Expiration date: 03/2025
Composition and form of issue:
Powder for preparation of solution for intravenous and intramuscular administration 1 flask:
Ceftriaxone 0.5g, 1g or 2g
in vials of 10 ml without a pack of cardboard or a pack of cardboard 10 vials, or in a box of 50 vials.
Powder for preparation of injection solution for intravenous infusion 1 flask:
Ceftriaxone 0.5g, 1g or 2g
in vials of 10 ml without a pack of cardboard or a pack of cardboard 10 vials, or in a box of 50 vials.
Solution for injection for intramuscular injection 1 flask:
Ceftriaxone 0.5g, 1g or 2g
in vials of 10 ml in a cardboard bundle of 1 or 10 vials, or in a box of 50 vials.
Characteristic:
Cephalosporin antibiotic of III generation for parenteral administration.
Pharmacological action:
Suppresses biosynthesis of bacterial cell wall, has bactericidal effect. Resistant to beta-lactamases produced by most gram-positive and gram-negative bacteria.
Pharmacokinetics:
In case of parenteral administration it penetrates well into tissues and body fluids. Bioavailability with the/m introduction is 100%, the time to reach Cmax when the/m introduction is 2-3 h When inflammation of the meningeal membranes penetrates well into the cerebrospinal fluid.
Cmax when administered at a dose of 50 mg/kg in blood plasma is 216 µg/ml, in liquorice — 5, 6 µg/ml.in adults, after 2-24 h after administration at a dose of 50 mg / kg, the concentration in the cerebrospinal fluid is many times higher than the minimum inhibitory concentrations for the most common pathogens of meningitis. Protein binding-85%, T1/ 2-5, 8-8, 7 h, distribution volume — 5, 78-13, 5 l, plasma Cl — 0, 58-1, 45 l/h, renal — 0, 32-0, 73 l/h.
In newborns up to 8 days and in the elderly over 75 years, T1 / 2 increases ~ 2 times. In adults, 50-60% is excreted in active form in the urine within 48 h. In renal failure the selection is slowing down. From 30 to 50% of the drug is excreted in the bile. Under the influence of intestinal flora turns into an inactive metabolite. In newborns ~ 70% of the administered dose is excreted by the kidneys.
Description of the pharmacological action:
Active against: gram-positive aerobes-Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus viridans, Streptococcus bovis gram — negative aerobic-Aeromonas spp., Alcaligenes spp., Branhamella catarrhalis (beta-lactamase-producing and non-reducing), Citroen spp., Enterobacter spp. (some strains are resistant), Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae (including strains producing penicillinase), Haemophilus parainfluenzae, Klebsiella spp., (incl. Klebsiella pneumoniae), Moraxella spp., Morganella morganii, Neisseria gonorrhoeae (including strains producing penicillinase), Neisseria meningitidis, Plesiomonas shigelloides, Proteus mirabilis, Proteus vulgaris, Providencia spp., Salmonella spp. (including Salmonella typhi), Serratia spp. (including Serratia marcescens), Shigella spp., Vibrio spp. (including Vibrio cholerae), Yersinia spp. (including Yersinia enterocolitica).
Also sensitive individual strains Pseudomonas aeruginosa anaerobes: Bacteroides spp. (including strains of Bacteroides fragilis), Clostridium spp. (except Clostridium difficile), Fusobacterium spp. (except Fusobacterium varium, Fusobacterium mortiferum), Peptococcus spp., Peptostreptococcus spp., as well as Treponema pallidum, Borrelia burgdorferi.
Resistant strains of Staphylococcus spp. exhibiting resistance to methicillin-resistant strains Enterococcus spp., Bacteroides spp.
Indications:
Peritonitis, sepsis, meningitis infection of the abdominal cavity (peritonitis, inflammatory diseases of the gastrointestinal tract, biliary tract, including cholangitis, empyema gallbladder), upper and lower respiratory tract diseases (including pneumonia, lung abscess, empyema), infections of bones, joints, skin and soft tissues, the urogenital zone (including gonorrhoea, pyelonephritis) infected wounds, burns, prevention of postoperative infection, diseases in persons with weakened immunity.
