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

    Composition:
    Ceftriaxone 0.5 g

    Ceftriaxone sodium in terms of ceftriaxone 0.5 g

    Ceftriaxone 1.0 g

    Ceftriaxone sodium in terms of ceftriaxone 1.0 g
    Description:Almost white or yellowish crystalline powder.
    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. Stable against βlactamases produced by most gram-positive and gram-negative microorganisms.

    It is active against gram-positive aerobic microorganisms - Staphylococcus aureus (including those producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. groups viridans), Gram-negative aerobic microorganisms - Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Borrelia burgdorferi, Acinetobacter calcoaceticus, Haemophilus Streptococcus pneumoniae, Streptococcus pyogenes, Viridans group Streptococci), Gram-negative aerobic microorganisms - Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Borrelia burgdorferi, Acinetobacter calcoaceticus, Haemophilus influenzae (including ampicillin-resistant and beta-lactamase-producing strains), Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis (including beta-lactamase-producing strains), Morganella morganii, Neisseria meningitidis, Neisseria gonorrhoeae (including penicillinase-forming strains), Proteus mirabilis, Proteus vulgaris, Serratia marcescens, many strains Pseudomonas aeruginosa, anaerobic microorganisms - Bacteroides fragilis, Clostridium spp. (most strains Clostridium difficile resistant), Peptostreptococcus spp., Peptococcus spp.

    Has activity in vitro for most strains of the following microorganisms, however, the safety and efficacy of ceftriaxone in the treatment of diseases caused by these microorganisms are not clinically established: aerobic gram-negative microorganisms - Citrobacter diversus, Citrobacter freundii, Providencia spp. (including Providencia rettgeri), Salmonella spp. (including Salmonella typhi), Shigella spp., aerobic Gram-positive microorganisms - Streptococcus agalactiae, anaerobic microorganisms - Prevotella (Bacteroides) bivius, Porphyromonas (Bacteroides) melaninogenicus.

    The drug is resistant to methicillin-resistant strains Staphylococcus spp., many strains of group streptococci D and strains Enterococcus spp. (Enterococcus faecalis), Clostridium difficile, many strains Bacteroides spp. (producing lactamases).

    Methicillin-resistant staphylococci are stable and to cephalosporins, at t.h. to ceftriaxone, and enterococci, at t.h. Enterococcus faecalis, also are stable to ceftriaxone.

    Pharmacokinetics:
    Suction
    After intramuscular injection ceftriaxone quickly and completely absorbed into the systemic circulation. It penetrates well into the tissues and body fluids: respiratory tract, bones, joints, urinary tract, skin, subcutaneous fat and abdominal cavity organs. When inflammation of the meningeal membranes well penetrates into the cerebrospinal fluid. Bioavailability of ceftriaxone with intramuscular injection is 100%.
    Distribution

    With intramuscular introduction of ceftriaxone in a dose of 0.5 g and 1.0 g of CmOh in blood plasma is 38 μg / ml and 76 μg / ml, respectively, with intravenous administration at a dose of 0.5 g, 1.0 g and 2.0 g - 82 μg / ml, 151 μg / ml and 257 μg / ml, respectively . In adults, 2-24 hours after the administration of the drug at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid is many times greater than the minimum inhibitory concentrations for the most common pathogens of meningitis.

    The equilibrium state is established within 4 days of the drug administration.

    Reversible binding to plasma proteins (albumins) is 83-95%.

    Volume of distribution (Vd) is 5,78-13,5 l (0,12-0,14 l / kg), in children - 0,3 l / kg.

    Penetrates through the placental barrier in small quantities.

    Excretion

    The half-life is 6-9 hours, which allows the drug to be applied once or twice a day.

    The plasma clearance is 0.58-1.45 l / h, the renal clearance is 0.32-0.73 l / h.

    It is excreted unchanged in 33-67% of the kidneys; 40-50% is excreted with bile into the intestine, where it is biotransformed into an inactive metabolite. About 50% is output within 48 hours.

    Pharmacokinetics in special clinical cases

    In newborn infants, 70% of the drug is excreted by the kidneys.

    In newborns and in elderly people (over the age of 75 years), as well as in patients with impaired renal and hepatic function, the half-life increases significantly.

