Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    One bottle contains 1.0 g of ceftriaxone sodium salt.

    Description:Almost white or yellowish crystalline powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:

    Ceftriaxone is a cephalosporin antibiotic III generation for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro suppresses the growth of most Gram-positive and Gram-negative microorganisms. Ceftriaxone is resistant to beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by most Gram-positive and Gram-negative bacteria). In vitro and in conditions of clinical practice ceftriaxone is usually effective against the following microorganisms:

    Gram-positive:

    Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus A (Str.pyogenes), Streptococcus V (Str. agalactiae), Streptococcus viridans, Streptococcus bovis.

    Note: Staphylococcus spp., resistant to methicillin, is resistant to cephalosporins, including ceftriaxone. Most strains of enterococci (for example, Streptococcus faecalis) also resistant to ceftriaxone.

    Gram-negative:

    Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are stable), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (at Tom number of Kl. pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are stable), Salmonella spp. (at Tom number of S. typhi), Serratia spp. (at Tom number of S. marcescens), Shigella spp., Vibrio spp. (at Tom number of V. cholerae), Yersinia spp. (at Tom number of Y. enterocolitica)

    Note: Many strains of these microorganisms, which in the presence of other antibiotics, for example, penicillins, cephalosporins of the first generations and aminoglycosides, are multiply stable, sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone as in vitro, and in experiments on animals. According to clinical data, in the primary and secondary syphilis, a good efficacy of ceftriaxone is noted.

    Anaerobic pathogens:

    Bacteroides spp. (including some strains of B. fragilis), Clostridium spp. (at Tom number of CI. difficile), Fusobacterium spp. (Besides F. mostiferum. F. varium), Peptococcus spp., Peptostreptococcus spp.

    Note: Some strains of many Bacteroides spp. (for example, in. fragilis), Developing beta-lactamase, resistant to ceftriaxone. To determine the sensitivity of microorganisms, discs containing ceftriaxone, So as shown, that in vitro to classical cephalosporins, certain strains of pathogens can be stable.

    Pharmacokinetics:
    With parenteral administration ceftriaxone well penetrates into tissues and body fluids.
    In healthy adults, the subjects for ceftriaxone are characterized by a long half-life period of about 8 hours. The area under the concentration curve - time in the blood serum for intravenous and intramuscular injection coincide. This means that the bioavailability of ceftriaxone when administered intramuscularly is 100%. With intravenous administration ceftriaxone quickly diffuses into the interstitial fluid, where its bactericidal action against pathogens sensitive to it persists for 24 hours.
    The half-life in healthy adults is about 8 hours. In newborns up to 8 days and in elderly people older than 75 years, the average half-life is approximately twice as large. In adults, 50-60% of ceftriaxone is excreted unchanged in urine,and 40-50% - also in unchanged form with bile. Under the influence of intestinal flora ceftriaxone turns into an inactive metabolite. In neonates, approximately 70% of the administered dose is excreted by the kidneys. With kidney failure or liver pathology in adults, the pharmacokinetics of ceftriaxone is almost unchanged, the half-life of elimination is only slightly prolonged. If the kidney function is impaired, the secretion with bile increases, and if liver pathology takes place, then the excretion of ceftriaxone by the kidneys increases. Ceftriaxone reversibly binds to albumin and this binding is inversely proportional to the concentration: for example, when the concentration of the drug in the serum is 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 albumins in the interstitial fluid, the concentration of ceftriaxone in it is higher than in serum.
    Penetration into the cerebrospinal fluid:
    In newborns and in children with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis, an average of 17% of the concentration of the drug in the blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis.24 hours after intravenous administration of ceftriaxone in a dose of 50-100 mg / kg body weight, the concentration in the cerebrospinal fluid exceeds 1.4 mg / l. In adults with meningitis, 2 to 25 hours after the administration of ceftriaxone at a dose of 50 mg / kg body weight, the concentration of ceftriaxone was many times greater than the minimum oppressive dose that is necessary to suppress the pathogens most commonly causing meningitis.
    Indications:
    Infections caused by susceptible to ceftriaxone pathogens: sepsis, meningitis, abdominal infections (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts), infections of bones, joints, connective tissue, skin, infection in patients with decreased immune system function, kidney infection and urinary tract infections, respiratory tract infections, especially pneumonia, as well as infections of the ear, throat and nose, genital infections, including gonorrhea.
    Prevention of infections in the postoperative period.
    Contraindications:

    Hypersensitivity to cephalosporins and penicillins.

    The first trimester of pregnancy.


    Dosing and Administration:

    For adults and for children over 12 years of age:

    The average daily dose is 1-2 g of ceftriaxone 1 time per day (after 24 hours).

    In severe cases or in cases of infections caused by moderately sensitive pathogens, a one-time daily dose may be increased to 4 g.

    For newborns, infants and children under 12 years of age:

    For a single daily dosage, the following regimen is recommended:

    For newborns (up to 2 weeks of age): 20-50 mg / kg of body weight per day (a dose of 50 mg / kg of body weight is not allowed to exceed in connection with the immature enzyme system of newborns).

    For infants and children under 12 years of age: The daily dose is 20-75 mg / kg body weight.

    In children with a body weight of 50 kg and above, the dosage for adults should be followed. A dose of more than 50 mg / kg body weight should be given as an intravenous infusion for at least 30 minutes.

    Duration of therapy: depends on the course of the disease.

