Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:Active substance: ceftriaxone sodium in terms of ceftriaxone 250 mg, 500 mg and 1 g.
    Description:From white to white with a yellowish hue of color, crystalline powder, slightly hygroscopic.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:

    Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use; Has bactericidal action due to inhibition of cell membrane synthesis; resistant to beta-lactamases, which are produced by gram-positive and gram-negative bacteria; in vitro is active against the following microorganisms:

    Gram-positive microorganisms

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

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

    Gram-negative microorganisms

    Aeromonas spp., Alcaligenes spp., Citrobacter spp., Enterobacter spp. (some strains are resistant),Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiellaspp. (including Klebsiella pneumoniae), Moraxella spp. (including Moraxella catarrhalis),Morganella morganii, Neisseria gonorrhoeae, Neisseria meningi­tidis, Borrelia burgdorferi, Proteusmirabilis, Proteus vulgaris, Providencia spp., Pseudomonas spp., Salmonella spp. (including Salmonellatyphi), Serratia spp. (including Serratia marcescens), Shigella spp., Vibrio spp. (at Tom number of Vibrio cholerae), Yersinia spp, (at Tom number of Yersinia enterocolitica).

    Note: Treponema pallidum is sensitive to ceftriaxone as in vitro, and in vivo.

    Anaerobic microorganisms

    Bacteroides spp. (including some strains Bacteroides fragilis), Clostridium spp. (BesidesClostridium difficile), Fusobacterium spp. (Besides Fusobacterium mostiferum, Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.

    Note: some strains Bacteroides spp. (eg, Bacteroides fragilis), Developing beta-lactamase, resistant to ceftriaxone.


    Pharmacokinetics:
    Time to reach the maximum concentration after intramuscular injection -2-3 hours, after intravenous administration - at the end of infusion. The maximum concentration after intramuscular injection of 0.5 g and 1 g is 38 μg / ml and 76 μg / ml, respectively, after intravenous administration of 0.5 g, 1. g and 2 g - 82 μg / ml, 151 μg / ml and 257 μg / ml, respectively.
    Connection with blood plasma proteins - 83-96%.
    The volume of distribution - 0.12-0.14 l / kg (5.78-13.5 l), in children - 0.3 l / kg.The plasma clearance is 0.58-1.45 l / h, the renal clearance is 0.32-0.73 l / h.
    The half-life (T1 / 2) after intramuscular injection is 5.8-8.7 hours; in children with meningitis after intravenous administration in doses of 50-75 mg / kg T1 / 2 - 4.3-4.6 hours.
    33-67% of the drug is excreted unchanged by the kidneys, the rest - with bile in the intestines, where the inactivation occurs.
    Ceftriaxone penetrates well into tissues and body fluids (lungs, heart, bile ducts, liver, tonsils, middle ear, nasal mucosa, bones, cerebrospinal fluid, pleural and synovial fluid, secretion of the prostate gland).
    Penetration into the cerebrospinal fluid
    In children, including newborns, with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid; in the case of bacterial meningitis, an average of 17% of the drug contained in the blood plasma diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis. 24 hours after intravenous administration of ceftriaxone at a dose of 50-100 mg / kg, its concentration in the cerebrospinal fluid exceeds 1.4 mg / l. In adults with meningitis, 2 to 24 hours after the administration of ceftriaxone at a dose of 50 mg / kg, the concentration of ceftriaxone in the cerebrospinal fluid is many times greater than the minimal inhibitory concentration for the most common meningitis pathogens.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to ceftriaxone:

    - respiratory tract infections, including pneumonia;

    - infections of the kidneys and urinary tract, including pyelonephritis;

    - infections of the pelvic organs;

    - infections of the skin and soft tissues, including infected wounds and burns;

    - infection of bones and joints;

    - infection of ENT organs;

    - Intra-abdominal infections, including peritonitis;

    - sepsis;

    - meningitis;

    - gonorrhea, soft chancre, syphilis;

    - Lyme disease (borreliosis);

    - Abdominal typhus, salmonellosis and salmonella carriage;

    - infection on the background of immunodeficiency. Prevention of postoperative infections.
    Contraindications:
    Hypersensitivity to ceftriaxone and other cephalosporins, carbapenems, penicillins; I trimester of pregnancy, lactation.
    Carefully:With renal and / or liver failure; with colitis, including in history; at a hyperbilirubinemia at newborns (especially, at premature newborns).
    Pregnancy and lactation:
    The use of ceftriaxone 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.
    If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
    Dosing and Administration:

    Applied intravenously (struyno, drip) or intramuscularly.

