Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular administration.
    Composition:One bottle contains ceftriaxone 0.25 g and 1 g in the form of ceftriaxone sodium salt.
    Description:The powder is white or white with a yellowish hue.
    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 the ratio of beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by the majority of gram-positive and gram-negative bacteria). 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. enterocolitica)

    Note: many strains of these microorganisms, which in the presence of other antibiotics, for example, penicillins, first-generation cephalosporins and aminoglycosides, are multiplying steadily, are 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 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.
    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 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 the form of 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. In renal failure or liver disease in adults pharmacokinetics ceftriaxone hardly changes, half-life period is lengthened 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 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, infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts), infections of bones, joints, connective tissue, skin, infection in patients with low immunity, infection of the kidneys and urinary tract pathways, respiratory tract infections (including pneumonia), as well as infections of LOP-organs, urogenital infections (including gonorrhea).
    Prevention of infections 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:

    The drug is used intramuscularly and intravenously.

    For adults and for children over 12 years old

    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 single 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 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 body weight.

    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 intravenous infusion, for at least 30 minutes.

    Duration of therapy

    Depends on the course of the disease.

    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 to the dose must be reduced accordingly. The best results were achieved with the following periods of therapy:

    Causative agent

    Duration of therapy

    Neisseria meningitidis

    4 days

    Haemophilus influenzae

    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 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 intramuscular injection, 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

    Duration of intravenous infusion is at least 30 minutes. For intravenous infusion of 2 g of the powder should be diluted with approximately 40 ml of a solution free of calcium, such as 0.9% sodium chloride solution, 5% dextrose solution, 10% dextrose solution, 5% fructose solution.

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

    On the part of the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, impaired taste, stomatitis, glossitis, pseudomembranous enterocolitis, impaired liver function (increased activity of "liver" transaminases, less often - alkaline phosphatase or bilirubin, cholestatic jaundice), dysbiosis .
    On the part of the hematopoiesis: leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in plasma clotting factor concentration (II, VII, IX, X), prolongation of prothrombin time.
    On the part of the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glycosuria, cylindruria, hematuria), oliguria, anuria.
    Local reactions: phlebitis, pain 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 byhemodialysis or peritoneal dialysis. Symptomatic measures are recommended for the treatment of overdose cases.
    Interaction:
    Combination Therapy
    Between the ceftriaxone and aminoglycosides, there is synergy in the effect on many gram-negative bacteria. Although it is impossible to predict the effect of such combinations in advance, it is justified to jointly assign them in cases of severe and life-threatening infections (for example, caused by Pseudomonas aeruginosa).
    In connection with the physical incompatibility of ceftriaxone and aminoglycosides, it is necessary to prescribe them separately in recommended doses!
    Incompatible with ethanol.
    NSAIDs and other inhibitors of platelet aggregation increase the chance of bleeding.
    With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of nephrotoxic effect increases.
    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:
    With simultaneous severe renal and hepatic insufficiency,The concentration of the drug in the plasma should be determined regularly.
    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 - disulfiramoid-like effects are possible (red face, spasm in the stomach, 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 that requires immediate therapy - first intravenously injected epinephrine, 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.
    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 of 0.25 g and 1.0 g.
    Packaging:Powder for solution for injection of 0.25 g and 1.0 g in bottles of 5 and 10 ml. One bottle together with instructions for use in a cardboard tutu.
    Storage conditions:List B. In the dark place at a temperature of no higher than 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 N015852 / 01
    Date of registration:18.11.2009
    The owner of the registration certificate:Alembic Pharmaceuticals, LimitedAlembic Pharmaceuticals, Limited India
    Manufacturer: & nbsp
    Representation: & nbspAlembic Pharmaceuticals, LimitedAlembic Pharmaceuticals, LimitedIndia
    Information update date: & nbsp21.11.2015
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