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

    1 bottle contains:

    Dosage

    Active substance:

    0.5 g

    1.0 g

    Ceftriaxone sodium (in terms of ceftriaxone)

    500 mg

    1000 mg


    Description:The powder is white or white with a yellowish hue.
    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 β-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 (including strains forming penicillinase), Haemophilus parainfluenzae ,, Klebsiella spp. (including Klebsiella pneumoniae), Moraxella catarrhalis (including penicillin-producing strains), 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.
    Has in vitro activity against most strains of the following microorganisms, although the clinical significance of this is unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp. (including 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:

    Bioavailability is about 100%. Time to reach the maximum concentration (Tcmax) after intramuscular (IM) administration - 2-3 hours after intravenous (IV) administration - at the end of infusion. The maximum concentration (Cmax) ceftriaxone after i / m administration of the drug in doses of 0.5 and 1.0 g - 38 and 76 mcg / ml, respectively. FROMmax with intravenous administration in doses of 0.5, 1.0 and 2.0 g - 82, 151 and 257 μg / ml, respectively. In adults 2-24 hours after the administration of a dose of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF) is many times greater than the minimumsuppressing concentration for the most common pathogens of meningitis. It penetrates well into CSF ​​with inflammation of the meninges. The connection with plasma proteins is 83-96%. The volume of distribution - 0.12 - 0.14 l / kg (5.78 - 13.5 l), in children - 0.3 l / kg, plasma clearance - 0.58-1.45 l / h, renal -0.32-0.73 l / h. The half-life period (T1 / 2) after IM is 5.8-8.7 hours after IV injection at a dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours; in patients on hemodialysis (creatinine clearance 0-5 ml / min) - 14.7 hours, with SC 15-15 ml / min - 15.7 hours, 16-30 ml / min - 11.4 hours, 31-60 ml / min - 12.4 hours. Output is unchanged: 33-67% - kidney; 40-50% - with bile in the intestine, where the inactivation occurs. In newborn infants, about 70% of the drug is excreted by the kidneys. Hemodialysis is ineffective.

    Indications:
    Infectious-inflammatory diseases caused by susceptible to ceftriaxone pathogens:
    - infections of the abdominal cavity organs (peritonitis, gastrointestinal tract infections, bile ducts);
    - Lower respiratory tract infections (including pneumonia, lung abscess, pleural empyema);
    - infections of bones and joints;
    - skin and soft tissue infections (including wound infections);
    - urinary tract infections (complicated and uncomplicated);
    uncomplicated gonorrhea;
    - infections of the pelvic organs;
    - bacterial meningitis;
    - bacterial septicemia;
    - Lyme disease (borreliosis);
    - prevention of postoperative infections;
    - infectious diseases in persons with weakened immunity.
    Contraindications:
    Hypersensitivity to ceftriaxone, other cephalosporins, penicillins, carbapenems, hyperbilirubinemia in newborns.
    Newborns, which are shown in / in the introduction of solutions containing calcium (Ca2 +).
    Carefully:Premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.
    Pregnancy and lactation:The use of the drug during pregnancy is only possible in that. If the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use the drug during lactation, breastfeeding should be stopped.
    Dosing and Administration:The drug is administered intravenously or intramuscularly.

    Adults and children over 12 years of age: 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.

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

    Uncomplicated gonorrhea: 250 mg IM once.

    Prevention of postoperative infections: depending on the degree of infectious risk, 1-2 g of the drug is administered once for 30-90 min before the operation. In operations on the colon and rectum, simultaneous (but separate) administration of the drug and one 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 children;

    Infant and young children (from 15 days to 12 years): 20-80 mg / kg body weight once a day (or divided into two applications). The total daily intake for children should not exceed 2 g.

    For the treatment of skin and soft tissue infections, the recommended daily intake in children is 50-75 mg / kg divided into 2 divided doses (every 12 hours). The total daily dose in children should not exceed 2 in

    With bacterial meningitis the children lTreatment starts at a dose of 100 mg / kg (but not more than 4 g) once a day, then 100 mg / kg / day (but not more than 4 g) once a day or divided into 2 divided doses (every 12 hours).Duration of treatment is 7-14 days.

    Children with a body weight of 50 kg and above appoint doses for adults. An IV dose of 50 mg / kg or higher should be administered drip for at least 30 minutes.

    To the elderly: the usual doses provided for adults, without adjusting 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 impaired liver function, there is no need to reduce the dose if the kidney function remains normal.

    When combined with severe renal and hepatic insufficiency should regularly determine the concentration of ceftriaxone in the plasma and, if necessary, adjust the dose of the drug. The daily dose should not exceed 2 g without determining the concentration of ceftriaxone in the blood plasma.