    Adults and children over 12 years of age

    1-2 g per day with an interval of 24 h or 0.5-1 g every 12 h. In severe cases or in infections whose causative agents have only mild sensitivity to ceftriaxone, the daily dose can be increased to 4 g.

    Older patients are given usual doses for adults without adjustments for age.

    Children

    Newborns (up to 2 weeks): 20-50 mg / kg once a day (interval 24 hours). The daily dose should not exceed 50 mg / kg of body weight. When determining the dose, no distinction is made between full and premature children.

    Children from the 3rd week to 12 years: 20-75 mg / kg once a day (interval 24 hours). The daily dose should not exceed 2 grams!

    Children with a body weight above 50 kg are prescribed doses for adults.

    Intravenous doses at a rate of 50 mg / kg or higher should be administered drip for at least 30 minutes.

    Duration of treatment

    Depends on the type and sensitivity of the pathogen and the severity of the disease; usually is 7-14 days; with a complicated infection, longer treatment may be required; infection caused by Streptococcus pyogenes, - not less than 10 days.

    The administration of ceftriaxone should be continued within 48-72 hours after the temperature normalization and bacteriological confirmation of the eradication of the pathogen.

    Dosing in special cases

    Bacterial meningitis in children from 3 weeks to 12 years: a dose of 100 mg / kg administered once a day (an interval of 24 hours). The daily dose should not exceed 4 grams! The duration of treatment for meningococcal meningitis is at least 4 days; with meningitis caused by Haemophilus influenzae, - 6 days, Streptococcus pneumoniae, - 7 days.

    Lyme disease \ 50 mg / kg (the highest daily dose is 2 g) for adults and children once a day for 14 days.

    Uncomplicated gonorrhea: 250 mg once intramuscularly.

    Prevention of postoperative infection: depending on the degree of infectious risk - 1-2 g intravenously once for 30-90 minutes before the operation. In operation on the large intestine ceftriaxone It is used in combination with drugs that affect the anaerobic flora.

    Sick from impaired renal function: in the case of preterminal renal failure (with creatinine clearance less than 10 ml / min), it is necessary that the daily dose does not exceed 2 g. In the remaining cases, no normal dose adjustment is required if normal liver function is performed.

    Sick from hepatic dysfunction: under the condition of normal kidney function, dose adjustment is not required.

    Severe renal and hepatic insufficiency: should regularly monitor the concentration of ceftriaxone in the blood plasma and, if necessary, adjust the dose.

    Patients on dialysis: additional administration of the drug after dialysis is not required. It is necessary to monitor the concentration of ceftriaxone in the serum for dose adjustment, since the rate of excretion of the drug in these patients may be reduced.

    For intramuscular injection the contents of the vial are dissolved as follows:

    Contents of the bottle Solvent (water for injection)

    250 mg 0.9 ml

    500 mg 1.8 ml

    1 g 3.6 ml

    After preparation, each ml of the solution contains about 250 mg of the drug in terms of ceftriaxone.

    Ceftriaxone is injected into a relatively large muscle (eg, buttock); Trial aspiration helps to avoid unintentional insertion into the blood vessel. It is recommended to inject no more than 1000 mg of the drug into one muscle.

    To reduce pain with intramuscular injection, instead of water for injection, use, if there are no contraindications, 1% lidocaine solution. Do not administer ceftriaxone solution in 1% lidocaine solution intravenously.

    For intravenous administration the contents of the vial are dissolved as follows:

    Contents of the bottle Solvent (water for injection)

    250 mg 2.4 ml

    500 mg 4.8 ml

    1 g 9.6 ml

    After preparation, each ml of the solution contains about 100 mg of the drug in terms of ceftriaxone. The solution is administered slowly for 2-4 minutes.

    For intravenous infusion dissolve 2 g of ceftriaxone in 40 ml of a calcium-free infusion solution (for example, 0.9% sodium chloride solution, 2.5%, 5% or 10% glucose solution (dextrose), 5% levulose solution, 0.45% sodium chloride solution and 2.5% glucose solution, 6% dextran 70 solution in 5% glucose solution). The solution is introduced for 30 minutes.

    Side effects:

    Allergic reactions: urticaria, chills or fever, rash, itching, rarely - bronchospasm, eosinophilia, erythema exudative multiform (including Stevens-Johnson syndrome), serum sickness, anaphylactic shock.

