Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    Active substance: ceftriaxone sodium 1000 mg (in terms of ceftriaxone).

    Description:
    Crystalline powder from white to white with a yellowish hue of color.

    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:
    Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use, it has bactericidal action, inhibits the synthesis of the cell membrane, in vitro inhibits the growth of most gram-positive and gram-negative microorganisms. Ceftriaxone is resistant to beta-lactamase enzymes, both penicillinase and cephalosporinase, produced by the majority of Gram-positive and Gram-negative bacteria). Effective against the following microorganisms:
    Gram-negative aerobes: Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains resistant to ampicillin), Haemophilus parainfluenzae, Klebssiella spp. (including Klebssiella pneumoniae), Neisseria gonorrhoeae (including strains forming and non-treating penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Morganella morganii, Serratia marcescens, Citrobacter freundii, Citrobacter diversus, Providencia spp., Salmonella spp. , Shigella spp., Acinetobacter calcoaceticus.
    A number of strains of the above microorganisms that exhibit resistance to other antibiotics, such as penicillins, cephalosporins, aminoglycosides, are sensitive to ceftriaxone. Individual strains of Pseudomonas aeruginosa are also sensitive to the drug.

    Gram-positive aerobes: Staphylococcus aureus (including strains that form penicillinase), Staphylococcus epidermidis (staphylococci, resistant to methicillin, are resistant to all cephalosporins, including ceftriaxone), Streptococcus pyogenes (beta-hemolytic group streptococci A), Streptococcus agalactiae (Group B Streptococcus), Streptococcus pneumoniae.

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

    Note: some strains of many Bacteroides spp. (eg, Bacteroides fragilis), Developing beta-lactamase, resistant to ceftriaxone. To determine the sensitivity of microorganisms, discs containing ceftriaxone, since it is shown that in vitro to classical cephalosporins, certain strains of pathogens can be stable.

    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.


    Pharmacokinetics:
    With intramuscular (IM) administration ceftriaxone is well absorbed from the site of administration and reaches high concentrations in the serum. Bioavailability of the drug is 100%.
    The average concentration in the plasma is achieved 2-3 hours after the injection. With repeated intravenous or intravenous (iv) doses of 0.5-2.0 g at intervals of 12 to 24 hours, there is accumulation of ceftriaxone at a concentration that is 15% -36% higher than the concentration reached at single injection. When administered at a dose of 0.15 to 3.0 g, the half-life is between 5.8 and 8.7 hours; volume of distribution - from 5.78 to 13.5 liters; the plasma clearance is 0.58-1.45 l / h, the renal clearance is 0.32-0.73 l / h. Ceftriaxone reversibly binds to blood plasma proteins. From 33% to 67% of the drug is excreted unchanged by the kidneys, the rest is excreted with bile into the intestine, where it is biotransformed into an inactive metabolite.
    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 plasma 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, concentrations in the cerebrospinal fluid exceed 1.4 mg / l. In adults with meningitis, 2-24 hours after the administration of 50 mg / kg of body weight, the concentration of ceftriaxone in the cerebrospinal fluid is many times greater than the minimal inhibitory concentrations for the most common meningitis pathogens.
    Indications:
    Infectious and inflammatory diseases caused by susceptible to ceftriaxone pathogens: sepsis, meningitis, typhoid fever, salmonellosis, disseminated borreliosis Lyme (early and late stages of the disease); infections of the abdominal cavity (peritonitis, biliary tract infections and gastrointestinal tract); infection of bones, joints, soft tissues, skin, as well as wound infections; infection in patients with low immunity; infections of the kidneys and urinary tract; infections of the lower respiratory tract (incl.pneumonia), as well as infections of the ENT organs; urogenital infections (including gonorrhea, soft chancre, syphilis). Prevention of infections in the postoperative period.
    Contraindications:Hypersensitivity to cephalosporins, penicillins and carbapenems.
    Carefully:With nonspecific ulcerative colitis, with violations of the liver and kidneys, with enteritis and colitis associated with the use of antibacterial drugs; premature and newborn children with hyperbilirubinemia; pregnant and lactating.
    Pregnancy and lactation:
    The use of ceftriaxone in pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus (ceftriaxone penetrates the placental barrier).
    If it is necessary to use ceftriaxone during lactation, the question of stopping breastfeeding (ceftriaxone excreted in breast milk).
    Dosing and Administration:

    The drug is used intramuscularly or intravenously.

