Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbspPowder for the preparation of solution for intravenous and intramuscular injection.
    Composition:
    one bottle contains the active substance ceftriaxone sodium trisecihydrate (in terms of ceftriaxone) 250, 500 and 1000 mg.

    Description:
    Crystalline powder, from white to white with a yellowish hue of color, is slightly 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 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 pneu- moniae), Moraxella catarrhalis, (including penicillinase-producing strains), Morganella morganii, Neisseria gonorrhoeae (including strains that form penicillinase),

    Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Serratia spp. (at t.h. Serratia marcescens); separate strains Pseudomonas aeruginosa also sensitive;

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

    Possesses activity in vitro at respect majority strains the following microorganism­basics, although clinical value of this unknown: Citrobacter diversus, Citrobacter freundii, Providencia spp., Providencia rettgeri, Salmonella spp., (including Salmonella typhi), Shigella spp .; Streptococcus agalactiae, Bacteroides bivius, Bacteroides melaninogenicus. Methicillin-resistant Staphylococcus spp. resistant to cephalosporins, in t.h. to ceftriaxone, many strains Streptococcus spp. groups D and Enterococcus spp, in t.h. Enterococcus faecalis, also resistant to ceftriaxone.

    Pharmacokinetics:Bioavailability is 100%, the time required to reach the maximum concentration (TCmax) after intramuscular (IM) administration is 2 to 3 hours, after intravenous (IV) administration - at the end of the infusion. The maximum concentration of Cmax after IM in doses of 0.5 and 1 g is 38 and 76 μg / ml, respectively.Cmax at iv introduction in doses of 0.5,1 and 2 g - 82,151 and 257 mkg / ml, respectively. In adults, 2 to 24 hours after administration at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF) is many times greater than the minimal inhibitory concentration (MIC) for the most common meningitis pathogens. It penetrates well into CSF ​​with inflammation of the meninges. Connection with plasma proteins - 83 - 96%. The volume 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 introduction at a dose of 50 - 75 mg / kg in children with meningitis - 4.3 - 4.6 hours; in patients who are on hemodialysis (creatinine clearance 0-5 ml / min), -14.7 hours, with SC 5-15 ml / min -15.7 h, 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 neonates, about 70% of ceftriaxone is excreted through the kidneys. Hemodialysis is ineffective.
    Indications:
    Bacterial infections caused by sensitive microorganisms: infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract (GI tract), bile ducts, including cholangitis, gallbladder empyema), pelvic infection, lower respiratory tract infection (in t.ch.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. Prevention of postoperative infections.
    Infectious diseases in persons with weakened immunity.
    Contraindications:Hypersensitivity (including to other cephalosporins, penicillins, carbapenems), hyperbilirubinemia in newborns, newborns, which showed intravenous administration of solutions containing Ca2 +.
    Carefully:
    premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy, lactation.

    Pregnancy and lactation:
    When pregnancy is used only if the intended benefit for the mother exceeds the risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
    Dosing and Administration:
    Intravenous, intramuscular. Do not use Ca2 + -containing solutions to dilute the preparation!
    In adults, the initial daily dose, depending on the type and severity of the infection, is 1 to 2 g 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, an additional injection of the drug from the group 5-nitroimidazoles is recommended. The dose for newborns is 20 - 50 mg / kg / day.
    For the treatment of infections of the skin and soft tissues, the recommended daily intake in children is 50 to 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 - 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 intake in children is 50 to 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 body weight should be given as an IV infusion for 30 minutes.
    In chronic renal failure (CRF) (CK 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).
    In patients with renal-hepatic insufficiency, the daily dose should not exceed 2 g without determining the concentration of ceftriaxone in the blood plasma. 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.
    Rules for the preparation and administration of solutions: Use only freshly prepared solutions.For the / m introduction, 0.25 or 0.5 g of the drug is dissolved in 2 ml, and 1 g in 3.5 ml of a 1% solution of lidocaine. Recommend to enter no more than 1 g in one buttock.
    For intravenous injection, 0.25 or 0.5 g is dissolved in 5 ml, and 1 g in 10 ml of water for injection. Enter into / in slowly (2-4 minutes).
    For intravenous infusions, dissolve 2 g in 40 ml of a solution that does not contain Ca2 + (0.9% sodium chloride solution (NaCl), 5-10% dextrose solution, 5% fructose solution). Doses of 50 mg / kg or more should be administered intravenously in drip, for 30 minutes.
    Side effects:

    Allergic reactions: fever, eosinophilia, skin rash, hives, itching, erythema multiforme, edema, anaphylactic shock, serum sickness, chills.

    From the nervous system: headache, dizziness.

    From the digestive system: diarrhea, nausea, vomiting, taste disorder, flatulence, stomatitis, glossitis, diarrhea, pseudomembranous enterocolitis, abdominal pain, pancreatitis, "sluggish phenomenon" of the gallbladder.

    From the hematopoiesis: anemia (including hemolytic), leukopenia, lymphopenia, leukocytosis, neutropenia, thrombocytopenia, thrombocytosis, eosinophilia. basophilia, hematuria; nasal bleeding, hemolytic anemia.

    From the genitourinary system: candidiasis of the vagina, vaginitis, glucosuria, hematuria, 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 activity of "hepatic" transaminases and alkaline phosphatase, hyperbilirubinemia, hypercreatininemia, hematuria, glucosuria, increased urea concentration, the presence of sediment in the urine.

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

    Overdose:Treatment: symptomatic. Hemodialysis and peritoneal dialysis are not effective.
    Interaction:
    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone.
    Antagonism with chloramphenicol in vitro.
    Pharmaceutically incompatible with solutions containing Ca2 + (including 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.
    Special instructions:
    In combination with severe renal and hepatic insufficiency, as well as in patients on hemodialysis, the concentration of ceftriaxone in the 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 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); Moreover, the starting role of precipitate formation in the bile ducts 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 vitamin 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 Ca2 + -containing solutions for intravenous administration and other age groups of patients, therefore ceftriaxone should not be mixed with Ca2 + -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 T1 / 2 ceftriaxone, the interval between the administration of ceftriaxone 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 (in / 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).
    Given the likelihood of side effects from the nervous system, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection of 250, 500 and 1000 mg.
    Packaging:Powder for the preparation of a solution for intravenous and intramuscular injection of 250, 500 and 1000 mg in glass bottles (type I) with a capacity of 5 or 10 ml, sealed with stoppers of gray butyl rubber, rolled with aluminum caps with additional packaging in the form of a plastic cap; on 1,3, 5, 30 or 50 bottles together with the instruction on application in a cardboard pack.
    Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    2.5 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N015109 / 01
    Date of registration:01.09.2008
    The owner of the registration certificate:Jepak InternationalJepak International India
    Manufacturer: & nbsp
    Representation: & nbspJEPAK INTERNATIONALJEPAK INTERNATIONALRussia
    Information update date: & nbsp23.11.2015
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