Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:Each vial contains an active substance: ceftriaxone sodium trisecihydrate (in terms of ceftriaxone) -0.5 g or 1.0 g.
    Description:Powder of almost white or yellowish color, hygroscopic.
    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. Active in relation to the following microorganisms:
    gram-positive aerobes - Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups of viridans; gram-matic 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 penicillinase-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 strains of group D streptococcus and enterococci, incl. Enterococcus faecalis, also resistant to ceftriaxone.
    Pharmacokinetics:Bioavailability is 100%, the time to reach the maximum concentration (TCmax) after the / m introduction - 2-3 hours, after IV introduction - at the end of the infusion. The maximum concentration (Cmах) after IM in doses of 0.5 and 1 g is 38 and 76 μg / ml, respectively. Cmax at iv in doses of 0.5, 1 and 2 g - 82, 151 and 257 μg / ml, respectively. In adults, 2-24 hours after administration at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF) is many times greater than the -minimum inhibitory concentration (MIC) for the most common pathogens of meningitis.It penetrates well into CSF ​​with inflammation of the meninges. Relationship with plasma proteins - 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 was 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 (CC 0-5 ml / min) - 14.7 hours, with KK 5-15 ml / min - 15.7 h, 16-30 ml / min-11.4 h, 31-year- 60 ml / min - 12.4 hours. In newborns, seniors and patients with impaired liver and kidney function, the elimination half-life is significantly prolonged, cumulation is possible.
    It is excreted unchanged - 33-67% by the kidneys; 40-50% - with bile in the intestine, where the inactivation occurs. About 70% of the drug is excreted through the kidneys in newborn infants. Hemodialysis is ineffective.
    Indications:Bacterial infections caused by microorganisms sensitive to ceftriaxone: infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts, including cholangitis, empyema of the gallbladder), infections of the pelvic organs, infections of the lower respiratory tract (including pneumonia, abscess of the lungs, pleural empyema), acute otitis media, infections of bones and joints, skin and soft tissues (incl.infected wounds and burns), urinary tract infections (complicated and uncomplicated), uncomplicated gonorrhea, bacterial meningitis, bacterial septicemia, Lyme disease. Prevention of postoperative infections. Infectious diseases in persons with weakened immunity.
    Contraindications:Hypersensitivity to ceftriaxone or to other group drugs, cephalosporins, penicillins, carbapenems; pregnancy (I trimester); Hyperbilirubinemia in newborns, newborns, which show intravenous administration of calcium-containing solutions; hypoalbuminemia, acidosis or decreased bilirubin binding.
    Carefully:Premature infants, renal and hepatic insufficiency, bleeding diseases of the digestive tract (ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs), breastfeeding, pregnancy (II-III trimester).
    Pregnancy and lactation:Contraindicated in the first trimester of pregnancy. In II-III trimesters, pregnancy is used only if the intended benefit to the mother exceeds the risk to the fetus. If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be solved, since ceftriaxone excreted in breast milk.
    Dosing and Administration:Intramuscularly (deep into the muscle), intravenously. Do not use calcium-containing solutions for dilution of the preparation! Ceftriaxone should not be mixed or administered simultaneously with calcium-containing solutions or drugs (even through separate infusomats).
    For adults and children over 12 years of age, the initial daily dose, depending on the type and severity of the infection, is 1-2 grams once a day or divided into 2 divided doses (every 12 hours), the total daily dose should not exceed 4 g.
    Lyme disease: adults and children - 50 mg / kg (but not more than-2 g) 1 time per day for 14 days.
    With uncomplicated gonorrhea - 250 mg IM once.
    For the prevention of postoperative complications - once 1 g for 30-60 minutes before the operation. In operations on the colon and rectum, additional administration of a drug from the 5-nitroimidazole group is recommended. The dose for newborns is 20-50 mg / kg / day.
    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 intake for 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) once a day or divided into 2 doses (every 12 hours). 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 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.
    With CRF (CC less than 10 ml / min) - the daily dose should not exceed 2 g; 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 should be at least 10 days.
    Children with skin and soft tissue infections - in a daily dose of 50-75 mg / kg once a day or 25-37.5 mg / kg every 12 hours, not more than 2 g / day. With average otitis media, once a month, 50 mg / kg, not more than 1 g. Patients with chronic renal insufficiency correction of the dose is required only with QC below 10 ml / min. In this case, the daily dose should not exceed 2 g.
    In patients with renal-hepatic insufficiency, the daily dose should not be exceed 2 g without determining the concentration of the drug in the blood plasma.
    Right-hander of preparation and introduction of solutions: only freshly prepared solutions should be used. Freshly prepared solutions of the drug are stable in for 6 hours at room temperature and for 24 hours at a temperature of 2-8 ° C.
    For intramuscular injection, 0.5 g of the drug is dissolved in 2 ml, and 1 g in 3 ml of 5% a solution of lidocaine or water for injection. The resulting solution can not be administered intravenously! When intramuscular introduction in one gluteal muscle is recommended to enter no more than 1 g of the drug.
    For intravenous administration, the drug is dissolved in sterile water for injection in ratio of 1:10 (0.5 g in 5 ml, 1 g in 10 ml).Enter intravenously slowly (during 2-4 min). For intravenous infusion, 2 g of the drug is dissolved in 40 ml of a solution free of calcium ions (0.9% sodium chloride solution, 5 % or 10% dextrose solution, 5% solution of levulose). Doses of 50 mg / kg or more should be administered intravenously in drip, for 30 minutes.
    The introduction of calcium-containing solutions or drugs is allowed no earlier than than 48 hours after the last injection / infusion of ceftriaxone.
    Side effects:

