Active substanceCeftriaxoneCeftriaxone
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:Ceftriaxone sodium, equivalent to ceftriaxone - 0.25 g; 0.5 g or 1.0 g.
    Description:Crystalline powder from white to yellowish color.
    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 most 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, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus A (Str.pyogenes), Streptococcus V (Str. Agalactiae), Streptococcus viridans, Streptococcus bovis.

    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 F. mostiferum. F. varium), Peptococcus spp., Peptostreptococcus spp.

    Note: some strains of many Bacteroides spp. (for example, in. 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.

    The area under the concentration-time curve in the blood serum for intravenous and intramuscular injection coincide. This means that the bioavailability of ceftriaxone when administered intramuscularly is 100%. With intravenous administration ceftriaxone quickly penetrates into the interstitial fluid, where its bactericidal action against sensitive microorganisms persists for 24 hours.

    Ceftriaxone reversibly binds to albumin and this binding is inversely proportional to the concentration: for example, when the concentration of the drug in the serum is less than 100 mg / l, ceftriaxone binding to proteins is 95%, and at a concentration of 300 mg / l, only 85%. Due to the lower content of albumins in the interstitial fluid, the concentration of ceftriaxone in it is higher than in serum.

    Maximum concentrations of the drug in the blood plasma (Cmax) after a single intramuscular injection at doses of 0.5 and 1 g are 38 μg / ml and 76 μg / ml respectively, the time to reach Cmax - 2-3 hours With a single intravenous administration of ceftriaxone in doses of 0.5 and 1 g Cmax in the blood plasma are reached at the end of the infusion and are 82 μg / ml and 151 μg / ml, respectively.

    The half-life in healthy adults is about 8 hours. In newborns up to 8 days and in elderly people older than 75 years, the average half-life is approximately twice as large. In adults, 50-60% of ceftriaxone is excreted unchanged in the urine, and 40-50% - with bile in the intestine, where the inactivation occurs. In neonates, approximately 70% of the administered dose is excreted by the kidneys. In renal failure or liver disease in adults pharmacokinetics ceftriaxone hardly changes, half-life period is lengthened slightly. If the kidney function is impaired, the excretion of bile increases, and if there is a pathology of the liver, then the excretion of ceftriaxone by the kidneys is enhanced. The half-life in patients on hemodialysis (creatinine clearance 0-5 ml / min) is 14.7 hours, with SC 5-15 ml / min-15.7 hours, at 16-30 ml / min- 11.4 parts, with a CK of 31-60 ml / min-12.4 hours.

    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 penetrates 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 weight, the 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 suppressive dose that is necessary to inhibit the microorganisms that most often cause meningitis.

    Indications:Infections caused by susceptible to ceftriaxone pathogens: bacterial septicemia, bacterial meningitis, infections of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, bile ducts), infections of bones, joints, connective tissue, skin, infection in patients with low immunity, kidney infections and urinary tract infections, respiratory tract infections (including pneumonia), acute otitis media, urogenital infections (including uncomplicated gonorrhea). Prevention of infections in the postoperative period.
    Contraindications:Hypersensitivity to cephalosporins, to penicillins and carbapenems. Hyperbilirubinemia in newborns; Newborns, who showed intravenous administration of solutions,containing calcium ions. Lactation period. The first trimester of pregnancy.
    Carefully:Premature infants, renal / hepatic insufficiency, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy II - III trimester.
    Pregnancy and lactation:The use of the drug in the II and III trimester of pregnancy is possible only on indications if the potential benefit to the mother exceeds the risk to the fetus. When prescribing the drug during lactation, it is necessary to stop breastfeeding.
    Dosing and Administration:
    The drug is used intramuscularly and intravenously.
    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;

    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. 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 not less than 10 days.

    For newborns

    For a single daily dosage, the following scheme is recommended:

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

    For infants and children under 12 years of age

    The daily dose is 20-75 mg / kg body weight.

    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 of body weight should be given as an intravenous infusion, for at least 30 minutes.

    For treatment skin and soft tissue infections the recommended daily intake in children is 50-75 mg / kg, divided into 2 divided doses (every 12 hours). The total daily intake for children should not exceed 2 g.

    In the treatment acute otitis media in children, a single intramuscular injection of the drug at a dose of 50 mg / kg is recommended (but not more than 1.0 g per day)

    Duration of therapy - depends on the course of the disease.

    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). Further - 100 mg / kg of body weight per day (no more than 4.0 g) once a day, divided into 2 doses (every 12 hours).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

    Uncomplicated gonorrhea

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

    Prevention in the pre- and postoperative period

    Before infected or suspected infected surgical interventions to prevent postoperative infections, depending on the danger of infection, for 30-90 min. before surgery, a single administration of ceftriaxone in a dose of 1.0 g is recommended. For operations on the colon and rectum, additional administration of a drug from the 5-nitroimidazole 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 with kidney failure (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 the blood plasma should be regularly monitored. (The daily dose should not exceed 2.0 g.). Patients on hemodialysis do not require an additional dose after a hemodialysis session, however, it is necessary to monitor the concentration of ceftriaxone in the blood plasma, since the excretion of the drug in such patients may be slowed down (dose adjustment may be required).

