Mode of action:
Cephalosporin antibiotic of the third generation. Has a bactericidal effect by inhibiting the synthesis of the bacterial cell wall. Ceftriaxone acetylates membrane-bound transpeptidase, breaking thus the cross-linking of the peptidoglycan necessary to ensure the strength and rigidity of the cell wall. Has a broad spectrum of antimicrobial activity, which includes a variety of aerobic and anaerobic gram-positive and gram-negative microorganisms. The drug is active against Gram-positive aerobes: Streptococcus group A, B, C, G, Str. pneumoniae, Staphylococcus aureus, St. epidermidis; Gram-negative aerobes: Enterobacter spp., Eschenchia coli, Haemophilus influenzae, H. parainfluenzae, Klebsiella spp. (including K. pneumoniae), Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, N. meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (including S. typni), Serratia spp. (including S. marcescens), Shigella spp., Yersinia spp. (including Y. enterocolitica), Treponema pallidum, Citrobacter spp., Aeromonas spp., Acinetobacter spp .; anaerobes: Actinomyces, Bacteroides spp. (including some strains of B. fraqilis), Clostridium spp. (but most strains of C. difficile are resistant), Peptococcus spp., Peptostreptococcus spp., Fusobacteriumspp. (including F. mortiferum and F. varium).
Pharmacokinetics:
After intramuscular administration is rapidly and completely absorbed. Bioavailability is 100%. The maximum concentration in plasma was 1.5 hours. Reversibly binds to plasma albumin (85% - 95%). The drug is retained permanently in the body. The minimum concentration of antimicrobial determined in the blood for 24 hours or more. Easily into the organs, body fluids (peritoneal, pleural, synovial, inflammation of the meninges - the spinal) bone tissue. Breast milk is determined 3 - 4% of the serum concentration (greater by intramuscular than when administered intravenously). The half-life of 5.8 - 8.7 hours, and significantly lengthens in people older than 75 years (16 h), children (6.5 days) and the newborn (up to 8 days). In the active form is released (up to 50%) by the kidneys within 48 hours. Partly excreted in the bile. With kidney failure is slowing down, possible cumulation.
Indications for use:
Ceftriaxone is indicated for the treatment of infectious diseases caused by microorganisms sensitive to it, including: - in infections of upper respiratory tract, upper and lower respiratory tract infections (acute and chronic bronchitis, pneumonia, lung abscess, empyema); - For infections of the skin and soft tissues (including streptoderma); - With infections of urogenital organs (pyelitis, acute and chronic pyelonephritis, cystitis, prostatitis, epididymitis, gynecological infections, uncomplicated gonorrhea); - With infection of the abdominal cavity (the biliary tract and the gastrointestinal tract, peritonitis); - In sepsis and bacterial septicemia; - When bone infections (osteomyelitis), joints; - With bacterial meningitis and endocarditis; - With chancroid, syphilis, Lyme disease (spirochetosis); - In typhoid fever; - Salmonellosis and salmonellonositelstve; - With infections in immunocompromised patients; - For the prevention of postoperative septic complications.
How to use:
Ceftriaxone is used intramuscularly and intravenously. Use only freshly prepared solutions.
For intramuscular administration, the preparation is dissolved in sterile water for injection in such ratios: 0.5 g was dissolved in 2 ml of water, 1 g - 3.5 ml water. Intramuscular injections are administered in the upper outer quadrant of the gluteus maximus deep enough. It is recommended to be administered no more than 1 g in one cheek. With a view to eliminating pain at the injection site may be used 1% lidocaine.
