Active substanceCefazolinCefazolin
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection vials / complete with a solvent - water for injections (ampoules).
    Composition:
    Active substance:

    Cefazolin sodium (in terms of cefazolin) 0.5 g / 1.0 g
    Inactive solvent component (if included): water for injection 2 ml or 5 ml
    Description:
    Preparation: white or white with a yellowish tinge crystalline powder.
    Solvent: colorless, transparent, odorless liquid.
    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. Has a wide spectrum of action, is active against Gram-positive (Staphylococcus spp., Staphylococcus aureus (not producing and producing penicilliase;Streptococcus pneumoniae, Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative bacteria (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:The time to reach the maximum concentration (TCmax) with intramuscular (IM) administration at a dose of 0.5 and 1 g is 2 and 1 hour, respectively; the maximum concentration (C max) is 38 and 64 μg / ml. After intravenous (iv) administration, TCmax - at the end of infusion, after iv injection, 1 g of Cmax - 180 μg / ml. Penetrates into the joints, tissues of the heart and blood vessels, into the abdominal cavity, kidneys and urinary tracts, placenta, middle ear, respiratory tract, skin and soft tissues. In small amounts excreted in breast milk. Concentration in the tissue of the gallbladder and 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 proteins is 85%. The half-life period (T1 / 2) with a / m introduction is 1.8 hours, with iv injection -2 hours. If the renal function T1 / 2 is 20-40h. It is mainly excreted by the kidneys in the unchanged form: within the first 6 hours, 60-90%, after 24 hours, 70-95%.After intravenous administration in doses of 0.5 and 1 g, Cmax in urine is 1 mg / ml and 4 mg / ml, respectively.
    Indications:
    Bacterial infections caused by microorganisms sensitive to cephazolnum: upper and lower respiratory tract, JIOP 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 cefazolin, drugs group cephalosporin and other β-lactam antibiotics (including penicillins and carbapenems), the period of neonatal (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: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 (streamwise 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:

    For the / m introduction, 0.5 g of the drug is dissolved in 2 ml of water for injection, 1 g in 4 ml of water for injection. For intravenous administration, a single dose of the drug is diluted in 10 ml of water for

    injections, then injected slowly, within 3-5 minutes. For IV injection drip 50-100 ml of 5-10% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, 5% hydrogen carbonate solution; infusion is carried out for 20-30 minutes (rate of administration - 60-80 drops per minute). During the dilution, vials should be vigorously shaken until completely dissolved.

    The average daily intake for adults is 1-4 g; the frequency of administration is 3-4 times a day. The maximum daily dose -

    6 g. The average duration of treatment is 7-10 days.

    Instructions on the dosing regimen for adults:

    Cefazolin is intended only for parenteral administration - intramuscularly and intravenously

    (streamwise 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:

    For the / m introduction, 0.5 g of the drug is dissolved in 2 ml of water for injection, 1 g in 4 ml of water for injection. For intravenous administration, a single dose of the drug is diluted in 10 ml of water for

    injections, then injected slowly, within 3-5 minutes. For IV injection drip 50-100 ml of 5-10% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, 5% hydrogen carbonate solution; infusion is carried out for 20-30 minutes (rate of administration - 60-80 drops per minute). During the dilution, vials should be vigorously shaken until completely dissolved.

    The average daily intake for adults is 1-4 g; the frequency of administration is 3-4 times a day. The maximum daily dose is 6 g. The average duration of treatment is 7-10 days.

    Instructions on the dosing regimen for adults:

    View

    infection

    Single dose

    Frequency of administration

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

    0.5-1 g

    After 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 aged 1 month and older cefazolin appoint a dose of 25-50 mg / kg body weight per day ,.

    Multiplicity of administration - 3-4 times a day. In severe infection, the daily dose of cefazoln can be increased to 100 mg / kg of body weight. Multiplicity of administration - 3-4 times a day.

    Application in adult patients with impaired function of night

    In patients with impaired renal function, a change in the dosage regimen is required in accordance with the value of creatinine clearance (CC): with a CC of 55 ml / min or more, or with a creatinine concentration in the blood plasma of 1.5 mg% or less, a full daily dose can be administered; with SC 54-35 ml / min or at a concentration of creatinine in blood plasma of 3-1.6 mg%, a full daily dose can be administered, but the intervals between injections should be increased to 8 hours: with SC 34-11 ml / min or more the concentration of creatinine in blood plasma is 4.5-3.1 mg% administered half the usual dose every 18-24 hours. All recommended doses are administered after the initial, appropriate indication and severity of the infection.

    Application in children with impaired renal function

    Children who have a creatinine clearance of 70 to 40 ml / min / 1.73 m2, 60% of the average daily dose of cefazolinum is administered after 12 hours. When the creatinine clearance is from 40 to 20 ml / min / 1.73 m2 25% of the average daily dose of cefazolin is administered after 12 hours. With a clearance of creatinine between 20 and 5 ml / min / 1.73 m2 10% of the average daily dose of cefazolin is administered after 24 hours. All recommended doses are administered after the initial, corresponding severity of the infection.