    In patients on hemodialysis with CC (creatinine clearance) 0-5 ml / min, the half-life is 14.7 hours; with SC 5-15 ml / min - 15.7 hours; with SC 16-30 ml / min - 11.4 hours; with a CK of 31-60 ml / min - 12.4 hours.

    In children with meningitis, the half-life after intravenous administration at a dose of 50-75 mg / kg is 4.3-4.6 hours.

    Ceftriaxone is not excreted by hemodialysis.

    Indications:Infectious and inflammatory diseases caused by microorganisms sensitive to ceftriaxone: infections of the abdominal cavity, including peritonitis, inflammatory diseases of the digestive tract, bile ducts (including cholangitis, empyema of the gallbladder), infections of the upper and lower respiratory tract and ENT organs including acute and chronic bronchitis, pneumonia, lung abscess, pleural empyema), epiglottitis, infections of bones and joints, skin and soft tissues, infections of the genitourinary system (including pyelitis, acute and chronic pyelonephritis, cystitis, prostatitis, epididymitis), infected wounds and burns, infections of the maxillofacial region, uncomplicated gonorrhea, including those caused by microorganisms that release penicillinase, sepsis and bacterial septicemia, bacterial meningitis and endocarditis, chancroid and syphilis, Lyme disease (tick-borne borreliosis), typhoid fever, salmonellosis and salmonella, infections in immunocompromised patients, prevention and treatment of postoperative infectious complications.
    Contraindications:Hypersensitivity to ceftriaxone and other cephalosporins, penicillins, carbapenems; first trimester of pregnancy, lactation.
    Carefully:Premature infants, renal and / or hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, second and third trimester of pregnancy.
    Pregnancy and lactation:
    The use of the drug during pregnancy is possible only in those cases when the intended use 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, breastfeeding should be stopped (excreted in breast milk).
    Dosing and Administration:

    The drug is administered intramuscularly or intravenously (either struino or drip). Adults and children over the age of 12 years appoint 1-2 g once a day. The maximum daily dose is not more than 4.0 g.

    Newborns under the age of 14 days appoint 20-50 mg / kg / day. The maximum daily dose of 50 mg / kg.

    Infant and young children (from 15 days to 12 years) appoint 20-80 mg / kg / body weight once a day.

    Children with body weight > 50 kg appoint doses intended for adults.

    Doses of 50 mg / kg or more for intravenous administration should be administered drip for at least 30 minutes.

    Patients of senile age should be administered usual doses intended for adults, without adjusting for age.

    The duration of the course is usually 4-14 days; with complicated infections, a longer duration of administration may be required. The drug should be continued for 2-3 days after the disappearance of symptoms and signs of infection.

    When bacterial meningitis in infants and young children, the dose is 100 mg / kg 1 time / day. The maximum daily dose is 4.0 g.

    The duration of therapy depends on the type of pathogen and can range from 4 days with meningitis caused by Neisseria meningitidis, up to 10-14 days with meningitis caused by sensitive strains Enterobacteriaceae.

    When Lyme disease: adults and children over 12 years of age are prescribed 50 mg / kg once a day, the maximum daily dose is 2.0 g. The duration of treatment is 14 days.

    When acute uncomplicated gonorrhea the drug is administered in / m once in a dose of 250 mg.

    With the aim of prevention of postoperative complications - once 1.0 g for 30-60 minutes before the operation.

    When operations on the colon and rectum - effectively simultaneous (but separate) administration of Ceftriaxone and one of the 5-nitroimidazoles group.

    In patients with impaired renal function, there is no need for dose adjustment if the liver function remains normal. In cases of preterminal renal failure of a severe degree with KK less than 10 ml / min, the daily dose of the drug should not exceed 2.0 g.

    In patients with impaired liver function, there is no need for dose adjustment if the kidney function remains normal.

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

    Patients who are on hemodialysis, additional administration of the drug after dialysis is not required. The rate of excretion of ceftriaxone in such patients may be reduced, so the concentration of the drug in the blood plasma should be monitored in order to timely dose correction.

    Rules for the preparation and administration of solutions

    Use only freshly prepared solutions.

