Effective against the following microorganisms: Gram-positive Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae , Streptococcus A (Str pyogenes.), Streptococcus V (Str agalactiae.), Streptococcus andriol dosage viridans, Streptococcus bovis. Note : Staphylococcus spp, methicillin-resistant, resistant and. cephalosporins, including ceftriaxone. Most enterococci (e.g., Streptococcus faecalis) are also resistant to ceftriaxone. Gramotriiatelnye Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp., (Some strains resistant), Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebssiella spp. (including Kl.pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Pseudomonas aeruginosa ( some resistant strains), Salmonella spp., Vibrio spp., (including V.cholerae). Yersinia spp, (including Y. Enterocolitica).. Note : Many strains of these microorganisms, which in the presence of other antibiotics, such as penicillins, cephalosporins, aminoglycosides and first generations multiply resistant, susceptible to ceftriaxone. Treponema pallidum susceptible to ceftriaxone both in vitro, and in animal experiments. According to clinical data in primary and secondary syphilis say good efficacy of ceftriaxone. Anaerobic pathogens Bacleroides spp. (including some strains B.fragilis), Clostridium spp. (including C1. difficile), Fusobacterium spp. (except F.mostiferum, F.varium), Peptococcus spp, Peptostreptococcus spp.. Note : some of the many strains of Bacteroides spp.(e.g., B.fragilis), beta-lactamase-producing resistant to ceftriaxone. To determine the sensitivity of microorganisms necessary to use discs containing ceftriaxone, since it is shown that m vitro to classical cephalosporin certain strains can be resistant pathogens.
For parenteral administration of ceftriaxone well penetrates the tissues and body fluids.
In healthy adult subjects for ceftriaxone is characterized by long, about 8 hours, the half-life. The areas under the curve concentration – time in blood serum after intravenous and intramuscular administration of the same. This means that the bioavailability of ceftriaxone administered intramuscularly is 100%. When intravenous ceftriaxone diffuses rapidly into the interstitial fluid, where its bactericidal activity against susceptible thereto pathogens retains for 24 hours.
Tsefiriakson reversibly bound to albumin, and this binding is inversely proportional to the concentration of, for example, at a concentration in the blood serum of the drug is less than 100 mg / l ceftriaxone binding protein is 95%, and at a concentration of 300 mg / l – 85% only. Due to the lower content of albumin in the interstitial fluid ceftriaxone concentration therein is higher than in blood serum.
The half-life in healthy adult subjects is about 8 hours. Newborn to 8 days and older than 75 years, the average half-life of approximately twice Adult ceftriaxone 50-60% released in unaltered form in urine, and 40-50% – in unmodified form with bile. Under the influence of the intestinal flora ceftriaxone converted into an inactive metabolite. In newborns about 70% of the administered dose excreted by the kidneys. When kidney failure or liver disease in adults pharmacokinetics of ceftriaxone is almost unchanged, elimination half-life is lengthened slightly. If renal function is impaired, increased excretion in the bile, and if there is a liver disease, the enhanced release of ceftriaxone kidneys. Penetration into the cerebrospinal fluid : in infants and in children with inflammation of the meninges ceftriaxone penetrates into the cerebrospinal fluid, while in the case of bacterial meningitis in the middle 17% of the serum concentration of the drug diffuses into the cerebrospinal fluid, which is about 4 times greater than in aseptic meningitis. 24 hours after intravenous administration of ceftriaxone 50-100 mg / kg concentration in the cerebrospinal fluid of the body exceeds 1.4 mg / l. In adult patients with meningitis through 2-25 hours after administration of ceftriaxone 50 mg / kg body weight concentration ceftriaxone repeatedly exceeded the minimum dose of depressing, which is needed to suppress the pathogen most frequently cause meningitis.
Infections caused by sensitive to ceftriaxone pathogens:
sepsis, meningitis, abdominal infections (peritonitis, inflammatory diseases of the gastrointestinal tract, biliary tract) infections of bones, joints, connective tissue, skin, infection in patients with lowered immunity, kidney and urinary tract infections, respiratory tract infections (including pneumonia), as well infection LOP organs, urogenital infections (including gonorrhea).
infections Prevention in the postoperative period.
Hypersensitivity to andriol dosage cephalosporins and penicillin.
The first trimester of pregnancy. Precautions – hyperbilirubinemia in newborns, premature babies, kidney / liver failure, ulcerative colitis, enteritis or colitis associated s use of antibacterial drugs, pregnancy trimester 2-3, period lactation.