    From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, taste disorder, stomatitis, glossitis, pseudomembranous colitis,a violation of liver function (increased activity of "liver" transaminases, less often - alkaline phosphatase or bilirubin, cholestatic jaundice), pseudocholithiasis of the gallbladder, dysbacteriosis.

    On the part of the organs of hematopoiesis: anemia, leukopenia, leukocytosis, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in plasma clotting factor concentration (II, VII, IX, X), prolongation of prothrombin time.

    From the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glucosuria, cylindruria, hematuria), rarely - oliguria, anuria.

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

    Other: headache, dizziness, nosebleeds, candidiasis.

    Overdose:
    The concentration of ceftriaxone in the blood plasma can not be reduced by dialysis. There is no specific antidote.
    Treatment: symptomatic.
    Interaction:
    Ceftriaxone, suppressing the intestinal flora, interferes with the synthesis of vitamin K, so with simultaneous administration with drugs,reducing platelet aggregation (for example, with non-steroidal anti-inflammatory drugs), the risk of bleeding increases.
    With a simultaneous appointment with anticoagulants, their effect is noted.
    With simultaneous administration with "loop" diuretics, the risk of developing nephrotoxic action increases.
    Ceftriaxone and aminoglycosides have a synergistic effect on many gram-negative bacteria.
    With simultaneous use with ethanol, disulfiram-like reactions (sudden rush of blood to the face, abdominal cramps, nausea, vomiting, headache, tachycardia, dyspnea) can be observed.
    Ceftriaxone should not be mixed with solutions containing calcium.
    A solution of ceftriaxone is not recommended to be mixed in one syringe or dropper with other antimicrobials.
    Special instructions:
    Patients with severe renal-hepatic insufficiency who are on hemodialysis should regularly monitor the concentration of the drug in the blood plasma. With prolonged treatment with ceftriaxone, it is necessary to regularly monitor the picture of peripheral blood, indicators of the functional state of the liver and kidneys.In rare cases, ultrasound gallbladder observed transient darkening ( "sludge '' - syndrome), associated with the formation of calcium ceftriaxone In this case, the drug should be discontinued and, if necessary, carry out symptomatic treatment Despite detailed medical history, we can not exclude the possibility of anaphylactic shock.. , which requires immediate therapy: first introduce epinephrine, then glucocorticosteroids.
    Ceftriaxone displaces bilirubin from its association with serum albumin.
    In the case of pseudomembranous colitis, the drug is canceled.
    Elderly and debilitated patients may require the appointment of vitamin K.

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection of 250 mg; 500 mg and 1 g.
    Packaging:
    Powder for solution for intravenous and intramuscular injection of 250 mg; 500 mg and 1 g / in complete with a solvent (water for injection) and without a solvent.
    250 mg or 500 mg of ceftriaxone in a glass bottle, a sealed with a rubber stopper and an aluminum cap rolled up with a plastic lid; 5 ml in-gical for injection in a glass vial or ampoule fault line of plastic (polyethylene) with a fault line.1 bottle with instructions for use or 50 bottles with 3-5 instructions for use in a cardboard pack; 1 bottle and 1 ampoule together with instructions for use in a cardboard box.
    For 1 g of ceftriaxone in a glass bottle, corked with a rubber stopper and rolled up with an aluminum cap with a plastic lid; 10 ml of water for injection into a glass ampoule with a fracture line or a plastic ampoule (polyethylene) with a fault line. 1 bottle with instructions for use or 50 bottles with 3-5 instructions for use in a cardboard pack; 1 bottle and 1 ampoule together with the instructions for use in a cardboard box.
    Storage conditions:
    Store in a dark place at a temperature of no higher than 25 ° C.
    The prepared solution should not be stored for more than 6 hours at a temperature of no higher than 25 ° C or not more than 24 hours in a refrigerator at a temperature of 2 ° C to 8 ° C.
    Keep out of the reach of children.
    Shelf life:
    3 years (Cefogram).
    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 N014422 / 01
    Date of registration:18.11.2008
    The owner of the registration certificate:Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.)Orchid Helsker (a division of Orchid Chemicals and Pharmaceuticals Ltd.) India
    Manufacturer: & nbsp
    Representation: & nbspOrchid Chemicals and Pharmaceuticals Co., Ltd.Orchid Chemicals and Pharmaceuticals Co., Ltd.Russia
    Information update date: & nbsp21.11.2015
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