    Perioperative prophylaxis:

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

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

    - for prolonged surgical operations (more than 2 hours), in addition, from 0.5 to 1 g intravenously or intramuscularly during the operation (you can enter the drug and during

    surgical operation, depending on its duration - through certain intervals of time);

    - during the postoperative period after the initial dose, doses from 0.5 g to 1 g 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, hives, itching,

    toxicodermia, bronchospasm, eosinophilia, angioedema, arthralgia, anaphylactic shock, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis.

    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).

    On the part of the digestive system: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, pseudomembranous colitis, cholestatic jaundice, hepatitis.

    On the part of the hematopoiesis system: leukopenia, neutropenia, thrombocytopenia, thrombocytosis, hemolytic anemia, lymphocytosis.

    Laboratory indicators: a positive Coombs reaction, an increase in the activity of "hepatic" transaminases, hypercreatininaemia, an increase in prothrombin time, a false positive urine reaction to glucose.

    Local reactions: when administered intramuscularly - soreness (at the injection site), with intravenous injection - phlebitis.

    Are common: fever.

    With long-term treatment - dysbacteriosis, superinfection caused by antibiotic-resistant strains, candidaemia (including candidiasis stomatitis), candidiasis vaginitis.

    Overdose:

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

    Laboratory indicators: increasing the concentration of creatinine, urea nitrogen in the blood;

    increased activity of liver enzymes and bilirubin concentration in the blood; falselya positive Coombs reaction; thrombocytosis, thrombocytopenia, eosinophilia, leukopenia, increased prothrombin time.

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

    Interaction:
    It is not recommended to apply cefazolin concomitantly with anticoagulants.
    With simultaneous use with "loop" diuretics (furosemide, ethacrynic acid) there is a blockade of tubular secretion of cefazolin (joint use should be avoided).
    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 microflora, prevents the synthesis of vitamin K.Therefore, with simultaneous use with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs, salicylates), the risk of bleeding increases. For the same reason, with simultaneous use with anticoagulants, there is an increase in the effect of anticoagulants.
    Do not use cefazolin together with antibacterial drugs that have a bacteriostatic mechanism of action (tetracyclines, sulfonamides, chloramphenicol), since in vitro studies have shown that antagonism exists between them.
    Cefazolin can cause disulfiram-like reactions when used concomitantly with ethanol.
    Special instructions:
    Patients with an allergy to penicillins, carbapenems in the anamnesis, may have an increased
    sensitivity to cephalosporin antibiotics. During treatment with cefazolinum it is possible to obtain a false-positive test of Coombs, as well as a false positive urine reaction to glucose. 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. The use of drugs that inhibit intestinal peristalsis is contraindicated. In patients with impaired renal function, the drug is used with caution, correction of the dosing regimen is necessary depending on the value of creatinine clearance (see "Method of administration and dose").
    Simultaneous use of aminoglycoside antibiotics increases the risk of nephrotoxicity, which requires careful monitoring of kidney function.
    It is necessary to avoid the simultaneous use of cefazolip and "loop" diuretics. During the treatment period, patients should refrain from drinking alcohol. With prolonged use of the drug, peripheral blood control and function
    Effect on the ability to drive transp. cf. and fur:During treatment, care should be taken when managing vehicles, mechanisms and other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g.
    Packaging:Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g bottles / complete with a solvent - water for injection (polyethylene ampoules) 2 ml, 5 ml.
    Primary packaging of medicinal product
    By 0.5 g or 1.0 g of the active substance in glass vials with a capacity of 10 ml, hermetically
    Corked with rubber stoppers, crimped aluminum caps with safety plastic caps. Each label is labeled with label paper, or written paper, or from polymer materials, self-adhesive.
    1 vial of the drug (0.5 g of active substance) and 1 vial of solvent with water for injection of 2 ml or 1 bottle of the drug (0.5 g of active substance) and 1 vial of solvent water for injection of 5 ml or 1 bottle with (1.0 g of active substance) and 1 ampoule with solvent water for injection of 5 ml are placed in a contour mesh box made of a polyvinylchloride film and foil of an aluminum printed lacquered.

    Secondary packaging of medicinal product
    1 bottle with the drug, together with the instruction for use, is placed in a pack of cardboard. The packets are placed in a group package.
    On 1 contour acheikova packing together with the instruction on application place in a pack from a cardboard. The packets are placed in a group package. 5, 10, 25, 50 or 100 vials with the preparation and with an equal number of instructions are placed in a box (for hospitals). On the box of cardboard paste a label. Boxes of cardboard are placed in a group package.
    Storage conditions:
    In the original packaging of the manufacturer at a temperature not exceeding 20 ° FROM.

    Shelf life:3 years. Do not use after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-003093
    Date of registration:14.07.2015
    Date of cancellation:2020-07-14
    The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.10.2015
    Illustrated instructions
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