Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsp
    powder for solution for intravenous and intramuscular administration

    Composition:In 1 vial contains - ceftriaxone sodium (in terms of ceftriaxone 1000 mg).
    Description:Powder from white to white with a yellowish hue of color.
    Pharmacotherapeutic group:Antibiotic-cephalosporin
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:
    Azaran is a cephalosporin antibiotic of the third generation of a broad spectrum of action for parenteral administration. Has a bactericidal effect due to inhibition of bacterial cell wall synthesis. Acetylates membrane-bound transpeptidases, thus violating the cross-linking of peptidoglycans necessary to ensure the strength and rigidity of the cell wall.
    Resistant to the action of beta-lactamases produced by most gram-positive and gram-negative bacteria.
    It is active against gram-positive aerobes - Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis; Gram-negative aerobes - Acinetobacter lwoffii, Acinetobacter anitratus, Aeromonas hydrophila, Alcaligenes faecalis, Alcaligenes odorans, Citrobacter spp., Enterobacter spp. (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including strains forming penicillinase), Haemophilus parainfluenzae, Klebssiella spp. (including Klebssiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (including strains forming penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (including Salmonella typhi), Serratia spp. (including Serratia marcescens), Shigella spp., Vibrio spp. (including Vibrio cholerae), Yersinia spp. (including Yersinia enterocolitica), Pseudomonas aeruginosa; anaerobes - Bacteroides spp. (including some strains of Bacteroides fragilis), Clostridium spp. (except Clostridium difficile), Fusobacterium spp. (except Fusobacterium mortiferum and Fusobacterium varium), Peptococcus spp., Peptostreptococcus spp.
    To ceftriaxone resistant strains Staphylococcus spp., Resistant to methicillin, strains Enterococcus spp. (Enterococcus faecalis), Clostridium difficile, many strains of Bacteroides spp., Producing beta-lactamases.
    Pharmacokinetics:After intramuscular (IM) injection quickly and completely absorbed. Bioavailability is 100%. It penetrates well into tissues and body fluids: in the respiratory tract, bones, joints, urinary tract, skin, subcutaneous tissue and abdominal cavity organs. Stable concentration of the drug in the blood is reached within 4 days. The maximum concentration (C max) after intravenous administration occurs after 2-3 hours, after intravenous (iv) Introduction - at the end of the infusion. Cmax after the / m introduction 0.5 g, 1 g - 38 mcg / ml, 76 mcg / ml, respectively.With IV 500 mg, 1 g, 2 g - 82 μg / ml, 151 μg / ml, 25.7 μg / ml, respectively. In adults, 2-24 hours after the administration of 50 mg / kg, the concentration in the cerebrospinal fluid (CSF) is many times greater than the minimum inhibitory concentration for the most common meningitis pathogens. It penetrates well into CSF ​​with inflammation of meningeal membranes. Reversibly binds to albumin plasma (83-95%). The drug passes through the placenta in small quantities.
    The half-life (T1 / 2) is 6-9 hours, which allows the drug to be used once a day. T1 / 2 after IV in the dose of 50-75 mg / kg in children with meningitis - 4.3-4.6 hours; in patients who are on hemodialysis (creatinine clearance of CK - 0-5 ml / min) - 14.7 hours, with KK - 5-15 ml / min - 15.7 h, with KK - 16-30 ml / min - 11.4 h, with QC - 31-60 ml / min - 12.4 hours. The distribution volume is 0.12-0.14 l / kg (5.78-13.5 l), in children 0.3 l / kg., The plasma clearance is 0.58-1.45 l / h, the renal clearance is 0.32-0.73 l / h. T1 / 2 is significantly longer in people older than 75 years, newborns and in patients with impaired renal and hepatic function. It is excreted within 48 hours by kidneys of 50-60% in unchanged form and with bile - 40-50% in the intestine, where conversion into an inactive metabolite occurs. About 70% of the drug is excreted through the kidneys in newborn infants. Hemodialysis is not effective.
    Indications:Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation: infections of the upper and lower respiratory tract (including pneumonia, lung abscess, pleural empyema); infections of the skin and soft tissues; infection of bones and joints; urinary tract infections (including pyelonephritis); infection of the abdominal cavity (peritonitis, gastrointestinal tract infections (shigellosis, salmonellosis), bile ducts, including cholangitis, empyema of the gallbladder); infectious inflammatory diseases of the pelvic organs; prevention and treatment of infections in surgical interventions; bacterial meningitis and endocarditis; sepsis; acute uncomplicated gonorrhea; Lyme disease.
    Contraindications:Hypersensitivity to ceftriaxone and other cephalosporins, penicillins, carbapenems.
    Carefully:
    If the liver and / or kidney function is impaired; in premature and newborn children with hyperbilirubinemia; with nonspecific ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs.

