Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsp
    Powder for solution for intramuscular and intravenous administration
    Composition:
    1 bottle contains:
    Ceftriaxone sodium salt, equivalent to ceftriaxone 1 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:

    Cephalosporin antibiotic III generation of a broad spectrum of action for parenteral administration. Bactericidal activity is due to the suppression of bacterial cell wall synthesis. It is characterized by resistance to the action of most beta-lactamases of gram-negative and gram-positive microorganisms.

    It is active against the following microorganisms: Gram-positive aerobes-Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups of viridans;

    Gram-negative aerobes: Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (incl.strains forming penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis (including strains forming penicillinase), Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (including Serratia marcescens); individual strains of Pseudomonas aeruginosa are also sensitive; anaerobes: Bacteroides fragilis, Clostridium spp. (except Clostridium difficile), Peptostreptococcus spp.

    It has in vitro activity against most strains of the following microorganisms: Citrobacter diversus, Citrobacter freundii, Providencia spp., Providencia rettgeri, Salmonella spp., (Including Salmonella typhi), Shigella spp .; Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus.

    Methicillin-resistant staphylococci are resistant to cephalosporins, incl. to ceftriaxone, many Streptococcus strains of group D and enterococci, incl. Enterococcus faecalis, also resistant to ceftriaxone.

    Pharmacokinetics:

    With intramuscular injection ceftriaxone is well absorbed from the injection site and reaches high concentrations in the blood plasma. Bioavailability of the drug is -100%. The average concentration in plasma is achieved 2-3 hours after intramuscular injection. With repeated intramuscular or intravenous administration in doses of 0.5-2 g at intervals 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 g, the half-life is between 5.8 and 8.7 hours; volume of distribution - from 5.78 to 13.5 liters; plasmathe 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-inflammatory diseases caused by susceptible to ceftriaxone pathogens: bacterial septicemia; bacterial meningitis; Lyme disease (borreliosis); infection of the abdominal cavity (peritonitis,infections of the biliary tract 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; respiratory tract infections and LOP-organs; infections of the genitals, including gonorrhea. Prevention of postoperative infections.
    Contraindications:Hypersensitivity to ceftriaxone, other cephalosporins, penicillins, carbapenems, hyperbilirubinemia in newborns, newborns, which show intravenous administration of calcium-containing solutions.
    Carefully:With caution appoint a drug for ulcerative colitis, with violations of liver and kidney function, with enteritis and colitis associated with the use of antibacterial drugs, premature infants.
    Pregnancy and lactation:

    The use of the drug during pregnancy is possible only in those cases when the intended use for the mother exceeds the potential risk to the fetus (ceftriaxone penetrates the placental barrier).

    If it is necessary to use the drug 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: 1-2 g once a day (every 24 hours) or 0.5-1 g every 12 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.

    Lyme disease (borreliosis): 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.

    Uncomplicated gonorrhea (caused by penicillin-forming and penicillin-anesthetic strains): single intramuscular injection of 250 mg of the drug.

    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 a drug from the group of 5-nitroimidazoles, for example, ornidazole, was well established.

    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): for the treatment of skin and soft tissue infections, the recommended daily dose is 50-75 mg / kg, divided into 2 doses (every 12 hours). The total daily dose in children should not exceed 2 g. For bacterial meningitis in children, the initial dose is 100 mg / kg (but not more than 4 g) once a day, then 100 mg / kg / day (but not more than 4 g) 1 time per day or divided into 2 doses (every 12 hours). The duration of treatment is 7-14 days.

    In the treatment of acute otitis media in children, a single IV IM is recommended in a dose of 50 mg / kg (but not more than 1 g).

    In the treatment of other infections in children, the recommended daily dose is 50-75 mg / kg, divided into 2 divided doses (every 12 hours). The total daily intake for children should not exceed 2 g.

    In children with a body weight of 50 kg and above, doses for adults are used.

    A dose of more than 50 mg / kg of body weight should be given as an IV infusion for 30 minutes.

    Elderly patients: usual doses for adults, without adjustments for age.

    In patients with impaired renal function There is no need to reduce the dose if the liver function remains normal. The daily dose of ceftriaxone should not exceed 2 g only in cases of renal insufficiency with creatinine clearance less than 10 ml / min.

    In patients with hepatic dysfunction there is no need to reduce the dose if the kidney function 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. The daily dose should not exceed 2 g without determining the concentration of the drug in the blood plasma.

    Patients on hemodialysis do not require an additional dose after a hemodialysis session, however, it is necessary to control the concentration of ceftriaxone in the plasma, since its excretion in such patients can be slowed down (dose adjustment may be required).

    Treatment with ceftriaxone should continue for at least 2 more days after the disappearance of symptoms and signs of infection. The course of treatment is usually 4-14 days; with complicated infections, a longer duration of administration may be required. The course of treatment for infections caused by Streptococcus pyogenes, must be at least 10 days.

    Rules for the preparation and administration of solutions: use only freshly prepared solutions.

