Active substanceCefotaximeCefotaxime
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:Active substance: Cefotaxime sodium in terms of cefotaxime - 1 g.
    Description:White or white with a yellowish tint powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.01   Cefotaxime

    Pharmacodynamics:

    Cefotaxime is a third generation cephalosporin antibiotic for parenteral administration. It acts bactericidal by blocking the peptidoglycan polymerase, disrupting the biosynthesis of the mucopeptide of the cell wall of the microorganism. It is resistant to beta-lactamases of gram-positive and gram-negative bacteria.

    Cefotaxime has a broad spectrum of action; in vitro is active against the following microorganisms:

    - Gram-positive, such as Staphylococcus aureus (including strains that produce beta-lactamase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes (beta-hemolytic streptococcus group A), other Streptococcus spp., Borrelia burgdorferi, some Enterococcus spp.

    (Note: staphylococci, resistant to methicillin / oxacillin, are resistant to cefotaxime; for gram-positive cocci cefotaxime less active than cephalosporins of the first and second generations);

    - Gram-negative, such as Acinetobacter spp. (strains Acinetobacter baumanii resistant), Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including ampicillin-resistant strains), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Morganella morganii, Neisseria gonorrhoeae (including strains that produce penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia spp., some strains Pseudomonas aeruginosa;

    - anaerobic such as Bacteroides spp., (most strains Bacteroides fragilis resistant), Clostridium spp. (most strains Clostridium difficile resistant), Fusobacterium spp. (including Fusobacterium hucleatum), Peptococcus spp., Peptostrepto- caboutccus spp.

    Pharmacokinetics:
    After a single intramuscular injection of 500 mg and 1.0 g of cefotaxime, the maximum concentration (Cmax) is reached within 30 minutes and is 11.7 μg / ml and 20.5 μg / ml, respectively; after intravenous administration, 500 mg, 1.0 g and 2.0 grams of C max are achieved after 5 minutes and are 38.9 μg / ml, 101.7 μg / ml and 214.4 μg / ml, respectively.
    30-50% of cefotaxime binds to blood proteins, mainly with albumins. Therapeutic concentration is created in most tissues and body fluids: in the myocardium, bones, gall bladder, skin and soft tissues, in synovial, pericardial, peritoneal, cerebrospinal and pleural fluids, as well as in sputum, bile and urine.
    The drug penetrates through the placental barrier, excreted in breast milk.20-36% of the intravenously administered dose is excreted by the kidneys unchanged; 15-25% - in the form of the main metabolite of deacetylcefotaxime, which has antibacterial activity; 20-25% - in the form of two other inactive metabolites. Partially cefotaxime is excreted with bile.
    After intravenous administration, 1.0 g of the drug every 6 hours for 14 days of cumulation was not detected.
    The half-life period (T1 / 2) in adults is 1-1.5 hours, slightly changing depending on the mode of administration. In patients older than 80 years, T1 / 2 increases to 2.5 hours. In patients with renal insufficiency, T1 / 2 does not exceed 2.5 hours. In children under one year with a birth weight of more than 1500 g with a single infusion of 50 mg / kg T1 / 2 is approximately 3.4 hours, and with a birth weight of less than 1500 g is about 4.6 hours.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to cefotaxi:

    - respiratory tract infections, including pneumonia;

    - urinary tract and kidney infections, including pyelonephritis;

    - infection of the abdominal cavity, including peritonitis;

    - sepsis;

    - meningitis;

    - rondocarditis;

    - infections of the pelvic organs;

    - infection of bones and joints;

    - infections of the skin and soft tissues, including wound and burn infections;

    - gonorrhea;

    - Lyme disease (borreliosis).Preventing the development of infection after surgery.
    Contraindications:Hypersensitivity to cephalosporins, penicillins, carbapenems; I trimester of pregnancy, lactation period; children's age to 2.5 years (for intramuscular injection).
    Carefully:If the kidneys and liver function is impaired; with nonspecific ulcerative colitis, including in the anamnesis; with severe heart failure, violation of heart rhythm; in newborns (for intravenous administration).
    Pregnancy and lactation:
    Use in the II and III trimesters of pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
    During lactation in the case of taking the drug, breastfeeding should be discontinued, since cefotaxime excreted in breast milk.
    Dosing and Administration:

    Cefotaxime is administered intravenously (jet, drip) or intramuscularly.