    For adults and for children over 12 years old The average daily dose is 1-2 g of ceftriaxone once a day or 0.5-1 g every 12 hours.

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

    For newborns 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 once a day (a dose of 50 mg / kg of body weight is not recommended because of the immature enzyme system of newborns).

    For infants and children under 12 years of age

    The daily dose is 20-75 mg / kg of body weight once a day. Children with a body weight of 50 kg and above should adhere to the dosage for adults. A dose of more than 50 mg / kg body weight should be given as an IV infusion for at least 30 minutes.

    Duration of therapy

    Depends on the course of the disease. As always with antibiotic therapy, ceftriaxone should be continued for at least 48-72 hours after the temperature is normalized and the eradication of the pathogen is confirmed.

    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). As soon as 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 meningitides

    4 days

    Haemophilus influenzae

    6 days

    Streptococcus pneumoniae

    7 days

    Sensitive

    10-14 days

    Enterobacteriaceae


    Gonorrhea

    For the treatment of gonorrhea caused by both generative and non-penicillinase-resistant strains, the recommended dose is 250 mg once intramuscularly.

    Borrelia Lyme:

    50 mg / kg (the highest daily dose -2g) for adults and children over 12 years, once a day for 14 days.

    Prevention in the pre- and postoperative period

    Before infected or presumptively 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

    In patients with impaired renal function, under the condition of 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 necessary to change.

    Intramuscular injection

    For the / m introduction, 1g of the drug should be diluted in 3.5ml of a 1% solution of lidocaine and injected deep into the relatively large muscle (gluteal), it is recommended to inject no more than 1g of the drug into one buttock. A solution of lidocaine can never be administered intravenously!

    Trial aspiration helps to avoid unintentional entry of the drug into the vessel.

    Intravenous administration

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

    Intravenous infusion

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

    Side effects:

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

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

    From the 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, basophilia.

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

    Local Reactions: phlebitis, soreness along the vein, soreness and infiltration at the site of the / m introduction.

    Other: headache, dizziness, nosebleeds, candidiasis, superinfection.

    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:Ceftriaxone, suppressing the intestinal flora, interferes with the synthesis of vitamin K. With simultaneous administration with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs, salicylates, sulfinpyrazone), the risk of bleeding increases. With a simultaneous appointment with anticoagulants, the effect of the latter is noted.
    Ceftriaxone and aminoglycosides have a synergistic effect on many Gram-negative bacteria.
    Incompatible with ethanol.
    Nonsteroidal anti-inflammatory drugs and other inhibitors of platelet aggregation increase the likelihood of bleeding.
    With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of developingnephrotoxic action.
    Pharmaceutically incompatible with solutions containing other antibiotics. Ceftriaxone Do not mix with solutions containing calcium.
    Special instructions:
    As with the use of other cephalosporins, anaphylactic reactions, including fatalities, were recorded, even in cases where the patient did not have any allergic reactions in the anamnesis. In case of allergic reactions, the drug should be discontinued and appropriate treatment should be prescribed. As with the use of other cephalosporins, the development of autoimmune hemolytic anemia is possible with drug treatment. Cases of severe hemolytic anemia in adults and children, including fatal cases, have been reported. In case of anemia, therapy with the drug should be discontinued. When

    cases of development of diarrhea caused by ceftriaxone Clostridium difficile (pseudomembriosis colitis), varying degrees of severity: from mild to colitis with fatal outcome. It is necessary to carefully collect the anamnesis, tk. cases of diarrhea caused by Clostridium difficile, more than 2 months after antibiotic therapy. In accordance with clinical indications, appropriate treatment should be prescribed (compensation for loss of fluid, electrolytes, protein, an antibiotic therapy for Clostridium difficile, surgery). When the development of isovdomembranous colitis is contraindicated the appointment of drugs that inhibit intestinal peristalsis. As with other antibacterial drugs, superinfection may develop.

