Active substanceCeftazidimeCeftazidime
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    1 bottle contains:

    Active substance: Ceftazidime Pentahydrate is equivalent to ceftazidime-2000.0 mg.

    Excipients: sodium carbonate.
    Description:White or light yellow crystalline powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.02   Ceftazidime

    Pharmacodynamics:
    Ceftazidime, a cephalosporin antibiotic of the third generation, has a bactericidal effect due to damage to the bacterial cell wall (acetylates membrane-bound transpeptide ase, violating the cross-linking of petyidoglycans necessary to ensure the strength and rigidity of the cell wall).

    Ceftazidime has a broad spectrum of antimicrobial activity. It is active against Gram-negative bacteria - Citrobacter spp. (including Citrobacter freundii, Citrobacter diversus), Enterobacter spp. (Including Enterobacter cloacae, Enterobacter aerogenes), Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus ducreyi, Klebssiella spp., Including Klebssiella pneumoniae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Pseudomonas spp. (Including Pseudomonas aeruginosa), Serratia spp., Pasteurella multocida, Gram-positive bacteria -Staphylococcus aureus, including strains producing and producing no penicillinase, Streptococcus agalactiae (Group B Streptococcus), Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococci groups A ), Streptococcus mitis, Streptococcus spp .; anaerobic bacteria -.... Propionibacterium spp, Clostridium spp, Fusobacterium spp, Bacteroides spp, (however many resistant strains of Bacteroides fragilis). Has a pronounced activity against Pseudomonas aeruginosa, a significantly lower activity - against streptococci

    (primarily Streptococcus pneumoniae). Resistant to the action of most beta-lactamases. Ceftazidime not active against methicillin-resistant staphylococci, Streptococcus feacalis, Enterococcus spp, Listeria monocytogenes, Campylobacter spp., Clostridium difficile.

    It is active in vitro against strains of the following microorganisms (the clinical significance of this activity is unknown): Clostridium perfringens, not including Clostridium difficile, Acinetobacter spp., Haemophilus parainfluenzae, Morganella morganii, Neisseria gonorrhoeae, Peptococcus spp., Peptostreptococcus spp., Providencia spp., Providencia rettgeri , Salmonella spp., Shigella spp., Staphylococcus epidermidis, Yersinia enterocolitica.
    Pharmacokinetics:
    After administration, the drug is rapidly distributed in the human body and ^ reaches therapeutic concentrations in most tissues and fluids,

    including synovial, pericardial and peritoneal fluid, as well as in bile, sputum and urine. Distribution also occurs in the bones, myocardium, gall bladder, skin and soft tissues in concentrations sufficient for the treatment of infectious diseases, especially in inflammatory processes that enhance the diffusion of the drug. Poorly penetrates through intact blood-brain barrier, but achieved by the drug in the cerebrospinal fluid therapeutic level is sufficient for the treatment of meningitis. Reversibly binds to plasma proteins (less than 15%), and the bactericidal action has only a free form. The degree of binding to proteins does not depend on the concentration. The maximum concentration for intramuscular injection of 0.5 g or 1 g in an hour is, respectively, 17 μg / ml and 39 μg / ml, with intravenous administration of 42 μg / ml and 69 μg / ml, respectively.

    The time to reach the maximum concentration with intramuscular injection is 1h, with intravenous administration - by the end of the infusion. The drug concentration of 4 μg / ml is maintained for 6 to 8 hours.The therapeutic concentration in the blood plasma is maintained for 8 to 12 hours. The half-life period with normal renal function is 1.8 hours; at disturbed -2,2 hours.

    The drug is not metabolized in the liver, a violation of the liver does not affect the pharmacokinetics of the drug. The dose in such patients remains normal.

    It is excreted unchanged in kidneys to 80-90% (70% of the administered dose is excreted in the first 4 hours during the day by glomerular filtration and tubular secretion equally.) If the renal function is impaired, a dose reduction is recommended.
    Indications:
    Ceftazidime is given to adults and children for the treatment of the following infectious diseases caused by microorganisms that are sensitive to the drug:

    - respiratory tract infections (bronchitis, infected bronchiectasis, pneumonia, lung abscess, pleural empyema, treatment of infections in patients with cystic fibrosis);

    - Infectious and inflammatory diseases of the ear, throat, nose (otitis media, mastoiditis, sinusitis);

    - infection of the kidneys and urinary tract (pyelitis, prostatitis, cystitis, urethritis, kidney abscess);

    ^ - skin and soft tissue infections (phlegmon, erysipelas, wound infections, mastitis,

    skin ulcer);

    - infection of bones and joints (osteomyelitis, septic arthritis);

    - infectious diseases of the abdominal cavity, gallbladder and bile ducts (cholangitis, cholecystitis, gall bladder empyema, retroperitoneal abscesses, diverticulitis, enterocolitis);

