Active substanceCeftazidimeCeftazidime
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  • Dosage form: & nbsp
    Powder for solution for intravenous and intramuscular administration

    Composition:
    1 bottle contains:

    Active substance: ceftazidime pentahydrate 1286 mg is equivalent to ceftazidime 1000 mg.

    Excipient: sodium carbonate q.s. up to 1286 mg.
    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 cell wall of bacteria (acetylates membrane-bound transpeptidases, violating the cross-linking of peptidoglycans 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), Klebssiella spp., incl. Klebssiella pneumoniae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Pseudomonas spp. (including Pseudomonas aeruginosa), Serratia spp., Pasteurella multocida, Gram-positive bacteria - Staphylococcus aureus, including strains of producing and non-producing penicillinase, Streptococcus agalactiae (Group B Streptococcus), Streptococcus pneumoniae, Streptococcus pyogenes (Group A beta-hemolytic streptococci ), Streptococcus mitis, Streptococcus spp .; anaerobic bacteria -Propionibacterium spp., Clostridium spp., Fusobacterium spp., Bacteroides spp., (however, many strains of Bacteroides fragilis are resistant). Has a pronounced activity against Pseudomonas aeruginosa, significantly less activity - for streptococci (primarily Streptococcus pneumoniae). Resistant to the action of most beta-lactamases. Ceftazidime is not active against Staphylococcus spp., 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 excretion, the drug is quickly distributed in the human body and reaches therapeutic concentrations in most tissues and liquids, 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. Poor penetration of the intact blood-brain barrier, but the therapeutic values ​​reached by the drug in the cerebrospinal fluid are sufficient for the treatment of meningitis.

    It binds back 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.

    Time to reach the maximum concentration for intramuscular injection - 1 hour, with intravenous administration - at the end of infusion. The concentration of the drug, equal to 4 μg / ml, persists for 6-8 hours. The therapeutic concentration in the blood plasma persists for 8-12 hours. The elimination half-life for normal renal function is -1.8 hours; with impaired - 2,2 h.

    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 by kidneys to 80-90% (70% of the administered dose is excreted in the first 4 hours during the day by glomerular filtration). In case of impaired renal function, 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:

    - infections of the respiratory tract (bronchitis, infected bronchocytosis, 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);

    - infections of the skin and soft tissues (phlegmon, erysipelas, wound infections, mastitis, skin ulcers);

    - 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:used in combination with diuretics and aminoglycosides. 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), the course of treatment can be increased to 21 days.

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

    - usually prescribed 1.0 g every 8 hours or 2.0 g every 12 hours;

    - 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;

    - in chronic renal failure: patients with severe infections can increase the maintenance dose by 50% or the frequency of drug administration;

    - In elderly patients, the recommended dose of ceftazidime should not exceed 3 g / day, especially in patients older than 80 years.

    After an initial dose of 1 g, adults with impaired renal function (including patients who undergo dialysis), a dose reduction may be required, such as is as follows:

    CREATINE CREATININE

    DOSE

    >50

    ml / min (0.83 ml / sec)

    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

    16-30 ml / min (0.27-0.50 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 concentration of ceftazidime in serum, which should not exceed 40 mg / l.

    The half-life of ceftazidime during hemodialysis is 3 to 5 hours.

    The maintenance dose should be repeated after each dialysis period.

    When peritoneal dialysis a drug ceftazidime can be included in dialysis

    liquid in a dose of 125 mg to 250 mg per 2 liters of dialysis fluid.

    Usual dose for children under 12 years:

    Demu in the age of up to 2 months. - intravenous infusion 25-60 mg / kg / day per day in 2 divided doses.

    Children from 2 months. and up to 12 years - intravenous infusion of 30 - 100 mg / kg per day (the frequency of administration 2-3 times a day).

    Children with immunity, cystic fibrosis and meningitis the drug can be prescribed in doses up to 150 mg / kg / day (maximum daily dose is 6.0 g) in 3 divided doses,

    The maximum daily intake for children should not exceed 6 g in 3 divided doses.

