Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:
    Each vial contains: sterile ceftriaxone sodium in terms of ceftriaxone anhydrous 1000 mg.

    Description:Crystalline powder from almost white to yellowish color.
    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 (penicillinase and cephalosporinase) of gram-positive and gram-negative 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 viridans;

    Gram-negative aerobes: Acinetobacter calcoaceticus, Borrelia burgdorferi, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae (including strains that form penicillinase), Haemophilus parainfluenzae, Klebsiella spp. (incl. Klebsiella pneumoniae), Moraxella catarrhalis, (including penicillin-producing strains), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase), Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (incl. Serratia marcescens); individual strains Pseudomonas aeruginosa are also sensitive.

    Anaerobes: Bacteroides fragilis, Clostridium spp. (Besides Clostridium difficile), Peptostreptococcus spp.

    Possesses activity in vitro at respect majority strains the following microorganisms, although clinical value of this unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp. (at t.h. 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 streptococci D and enterococci, incl. Enterococcus faecalis, also resistant to ceftriaxone.

    Pharmacokinetics:Bioavailability of the drug is 100%; the time to reach the maximum concentration (TCmax) after intramuscular injection - 2-3 hours, after intravenous injection - at the end of the injection. The maximum concentration (Cmax) after intramuscular injection of 1 g of the drug is about 76 μg / ml, with intravenous administration - about 151 μg / ml. In adults, 2-24 hours after administration at a dose of 50 mg / kg, the concentration incerebrospinal fluid (CSF) many times exceeds the minimum inhibitory concentration (MIC) 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 clearance - 0,32-0,73 l / h. The half-life (T1 / 2) after intramuscular injection is 5.8-8.7 hours after intravenous administration 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 h, 31-60 ml / min - 12.4 h. It is excreted unchanged - 33-67% by the kidneys; 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 microorganisms sensitive to ceftriaxone: infections of the abdominal cavity organs (peritonitis, inflammatory diseases of the gastrointestinal tract (GI tract), bile ducts, including cholangitis, empyema of the gallbladder), pelvic infection, lower respiratory tract infections including pneumonia, lung abscess, pleural empyema),acute otitis media, infections of bones and joints, skin and soft tissues (including infected wounds and burns), urinary tract infections (complicated and uncomplicated), uncomplicated gonorrhea, bacterial meningitis, bacterial septicemia, Lyme disease (borreliosis).
    Prevention of postoperative infections.
    Infectious diseases in persons with weakened immunity.
    Contraindications:Hypersensitivity to ceftriaxone (including other cephalosporins, penicillins, carbapenems), hyperbilirubinemia in newborns, newborns, who are shown intravenous administration of solutions containing calcium.
    Carefully:Premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy, the period of breastfeeding.
    Pregnancy and lactation:
    The use of the drug TOROcef® in pregnancy is possible only in those cases when the prospective benefit 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 intravenously and intramuscularly. Do not use calcium-containing solutions to dilute the preparation!

    Adults and children over 12 years of age: 1-2 g once a day (every 24 hours). In severe cases, the daily dose may be increased, but should not exceed 4 g.

    Dosing in special cases

    Lyme disease: adults and children over 12 years of age - 50 mg / kg once a day for

    14 days. The maximum daily dose is 2 g.

    Uncomplicated gonorrhea: 250 mg intramuscularly once.

    Prevention of postoperative infections: 1 g intravenously once for 30-60 minutes before the operation. In operations on the colon and rectum, simultaneous (but separate!) Administration of ceftriaxone and a drug from the group 5-nitroimidazoles.

    Patients with chronic renal insufficiency (CRF), dose adjustment is required only when creatinine clearance is less than 10 ml / min. In this case, the daily dose should not exceed 2 g. Patients on hemodialysis,no additional dose is required after a hemodialysis session, however, it is necessary to control the concentration of ceftriaxone in the plasma, since its excretion in such patients may be slowed down (dose adjustment may be required).

    In patients with renal and hepatic impairment the daily dose should not exceed 2 g without determining the concentration of ceftriaxone in the plasma.

    Dosage regimen for children

    Newborns (up to 2 weeks): 20 - 50 mg / kg of 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.

    Breast children and children from 15 days to 12 years: the maximum daily dose is 50-75 mg / kg of body weight once a day or divided into two doses. Children with a body weight of 50 kg and above are prescribed doses for adults.

    Doses of 50 mg / kg body weight or more should be administered intravenously drip for at least 30 minutes.

    The length of the course depends on the nature and severity of the disease.

    When 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 divided doses (every 12 hours). The duration of treatment is 7-14 days. For treatment skin and soft tissue infections recommended daily dose in children is 50-75 mg / kg once a day or divided into 2 doses (every 12 hours). The total daily intake for children should not exceed 2 g.

    In the treatment acute otitis media in children It is recommended a single intramuscular injection at a dose of 50 mg / kg (but not more than 1 g).

    In the treatment 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.

    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:

    For intramuscular injection: 1 g of the drug is dissolved in 3.6 ml of sterile water for injection and injected deeply into the gluteus muscle. It is recommended to inject no more than 1 g of the drug into one buttock. To reduce pain as a solvent, 1% lidocaine solution can be used. A solution of lidocaine can not be administered intravenously!