    Pregnancy and lactation:The use of the drug during pregnancy is possible only in cases where the intended use for the mother exceeds the potential risk to the fetus.If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be solved.
    Dosing and Administration:

    The drug Azaran should be used intramuscularly or intravenously struino or drip!

    Standard dosing.

    Adults and children over 12 years of age: the usual dose is 1-2 grams per day (every 24 hours). In severe cases, the maximum daily intake for adults is 4 g.

    Newborns under the age of 14 days - 20-50 mg / kg of body weight once a day. The maximum daily dose should not exceed 50 mg / kg of body weight.

    When determining the dose, no distinction is made between full and premature children.

    Children aged 15 days to 12 years - 20-80 mg / kg body weight once a day.

    Children with a body weight above 50 kg are prescribed doses for adults.

    Intravenous doses equal to or greater than 50 mg / kg body weight should be administered as infusions for at least 30 minutes.

    The duration of the course usually does not exceed 10 days. The introduction of the drug is recommended to continue for another 2-3 days after the normalization of body temperature and the disappearance of symptoms.

    Dosing in special cases.

    For the prevention of postoperative complications - once, 1-2 g (depending on the degree of infectious risk) for 30-90 minutes before the operation. In operations on the colon and rectum, additional administration (but separate) of the drug from the 5-nitroimidazoles group is recommended.

    In acute, uncomplicated gonorrhea - IM once, 250 mg.

    Borreliosis Lyme - 50 mg / kg of body weight (the highest daily dose is 2 g) for adults and children, once a day for 14 days.

    In bacterial meningitis in infants and young children - 100 mg / kg body weight (but not more than 4 g) 1 time per day. The duration of treatment depends on the pathogen and can range from 4 days for Neisseria meningitidis up to 10-14 days for sensitive strains Enterobacteriaceae.

    Patients with impaired renal function there is no need to reduce the dose, if the function liver remains normal. The daily dose of Azaran should not exceed 2 g, only in cases of preterminal renal failure (creatinine clearance less than 10 ml / min).

    In patients with impaired liver function there is no need to reduce the dose, if the function kidneys remains normal.

    When combined with severe renal and hepatic insufficiency should regularly determine the concentration of ceftriaxone in the plasma and, if necessary, adjust its dose.

    Patients on dialysis additional introduction of the drug after dialysis is not required, because ceftriaxone not removed during hemodialysis. However, the concentration of ceftriaxone in the serum should be monitored for possible dose adjustment, since the rate of excretion in these patients may be reduced.

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

    Preparation of solution for intramuscular injection:

    - 1000 mg of the drug are dissolved in 3.6 ml of water for injection, 1 ml of the resulting solution contains about 250 mg in terms of ceftriaxone. If necessary, a more dilute solution can be used.

    - 1000 mg of the drug are dissolved in 3.5 ml of a 1% solution of lidocaine.

    The resulting solution is injected deep into a relatively large muscle (buttock or thigh muscle). Do not administer more than 1000 mg of the drug in one muscle.

    Solutions containing lidocaine can not be administered intravenously!

    Preparation of solution for intravenous administration:

    1000 mg of the drug are dissolved in 9.6 ml of water for injection, 1 ml of the resulting solution contains about 100 mg in terms of ceftriaxone. The solution is injected slowly for 2-4 minutes.