    Allergic reactions: urticaria, rash, itching, erythema, fever or chills, swelling, serum sickness, abdominal pain, allergic dermatitis, bronchospasm, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

    From the nervous system: dizziness and headache.

    From the digestive system: nausea, vomiting, taste disorders, flatulence, stomatitis, glossitis, diarrhea, dysbiosis, pseudomembranous colitis.

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

    From the side of the hemostasis system: hematuria, nasal bleeding, hemolytic anemia.

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

    Local reactions: with iv introduction - phlebitis, tenderness, compaction along the vein, in / m introduction - soreness, sensation of heat, tightness or condensation at the injection site.

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

    Other: increased sweating, "hot flashes" of blood.

    Undesirable reactions with a frequency of less than 0.1%: abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, cholelithiasis, bronchospasm, colitis, dyspepsia, epistaxis, bloating, "sluggish phenomenon" of the gallbladder, glucosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitations, convulsions, serum sickness.

    Overdose:
    Symptoms: with prolonged administration, there may be diarrheal disorders.
    Treatment: symptomatic therapy (there is no specific antidote), is not eliminated by dialysis.
    Interaction:
    Simultaneous administration of ceftriaxone and calcium-containing solutions or medicines may result in lung and kidney damage or death in newborns.
    Pharmaceutically incompatible with calcium-containing solutions (including Hartman and Ringer's solution), as well as with amsacrine, vancomycin, fluconazole, and aminoglycosides.
    Antagonism with chloramphenicol in vitro.
    Together with aminoglycosides, it has a synergistic effect on many gram-negative bacteria. It does not contain N-metiltiotetrazolnoy group, therefore the interaction with ethanol did not lead to the development disulfiramopodobnyh reactions inherent in some cephalosporins.
    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Nonsteroidal anti-inflammatory drugs and other inhibitors of platelet aggregation increase the likelihood of bleeding. With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of nephrotoxic effect increases.
    Special instructions:
    With simultaneous renal and hepatic insufficiency, patients who are on hemodialysis should regularly determine the concentration of the drug in the plasma.
    With long-term treatment, monitor blood hematologic parameters, indicators of the functional state of the liver and kidneys.
    In rare cases with ultrasound of the gallbladder, blackouts (precipitates of the calcium salt of ceftriaxone) are observed, 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 developed, possibly, as a result of obstruction of the biliary tract, are described. Most patients had risk factors for congestion of the biliary tract (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.
    Ceftriaxone does not contain an N-methylthio-tetrazole 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-Ca2 + 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 other age groups of patients, therefore ceftriaxone not be mixed with calcium-containing solutions (including those for parenteral nutrition) and administered simultaneously, including through separate accesses for infusions at different sites.
    Theoretically, based on the calculation of 5 T1 / 2 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 IM 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).
    Effect on the ability to drive transp. cf. and fur:
    For the treatment period, care must be taken when driving and potentially dangerous mechanisms due to possible dizziness, which can lead to a slowing of the speed of psychomotor reactions and a decrease in the ability to concentrate.

    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 0.5 g and 1.0 g.


    Packaging:
    0.5 g or 1.0 g in bottles with a capacity of 10 ml. Each vial with instructions for use is placed in a pack of cardboard.
    Packaging for hospitals: 20 or 40 bottles with an equal number of instructions but the application is placed in group boxes.

    Storage conditions:In a dry, protected from light 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 expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000937
    Date of registration:18.10.2011
    Date of cancellation:2016-10-18
    The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus
    Manufacturer: & nbsp
    BELMEDPREPARATY, RUP Republic of Belarus
    Information update date: & nbsp16.11.2015
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