    - infectious diseases of the pelvic organs;

    - septicemia, peritonitis, severe purulent-septic conditions;

    - meningitis;

    - gonorrhea.
    Contraindications:Hypersensitivity to ceftazidime and to the group of cephalosporins and penicillins.
    Carefully:Renal failure, neonatal period, colitis in history, patients with malabsorption syndrome (increased risk of decreased prothrombin activity, especially in persons with severe renal and / or liver failure).
    Pregnancy and lactation:
    During pregnancy ceftazidime appoint only if the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be solved.
    Dosing and Administration:

    Ceftazidime is administered intravenously (either jet or drip) or intramuscularly (should be injected into large muscles).The dose of the drug is determined individually, taking into account the severity of the disease, localization of infection and sensitivity of the pathogen, age and body weight, kidney function. The duration of treatment is 7-14 days. In infections caused by Pseudomonas aeruginosa (pneumonia, in patients with cystic fibrosis, meningitis) treatment course can be increased up to 21 days.

    Usual dose for adults and children over 12 years of age:

    - with complicated infections of the urinary tract intramuscularly or

    intravenously, 500 mg - 1 g every 8-12 hours;

    - with uncomplicated pneumonia and skin infections intramuscularly or intravenously, 500 mg - 1 g every 8 hours;

    - in cystic fibrosis, lung infections caused by Pseudomonas spp. from 100 to 150 mg / kg / day, the frequency of administration - 3 times a day (dose up to 9 g / day in such patients did not cause complications);

    - at infections of bones and joints intravenously on 2 g every 12 h;

    - with extremely severe or life-threatening infections (including patients with neutropenia) intravenously, 2 g every 8 hours.

    After an initial loading dose of 1 g, adults with impaired renal function (including patients undergoing dialysis) may require a dose reduction as indicated below:

    CREATINE CREATININE

    DOSE

    > 50 ml / min (0.83 ml / s)

    See section "Usual dose for adults and children over 12 years of age"

    31-50 ml / min (0.52-0.83 ml / sec)

    1 g every 12 h

    16 to 30 ml / min (0.27 to 0.50 ml / s)

    1 g every 24 h

    6-15 ml / min (0.10 to 0.25 ml / s)

    500 mg every 24 hours

    <5 ml / min (0.08 ml / s)

    500 mg every 48 hours

    Patients undergoing hemodialysis

    1 g after each session hemodialysis

    Patients undergoing peritoneal dialysis

    500 mg every 24 hours

    These indicators are approximate. In such patients it is recommended to monitor the serum level of the drug, which should not exceed 40 mg / l.

    The half-life of the drug during hemodialysis is 3 to 5 hours. The appropriate dose of the drug should be repeated after each period of dialysis.

    When peritoneal dialysis a drug ceftazidime can be included in dialysis fluid at a dose of 125 mg to 250 mg per 2 liters of dialysis fluid.

    Usual dose for children under 12 years:

    Children under 2 months. - intravenous infusion of 30 mg / kg / day / day (the frequency of administration 2 times a day).

    Children from 2 months. and up to 12 years - intravenous infusion 30 - 50 mg / kg per day (the frequency of administration 3 times a day).

    Dosage up to 150 mg / kg / day every 12 hours prescribed for children with reduced immunity, cystic fibrosis, meningitis. The maximum daily intake for children should not exceed 6 g.

    PREPARATION OF SOLUTIONS 1. "PRIMARY" DEVELOPMENT

    2.0 g

    3 ml of water for injection

    10 ml of water for injection

    with intramuscular

    for intravenous

    administered.

    administered.

    In the prepared solution, small bubbles of carbon dioxide may be present, which does not affect the effectiveness of the preparation.

    2. "SECONDARYE "BREEDING

    For intravenous DROPS introduction, the preparation solution prepared in the manner described above ceftazidime further dilute in 50 - 100 ml of one of the following solvents intended for intravenous administration:

    - 0.9% solution of sodium chloride;

    - Ringer's solution;

    - lactated Ringer's solution

    - dextrose solution 5%;

    - dextrose solution 5% with 0.9% sodium chloride solution;

    - 10% dextrose solution.

    During the dilution the vials with the preparation should be vigorously shaken until the contents are completely dissolved. Before introducing the solution, you should visually check that there are no foreign particles or sediment.

    Side effects:

    Allergic reactions: urticaria, fever, eosinophilia, skin itch, toxic epidermal necrolysis (Lyell's syndrome), multiforme exudative erythema (incl.Stevens-Johnson syndrome), angioedema, bronchospasm, anaphylactic shock.

    Local reactions: with iv introduction - phlebitis; with the / m introduction - soreness, burning, compaction at the injection site.

    From the nervous system: headache, dizziness, paresthesia, convulsive seizures, encephalopathy, "fluttering" tremor.