    Patients undergoing hemodialysis additional introduction of the drug after dialysis is not required. It should, however, monitor the concentration of ceftriaxone in the plasma, since the rate of excretion in these patients may decrease (dose adjustment may be required). The duration of treatment depends on the nature and severity of the disease.Treatment with the drug should continue for at least 2 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 an intravenous injection, 500 mg of the drug is dissolved in 2 ml, 1.0 g in 3.6 ml of water for injection and injected deeply into the gluteus muscle. After preparation, each ml of the solution contains about 250 mg in terms of ceftriaxone. It is recommended to inject no more than 1.0 g in one buttock. To reduce pain as a solvent, 1% lidocaine solution can be used. The solution containing lidocaine, can not be administered intravenously!

    For IV injection 500 mg of the drug in 4.8 ml is dissolved, and 1.0 g is 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 injected iv slowly for 2-4 minutes.

    The IV infusion should last at least 30 minutes. To prepare the solution, dilute 2.0 g of the drug in 40 ml of water for injection or one of the following infusion solutions,not containing calcium ions: 0.9% solution of sodium chloride, 5%, 10% dextrose solution, 5% solution of fructose.

    Ceftriaxone solutions should not be mixed or added to solutions containing others. antibiotics or other solvents, with the exception of those listed above, because of the possible incompatibility.

    Side effects:

    From the nervous system: headache, dizziness, convulsions.

    From the digestive system: diarrhea, nausea, vomiting, stomatitis, glossitis, abdominal pain, colitis, indigestion, taste disturbance, flatulence, pseudomembranous colitis, jaundice, cholelithiasis, "sludge-phenomenon" of the gallbladder.

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

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

    Allergic Reagents: rash, itching, fever or chills, allergic dermatitis, hypersensitivity pneumonitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome,toxic epidermal necrolysis (Lyell's syndrome), anaphylactic or anaphylactoid reactions, bronchospasm, serum sickness.

    Local Reakies: with iv introduction - phlebitis, tenderness, compaction along the vein; v / m - introduction - soreness, sensation of warmth, tightness or condensation at the injection site.

    Laboratory indicators: increase (decrease) in prothrombin time, increase in thromboplastin time, increase in activity of "hepatic" transaminases and alkaline phosphatase (ALF), hyperbilirubinemia, hypercreatininemia, increased urea concentration, presence of sediment in urine.

    Other: increased sweating, "hot flashes" of blood, epistaxis, pancreatitis, palpitation.

    Overdose:When an overdose of hemodialysis and peritoneal dialysis does not reduce the concentration of the drug. There is no specific antidote. Treatment of an overdose is symptomatic.
    Interaction:
    Antibiotics, acting bacteriostatically, reduce the bactericidal effect of ceftriaxone.
    Antagonism with chloramphenicol in vitro.
    It is pharmaceutically incompatible with solutions containing Ca2 + (incl.Hartman and Ringer's solution), as well as% with amsacrine, vancomycin, fluconazole, and aminoglycosides. It does not contain N-metiltiotetrazolnoy group, therefore the interaction with ethanol did not lead to the development disulfiramopodobnyh reactions inherent in some cephalosporins. There is synergy between ceftriaxone and aminoglycosides against many Gram-negative bacteria. Because of the pharmaceutical incompatibility of ceftriaxone and aminoglycosides, they should be administered separately in the recommended doses for them.
    Special instructions:In combination with severe renal and hepatic insufficiency, as well as in patients on hemodialysis, the concentration of ceftriaxone 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, ultrasound examination (ultrasound) of the gallbladder shows darkening, (precipitates of the calcium salt of ceftriaxone), which disappear after the 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, possibly, due to, biliary obstruction, have been described. Most patients had risk factors, congestion of biliary tracts (previous drug therapy, severe co-morbidities, completely parenteral nutrition); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. When using the drug, rare cases of prothrombin time change are described. Patients with vitamin K deficiency (impaired synthesis, eating disorder) 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-Ca2 + precipitates in the lungs and kidneys of newborns are described. Theoretically, there is a probability of interaction of ceftriaxone with Ca2 + -containing solutions for intravenous administration and in other age groups of patients, so the drug should not be mixed with Ca2 + -containing solutions (including for parenteral nutrition), and also administered simultaneously, in t .h.through separate accesses for infusions at different sites. The interval between the administration of the preparation and Ca2 + -containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral Ca2 + -containing preparations, as well as ceftriaxone for intramuscular administration with Ca2 + -containing drugs (iv and oral) are absent. When treatment with the drug may be false-positive results of the Coombs sample, a sample for galactosemia, in determining glucose in the urine (glucose is recommended to determine only by enzyme method).
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g.

    Packaging:
    For 0.5 or 1.0 g of active substance is placed in bottles of glass, sealed with stoppers, crimped aluminum caps. 1 bottle is placed in a cardboard box together with instructions for use.
    10 bottles are placed in a box of cardboard box along with instructions for use.
    For hospitals: 50 bottles are placed in a box, from cardboard box together with an application of an equal number of instructions for use.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    2.5 years.
    Do not use the product after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001551
    Date of registration:01.03.2012
    Date of cancellation:2017-03-01
    The owner of the registration certificate:REDKINSKY EXPERIMENTAL FACTORY, CJSC REDKINSKY EXPERIMENTAL FACTORY, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp15.11.2015
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