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

    Composition:
    Ceftriaxone sodium in terms of active substance - 1.0 g (1 g of ceftriaxone corresponds to 1.079 g of ceftriaxone sodium).
    Description:Almost white or yellowish crystalline powder.
    Pharmacotherapeutic group:Antibiotic-cephalosporin.
    ATX: & nbsp

    J.01.D.D.04   Ceftriaxone

    Pharmacodynamics:

    Ceftriaxone is a third generation cephalosporin antibiotic for parenteral use, has a bactericidal effect, inhibits the synthesis of the cell membrane, in vitro suppresses the growth of many gram-positive and gram-negative microorganisms. Ceftriaxone is resistant to beta-lactamase enzymes (both penicillinase and cephalosporinase, produced by the majority of Gram-positive and Gram-negative bacteria).Effective against the following microorganisms:

    Gram-positive

    Staphylococcus aureus (including strains producing penicillinase), Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyo­genes, Streptococcus viridans.

    Note: Staphylococcus spp., resistant to methicillin, is resistant to cephalosporins, including ceftriaxone. Most strains of enterococci (for example, Streptococcus faecalis) also resistant to ceftriaxone.

    Gram-negative

    Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (some strains are stable), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp. (at Tom number of Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa (some strains are stable), Salmonella spp. (at Tom number of Salmonella typhi), Serratia spp. (at Tom number of Serratia marcescens), Shigella spp., Vibrio spp. (at Tom number of Vibrio cholerae), Yersinia spp. (at Tom number of Yersinia enterocolitica)

    Note: many strains of these microorganisms, which in the presence of other antibiotics, for example, penicillins, first-generation cephalosporins and aminoglycosides, are multiplying steadily, are sensitive to ceftriaxone. Treponema pallidum is sensitive to ceftriaxone as in vitro, and in experiments on animals. According to clinical data, in the primary and secondary syphilis, a good efficacy of ceftriaxone is noted.

    Anaerobic pathogens

    Bacteroides spp. (including some strains Bacteroides fragilis), Clostridium spp. (at Tom number of Clostridium difficile), Fusobacterium spp. (Besides Fusobacterium mostiferum, Fusobacterium varium), Peptococcus spp., Pepto- streptococcus spp.

    Note: some strains of many Bacteroides spp. (eg, Bacteroides fragilis), Developing beta-lactamase, resistant to ceftriaxone. To determine the sensitivity of microorganisms, discs containing ceftriaxone, since it is shown that in vitro to classical cephalosporins, certain strains of pathogens can be stable.

    Pharmacokinetics:

    With parenteral administration ceftriaxone well penetrates into tissues and body fluids.

    Bioavailability is 100%, the time to reach the maximum concentration in the blood serum (Tcmah) after intramuscular injection - 2-3 hours, after intravenous administration - at the end of infusion. The maximum concentration (Cmax) after intramuscular injection in doses of 0.5 and 1 g - 38 and 76 μg / ml, respectively. FROMmah at intravenous in doses of 0,5; 1 and 2 g - 82,151 and 257 μg / ml, respectively. Well penetrates into the cerebrospinal fluid 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 - 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 who are on hemodialysis (KK 0-5 ml / min - 14.7 h, KK 5-15 ml / min - 15.7 h), 16-30 ml / min - 11.4 h, 31-60 ml / min - 12.4 hours.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.

    Penetration into the cerebrospinal fluid: in newborns and in children with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis, an average of 17% of the concentration of the drug in the blood serum diffuses into the cerebrospinal fluid, which is approximately 4 times greater than with aseptic meningitis. 24 hours after intravenous administration of ceftriaxone in a dose of 50-100 mg / kg body mass concentration in the cerebrospinal fluid exceeds 1.4 mg / l. In adults with meningitis, 2 to 25 hours after the administration of ceftriaxone at a dose of 50 mg / kg body weight, the concentration of ceftriaxone was many times greater than the minimum oppressive dose that is necessary to suppress the pathogens most commonly causing meningitis.

