Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for solution for injection.
    Composition:
    Each vial contains:

    Active substance:

    Ceftriaxone sodium 1.193 g equivalent to ceftriaxone anhydrous 1 g.
    Description:
    The powder is almost white or 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, 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 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:

    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 enterocolotica).

    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 animal experiments Clinical data for primary and secondary syphilis indicate a good efficiency of ceftriaxone.

    Anaerobic pathogens:

    Bacteroides spp. (including some strains of B. fragilis), Clostridium spp. (at Tom number of FROM1. 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, 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.
    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% is also unchanged in 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, 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.
    Penetration into the cerebrospinal fluid:
    In newborns and in children with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid,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 LOP-organs, genital infections, including gonorrhea. Prevention of infection in the postoperative period.
    Contraindications:Hypersensitivity to cephalosporins and penicillins. The first trimester of pregnancy.
    Carefully:
    hyperbilirubinemia in newborns, premature infants, renal / hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy, lactation.

    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 scheme 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,

    appoint them in recommended doses separately!

    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 influenza

    6 days

    Streptococcus pneumoniae

    7 days

    Sensitive Enterobacteriacease

    10-14 days

    Gonorrhea:

    For the treatment of gonorrhea caused by both generative and non-penicillinase-resistant 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: 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 kidney function in the preterminal stage is insufficient (creatinine clearance below 10 ml / min), that the daily dose of ceftriaxone does not exceed 2 g. In patients with impaired hepatic 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 administration:

    For intramuscular administration, 1 g 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 1 g 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:

    Allergic reactions: urticaria, chills or fever, rash, itching, rarely - bronchospasm, eosinophilia, Stevens-Johnson syndrome, erythema polymorphic exudative, 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), dysbacteriosis.

    From the hematopoiesis: leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decreased plasma clotting factors (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, 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 and aminoglycosides have a synergistic effect on many Gram-negative bacteria. Incompatible with ethanol.
    NSAIDs and other inhibitors of platelet aggregation increase the chance of bleeding.
    With simultaneous use with "loop" diuretics, etc.nephrotoxic drugs increases the risk of developing a nephrotic effect.
    Pharmaceutically incompatible with solutions containing other antibiotics.
    Do not mix in one infusion bottle or in one syringe with another antibiotic (chemical incompatibility).
    Special instructions:
    Ceftriaxone is used only in a hospital.
    With simultaneous severe renal and hepatic insufficiency, the concentration of the drug in the plasma should be regularly determined.
    In patients who are on hemodialysis, it is necessary to monitor the concentration of ceftriaxone in the plasma, tk. they can decrease the rate of its excretion. 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 that disappear after cancellation (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and conduct symptomatic treatment).
    During treatment, the use of ethanol is contraindicated - disulfiramide-like effects are possible (facial flushing, stomach and stomach spasms, nausea, vomiting, headache, lowering 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, which requires immediate therapy - first inject adrenaline, then glucocorticoids.
    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. With prolonged use, periodic monitoring of the blood formula is necessary. Freshly prepared ceftriaxone solutions are physically and chemically stable for 6 hours at room temperature.
    When appointing during lactation, it is necessary to cancel breastfeeding. Elderly and debilitated patients may require the appointment of vitamin K.
    Form release / dosage:
    Powder for solution for injection at 250 mg, 500 mg and 1.0 g.
    Packaging:
    For 250 mg, 500 mg or 1 g of the drug is placed in a bottle of clear, colorless, neutral glass,It is sealed with a rubber stopper under an aluminum run-off and closed with a plastic cap. One bottle together with the instruction for use is placed in a pack of cardboard.
    Storage conditions:In dry, the dark place at a temperature below 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N014470 / 01
    Date of registration:10.09.2008
    The owner of the registration certificate:Ipka Laboratories Ltd.Ipka Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspIPKA LABORATORIES LTD. IPKA LABORATORIES LTD. India
    Information update date: & nbsp22.11.2015
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