1 vial contains Ceftriaxone sodium equivalent to Ceftriaxone 1000 mg.
Dosage form. Powder for preparation of solution for injection.
basic physical and chemical properties:crystalline powder from white to yellowish-orange.
Antibacterial agents for systemic use. Cephalosporins of the III generation. Ceftriaxone. ATC code J01D D04.The
Ceftriaxone - cephalosporin antibiotic III generation for parenteral use. Has a bactericidal effect, inhibits the synthesis of cell membranes,in vitro growth of most gram-positive and gram-negative microorganisms. Ceftriaxone is resistant to beta-lactamase enzymes (both penicillinases and cephalosporinases produced by most gram-positive and gram-negative bacteria). Effective against such microorganisms as:
gram:Staphylococcus aureus,Streptococcus pneumoniae,Streptococcus A(Streptococcus pyogenes),Streptococcus(Streptococcus agalactiae),Streptococcus viridans, Streptococcus bovis.
note: Staphylococcus spp.,Resistant to meticiline resistant as well to cephalosporins, including Ceftriaxone. Most strains of enterococci (e.g.,Streptococcus faecalis) is also resistant to Ceftriaxone;
gram negative:Aeromonas spp., Alcaligenes spp.,Branhamella catarrhalis,Citroen spp.,Enterobacter spp. (some strains are resistant),Escherichia coli,Haemophilus ducreyi,Haemophilus influenzae Haemophilus parainfluenzae Klebsiella spp. (including TheKlebsiella pneumoniae),Moraxella spp.,Morganella morganii,Neisseria gonorrhoeae,Neisseria meningitidis,Plesiomonas shigelloides,Proteus mirabilis,Proteus vulgaris,Providencia spp.,Pseudomonas aeruginosa(some strains are resistant),Salmonella spp.,Serratia spp. (includingS. marcescens),Shigella spp.,Vibrio spp.,Yersinia spp. (includingY. enterocolitica).
Many strains of the above-mentioned microorganisms, which reproduce without changing the rate of separation in the presence of other antibiotics, such as penicillins, cephalosporins of the first generations and aminoglycosides, are sensitive to Ceftriaxone.Treponema pallidumis sensitive to Ceftriaxone both in vitroand in animal experiments. According to clinical data, primary and secondary syphilis noted high efficiency of Ceftriaxone;
anaerobic pathogens:Bacteroides spp.,Clostridium spp.,Fusobacterium spp. (exceptF. mostiferum,F. varium),Peptococcus spp.,Peptostreptococcus spp.
note:some strains of manyBacteroides spp. (for example,B. fragilis), producing of beta-lactamases, resistant to Ceftriaxone. To determine the sensitivity of microorganisms, disks containing Ceftriaxone should be used, sincein vitrocertain strains of pathogens exhibit resistance to classical cephalosporins.
with parenteral administration Ceftriaxone penetrates well into tissues and body fluids.
the Area under the curve "concentration-time" in the serum of intravenous and intramuscular administration of the same. This means that the bioavailability of Ceftriaxone when administered is 100%.
Emcef communicates reversibly with albumin and this binding is inversely proportional to the concentration: for example, at serum concentrations of less than 100 mg/l, the binding of Ceftriaxone to proteins is 95%, and at a concentration of 300 mg/l - only 85 %. Due to the lower content of albumin in interstitial fluid Ceftriaxone concentration in it is higher than in blood serum.
the half-life of healthy patients is around 8:00. Infants under 8 days of age and those over 75 years of age have an average half-life of about 2 times longer. In adults, 50-60% of Ceftriaxone is excreted unchanged in urine, and 40-50% - also unchanged in bile. Under the influence of intestinal flora Ceftriaxone turns into an inactive metabolite. In newborns, about 70% of the administered dose is excreted by the kidneys. In renal insufficiency or liver pathology in adults, the pharmacokinetics of Ceftriaxone almost does not change, the half-life period increases somewhat. If only broken function of kidneys, increases the secretion with the bile, if liver function is compromised - increased allocation of Ceftriaxone in the kidneys.
Penetration into cerebrospinal fluid:in children, including newborns, when the cerebral membrane is inflamed, Ceftriaxone penetrates into the liquor, while in the case of bacterial meningitis, on average, 17% of the concentration of the drug in the serum diffuses into the cerebrospinal fluid, which is about 4 times more than in aseptic meningitis. In adults with meningitis, 2-25 hours after the administration of Ceftriaxone at a dose of 50 mg/kg body weight concentration is many times higher than the minimum dose required to suppress pathogens causing meningitis.
Infections caused by Ceftriaxone-sensitive microorganisms:The
Preoperative prevention of infections in surgical interventions on the organs of the gastrointestinal tract, biliary tract, urinary tract and gynecological procedures, but only in cases of potential or known contamination.
when prescribing the drug, it is necessary to adhere to the official recommendations for antibiotic therapy and in particular recommendations for the prevention of antibiotic resistance.
Hypersensitivity to cephalosporins. If the patient has hypersensitivity to penicillin, the possibility of a cross allergic reaction to Ceftriaxone should be taken into account.
Ceftriaxone is contraindicated in preterm infants 41 weeks based on the period of prenatal development (gestational age + age after birth).
hyperbilirubinemia in newborns and preterm infants. In studiesin vitroit has been shown that Ceftriaxone can displace bilirubin from its Association with serum albumin of blood, which can lead to the risk of developing encephalopathy caused by bilirubin.
Ceftriaxone is contraindicated for infants aged ? 28 days for use if necessary (or anticipated need) of treatment with intravenous solutions containing calcium, including intravenous infusions that contain calcium, such as parenteral nutrition, due to the risk of the occurrence of precipitates of calcium salts of Ceftriaxone (see "Method of application and dosage").
in newborns and premature infants described the occurrence of precipitates in the lungs and kidneys, resulting in death with the simultaneous introduction of Ceftriaxone and calcium preparations. In some of these cases, the same infusion systems were used for intravenous administration for Ceftriaxone and calcium-containing solutions, and in some infusion systems, the occ