    Preparation of a solution for intravenous infusion:

    2 g of the drug is dissolved in 40 ml of water for injection or one of the infusion solutions that do not contain calcium (0.9% sodium chloride solution, 0.45% sodium chloride solution + 2.5% dextrose solution, 5% or 10% % dextrose solution, 6% dextran solution in 5% dextrose solution, 6-10% solution of hydroxyethylated starch). The duration of the infusion should be at least 30 minutes.

    The prepared solution should be stored in a dark place at room temperature (25 ° C) and

    use for 6 hours or in a dark place at temperature from 2 to 8 ° C and

    use within 24 hours.

    Side effects:

    Allergic reactions: urticaria, chills, or fever, itching, rarely - bronchospasm, eosinophilia, erythema exudative multiforme (including Stevens-Johnson syndrome), anaphylactic shock, serum sickness.

    From the nervous system: headache, dizziness.

    From the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glycosuria, cylindruria, hematuria), oliguria, anuria.

    From the digestive system: nausea, vomiting, taste disorder, flatulence, diarrhea or constipation, abdominal pain, stomatitis, glossitis, pseudomembranous enterocolitis, impaired liver function (increased activity of "liver" transaminases, less often - alkaline phosphatase or bilirubin, cholestatic jaundice), pseudo-cholelithiasis of the gallbladder ("sludge''-syndrome), a dysbacteriosis.

    From the hematopoiesis: anemia, leukopenia, leukocytosis, lymphopenia, neutropenia, granulocytopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in the concentration of plasma clotting factors (II, VII, IX, X), prolongation of prothrombin time.

    Local reactions: with iv introduction - phlebitis, pain along the vein; in / m introduction -pain in the injection site and infiltration.

    Other: nose bleeding, candidomycosis and other superinfections.

    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:
    Ceftriaxone and aminoglycosides have a synergistic effect on many gram-negative bacteria (including Pseudomonas aeruginosa),both drugs must be administered separately in the recommended doses for them. Incompatible with ethanol (see section Special instructions)
    Ceftriaxone, suppressing the intestinal flora, interferes with the synthesis of vitamin K. With simultaneous administration with drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs, salicylates, sulfinpyrazone), the risk of bleeding increases.
    With a simultaneous appointment with anticoagulants, the effect of the latter is noted. With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of nephrotoxic action increases.
    Pharmaceutically incompatible with solutions containing other antibiotics (incl. vancomycin and aminoglycosides), and solutions containing fluconazole. Ceftriaxone Do not mix with solutions containing calcium (for example, Ringer's solution).
    Special instructions:
    Use only in inpatient medical institutions!
    With simultaneous severe renal and hepatic insufficiency, in patients who are on hemodialysis, the concentration of the drug 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, with ultrasound of the gallbladder, darkening is observed, which disappear after the cessation of treatment (even if this phenomenon is accompanied by pain in the right hypochondrium, recommend continued antibiotic prescription and symptomatic treatment).
    During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (red face, spasm in the stomach and in the stomach, nausea, vomiting, headache, lowering blood pressure, tachycardia, dyspnea).
    Despite the detailed history, which is the rule for other cephalosporin antibiotics, one can not exclude the possibility of developing an anaphylactic shock that requires immediate therapy - first intravenously injected epinephrine, then glucocorticosteroids.
    In vitro studies have shown that, like other cephalosporin antibiotics, ceftriaxone is able to displace bilirubin, associated with serum albumin. Therefore, in newborns with hyperbilirubinemia and, especially, in preterm infants, the use of ceftriaxone requires even greater caution.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular administration of 1000 mg.

    Packaging:
    For 1000 mg of powder in a bottle of colorless glass, sealed with a combined lid of rubber, metal and plastic with the control of the first autopsy. 1.10 or 50 bottles with instructions for use in a pack of cardboard.
    Storage conditions:
    List B.

    Store in a dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children!
    Shelf life:
    3 years.

    Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N015049 / 01
    Date of registration:31.10.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia
    Manufacturer: & nbsp
    Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia
    Information update date: & nbsp04.02.2017
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