Ceftriaxone resistant beta in relation lactamase enzymes (both penicillinase and cephalosporinase produced by most gram-positive and gram-negative bacteria). Effective anavar results against the following microorganisms:
Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus A (Str.pyogenes), Streptococcus V (Str. Agalactiae), Streptococcus viridans, Streptococcus bovis.
Note: . Staphylococcus spp, methicillin-resistant, and resistant to cephalosporins, including ceftriaxone. Most strains of enterococci (e.g., Streptococcus faecalis) are also resistant to ceftriaxone.
Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis, Citrobacter spp., Enterobacter spp. (Some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella 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. (Including S. typhi), Serratia spp. (Including S. marcescens), Shigella 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 celebrate good efficacy of ceftriaxone.
Bacteroides spp. (Including some strains of B. fragilis), Clostridium spp. (Including Cl. 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 as shown in vitro that the classical cephalosporin defined strains of pathogens may be resistant.
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 area 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 quickly into the interstitial fluid, where its bactericidal activity against pathogens sensitive to it retains for 24 hours.
Ceftriaxone is reversibly bound to albumin and is inversely proportional to the concentration of the binding, for example, when the serum concentration 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 concentration in the interstitial fluid ceftriaxone it is higher than in serum.
The half-life in healthy adult subjects is about 8 hours. Newborn to 8 days and the elderly over 75 years, the average half-life of approximately twice. In adults, 50-60% of ceftriaxone is excreted unchanged form in the urine, and 40-50% – in unchanged 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 pathology of the liver, the kidneys is enhanced release of ceftriaxone.
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, an average of 17% of the serum concentration of the drug diffuses into the cerebrospinal fluid, which is about 4 times more than aseptic meningitis. 24 hours after intravenous administration of ceftriaxone 50-100 mg / kg body weight concentration in the cerebrospinal fluid higher than 1.4 mg / l. In adult patients with meningitis over 2-25 hours after administration of ceftriaxone 50 mg / kg body weight several times higher than the concentration of ceftriaxone depressing the minimum dose required to inhibit the pathogens most frequently causing meningitis.
Indications for use:
Infections caused by pathogens sensitive to ceftriaxone:
sepsis, meningitis, abdominal infections (peritonitis, inflammatory disease of the gastrointestinal tract, bile ducts), bone infection, joints, connective tissue, skin, infection in patients with reduced immunity, kidney and urinary tract infections, respiratory tract infections (including .ch. pneumonia), and upper respiratory tract infections, urogenital infections (including gonorrhea).
Preventing infections in the postoperative period.
Hypersensitivity to cephalosporins and penicillin.
The first trimester of pregnancy.
Be wary – hyperbilirubinemia in newborns, premature babies, kidney / liver failure, ulcerative colitis, enteritis or colitis associated with the use of antibacterial drugs, pregnancy trimester 2-3, lactation.
Dosage and administration:
The drug is administered intravenously and intramuscularly.
For adults and children over 12 years
The average daily dose is 1-2 g of ceftriaxone 1 time per day (24 hours).
In severe cases, or in cases of infections caused by moderately susceptible pathogens single daily dose may be increased to 4 g
The following scheme is recommended for single daily dosage:
For infants (up to two weeks of age): 20-50 mg / kg body weight per day (dose of 50 mg / kg body weight do not exceed the recommended due to immature newborn enzyme system).
For infants and children up to 12 years
The daily dose is 20-75 mg / kg body weight.
Children with 50 kg of body weight and higher dosages should be followed for adults. The dose of 50 mg / kg of body weight should be administered by intravenous infusion for at least 30 minutes.
Duration of therapy
Depending on the course of the disease.
For the treatment of gonorrhea caused by both generators and neobrazuyuschimi penicillinase 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 post-operative infections, depending on the risk of infection for 30-90 minutes prior to surgery recommended single administration at a dose of ceftriaxone 2.1 g
The lack of renal and hepatic function
In patients with impaired renal function, under normal liver function, reduce the dose of ceftriaxone is not necessary. Only when preterminal renal failure in step (creatinine clearance less than 10 mL / min) necessary to ceftriaxone daily dose does not exceed 2 g
In patients with impaired liver function, while maintaining renal function, reduce the dose of ceftriaxone is also not necessary.
In the cases of simultaneous presence of severe liver disease and kidney concentration of ceftriaxone in the serum should be regularly monitored. In patients undergoing hemodialysis, dose after the procedure there is no need to change.
For intramuscular injection 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 a maximum of 1 g in one buttock. Lidocaine solution should never be administered intravenously!
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.
The duration of an intravenous infusion for at least 30 minutes.
For intravenous infusion of 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 polymorphous exudative (including Stevens-Johnson syndrome), anavar results serum sickness, angioedema, anaphylactic shock.
From the 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), goiter .
From the side of hematopoiesis: leukopenia, neutropenia, granulocytopenia, lymphopenia, thrombocytosis, thrombocytopenia, hemolytic anemia, anticoagulation, lowering the concentration of plasma coagulation factors (II, VII, IX, X), prolonged prothrombin time.
From the urinary system: renal dysfunction (azotemia, increased blood urea, 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.
Excessively high concentrations of ceftriaxone in plasma can not be reduced by hemodialysis or peritoneal dialysis. For treatment of overdose symptomatic measures are recommended.
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 administered in their recommended doses separately!
Incompatible with ethanol.
NSAIDs, and others. Platelet aggregation inhibitors increase the chance of bleeding.
In an application with the “loop” diuretics, etc. Increased risk of nephrotoxic drugs nephrotoxic effect.
Pharmaceutically compatible with solutions containing other. Antibiotics.
You can not mix in the same infusion vial or a syringe with other antibiotic (chemical incompatibility).
When simultaneous severe renal and hepatic failure, regularly determine the concentration of drug in the plasma.
In patients on hemodialysis, you must monitor the concentration of ceftriaxone in plasma, because they its elimination rate may be reduced.
With 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 the cancellation (even if this phenomenon is accompanied by pain in the right upper quadrant, recommended the continuation of the appointment of an antibiotic and conduct symptomatic treatment).
During treatment contraindicated use of ethanol – can disulfiramopodobnye effects (flushing, stomach cramps, nausea, vomiting, headache, decreased blood pressure, tachycardia, shortness of breath).
Despite 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 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 anavar results greater care.
Freshly prepared solutions ceftriaxone physically and chemically stable for 6 hours at room temperature.