    From the genitourinary system: candidiasis vaginitis, impaired renal function.

    On the part of the national system: nausea, vomiting, diarrhea, abdominal pain, colitis, cholestasis, oropharyngeal candidiasis.

    From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, lymphocytosis, hemolytic anemia, hemorrhages.

    Other: nosebleeds, candidiasis, superinfection.

    Laboratory indicators: hyperkreatininemia, increased urea concentration, false positive urine response to glucose, increased activity of "hepatic" transaminases and alkaline phosphatase, hyperbilirubinemia, an increase in prothrombin time.

    Overdose:
    Symptoms: dizziness, paresthesia, headache, convulsive seizures, deviations in the results of laboratory tests.

    Treatment: since there is no specific antidote, overdose treatment is symptomatic and supportive. In case of severe overdose, when conservative therapy is unsuccessful, the concentration of the drug in the blood can be reduced by hemodialysis.
    Interaction:
    Pharmacologically incompatible with aminoglycosides (significant mutual inactivation: with simultaneous use these drugs should be administered to different parts of the body) and vancomycin (forms a precipitate depending on the concentration, if necessary, administer two drugs through a single tube, between their use of the IV system should be Rinse). Do not use sodium bicarbonate solution as a solvent (carbon dioxide is formed, this may require the gas to be discharged outside). Loop diuretics, aminoglycosides, vancomycin, clindamycin reduce the clearance of ceftazidime, as a result of which the risk of nephrotoxic action increases.

    Bacteriostatic antibiotics (incl. chloramphenicol) reduce the effectiveness of the drug.

    Pharmaceutically compatible with the following solutions: at a concentration of ^ 1 to 40 mg / ml - sodium chloride 0.9%, sodium lactate, Hartmann's solution, dextrose

    5%, sodium chloride 0.225% and dextrose 5%, sodium chloride 0.45% and dextrose 5%, sodium chloride 0.9% centner dextrose 5%, sodium chloride 0.18% and dextrose 4%, dextrose 10%, dextran 40: 10% in a solution of sodium chloride 0.9%, dextran 40: 10% in a 5% dextrose solution, dextran 70: 6% in a solution of sodium chloride 0.9%, dextran 70: 6% in a 5% dextrose solution.

    At a concentration of 0.05 to 0.25 mg / ml ceftazidime compatible with the solution for intraperitoneal dialysis (lactate).

    For the / m introduction ceftazidime can be diluted with a solution of lidocaine hydrochloride 0.5% or 1%. Both components remain active if ceftazidime is added to the following solutions (concentration of ceftazidime 4 mg / ml): hydrocortisone (hydrocortisone sodium phosphate) 1 mg / ml in a 0.9% sodium chloride solution or 5% dextrose solution, cefuroxime (cefuroxime 3 mg / ml in a solution of sodium chloride 0.9%, cloxacillin (cloxacillin sodium) 4 mg / ml in a solution of sodium chloride 0.9%, heparin 10 IU / ml or 50 IU / ml in a solution of sodium chloride 0.9% potassium chloride 10 mEq / L or 40 mEq / L in a 0.9% sodium chloride solution. When mixing a solution of ceftazidime (500 mg in 1.5 ml of water for injection) and metronidazole (500 mg / 100 ml), both components remain active.
    Special instructions:
    Patients with a history of allergic reactions to penicillins are noted to have cross-sensitivity to cephalosporins. Ceftazidime can inhibit the synthesis of vitamin K due to the suppression of intestinal flora, which can cause a decrease in the level of vitamin-dependent

    The factors of blood coagulation, and in rare cases lead to hypothrombinemia. In elderly and weakened patients, in patients with impaired liver function and in people with malnutrition, the risk of bleeding is highest.

    During treatment with ceftazidime, a false-positive Coombs reaction and a false positive urine reaction to glucose are possible.

    Some patients may develop pseudomembranous colitis during or after the administration of ceftazidime. In mild cases, it is sufficient to discontinue the drug, and in more severe cases it is recommended to restore the input-salt and protein balance, appoint metronidazole, bacitracin or vancomycin. During treatment can not be used ethanol - possible effects similar to the action of disulfiram (facial hyperemia, epigastric spasm, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).

    With prolonged use, as well as in patients with severe hepatic or renal insufficiency, it is necessary to control the concentration of ceftazidime in the blood plasma.
    Effect on the ability to drive transp. cf. and fur:

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 2.0 g.


    Packaging:By 2.0 g of the active substance of the powder in a clear glass bottle, sealed with a rubber stopper, crimped with an aluminum cap. Each vial with instructions for use is placed in a cardboard box.
    Storage conditions:In a dry 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 expiry date printed on the label!
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004892/09
    Date of registration:19.06.2009
    The owner of the registration certificate:Agio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAgio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd.
    Information update date: & nbsp13.05.2016
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