    Combination therapy:

    In the experiments it was proved that synergism takes place between ceftriaxone and aminoglycosides on the effect on many Gram-negative bacteria. Although it is impossible to predict the potentiated effect of such combinations in advance, in cases of severe and life-threatening infections (for example,Pseudomonas aeruginosa) their joint appointment is justified.

    In connection with the physical incompatibility of ceftriaxone and aminoglycosides, it is necessary to prescribe them separately in recommended doses!

    Meningitis:

    In bacterial meningitis in newborns and in children, the initial dose is 100 mg / kg of body weight once a day (maximum 4 g). Once it was possible to isolate the pathogenic microorganism and determine its sensitivity, the dose should be reduced accordingly. The best results were achieved with the following periods of therapy:

    Causative agent

    Duration of therapy

    Neisseria meningitidis

    4 days

    Haemophilus influenzae

    6 days

    Streptococcus pneumoniae

    7 days

    Sensitive Enterobacteriacease

    10 -14 days

    Gonorrhea: For the treatment of gonorrhea caused by both generative and non-causative

    penicillinase strains, the recommended dose is 250 mg once intramuscularly.

    Prevention in the pre- and postoperative period:

    Before infected or suspected infected surgical interventions to prevent postoperative infections, depending on the risk of infection, one-time administration of ceftriaxone in a dose of 1-2 g is recommended 30-90 minutes prior to surgery.

    Lack of kidney and liver function: patients with impaired renal function, provided normal liver function, a dose of ceftriaxone is not necessary to reduce. Only if the kidneys are deficient in the preterminal stage (creatinine clearance below 10 ml / min) it is necessary that the daily dose of ceftriaxone does not exceed 2 g.

    In patients with impaired liver function, if the function of the kidneys is maintained, the dose of ceftriaxone should not be reduced.

    In cases of simultaneous presence of severe pathology of the liver and kidneys, the concentration of ceftriaxone in serum should be monitored regularly. In patients undergoing hemodialysis, the dose of the drug after this procedure is not changed necessity.

    Intramuscular administration:

    For intramuscular injection, 1g of the drug should be diluted in 3.5 ml of a 1% solution of lidocaine and inserted deep into the gluteal muscle, it is recommended to inject no more than 1g of the drug into one buttock. A solution of lidocaine can never be administered intravenously!

    Intravenous administration:

    For intravenous injection, 1 g of the drug should be diluted in 10 ml of sterile distilled water and administered intravenously slowly for 2-4 minutes.

    Intravenous infusion:

    The duration of the intravenous infusion is at least 30 minutes. For intravenous infusion, 2 g of powder should be diluted in approximately 40 ml of calcium free solution, for example: 0.9% solution of sodium chloride, 5% glucose solution, 10% glucose solution, 5% levulose solution.

    Side effects:
    Systemic side effects: from the gastrointestinal tract (about 2% of patients): diarrhea, nausea, vomiting, stomatitis and glossitis.
    Changes in the blood picture (about 2% of patients) in the form of eosinophilia, leukopenia, granulocytopenia, hemolytic anemia, thrombocytopenia.
    Skin reactions (about 1% of patients) in the form of exanthema, allergic dermatitis, urticaria, edema, erythema multiforme.
    Other rare side effects: headaches, dizziness, increased activity of liver enzymes, congestion in the gallbladder, oliguria, increased serum creatinine content, mycosis in the genital area, chills, anaphylaxis, or anaphylactic reactions. It is extremely rare to notice pseudomembranous enterocolitis and blood clotting disorder.
    Local side effects: After intravenous administration, phlebitis was noted in some cases.This phenomenon can be prevented by slow administration (within 2-4 minutes) by administration of the drug. The described side effects usually disappear after discontinuation of therapy.

    Overdose:
    Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis. Symptomatic measures are recommended for the treatment of overdose cases.

    Interaction:
    Do not mix in one infusion bottle or in one syringe with another antibiotic (chemical incompatibility).

    Special instructions:
    Despite the detailed collection of anamnesis, which is the rule for other cephalosporin antibiotics, one can not exclude the possibility of developing an anaphylactic shock, which requires immediate therapy - first inject adrenaline, then glucocorticoids.
    Sometimes, with ultrasound examination of the gallbladder, there is a shadow indicating the deposition of precipitation. This symptom disappears after ceftriaxone therapy is discontinued or temporarily discontinued. Even in the presence of a pain syndrome, such cases do not require surgical intervention, conservative treatment is sufficient.
    In vitro studies have shown that, like other cephalosporin antibiotics ceftriaxone is able to displace bilirubin, associated with serum albumin. Therefore, in newborns with hyperbilirubinemia and, especially, in preterm infants, the use of ceftriaxone requires even greater caution.
    Since the drug penetrates into breast milk, do not continue breastfeeding during treatment with ceftriaxone.
    With prolonged use, periodic monitoring of the blood formula is necessary.
    Ceftriaxone is used only in a hospital!
    Form release / dosage:Powder for solution for injection for 1.0 g.
    Packaging:Powder for solution for injection 1.0 g in glass bottles, each bottle is packed in a cardboard box with instructions for medical use.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:
    3 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N013445 / 01-2001
    Date of registration:31.07.2008
    The owner of the registration certificate:Vertex ExportsVertex Exports India
    Manufacturer: & nbsp
    Information update date: & nbsp23.11.2015
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