    Adults and children over 12 years of age (with a body weight of 50 kg or more)

    AT table 1 the recommended dose, frequency and route of administration, depending on the type infection.

    Table 1

    Type of infection

    Daily dose

    Single dose, frequency and route of administration

    Uncomplicated infections of moderate severity

    2.0-6.0 g

    1.0-2.0 g every 8-12 hours intramuscularly or intravenously

    Infections of severe course

    6.0-8.0 g

    2.0 g every 6-8 h intravenously

    Life-threatening infections

    Up to 12.0 g

    2.0 g every 4-8 h intravenously

    With uncomplicated gonorrhea

    0.5-1.0 g

    0.5 - 1.0 g once intramuscularly

    The maximum daily dose should not exceed 12.0 g.

    Patients with impaired renal function

    When the creatinine clearance is less than 20 ml / min / 1.73 m2 the daily dose is recommended to be reduced by 2 times.

    Patients on hemodialysis

    1.0-2.0 g per day, depending on the severity of the infection. On the day of dialysis, the drug is administered after the procedure.

    Children under 12 years old

    Newborns, including premature infants At the age of 1 week - 50 mg / kg body weight every 12 hours intravenously. At the age of 1 -4 weeks - 50 mg / kg body weight every 8 hours intravenously. Children from 1 month to 12 years (with a body weight of less than 50 kg)

    50-180 mg / kg / day 4 or 6 times a day in equal doses intramuscularly (only for children over 2.5 years old) or intravenously; In severe infection, including meningitis, the daily dose is increased to 100-200 mg / kg / day.

    At a body weight of 50.0 kg or more, a dosage for adults is recommended (see Fig. Table 1).

    Duration of therapy

    It is established individually depending on the type of microorganism, its sensitivity to cefotaxime and the nature of the disease.After temperature normalization or bacteriological confirmation of the eradication of the causative agent, the administration of cefotaxime should be continued for another 2-3 days; for infections caused by beta- hemolytic streptococcus group A, the drug is administered for at least 10 days; it may take several weeks to treat a chronic infection.

    Prevention of infection during surgical interventions

    Before the surgical operation, 1.0 g of the drug is administered intramuscularly or intravenously before or during anesthesia; at a cesarean section 1,0 g enter intravenously slow (!) immediately after applying the clamps to the umbilical cord.

    Further, according to the indications, it is possible to re-administer 1.0 g of the drug intramuscularly or intravenously via 6-12 hours.

    Intravenous administration

    Streaming

    The drug is dissolved in 10 ml of water for injection, as indicated in table 2; injected slowly for 3-5 minutes. The jet preparation should not be administered for less than 3 minutes!

    Drip

    The drug is dissolved in 50-100 ml of a 0.9% solution of sodium chloride or 5% glucose solution (dextrose), as indicated in Table 2. The duration of the infusion is 50-60 minutes.

    As a solvent can not use sodium hydrogen carbonate solution for injection!

    Intramuscular injection

    The solution is prepared as indicated in Table 2, using water for injection or 1% solution of lidocaine hydrochloride; injected into a relatively large muscle, for example, the upper outer quadrant of the buttocks.

    With intramuscular injection, aspiration should be performed to prevent the needle from entering the vessel and to prevent the injection of a solution, especially lidocaine, into the blood!

