Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsp
    Powder for the preparation of solution for intravenous and intramuscular injection.

    Composition:
    each bottle contains:

    active substance: ceftriaxone (in the form of ceftriaxone sodium) 1.0 g

    Description:
    From white to white with a yellowish hue of color powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:

    Ceftriaxone-Vial is a semi-synthetic cephalosporin antibiotic of the third generation of a broad spectrum of action.

    The bactericidal activity of ceftriaxone is due to the suppression of the synthesis of cell membranes. The drug is highly resistant to the action of beta-lactamases (penicillinase and cephalosporinase) Gram-positive and Gram-negative microorganisms. Ceftriaxone-Vial is active against the following microorganisms:

    Gram-negative aerobes: Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains resistant to ampicillin), Haemophilus parain- fluenzae, 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 Pseudomonas aerugenosa 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., Clostridium spp. (with the exception of Clostridium difficile).

    Pharmacokinetics:With intramuscular injection 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 intramuscular or intravenous administration in doses of 0.5-2.0 g with an interval of 12 to 24 hours, there is accumulation of ceftriaxone in a concentration that is 15-36% higher than the concentration achieved with a 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. Have of adults patients with meningitis after 2-24 hours, after administration of a dose of 50 mg / kg of body weight, the concentration of ceftriaxone in the cerebrospinal fluid is many times greater than the minimum inhibitory concentrations for the most common pathogens of meningitis.
    Indications:
    Infections caused by susceptible pathogens: sepsis; meningitis; 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 weakened immunity; infections of the pelvic organs; infections of the kidneys and urinary tract; infections of the respiratory tract, especially pneumonia, and infections of the ENT organs; infections of the genitals, including gonorrhea.
    Prevention of infections after surgery.
    Contraindications:
    Hypersensitivity to cephalosporins.

    Carefully:Assign the drug with 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-Vial during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus (ceftriaxone penetrates the placental barrier).
    If Ceftriaxone-Vial is needed 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

    Adults and children over 12 years of age: for 1-2 g once a day (every 24 hours). In severe cases or infections, the causative agents of which have only moderate sensitivity to ceftriaxone, the daily dose can be increased to 4 g.

    Newborns (up to 2 weeks): 20-50 mg / kg body weight once a day. The daily dose should not exceed 50 mg / kg of body weight. When determining the dose, there is no need to distinguish between full and premature babies.

    Infants and young children (from 15 days to 12 years): 20-80 mg / kg body weight once a day.

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

    Intravenous doses of 50 mg / kg or higher should be administered drip 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-Vial 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

    When bacterial meningitis in infants and young children treatment starts with a dose of 100 mg / kg (but not more than 4 g) 1 time per day. After identifying the pathogen and determining its sensitivity, the dose can be reduced accordingly. The best results with meningococcal meningitis were achieved with a treatment duration of 4 days, with meningitis caused by Haemophilus influenzae - 6 days, Streptococcus pneumoniae - 7 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 (caused by penicillinase-forming and penicillin-zoned strains): single intramuscular injection of 250 mg Ceftriaxone-Vial.

    Prevention of postoperative infections, depending on the degree of infectious risk, 1-2 g of Ceftriaxone-Vial is administered once 30-90 minutes before the operation. In operations on the colon and rectum, the simultaneous (but separate) administration of Ceftriaxone-Vial and one of the 5-nitroimidazoles, for example, ornidazole, was well established.In patients with impaired renal function there is no need to reduce the dose, if the function liver remains normal. The daily dose of the drug should not exceed 2 g only in cases of preterminal renal failure (creatinine clearance less than 10 ml / min). In patients with hepatic dysfunction there is no need to reduce the dose, if the function kidneys remains normal.

    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 g 3.6 ml

    After preparation, each 1 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-Vial is injected into a relatively large muscle; 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 buttock. To reduce pain with intramuscular injections, the drug should be administered with a 1% solution of lidocaine (intragenic). 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 injection)

    1 g 9.6 ml

    After preparation, each 1 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-Vial 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"-a syndrome), a dysbacteriosis.

    From the hematopoiesis: anemia, leucopenia, leucocytosis, neutropenia, granulocytopenia, lymphocytopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, reducing the concentration of flame coagulation factors (II, VII, IX, X), an elongation of prothrombin time.

    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:In case of an overdose, hemodialysis and peritoneal dialysis will not reduce the concentration of the drug.There is no specific antidote. Treatment of an overdose is symptomatic.
    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:
    With simultaneous severe renal and hepatic insufficiency, in patients who are on hemodialysis, the concentration of the drug in the 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.
    In rare cases with ultrasound of the gallbladder, blackouts are observed, which disappear after the treatment is discontinued (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and to conduct symptomatic treatment). 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).
    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.
    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-Vial requires even greater caution. Elderly and debilitated patients may require the appointment of vitamin K.
    Form release / dosage:Powder for solution for intravenous and intramuscular injection 1 g.
    Packaging:1 g (in terms of ceftriaxone) in hermetically sealed vials of colorless transparent glass. The bottle is sealed with a rubber stopper, crimped with an aluminum cap with a plastic cap for monitoring the first opening or without it. 1 bottle together with the instruction for use is placed in a cardboard box.
    For 10, 50, 100 vials together with the instruction for use are placed in a cardboard box (for hospitals).
    Storage conditions:
    Store in a dry place, protected from light and out of reach of children, at a temperature of no higher than 25 ° C.

    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000023
    Date of registration:06.11.2007
    The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.11.2015
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