    For intramuscular injection: the contents of the vial (1 g) are dissolved in 3.6 ml of water for injection. 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, the Axon drug is injected into a relatively large muscle; Trial aspiration helps to avoid unintentional insertion into the blood vessel. It is recommended to inject not a bolt of 1000 mg of the drug into one relatively large 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 (1 g) are dissolved in 9.6 ml of water for injection. 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 dissolved 2 g in 40 ml of sterile water for injection or one of infusion solutions not containing calcium (0.9% sodium chloride, 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: rash, itching, fever or chills, allergic dermatitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell syndrome, allergic pneumonitis, anaphylaxis, bronchospasm, serum sickness.

    From the nervous system: headache, dizziness, convulsions.

    From the digestive system: diarrhea, nausea, vomiting, taste disorder, stomatitis, glossitis, pseudomembranous colitis, abdominal pain, colitis, dyspepsia, bloating, "sluggish phenomenon" of the gallbladder, jaundice, cholelithiasis, pancreatitis.

    From the hematopoiesis: anemia (including hemolytic), leukopenia, lymphopenia, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia, agranulocytosis, basophilia, leukocytosis, lymphocytosis, monocytosis, granulocytopenia.

    From the genitourinary system: candidiasis of the vagina, oliguria, vaginitis, glucosuria, hematuria, nephrolithiasis.

    Local reactions: with iv introduction - phlebitis, tenderness, compaction along the vein; Intramuscular injection - soreness, sensation of warmth, tightness or condensation at the injection site. Laboratory indicators: increase (decrease) in prothrombin time, increase in thromboplastin time,increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, increasing kontseshratsii urea, the presence of sediment in the urine.

    Other: increased sweating, "hot flashes" of blood, nosebleeds, a feeling of palpitations.

    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:

    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Antagonism with chloramphenicol in vitro.

    Pharmaceutical interaction

    Ceftriaxone solutions should not be mixed or administered simultaneously with other antimicrobial agents. Pharmaceutically compatible with solutions containing calcium ions (including Hartman and Ringer's solution), and also with amsacrine, vancomycin, aminoglycosides and fluconazole.

    It does not contain N-metiltiotetrazolnoy group, therefore the interaction with ethanol did not lead to the development disulfiramopodobnyh reactions inherent in some cephalosporins.

    Ceftriaxone, suppressing the intestinal flora, prevents the synthesis of vitamin K.With simultaneous administration with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory agents, salicylates, sulfinpyrazone), increases the risk of bleeding. With a simultaneous appointment with anticoagulants, the effect of the latter is noted.

    With simultaneous use with "loop" diuretics, the risk of developing nephrotoxic action increases.

    Ceftriaxone and aminoglycosides have a synergistic effect on many Gram-negative bacteria.

    Special instructions:

    When concomitant severe renal and hepatic failure, as well as in patients on hemodialysis, should be regularly to determine the concentration of drug in plasma.

    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, gallbladder marked darkening (precipitates the calcium salt of ceftriaxone) by ultrasound (US), which disappear after cessation of treatment. With the development of the symptoms or signs indicating the possible gallbladder disease, or in the presence of ultrasound signs "sludge phenomenon" is recommended to stop administering the drug.

    When using the drug, rare cases of pancreatitis, which developed, possibly, as a result of obstruction of the biliary tract, are described. Most patients had risk factors for congestion in the biliary tract (previous drug therapy, severe co-morbidities, complete parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. Ceftriaxone does not contain an N-methylthiotetrazol group, which causes disulfiram-like effects with simultaneous use of ethanol and bleeding that are inherent in some cephalosporins.

    When using the drug, 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. 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 others.age groups of patients, therefore ceftriaxone should not be mixed with calcium-containing solutions (including for parenteral nutrition), and also administered simultaneously, incl. through separate accesses for infusions at different sites. Theoretically, based on the calculation of 5 half-lives of ceftriaxone, the interval between the administration of ceftriaxone and calcium-containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral calcium-containing preparations, as well as ceftriaxone for intramuscular administration with calcium-containing drugs (iv and oral) are absent.

    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 the drug, both in the background of taking, and after 2-3 weeks. after discontinuation of treatment, the development of diarrhea caused by Clostridium difficile (pseudomembranous colitis) is possible. In mild cases, it is sufficient to discontinue treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein,the appointment of vancomycin, metronidazole. Do not use drugs that inhibit the intestinal motility. When using ceftriaxone (as well as other antibiotics), the development of superinfection is possible, which requires the withdrawal of the drug and the appointment of appropriate treatment.

    Effect on the ability to drive transp. cf. and fur:Patients using ceftriaxone, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
    Form release / dosage:
    Powder for solution for intramuscular and intravenous administration 1 g.
    Packaging:
    1 g in a transparent sterile type III FS bottle, closed with a sterile gray stopper made of butyl rubber with a metal run-off and clogged with a dark blue polypropylene snapper seal.
    One bottle together with the instruction for use is placed in a cardboard box.
    Storage conditions:In a dry, the dark 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 expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-002684
    Date of registration:05.03.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:Ajanta Pharma, Ltd.Ajanta Pharma, Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp04.07.2017
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