    Preparation of solutions

    AT table 2 The volumes of solvent are presented depending on the required dosage and pathway administration, as well as the approximate concentrations of the preparation obtained.

    table 2

    Dosage and route of administration

    Volume of solvent (ml)

    Final volume (ml)

    Approximate concentration (mg / ml)

    Intravenous administration (jet)

    500 mg

    10

    10,2

    50

    1.0 g

    10

    10,4

    95

    2.0 g

    10

    11,0

    180

    Bnutrient introduction (drip)

    1.0 g

    50-100

    50-100

    20-10

    1 2.0 g

    50-100

    50-100

    40-20

    Intramuscular injection

    500 mg

    2

    2,2

    230

    1.0 g

    3

    3,4

    300

    2.0 g

    5

    6,0

    330

    The resulting solution should not contain any foreign mechanical inclusions!

    Side effects:

    Allergic reactions: urticaria, chills, rash, itchy skin; rarely - bronchospasm, eosinophilia, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), angioedema, anaphylactic shock.

    From the central nervous system: headache, dizziness.

    From the urinary system: a violation of kidney function, oliguria, interstitial nephritis.

    On the part of the organs of hematopoiesis: hemolytic anemia, leukopenia, granulocytopenia, thrombocytopenia, agranulocytosis, hypocoagulation.

    From the gastrointestinal tract: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, dysbiosis, impaired liver function; rarely - stomatitis, glossitis, pseudomembranous colitis.

    From the cardiovascular system: rarely - potentially life-threatening arrhythmias with rapid jet infusion through the central venous catheter.

    Laboratory indicators: azotemia, increased urea concentration in the blood, increased activity of "liver" transaminases and alkaline phosphatase, hypercreatininaemia, hyperbilirubinemia, false positive Coombs test.

    Local reactions: pain along the vein, phlebitis; morbidity and infiltration at the site of intramuscular injection.

    Other: vaginal and oral candidiasis.

    Overdose:
    It is possible to develop reversible encephalopathy in the case of large doses,especially in patients with renal insufficiency.
    Symptoms: convulsions, tremor, neuromuscular agitation.
    Treatment: symptomatic. There is no specific antidote.
    Interaction:
    Pharmaceutically incompatible with aminoglycosides in one syringe or dropper. With the simultaneous use of cefotaxime with aminoglycosides, polymyxin B or "loop" diuretics, the probability of kidney damage increases.
    When combining cefotaxime with antiaggregants (including non-steroidal anti-inflammatory drugs), the risk of bleeding increases.
    Probenecid slows down the excretion of cefotaxime and increases its plasma concentration.
    Special instructions:
    Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. If any allergic reaction occurs, the drug should be discontinued.
    When symptoms of pseudomembranous colitis appear, the drug is canceled; at moderate to severe and severe course of this complication appoint vancomycin or metroni-dazol.
    When treating the drug for more than 10 days, regular monitoring of the peripheral blood pattern is necessary.
    Elderly patients may need to monitor kidney function. During treatment with cefotaxime, a false positive urine sample can be taken for glucose (using non-enzymatic methods for determining glucose in the urine).

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 1 g.

    Packaging:
    Powder for the preparation of solution for intravenous and intramuscular administration 1 g complete with a solvent (water for injection) or without a solvent. 1 g of cefotaxime in a bottle of colorless glass, corked with a cork of rubber, rolled up with an aluminum cap with a plastic lid; 10 ml of water for injection into a plastic ampoule (polyethylene) with a fault line. 1 bottle with instructions for use in a cardboard box. For 1 bottle and
    1 ampoule together with instructions for use in a cardboard box. For 50 bottles with an equal number of instructions for use in a cardboard box (for hospitals).

    Storage conditions:
    Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years (Tax-O-Bid).
    3 years and 3 months (Solvent - water for injection).
    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012988 / 01
    Date of registration:23.07.2009
    Manufacturer: & nbsp
    Representation: & nbspOrchid Chemicals and Pharmaceuticals Co., Ltd.Orchid Chemicals and Pharmaceuticals Co., Ltd.Russia
    Information update date: & nbsp01.11.2015
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