    For intravenous administration 1 g of the drug is dissolved in 9.6 ml of sterile water for injection.After preparation, each ml of the solution contains about 100 mg of ceftriaxone. The solution is injected slowly for 2-4 minutes.

    For intravenous infusion: dissolve 2 g of the drug in 40 ml of water for injection or one of the infusion solutions that do not contain calcium (0.9% sodium chloride solution, 5-10% dextrose solution, 5% solution of fructose). Doses of 50 mg / kg or more should be administered intravenously (iv) drip for 30 minutes. Use only freshly prepared solutions.

    Drug solutions should not be mixed or added to solutions containing other antimicrobial agents or other solvents, other than those listed, because of possible incompatibility.

    Side effects:

    The incidence of side effects is indicated according to the following definitions: very often more than 1/10, often more than 1/100 and less than 1/10, infrequently more than 1/1000 and less than 1/100, rarely more than 1/10000 and less than 1 / 1000, very rarely - less than 1/10000, including isolated cases.

    From the hematopoiesis: rarely - eosinophilia, leukopenia, granulocytopenia; very rarely, including isolated cases - thrombocytosis, thrombocytopenia, a slight increase in prothrombin time, individual cases of agranulocytosis (<500 cells / μl),most of them developed after 10 days of treatment and a cumulative dose of 20 g or more, anemia (including hemolytic), neutropenia, lymphopenia.

    From the digestive system: infrequently - stomatitis, glossitis, nausea, vomiting, abdominal pain, diarrhea or constipation, very rarely - a taste disorder, pseudomembranous colitis.

    From the nervous system: infrequently - headache, dizziness.

    From the genitourinary system: infrequently - oliguria, candidiasis of the vagina, vaginitis; rarely - the formation of calculi in the kidneys, mainly in children older than 3 years, who received either large daily doses of the drug (> 80 mg / kg / day), or cumulative doses of more than 10 g, as well as those who had additional risk factors (restriction of fluid intake, bed rest, etc.). The formation of calculi in the kidneys can be asymptomatic or manifest clinically, can lead to kidney failure and reversibly after discontinuation of therapy with the drug.

    Local Reactions: often - with intravenous injection - phlebitis, soreness, tightening along the vein (phlebitis can be avoided by injecting the drug slowly for 2-4 minutes); when administered intramuscularly, tenderness, sensation of heat, tightness, or compaction at the site of administration.

    Allergic reactions: often - hives, rash, itching; infrequently - chills or fever. Laboratory indicators: often - increased urea concentration, increased activity of "liver" transaminases; rarely - increased activity of alkaline phosphatase (AF), hyperbilirubinemia, hypercreatininaemia, the presence of sediment in the urine.

    Other: rarely - increased sweating, blood flushes, allergic pneumonitis, basophilia, cholelithiasis, bronchospasm, colitis, dyspepsia, epistaxis, pancreatitis, bloating, "sluggish phenomenon" of the gallbladder, glucosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, palpitations, convulsions, serum sickness, allergic dermatitis, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell syndrome, anaphylactic or anaphylactoid reactions.

    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:
    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Antagonism with chloramphenicol in vitro.
    It does not contain N-metiltiotetrazolnoy group, therefore the interaction with ethanol did not lead to the development disulfiramopodobnyh reactions inherent in some cephalosporins.
    Pharmaceutically incompatible with solutions containing calcium (including Hartman and Ringer's solution), as well as with amsacrine, vancomycin, fluconazole, and aminoglycosides.

    Special instructions:
    With simultaneous severe renal and hepatic insufficiency, as well as in patients on hemodialysis, the concentration of the drug in plasma should be regularly determined.
    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 the drug is used, rare cases of pancreatitis have been described, possibly due to obstruction of the biliary tract.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-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 in other 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 5 half-lives of ceftriaxone interval between administration of ceftriaxone and calcium solutions should be at least 48 hours. The data on possible interaction of ceftriaxone with oral calcium-containing agents, and ceftriaxone for the / m of a calcium-containing preparations (in / 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).
    As with the use of other cephalosporins, even with careful collection of anamnesis, one can not exclude the possibility of developing an anaphylactic shock.
    As with other antibacterial drugs, the use of ceftriaxone may lead to the development of superinfection.
    Use caution when using ceftriaxone in people who have concomitant bowel disease, especially colitis.If diarrhea occurs during treatment with ceftriaxone, caution should be exercised because of the possible development of pseudomembranous colitis. If a diagnosis of antibiotic-associated diarrhea or pseudomembranous colitis is established, ceftriaxone should be discontinued and appropriate treatment should be prescribed.

    Effect on the ability to drive transp. cf. and fur:During the period of application of the drug, care must be taken when driving a car and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.
    Packaging:
    For 1000 mg in a transparent glass bottle with a capacity of 15 ml, corked with a rubber stopper with aluminum rolling and a plastic cap. 1 bottle is placed in a cardboard box with instructions for use. Or 1 The bottle is placed in a cardboard box with instructions for use. 50 cardboard packs are placed in a cardboard box.
    Storage conditions:Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.
    Shelf life:
    2 of the year.
    Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N012503 / 01
    Date of registration:03.02.2012
    The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India
    Information update date: & nbsp15.11.2015
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