    Intramuscular injection

    For intramuscular injection of 0.25 g and 0.5 g of the drug, it is necessary to dissolve it in 2.0 ml of a 1% solution of lidocaine, and for 1 g of the drug - in 3.5 ml of a 1% solution of lidocaine and insert deep into the gluteus muscle (it is recommended to administer not more than 1 g of the drug in one buttock). A solution of lidocaine can never be administered intravenously!

    Intravenous administration

    For intravenous injection, 0.25 g or 0.5 g of the drug should be dissolved in 5 ml, and for 1 g - in 10 ml of sterile distilled water and administered intravenously slowly over 2-4 min.

    Intravenous infusion

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

    Rules for the preparation and administration of solutions: Use only freshly prepared solutions.

    Side effects:

    Allergic reactions: urticaria, chills or fever, rash, itching, bronchospasm, eosinophilia, allergic dermatitis, allergic pneumonitis, erythema, polymorphic exudative (including Stevens-Johnson syndrome), Lyell syndrome, serum sickness, angioedema, anaphylactic shock.

    From the digestive system: nausea, vomiting, diarrhea or constipation, flatulence, abdominal pain, taste disorder, stomatitis, glossitis, pseudomembranous colitis, impaired liver function (increased activity of "liver" transaminases, less often - alkaline phosphatase or bilirubin, cholestatic jaundice), cholelithiasis, dysbiosis.

    On the part of the organs of hematopoiesis: anemia, leukopenia, monocytosis, lymphocytosis, neutropenia, granulocytopenia, lymphopenia,thrombocytopenia, thrombocytopenia, hemolytic anemia, hypocoagulation, decrease in the concentration of plasma clotting factors (II, VII, IX, X), lengthening (or decreasing) prothrombin time, basophilia.

    From the side of the urinary system: renal dysfunction (azotemia, increased urea in the blood, hypercreatininaemia, glycosuria, cylindruria, hematuria), oliguria, anuria, nephrolithiasis, the presence of sediment in the urine.

    Local reactions: when administered intramuscularly - soreness, sensation of heat, tightness at the injection site; at intravenous introduction - condensation on a course veins, morbidity, phlebitis.

    Other: headache, dizziness, nosebleeds, palpitations, sudoras, vaginitis, candidiasis, superinfection.

    Overdose:

    Symptoms: dizziness, nausea, vomiting. There is no specific antidote.

    Excessively high concentrations of ceftriaxone in the plasma can not be reduced by hemodialysis or peritoneal dialysis, because they are ineffective. Treatment of an overdose is symptomatic.

    Interaction:

    Bacteriostatic antibiotics reduce the bactericidal effect of ceftriaxone.Antagonism with chloramphenicol in vitro.

    Nonsteroidal anti-inflammatory drugs and other inhibitors of platelet aggregation increase the likelihood of bleeding.

    With simultaneous use with "loop" diuretics and other nephrotoxic drugs, the risk of developing nephrotoxic action increases.

    Pharmaceutically incompatible with calcium-containing solutions (including Hartman and Ringer's solution), as well as with amsacrine, fluconazole, and aminoglycosides.

    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 excretion of ceftriaxone. 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 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); However, the starting role of precipitate formation in the biliary tract under the influence of ceftriaxone can not be ruled out. 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 injected simultaneously, incl. through separate accesses for infusions at different sites.Theoretically, based on the calculation of 5 T 1/2 ceftriaxone, the interval between the administration of ceftriaxone and calcium-containing solutions should be at least 48 hours. Data on the possible interaction of ceftriaxone with oral calcium-containing preparations, as well as ceftriaxone for intramuscular administration with calcium-containing drugs intravenous 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). During treatment, the use of ethanol is contraindicated - disulfiramoid-like effects are possible (reddening of face, spasm in the stomach, nausea, vomiting, headache, lowering of 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 glucocorticoids.

    In vitro studies have shown that, like other cephalosporin antibiotics ceftriaxone is able to displace bilirubin, associated with serum albumin.

    Elderly and debilitated patients may require the appointment of vitamin K.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care should be taken when driving vehicles and when engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, because the drug may cause dizziness, headache, seizures and other side effects that may affect on the above abilities.
    Form release / dosage:
    Powder for the preparation of solution for intravenous and intramuscular injection 0.25 g, 0.5 g, 1.0 g.
    Packaging:

    0.25 g or 0.5 g in a 5 ml glass vial.

    1.0 g in a 10 ml glass vial. 1 bottle together with the instruction for use is placed in a cardboard box.

    Storage conditions:In a dry place at a temperature of no higher than 30 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011722 / 01
    Date of registration:30.08.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India
    Manufacturer: & nbsp
    Representation: & nbsp"UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")""UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")"India
    Information update date: & nbsp28.11.2017
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