    Indications:Infectious-inflammatory diseases caused by susceptible to ceftriaxone pathogens: sepsis, meningitis, infections of the abdominal cavity (peritonitis, gastrointestinal tract infections,bile-excreting tracts); disseminated borreliosis of Lyme, infections of bones, joints, soft tissues, skin, infection in patients with low immunity; infection of the kidneys and urinary tract, respiratory tract infections (including pneumonia), as well as infections of the LOP-organs, urogenital infections (including gonorrhea). Prevention of infections in the postoperative period.
    Contraindications:Hypersensitivity to cephalosporins, penicillins and carbapenems. The first trimester of pregnancy.
    Carefully:
    Hyperbilirubinemia in newborns, premature infants, renal / hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy 2-3 trimester, lactation.

    Pregnancy and lactation:
    In pregnant women in the 2nd - 3rd trimester, the drug should be used only if the intended benefit to the mother exceeds the potential risk to the fetus.
    When appointing during lactation, it is necessary to cancel breastfeeding.

    Dosing and Administration:

    The drug is used intramuscularly and intravenously.

    For adults and for children over 12 years old

    The average daily dose is 1-2 g of ceftriaxone once a day or 0.5-1 g every 12 hours.

    In severe cases or in cases of infections caused by moderately sensitive pathogens, the daily dose may be increased to 4 g.

    For newborns

    For newborns (up to 2 weeks of age): 20-50 mg / kg of body weight per day (a dose of 50 mg / kg of body weight is not recommended because of the immature enzyme system of newborns).

    When determining the dose, there is no need to distinguish between full and premature babies.

    For infants from 15 days and children under 12 years of age

    The daily dose is 20-80 mg / kg of body weight once a day.

    Children with a body weight of 50 kg and above should adhere to the dosage for adults. A dose of more than 50 mg / kg body weight should be given as an intravenous infusion, for at least 30 minutes.

    Duration of therapy

    Depends on the nature of the severity of the disease. As always with antibiotic therapy, the drug should be continued for at least 48 to 72 hours after the normalization of body temperature and confirmation of eradication of the pathogen.

    Meningitis

    In bacterial meningitis in newborns and in children, the initial dose is 100 mg / kg of body weight once a day (maximum 4 g).Once it was possible to isolate the pathogenic microorganism and determine its sensitivity, the dose should be reduced accordingly. The best results were achieved with the following periods of therapy:

    Causative agent

    Duration of therapy

    Neisseria meningitidis

    4 days

    Haemophilus influenzae

    6 days

    Streptococcus pneumoniae

    7 days

    Sensitive Enterobacteriacease

    10-14 days

    Gonorrhea

    For the treatment of gonorrhea caused by both generative and non-penicillinase-resistant strains, the recommended dose is 250 mg once intramuscularly.

    Borreliosis Lyme

    50 mg / kg (the highest daily dose of 2 g) for adults and children over 12 years, 1 time per day for 14 days.

    Prevention in the pre- and postoperative period

    Depending on the danger of infection, one-time administration of ceftriaxone in a dose of 1-2 g is recommended 30-90 minutes prior to surgery. For operations on the colon and rectum, additional administration of the drug from the 5-nitroimidazoles group is recommended.

    Lack of kidney and liver function

    In patients with impaired renal function, under the condition of normal liver function, a dose of ceftriaxone is not necessary to reduce. Only if the kidneys are deficient in the preterminal stage (creatinine clearance below 10 ml / min) it is necessary that the daily dose of ceftriaxone does not exceed 2 g.

    In patients with impaired liver function, if the function of the kidneys is maintained, the dose of ceftriaxone should not be reduced.

    In cases of simultaneous presence of severe pathology of the liver and kidneys, the concentration of ceftriaxone in serum should be monitored regularly. In patients undergoing hemodialysis, the dose of the drug after this procedure is not necessary to change. It should, however, monitor the concentration of ceftriaxone in the serum for the possibility of dose adjustment. Since the rate of excretion in these patients may be reduced.

    Intramuscular injection

    For intramuscular injection, 1 g of the drug is dissolved in 3.5 ml of a 1% solution of lidocaine and injected deep into the relatively large muscle (gluteal), it is recommended to inject no more than 1 g of the drug into one muscle. Trial aspiration avoids overdose. A solution of lidocaine can never be administered intravenously!

    Intravenous administration

    For intravenous injection, 1 g of the drug is dissolved in 10 ml of water for injection, administered intravenously slowly for 2-4 minutes.