    For intramuscular injection 0.25 g or 0.5 g of the drug are dissolved in 2 ml and 1.0 g in 3.5 ml of water for injection. To reduce pain with I / m injections, the drug should be administered with a 1% solution of lidocaine.Enter deep into the gluteus muscle or into the muscle of the thigh. Do not administer more than 1.0 g per muscle. Lidocaine chloride solution can not be administered iv.

    For intravenous administration 0.25 g or 0.5 g is dissolved in 5 ml, and 1.0 g of the preparation in 10 ml of water for injection. The solution is injected for 2-4 minutes.

    For intravenous infusion 2.0 g of the drug is dissolved in 40 ml of water for injection or one of the solutions that do not contain calcium (0.9% sodium chloride solution, 0.45% sodium chloride solution + 2.5% dextrose solution, 5% solution dextrose, 10% dextrose solution, 6% dextran solution in 5% dextrose solution, 6-10% solution of hydroxyethylated starch). The solution is introduced for 30 minutes.

    Side effects:

    Allergic reactions: rash, itching, fever, chills.

    From the nervous system: headache, dizziness.

    On the part of the digestive system: diarrhea, nausea, vomiting, taste disorder, flatulence, pseudomembranous colitis.

    On the part of the hematopoiesis system: with prolonged use in high doses, changes in the pattern of peripheral blood (anemia, including hemolytic), eosinophilia, thrombocytosis, leukopenia, neutropenia, lymphopenia, thrombocytopenia) are possible.

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

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

    Other: increased sweating, flushes of blood to the face.

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

    Other: stomatitis, glossitis, oliguria, rash, allergic dermatitis, urticaria, edema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome.

    Overdose:
    Currently, cases of drug overdose Ceftriaxone not reported. Symptoms of an overdose are an increase in the side effects of the drug-cm. higher.
    Treatment: symptomatic. There is no specific antidote. Hemodialysis and peritoneal dialysis are not effective.

    Interaction:

    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone. Ceftriaxone and aminoglycosides possess synergism with respect to many Gram-negative bacteria (incl. Pseudomonas aeruginosa), drugs should be administered separately in the recommended doses.

    Ceftriaxone, suppressing the intestinal flora, interferes with the synthesis of vitamin K. With simultaneous administration with drugs that reduce platelet aggregation (NSAIDs, salicylates, sulfinpyrazone), the risk of bleeding increases.

    With a simultaneous appointment with anticoagulants, there is an increased anticoagulant effect.

    At simultaneous appointment with "loop" diuretics and other nephrotoxic drugs, the risk of nephrotoxic action increases. Does not interact with probenecid.

    Pharmaceutical interaction

    Ceftriaxone should not be mixed with solutions containing calcium (including Hartman and Ringer's solution).

    Pharmaceutically it is not compatible with solutions containing other antibiotics, incl.with amsacrine, vancomycin, fluconazole and aminoglycosides.

    Special instructions:
    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, blackouts (precipitates of the calcium salt of ceftriaxone) are observed, which disappear after the drug is discontinued.
    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 Ca2 + -containing solutions for intravenous administration and in 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.
    Data on the possible interaction of ceftriaxone with oral calcium-containing preparations, as well as ceftriaxone for intramuscular 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).
    Despite the detailed history of the anamnesis, it is impossible to exclude the possibility of developing an anaphylactic shock, which requires immediate therapy: first enter intravenously epinephrine, then - glucocorticosteroids.
    In vitro studies have shown that, like other cephalosporins, 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 great caution.

    Effect on the ability to drive transp. cf. and fur:No data available.
    Form release / dosage:
    Powder for solution for intravenous and intramuscular injection 0.5 g, 1.0 g.


    Packaging:
    By 0.5 g or 1.0 g of ceftriaxone in a vial of colorless glass. The bottle is sealed with a sterile rubber stopper and crimped with an aluminum cap with a plastic lid. For 1 bottle together with instructions for medical use in a cardboard bundle.
    Packing for hospitals: 25 vials of 0.5 g or 1.0 g together with instructions for medical use in a cardboard box. Vials are separated between the rows by cardboard pads.
    Storage conditions:
    In a dry, the dark 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 expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002002
    Date of registration:18.02.2013
    Date of cancellation:2018-02-18
    The owner of the registration certificate:RAFARMA, CJSC RAFARMA, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp14.11.2015
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