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Cefotaxim-sanita

Cefotaxim-sanita

International Nonproprietary Name:

Cefotaxim (in sodium salt form).

Pharmaceutical form:

Powder for Injection solution preparation
  • Properties

    Pharmacological properties:

    Third-generation cephalosporin antibiotic. The chemical nature of cefotaxim is close to the cephalosporin antibiotics of the first and second generations.

    Possesses high tropicity to the penicillin-binding proteins of the microbial membrane, blocks the peptidoglycan polymerase, disrupts the biosynthesis of the mucopeptide of the cell wall of microorganisms.

    The drug has a wide range of antimicrobial effects: affects bacteriocidal to Gram-positive and Gram-negative microorganisms resistant to other cephalosporins, penicillins and other antimicrobial agents.

    Effective against Staphylococcus aureus (including penicillinase), Staphylococcus epidermidis, certain strains of Enterococcus spp., Streptococcus pneumoniae, Streptococcus pyogenes (group A beta-hemolytic streptococci), Streptococcus agalactiae (group B Streptococcus), Bacillus subtilis, Bacillus Mycoides, Corynebacterium Diphtheriae, Erysipelothrix insidiosa, Eubacterium, Enterobacter aerogenes, Enterobacter cloacaae, Escherichia coli, Haemophilus influenzae, including ampicillin-resistant strains, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae (including strains , Producing penicillinase), Propionibacterium, Proteus mirabilis, Proteus vulgaris, Proteus inconstans, Serratia marcescens, Ci Trobacter spp., Salmonella spp., Providencia rettgeri, Shigella spp., Serratia spp., Veillonella, Yersinia, Bordetella pertussis, Moraxella, Aeromonas hydrophilia, Fusobacterium, Bacteroides spp., Clostridium species, Peptostreptococcus species, Peptococcus spp. In relation to gram-positive cocci less active than cephalosporins of I and II generation.

    Resistant to cefotaxim: Acinetobacter baumannii, Bacteroides fragilis; Clostridium difficile; Enterococcus spp .; Gram-negative anaerobes: Listeria monocytogenes, methicillin-resistant staphylococci, Pseudomonas aeruginosa, Stenotrophomonas maltophilia.

     

    Pharmacokinetics

    After a single intramuscular (i/m) injection to healthy volunteers, 0.5 g or 1 g, the maximum concentration (Cmax) (11.7 and 20.5 μg / ml, respectively) is achieved within 30 minutes. In five minutes after intravenous (i/v) injection, 0.5 g, 1 g or 2 g of Cmax is 38.9; 101.7 and 214.4 μg / ml, respectively. Binding to blood plasma proteins (mainly albumins) is 25-40%.  Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and liquids (synovial, pericardial, peritoneal, spinal, pleural effusion), sputum, bile, urine. Passes through the placenta, penetrates into breast milk. The half-life period (T1 / 2) of plasma is approximately 1 hour, regardless of the route of administration. 

    It is excreted by the kidneys - about 60% of the administered dose is excreted within 6 hours after infusion start.         Approximately 20-36% of cefotaxim is excreted unchanged, 15-25% in the form of deacetylcefotaxim (the main metabolite), which has antibacterial activity, 20-25% - in the form of two other inactive metabolites - M2 and M3.  For repeated i/v injections in a dose of 1 g every 6 hours for 14 days, a cumulation is not observed.

    In newborns, T1 / 2 cefotaxim is 0.75-1.5 hours, in immature infants - 1.4-6.4 hours. In impaired kidney function T1 / 2 does not exceed 2.5 h and in later life (over 80 years) T1 / 2 increases approximately 2 times (up to 2.5 h). 
  • Indications

    Severe bacterial infections caused by susceptible microorganisms: respiratory tract infections and ENT organs (with the exception of enterococcal), skin and soft tissues (including infected wounds and burns), bones and joints, urinary tract, pelvic organs, obstetric-gynecological (including chlamydia, gonorrhea, including Caused by microorganisms that release penicillinase), bacteremia, septicemia, peritonitis, intra-abdominal infections, bacterial meningitis (with the exception of listeriosis), endocarditis, Lyme disease, typhoid fever, infections with immunodeficiency; Prevention of infections after surgery (including on the GI tract).

  • Contraindications

    Hypersensitivity to the drug (including penicillins, other cephalosporins, carbapenems), pregnancy period, especially I trimester (adequate and strictly controlled studies have not been conducted), breastfeeding (penetartes breast milk), history of bleeding, enterocolitis , Children's age - up to 2.5 years (for the i/m injection). 

  • Dosage and Administration

    Parenteral: i/v (By stream or drop) and i/ m. The dosage and treatment duration are determined individually, depending on the indications and severity of the infection.

    For the i/ m injection, dissolve 0.5 g of the drug in 2 ml, 1 g - in 3 ml of water for injection.  Enter deep into the gluteal muscle.

    For i/v injection, dissolve 0.5 g of the drug in 2 ml, 1 g - in 4 ml of water for injection.   Inject slowly for 3-5 minutes.

    For intravenous drop infusion, dissolve 1-2 g of the drug in 50-100 ml of a 5% of glucose solution or sodium chloride solution 0.9% isotonic for injection. Inject for 50-60 minutes.

    A normal daily for adults and children over 12 years is 1 g every 8 hours. In severe cases, the dose is increased to 2 g every 12 hours or increasing the number of administrations up to 3-4 times a day, bringing the total daily dose to 12 g maximum (in meningitis).     In acute gonorrhea, inject 0.5-1 g i/m once.

    Daily dose for newborns and young children is 50-200 mg / kg per day i/v, divided into separate receptions with intervals between them from 12 to 6 hours. For immature infants, the daily dose should not exceed 50 mg / kg. In cases of kidney function, the dose should be reduced. In the initial anuria (creatinine release 5 ml / min), usually reduce the dose by half.

    Rules for the injection solution preparation: For intravenous injection, water for injection is used as a solvent (1 g is diluted in 4 ml of a solvent); For intravenous infusion, 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1 g diluted in 50 - 100 ml solvent). The duration of the infusion is 50-60 minutes. For intramuscular injection water for injection or 1% lidocaine solution (1 g diluted in 4 ml of solvent) is used. 

  • Drug form

    Powder for the preparation of an injection solution of 1,0 g in vials.