    PREPARATION OF SOLUTIONS

    1. "PRIMARY" BREEDING

    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. "SECONDARY" 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;

    - l Ringer's activated solution;

    - 5% dextrose solution;

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

    - 10% solution of dextrose.

    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: rash, fever, eosinophilia, pruritus, toxic epidermal necrolysis (Lyell's syndrome), erythema multiforme (including Stevens-Johnson syndrome), angioedema, bronchoconstriction, anaphylactic shock, fever.

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

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

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

    From the digestive system: nausea, vomiting, diarrhea, abdominal pain, colitis, cholestasis, oropharyngeal candidiasis, pseudomembranous colitis.

    From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, lymphocytosis, hemolytic anemia, hemorrhages, thrombophlebitis, thrombocytosis, agranulocytosis, false-positive Coombs test.

    Other, nosebleeds, candidiasis, superinfection, unpleasant taste in the mouth, lowering blood pressure, jaundice, myoclonia.

    Laboratory indicators: hyperkreatininemia, increased urea concentration, false positive urine reaction to glucose, increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, increased prothrombin time.

    Overdose:Symptoms: dizziness, paresthesia, headache, convulsions, abnormalities 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:
    Applying high doses of aminoglycosides simultaneously with the drug Ceftazidime, it is necessary to closely monitor the kidney function because of the potential nephrotoxicity and ototoxicity of aminoglycoside antibiotics. Nephrotoxicity was noted after simultaneous use of other cephalosporins with diuretics, such as furosemide.

    Ceftazidime concentration from 1 to 40 mg / ml is compatible with such parenteral solutions: 0.9% solution of sodium chloride for injection; 5% and 10% glucose solutions for injection; 6 M sodium lactate for injection, 5% glucose solution and 0.9% sodium chloride for injection; Ringer's solution with lactate and 5% dextrose solution for injection.

    To avoid possible drug interactions with other drugs, drug solutions ceftazidime (as well as most other L-lactam antibiotics) should not be simultaneously administered with solutions of metronidazole, vancomycin, gentamicin, tobramycin sulfate and netilmicin sulfate.In the case of ceftazidime with these drugs, each antibiotic should be administered separately.

    For the / m introduction ceftazidime can be diluted with 0.5% or 1% lidocaine hydrochloride solution. 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 solution of sodium chloride 0.9% or a solution of 5% dextrose, 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 0.9% solution of sodium chloride, potassium chloride 10 mEq / L or 40 mEq / L in a 0.9% solution of sodium chloride.
    When mixing ceftazidime solution (500 mg in 1.5 ml of water for injection) and metronidazole (500 mg / 100 ml), both components remain active. Ceftazidime, like other antibiotics, can disrupt the intestinal microflora, which can lead to a decrease in the reabsorption of estrogens and a decrease in the effectiveness of combined oral hormonal contraceptives.
    Special instructions:
    When developing an allergic reaction to ceftazidime, the drug should be immediately discontinued, in severe cases, epinephrine, hydrocortisone,antihistamines and other emergency measures.

    Patients with a history of allergic reactions to penicillins are noted to have cross-sensitivity to cephalosporins.

    Ceftazidime may interfere with the synthesis of vitamin K due to suppression of intestinal flora, which can cause a decrease in the concentration of vitamin K-dependent clotting factors, 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. When used simultaneously with nephrotoxic drugs, such as aminoglycosides and diuretics (furosemide), it is necessary to monitor kidney function.During treatment it is necessary to constantly assess the patient's condition. In the treatment of ceftazidime, some initially sensitive strains may develop resistance, so periodic testing should be conducted for susceptibility to antibiotics.
    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.

    Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention.
    Form release / dosage:
    Powder for solution for intravenous or intramuscular administration 1 g


    Packaging:By 1.0 g of the active substance of the powder into a clear glass vial, 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.
    Shelf life:2 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011799 / 01
    Date of registration:21.12.2011
    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: & nbsp10.05.2016
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