18-24 hours. All recommended doses are administered after the initial dose corresponding to the indication and severity of the infection.

    Children who have a creatinine clearance of 70 to 40 ml / min / 1.73 m2, 60% of the average daily dose of cefazolin, divided into two injections, is administered.

    Children who have a creatinine clearance of 40 to 20 ml / min / 1.73 m2, 25% of an average daily dose of cefazolin, divided into two injections, is administered. In the case of creatinine clearance, 10% of the average daily dose of cefazolin is given between 20 and 5 ml / min / 1.73 m at intervals of 24 hours. All recommended doses are administered after the initial dose corresponding to the severity of the infection.

    Preoperative prophylaxis:

    To prevent infections during surgical interventions, the dosage of cefazolin depends on the type and duration of the operation.

    - 1 gram is administered intravenously or intramuscularly for 30 minutes - 1 hour before the beginning of the surgery (the dose is sufficient for minor surgical interventions of short duration);

    - with prolonged surgical operations (more than 2 hours), in addition, from 0.5 g to 1 g intravenously or intramuscularly during the operation itself (depending on the duration, it can also be administered during a surgical operation at regular intervals);

    - during the postoperative period after the initial dose, doses of 0.5 g to 1 g are administered intravenously or intramuscularly with an interval of 6-8 hours for 24 hours;

    - if a potential infection can pose a threat to the patient (for example, after heart surgery or after extensive orthopedic operations, such as arthroplasty), it is recommended to continue the post-operative administration of cefazolin for a period of 3 to 5 days. It is important to comply with the above dates so that sufficient concentrations of antibiotic are already present in the serum and tissues of the patient during the surgical incision.

    Side effects:

    Allergic reactions: hyperthermia, skin hyperemia, skin rash, urticaria, skin itch, toxicodermia, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, multiforme exudative erythema (including Stevens-Johnson syndrome).

    On the part of the respiratory system: suffocation, shortness of breath.

    From the nervous system: dizziness, convulsions.

    From 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 the concentration of urea nitrogen and creatinine in the blood).

    From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain, pseudomembranous colitis, cholestatic jaundice, hepatitis.

    On the part of the hematopoiesis system: leukopenia, neutropenia, thrombocythemia, thrombocytosis, hemolytic anemia. With long-term treatment - dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidiasis (including candidiasis stomatitis).

    Laboratory indicators: false-positive Coombs reaction, increased activity of "liver" transaminases, hypercreatininaemia, increased prothrombin time, false positive urine reaction to glucose.

    Local reactions: with the / m introduction - soreness (at the injection site), with / in the introduction - phlebitis.

    Overdose:
    Pain, inflammatory reactions at the injection site; dizziness, headache, paresthesia, the possible development of seizures (especially in patients with kidney disease).
    Laboratory indicators: elevated concentrations of creatinine, blood urea nitrogen, liver enzymes and bilirubin; false-positive reaction of Coombs; 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 ineffective.
    Interaction:
    It is not recommended to appoint cefazolin concomitantly with anticoagulants. With simultaneous use with "loop" diuretics (furosemide, ethacrynic acid) there is a blockade of tubular secretion of cefazolin (should be avoided together).
    The renal clearance of cefazolin decreases with simultaneous administration of probenecid, which leads to increased and longer cefazolin concentrations in the blood.
    Synergism of antibacterial action is noted in combination with aminoglycoside antibiotics, vancomycin, rifampicin. Aminoglycosides increase the risk of kidney damage. Pharmaceutically incompatible with aminoglycosides (mutual inactivation).
    Cefazolin, suppressing the intestinal flora, interferes with the synthesis of vitamin K. Therefore, with the simultaneous use with drugs that reduce platelet aggregation (nonsteroidal anti-inflammatory drugs (NSAIDs), salicylates), the risk of bleeding increases.For the same reason, with simultaneous use with anticoagulants, there is an increase in anticoagulant activity. Do not use cefazolin together with antibacterial drugs having a bacteriostatic mechanism of action (tetracyclines, sulfonamides, erythromycin, chloramphenicol), since in vitro studies have shown that antagonism exists between them. Cefazolin may cause disulfiram - similar reactions with simultaneous application with ethanol.
    Special instructions:
    Patients who had a history of allergic reactions to penicillins, 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 the drug is used, there may be an exacerbation of diseases of the gastrointestinal tract, especially colitis. When there is severe diarrhea, characteristic of pseudomembranous colitis, cefazolin should be canceled and appropriate treatment prescribed. During the treatment period, patients should refrain from drinking alcohol.With long-term use of the drug, control of the peripheral blood picture and kidney function is necessary.
    Effect on the ability to drive transp. cf. and fur:Care should be taken when driving a vehicle and other potentially dangerous mechanisms.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 1.0 g.


    Packaging:
    1.0 g of active substance in vials.
    1. 50 bottles per box of cardboard with an investment of 3 to 5 instructions for the use of the drug (for hospitals).
    2. 1; 5 or 10 bottles in an individual pack of cardboard along with instructions for use.
    3. Packaging complete with a solvent - water for injection. The kit includes:
    a) 1 bottle with the drug and 1 ampoule with water for injection for 5 ml;
    b) 5 bottles of the drug and 5 ampoules of water for injection for 5 ml;
    at) 10 vials of the drug and 10 ampoules of water for injection for 5 ml. The kit is placed in an individual pack of cardboard, along with instructions for medical use, an ampoule or ampoule knife with a knife.
    When using ampoules with incisions, a ring of fracture or a break point, the ampoule opener or the ampoule scaper is not inserted.
    Storage conditions:
    In the 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:LS-001403
    Date of registration:17.04.2013
    The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.10.2015
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