    When using ceftriaxone, rare cases of prothrombin time change are described. Patients with vitamin K deficiency (impaired synthesis, eating disorders) may need to monitor prothrombin time and prescribe vitamin K (10 mg / week) with an increase in prothrombin time before or during therapy. In rare cases, gallbladder marked darkening (precipitates the calcium salt of ceftriaxone) by ultrasound (US), which disappear after cessation of treatment. With the development of symptoms or signs indicating a possible gallbladder disease, or if there are ultrasound signs of a "sluggish phenomenon," it is recommended that the drug be discontinued.With the use of ceftriaxone, rare cases of pancreatitis that develop, possibly, as a result of biliary tract obstruction are described. Most patients had risk factors for congestion in the biliary tract (eg, previous drug therapy, severe co-morbidities, completely parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. Like other cephalosporins ceftriaxone can displace bilirubin from association with serum albumin. In combination with severe renal and hepatic insufficiency, as well as in patients on hemodialysis, the concentration of ceftriaxone in the blood plasma should be regularly determined. With long-term treatment, it is necessary to regularly monitor the picture of peripheral blood, indicators of the functional state of the liver and kidneys. Cases of fatal reactions as a result of deposition of ceftriaxone-calcium precipitates in the lungs and kidneys of newborns are described. Theoretically there is a probability of interaction of ceftriaxone with calcium-containing solutions for intravenous administration and in other age groups of patients, therefore ceftriaxone not be mixed with calcium-containing solutions (including for parenteral nutrition) and administered simultaneously, including through a separate access for infusion at different sites. Theoretically, based on the calculation of 5 T1 / 2 ceftriaxoa, the interval between the administration of ceftriaxone and calcium-containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxoa with calcium-containing preparations for oral administration, as well as cefrioxone for intramuscular administration with calcium-containing drugs or for oral administration) are not available. In the treatment of ceftriaxone, false-positive results of Coombs test, a test for galactosemia, glucose in urine (glucosuria is recommended to be determined only by enzyme method). When using lidocaine as a solvent, the information given in the lidocaine application instruction must be taken into account; and also that the lidocaine solution is used as a solvent only when administered intramuscularly.


    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles,work with mechanisms and engage in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular injection of 1000 mg.
    Packaging:
    Powder for the preparation of a solution for intravenous and intramuscular injection of 1000 mg in bottles with a capacity of 10, 20 ml, hermetically sealed with rubber stoppers and crimped with aluminum caps.
    Solvent - "Lidocaine", injection for 10 mg / ml, produced by JSC "Dalhimpharm", Russia (registration certificate No. P N001261 ​​/ 01).
    1. For 1, 2, 5 and 10 vials with the drug, together with the instructions for use, put in a pack of cardboard.
    2. 50 vials with the drug together with 5 instructions for use and 100 vials with 10 instructions for use are placed in a cardboard box (for hospitals).
    3. 1 bottle of drug and 1 ampoule with a solvent, along with instructions for medical use, are placed in a pack of cardboard.
    Storage conditions:
    In a dry, dark place at a temperature of 15 ° C to 25 ° C.

    Shelf life:
    2 years.
    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000538
    Date of registration:12.05.2011 / 06.02.2015
    Expiration Date:12.05.2016
    The owner of the registration certificate:RUZFARMA, LLC RUZFARMA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp18.11.2015
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