    Intravenous infusion

    For intravenous infusion 2 g of the powder should be dissolved in approximately 40 ml of a solution that does not contain calcium, for example: in a 0.9% solution of sodium chloride, in a 5% dextrose solution, in a 10% solution of dextrose, 5% solution of fructose. Duration of intravenous infusion is at least 30 minutes.

    Side effects:

    Allergic reactions: urticaria, oesnoob or fever, rash, itching, anaphylaxisToid reactions, allergic dermistit, toxic epidermal necroLys (Lyell's syndrome), bronchospasm, eozinophilia, erythema polymorphic exuDative (including Stevens-Johnson), serum sickness, angyneurotic edema, anaphylaxisshock.

    From the gastrointestinal tractnausea, vomiting, diarrhea, flatulence, abdominal pain, dyspepsia, stomatitis, glossitis, dyspepsia, pancreatitis, pseudomembranous enterocolitis, impaired liver function (increased activity of "liver" transaminases, less often - alkaline phosphatase, hyperbilirubinemia, cholestatic jaundice), cholelithiasis , "sluggish phenomenon" of the gallbladder.

    On the part of the hematopoiesis: leukopenia, neutropenia, granulocytopenia, lymphopenia, leukocytosis, lymphocytosis, monocytosis, thrombocytosis,agranulocytosis, thrombocytopenia, basophilia, hemolytic anemia, hypocoagulation, increase (decrease) in prothrombin time, increase in thromboplastin time.

    On the part of the genitourinary system: renal dysfunction (increased urea concentration in the blood, hypercreatininaemia, glucosuria, hematuria), oliguria, nephrolithiasis, the presence of sediment in the urine, vaginitis, fungal infection of the genital organs.

    Local reactions: phlebitis, soreness and compaction along the vein, with a / m introduction - soreness, sensation of heat, tightness in the place of injection. Other: headache, dizziness, vertigo, nasal bleeding, convulsions, increased sweating, "hot flashes" of the blood, palpitation, the formation of precipitates in the lungs, allergic pneumonitis, superinfection.

    Overdose:Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis. Symptomatic measures are recommended for the treatment of overdose cases.
    Interaction:
    Ceftriaxone and aminoglycosides have a synergistic effect on many Gram-negative bacteria.
    Incompatible with ethanol.
    Ceftriaxone, suppressing the intestinal flora, prevents the synthesis of vitamin K.
    Interaction with anticoagulants, nonsteroidal anti-inflammatory drugs and other inhibitors of platelet aggregation increases the likelihood of bleeding.
    With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of developing nephrotoxic action increases.
    Pharmaceutically incompatible with solutions containing other antibiotics; solutions containing calcium.
    Special instructions:
    With simultaneous severe renal and hepatic insufficiency, the concentration of the drug in the plasma should be regularly determined.
    In patients who are on hemodialysis, it is necessary to monitor the concentration of ceftriaxone in the plasma, tk. they can decrease the rate of its excretion.
    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 are observed that disappear after cancellation (even if this phenomenon is accompanied by pain in the right hypochondrium, it is recommended to continue the prescription of the antibiotic and conduct symptomatic treatment).
    During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (red face, spasm 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.
    Elderly and debilitated patients may require the appointment of vitamin K.
    Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles, working with mechanisms and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
    Form release / dosage:Powder for solution for intravenous and intramuscular injection, 1.0 g.
    Packaging:
    1.0 g of active substance into bottles of a glass tube for medicinal products.
    1. Vials with a drug of 50 pieces are placed in boxes of cardboard with an enclosure of instructions for the use of the drug (for hospitals).
    2. Vials with preparation 1; 5 or 10 pieces are stacked in individual packs of cardboard along with instructions for the use of the drug.
    3. Packaging of the preparation complete with a solvent - water for injection (for intravenous administration).
    The kit includes:
    a) a vial with a preparation and 2 ampoules with water for injections on 5 ml;
    b) 5 bottles of the drug and 10 ampoules of water for injection for 5 ml;
    at) 10 vials with the drug and 20 ampoules with water for injection for 5 ml.
    The kit is placed in individual packs of cardboard along with instructions for the use of the drug, a knife ampoule or scarifier. When using ampoules with notches, rings or dots, the ampoule opener or scarifier is not inserted.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C. In a place inaccessible to children.

    Shelf life:2 years.Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001456 / 01
    Date of registration:23.07.2008
    The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.11.2015
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