For intravenous administration, the drug was dissolved in sterile water for injection (0.5 g dissolved in 5 ml, 1 g - 10 mL of solvent). Administered by slow intravenous injection (within 2 - 4 minutes). For intravenous infusion of 2 g of the drug is dissolved in 40 ml of a solution containing no calcium ions (sodium chloride 0.9% and glucose 5% or 10% solution of 5% levulose). The dose of 50 mg / kg of body weight should be administered more intravenously for at least 30 minutes. Children - newborns (to two weeks of age) and preterm daily dose is 20-50 mg / kg body weight one time daily (dose 50 mg / kg body weight does not exceed the permitted). In bacterial meningitis in infants starting dose is 100 mg / kg of body weight once a day (maximum 4 g). After isolation of the pathogen and to determine its sensitivity dose should be reduced accordingly; - From West weeks to 12 years - 50 - 80 mg / kg per day in 2 of the introduction (in children with a body weight of 50 kg or more should comply with the dosage for adults); - For adults and children over 12 years of drug is given by 1 - 2, 1 g once a day, if necessary - to 4 g (preferably 2 administration after 12 hours). The duration of treatment depends on the type of infection and the severity of the condition. Once the symptoms of infection and normalization of body temperature is recommended to continue the use for at least three days. In uncomplicated gonorrhea adults administered intramuscularly 0.25 g Ceftriaxone. To prevent postoperative infection adult is administered 1 g once for 2.1 - 2 hours before surgery intravenously as an infusion over 15 - 30 minutes at a concentration of 10-40 mg / ml.
In patients with impaired renal function while maintaining liver function should not reduce the dose of Ceftriaxone. Only in the case preterminalnoi renal failure (creatinine clearance less than 10 mL / min), the daily dose should not exceed 2 g
Side effects:
Ceftriaxone is relatively well tolerated. In some cases, possible: - on the part of the digestive system: nausea, vomiting, diarrhea, transient elevation of liver transaminases, cholestatic jaundice, hepatitis, pseudomembranous colitis; - Allergic reactions: skin rash, pruritus, eosinophilia, rarely - angioedema; - The part of the blood coagulation system: hypoprothrombinemia; - The part of the urinary system: interstitial nephritis.
Effects caused by chemotherapeutic action - candidiasis.
Local reactions: phlebitis (intravenous injection); soreness at the injection site (intramuscular injection).
Contraindications:
Hypersensitivity to ceftriaxone and other cephalosporins, penicillins, first trimester of pregnancy, breast-feeding (at the end of treatment), renal and hepatic failure.
Pregnancy:
The drug is contraindicated for use in the I trimester of pregnancy. When administered during lactation breastfeeding should be abolished.
Interaction with other drugs:
Pharmaceutically compatible with other antimicrobial agents in the same volume. Ceftriaxone, suppressing the intestinal flora, prevents the synthesis of vitamin K. Therefore, while the use of drugs that reduce platelet aggregation (non-steroidal anti-inflammatory drugs, sulfinpyrazone), increases the risk of bleeding. For this reason, while the use of anticoagulants has increased, the anticoagulant action. While the use of "loop" diuretics increases the risk of nephrotoxicity.
Overdose:
With prolonged use of high doses of Ceftriaxone may change in the pattern of blood (leucopenia, neutropenia, thrombocytopenia, hemolytic anemia).
Treatment: symptomatic (excessively high concentrations of the drug can not be reduced by hemodialysis or peritoneal dialysis).
Product:
Powder for solution for injection of 0.5, 1.0, or 2.0 g vials.
Storage Conditions:
Store in a dark place at a temperature not exceeding 25 ° C. Shelf life - 2 years. Keep out of the reach of children.
Conditions of supply of pharmacies - with a prescription.
Crystalline powder of white or white with a slightly yellowish tint, slightly hygroscopic.
One vial comprises the ceftriaxone sodium sterile based on ceftriaxone - 0.5 g or 1.0 g
In addition:
With careful use in patients with hyperbilirubinemia in neonates, premature babies, patients prone to allergic reactions.
Elderly or debilitated patients may require vitamin K.
When hypertension and disruption of water and electrolyte balance is necessary to check the level of sodium in the plasma.
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