Dosage and administration :
The drug is administered intravenously and intramuscularly. For adults and children over 12 years of average daily dose is 1-2 g of ceftriaxone 1 per day (24 hours). In severe cases, or in cases of infections caused by moderately susceptible pathogens , a single daily dose may be increased to 4 years for newborns following scheme is recommended for single daily dosage: For infants (up to two weeks of age): 20-50 mg / kg of body weight per day (a dose of 50 mg / kg of body weight is not recommended to exceed due to immature newborn enzyme system). for infants and children up to 12 years of daily dose is 20-75 mg / kg body weight. in children weighing 50 kg and above should be followed dosage for adults. The dose of 50 mg / kg of body weight should be administered by intravenous infusion for at least 30 minutes. The duration of therapy – Depends on the disease. Meningitis In bacterial meningitis in infants and children initial dose of 100 mg / kg body weight once daily (maximum 4 g). For the treatment of gonorrhea, called as an image and not penicillinase forming strains, the recommended dose is 250 mg intramuscularly. Prevention in the pre- and postoperative period before infected or suspected infected surgical interventions for the prevention of postoperative infections, depending on the risk of infection, for 30-90 minutes prior to surgery is recommended single injection of ceftriaxone in a dose of 1-2 g Insufficient renal and hepatic function in patients with impaired renal function, under normal liver function, reduce the dose of ceftriaxone is not necessary. Only with kidney failure in preterminal stage (creatinine clearance below 10 ml / min), it is necessary that the daily dose of ceftriaxone should not exceed 2 years in patients with impaired liver function, while maintaining renal function, reduce the dose of ceftriaxone is also not necessary. In the case of simultaneous the presence of severe liver disease and kidney failure in the serum concentration of ceftriaxone should be regularly monitored. In patients undergoing hemodialysis, the dose after this procedure, there is no need to change. Intramuscular administration For intramuscular administration of 1 g of the drug should be diluted in 3.5 mL of 1% lidocaine and enter deeply into the gluteal muscle, it is advisable to enter no more than 1 g preparation of one buttock. Lidocaine solution should never be administered intravenously! Intravenous administration For intravenous injection of 1 g of the drug must dissolve in 10 ml of sterile distilled water and administered by slow intravenous injection over 2-4 minutes. Intravenous infusion duration of an intravenous infusion for at least 30 minutes. For intravenous infusion 2 g of the powder should be diluted with approximately 40 ml of solution free of calcium, such as 0.9% sodium chloride solution, 5% dextrose solution, 10% dextrose, 5% fructose solution.
Side effects : Allergic reactions : rash, chills or fever, rash, pruritus, rarely – bronchospasm, eosinophilia, erythema polymorph, exudative (including Stevens-Johnson syndrome), serum sickness, angioedema, anaphylactic shock. Digestive system : nausea, vomiting, diarrhea or constipation, bloating, abdominal pain, taste disturbance, stomatitis, glossitis, pseudomembranous enterocolitis, liver dysfunction (increased activity of “liver” transaminases, less often – ALP or bilirubin, cholestatic jaundice), dysbiosis. From the of hematopoiesis : leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, anticoagulation, lowering the concentration of plasma clotting factors (I, VII, IX, X), prolonged prothrombin time. From the urinary system : azotemia, elevated levels of urea blood hypercreatininemia, glycosuria, cylindruria, hematuria, oliguria, anuria. Local reactions : phlebitis, pain along the vein, pain and infiltration in the ground / m introduction. Other : headache, dizziness, nosebleeds, candidiasis, superinfection.
Drug Interactions : Combination therapy between ceftriaxone and aminoglycosides on effect on many Gram-negative bacteria is synergism. Although predict enhancement of the effect of such combinations can not be, in cases of severe and life-threatening infections (eg, caused by Pseudomonas aeruginosa) justified their co-administration. Due to physical incompatibility between ceftriaxone and the aminoglycoside should be prescribed them in the recommended doses separately! Incompatible with ethanol. NSAIDs and et al. platelet aggregation inhibitors increase the chance of bleeding. in an application with the “loop” diuretics, etc. the risk of increased nephrotoxic drugs nephrotoxic effect. Pharmaceutical incompatible with solutions containing other. antibiotics. You can not mix in the same infusion vial or a syringe with other antibiotic (chemical incompatibility).
Excessively high concentrations of ceftriaxone plasma can not be reduced by hemodialysis or peritoneal dialysis. For treatment of overdose symptomatic measures are recommended.
Special instructions :
. When simultaneous severe renal and hepatic impairment should be regular monitoring of the concentration of drug in plasma
in patients on hemodialysis, you must monitor the concentration of ceftriaxone in plasma, because have its elimination rate may be reduced.
In the long-term treatment should be regularly monitored picture peripheral blood, indicators of the functional state of the liver and kidneys.
In rare cases, ultrasound gallbladder marked darkening, which disappear after canceling (Lager if this phenomenon is accompanied by pain in the right upper quadrant, recommends continuation of the appointment of an antibiotic and conduct symptomatic treatment).
During treatment contraindicated use of ethanol – can disulfiramopodobnye effects (redness of the face, a spasm in the stomach, nausea, vomiting, headache, decreased blood pressure, tachycardia, shortness of breath).
in spite of the detailed medical history, that is the rule for other cephalosporin antibiotics, we can not exclude the possibility of an anaphylactic shock, which requires immediate treatment – first intravenous epinephrine, followed by glucocorticoids.
Studies in vitro have shown that, like andriol dosage other cephalosporin antibiotics ceftriaxone is able to displace bilirubin bound to albumin serum. Therefore, in infants with hyperbilirubinemia and especially in premature infants, the use of ceftriaxone requires even greater care.
Freshly prepared solutions of ceftriaxone is physically and chemically stable for 6 hours at room temperature.
In the appointment during lactation should be abolished breastfeeding.
Elderly or debilitated patients may require the appointment of vitamin K.