Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    Active substance: ceftriaxone sodium 1.0 g.

    Description:
    White or white with a yellowish tint powder.

    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:

    Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro suppresses the growth of many 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). In vitro and in conditions of clinical practice ceftriaxone is usually effective against the following microorganisms: Gram-positive aerobes:

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

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

    Gram-negative aerobes:

    Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (including Kl. pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitides, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are resistant), Salmonella spp. (including Salmonella marcescens), Shigella spp., Vibrio spp. (including Vibrio cholerae), Yersinia spp. (including Yersinia 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 microorganisms: Bacteroides spp. (including some strains Bacteroides fragilis), Clostridium spp. (with the exception of 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.

    Pharmacokinetics:
    With parenteral administration ceftriaxone well penetrates into tissues and body fluids.
    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.
    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, ceftriaxone binding 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.
    The half-life in adults is about 8 hours. In newborns up to 8 days, 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 kidney form, and 40-50% is also unchanged through the intestine. 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 renal insufficiency or liver pathology in adults, the pharmacokinetics of ceftriaxone is almost unchanged, the half-life elongates slightly. 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.
    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 of body weight, the concentration of the drug in the cerebrospinal fluid is many times greater than the minimum inhibitory concentrations for the most common meningitis pathogens.
    Indications:
    Infectious-inflammatory diseases caused by microorganisms sensitive to ceftriaxone: sepsis; meningitis; disseminated borreliosis Lyme (early and late stages of the disease); infection of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts); infection of bones, joints, connective tissue, skin; infection in patients with weakened immunity; infections of the pelvic organs; infections of the kidneys and urinary tract; infections of the respiratory tract (especially pneumonia) and LOP-organs; infection of the genitals, including gonorrhea.
    Prevention of infections in the postoperative period.
    Contraindications:
    Hypersensitivity to ceftriaxone, to other cephalosporins, penicillins, carbapenems.

    Carefully:Assign the drug 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; pregnancy and lactation.
    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 administered intramuscularly or intravenously.

    Standard dosing regimen

    For adults and for children over 12 years of age:

    The average daily dose is 1-2 g of ceftriaxone once a day (every 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 (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 allowed to exceed in connection with the immature enzyme system of newborns).When determining the dose, there is no need to distinguish between full and premature babies. For infants and children under 12 years (from 15 days to 12 years): The daily dose is 20-80 mg / kg body weight.

    Children with a body weight of 50 kg and above should be given doses for adults. The drug at a dose of 50 mg / kg body weight and more should be administered as an intravenous infusion for at least 30 minutes.

    Patients of senile age: usual doses for adults, without adjustments for age.

    Duration of treatment 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.

    Dosing in special cases:

    Meningitis:

    In bacterial meningitis in infants and young children, the initial dose is 100 mg / kg 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

    Causative agent

    Duration of therapy

    Neisseria meningitidis

    4 days

    Haemophilus influenzae

    6 days

    Streptococcus pneumoniae

    7 days

    Sensitive Enterobacteriaceae

    10-14 days

    Borrelia Lyme: 50 mg / kg (the highest daily dose is 2 g) for adults and children over 12 years of age once a day for 14 days.

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

    Prevention of postoperative infections, depending on the degree of infectious risk, 1-2 g of ceftriaxone is administered once 30-90 minutes before the start of the operation. In operations on the colon and rectum, simultaneous (but separate) administration of ceftriaxone and one of 5-nitroimidazoles has proved to be well established.

    Lack of kidney and liver function:

    In patients with impaired function of the kidneys, with normal liver function, there is no need to reduce the dose of ceftriaxone. 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 function of the liver, provided that the function of the kidneys is preserved, a dose of ceftriaxone is also not necessary to reduce.

    When combination of severe renal and hepatic insufficiency should regularly determine the concentration of ceftriaxone in the plasma and, if necessary, adjust its dose.

    Patients on dialysis additional introduction of the drug after dialysis is not required. It should, however, control the concentration of ceftriaxone in the serum for possible dose adjustment, since the rate of excretion of the drug in these patients may be reduced.

    Mode of application

    For intramuscular injection:

    The contents of the vial are dissolved as follows:

    Contents of the bottle Solvent (water for injection)

    1.0 g 3.5 ml

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

    If necessary, a more dilute solution may be used. As with other intramuscular injections ceftriaxone injected into a relatively large muscle (gluteal); 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 injections, the drug should be administered with a 1% solution of lidocaine. Do not inject lidocaine solution intravenously.

    For intravenous administration:

    The contents of the vial are dissolved as follows:

    Contents of the bottle Solvent (water for injections)

    1.0 g 10.0 ml

    After preparation, each ml of the solution contains about 100 mg 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 sterile water for injection or one of the infusion solutions that do not contain calcium (0.9% sodium chloride solution, 2.5%, 5% or 10% dextrose solution, 5% levulose solution, 6% dextran solution in dextrose) . 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 disturbance, stomatitis, glossitis, enterocolitis, pseudomembranous, liver dysfunction (increased activity "liver" enzymes, at least - alkaline phosphatase, or bilirubin, cholestatic icterus), gallbladder psevdoholelitiaz ("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.

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

    Local reactions: phlebitis, pain along the veins; morbidity 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. 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. Incompatible with ethanol.
    Pharmaceutical interaction
    Ceftriaxone solutions should not be mixed or administered simultaneously with other antimicrobial agents. Ceftriaxone Do not mix with solutions containing calcium.

    Special instructions:
    Despite the detailed history, which is the rule for other cephalosporin antibiotics, one can not exclude the possibility of developing an anaphylactic shock that requires immediate therapy - first intravenously injected epinephrine, then glucocorticosteroids.
    With simultaneous severe renal and hepatic insufficiency, patients who are on hemodialysis should regularly determine the concentration preparation at plasma.
    During treatment, the use of ethanol is contra-indicated - disulfiramoid-like effects are possible (facial flushing, stomach and stomach spasms, nausea, vomiting, headache, lowering of blood pressure, tachycardia, dyspnea).
    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.
    Elderly and debilitated patients may require the appointment of vitamin K.
    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. Ceftriaxone It is used only in a hospital.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection, 1.0 g.
    Packaging:
    Powder for the preparation of a solution for intravenous and intramuscular injection of 1.0 g of active substance in a vial of clear glass, sealed with a plug of chlorobutyl rubber,Crimped aluminum cap with safety plastic lid. 1 bottle with instructions for use in a cardboard box.
    For hospitals: 50 bottles together with instructions for use in a cardboard box
    Storage conditions:In a dry, protected from light 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 expiration of the period indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N012822 / 01
    Date of registration:23.06.2008
    The owner of the registration certificate:Aquarium EnterpriseAquarium Enterprise India
    Manufacturer: & nbsp
    Representation: & nbspAquarium EnterpriseAquarium EnterpriseIndia
    Information update date: & nbsp24.11.2015
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