Contraindications:
Hypersensitivity (W. to penicillins), pregnancy (1 trimester).
Application for pregnancy and breastfeeding:
Contraindicated in the first trimester of pregnancy. At the time of treatment should stop breastfeeding.
Side effect:
From the nervous system and sensory organs: headache, dizziness.
From the cardiovascular system and blood (hematopoiesis, hemostasis): leukopenia, neutropenia, granulocytopenia, thrombocytopenia, hemolytic anemia.
From the digestive tract: nausea, vomiting, stomatitis, glossitis, diarrhea, cholestasis, pseudomembranous enterocolitis, increased activity of hepatic transaminases.
Allergic reactions: about 1% - urticaria, fever, eosinophilia, rash, itching, urticaria, exanthema, allergic dermatitis, exudative erythema multiforme, swelling, anaphylactic shock.
Other: oliguria, anticoagulation, vomiting uremia, hypercreatininemia, elevated levels of urea candidiasis etc. superinfection while on/in the introduction — phlebitis, pain along the vein when the/m a — soreness at the injection site.
Drug interaction:
Synergism of antibacterial action is noted at simultaneous appointment with aminoglycoside antibiotics. Pharmacologically incompatible with solutions of other antibiotics. When used with aminoglycosides increases (mutually) activity against many gram-negative bacteria.
Method of application and doses:
In/m (deep in the gluteus muscle) or/in (drip for 30 min or bolus, injected slowly for 2-4 minutes). For the / m introduction 1 g dissolved in 3, 5 ml 1% lidocaine. For in / in the contents of 1 vial diluted in 10 ml of water for injection. For in/infusions dissolve 2 g in 40 ml of 0, 9% sodium chloride solution, 0, 45% sodium chloride solution containing 2, 5% glucose, 5% glucose solution, 10% glucose solution, 5% fructose solution or 6% dextran solution.
Adults and children over 12 years (weighing more than 50 kg) — 1-2 g 1 time per day, in severe cases or in cases of infections caused by moderately sensitive pathogens, the daily dose is increased to 4 g (divided into 2 injections). Newborns (up to 2 weeks) — 20-50 mg/kg/day, infants and children under 12 years-20-80 mg/kg/day.
Doses of 50 mg/kg or more should be administered in the form of in / infusion for 30 minutes.the Duration of treatment depends on the nature of the disease.
In bacterial meningitis, infants and young children, the initial dose is 0, 1 g/kg 1 time per day (the maximum dose is 4 g). The duration of treatment depends on the pathogen and can range from 4 days for Neisseria meningitidis to 10-14 days for sensitive strains of Enterobacteriaceae family.
Prevention of infectious diseases in the pre-and postoperative period-30-90 minutes before surgery — 1-2 g (more/in).
In the treatment of gonorrhoea-in / m 0, 25 g once.
In renal insufficiency (CL creatinine less than 10 ml/min) daily dose — no more than 2 g (in violation of renal and / or liver function, as well as in patients on hemodialysis, it is necessary to monitor the concentration of Ceftriaxone in blood plasma, because it decreases the rate of excretion).
Precautionary measures:
Be wary hyperbilirubinemia (newborn and preterm children), ulcerative colitis.
With simultaneous renal and hepatic insufficiency, in patients on hemodialysis, it is necessary to regularly determine the concentration in blood plasma. With long-term treatment, it is necessary to regularly monitor the picture of peripheral blood, the indicators of the functional state of the liver and kidneys.
In rare cases, when ultrasound gallbladder darkening is observed, which disappears after discontinuation of the drug (even if this phenomenon is accompanied by pain in the right hypochondrium, it is necessary to continue treatment with an antibiotic and prescribe symptomatic therapy)
Special instruction:
Freshly prepared solutions are stable for 6 h at room temperature.
Storage conditions:
The prepared solution is suitable for use for 6 hours at a temperature of 5 to 25 °C and 24 hours at a temperature of 2 to 5 °C.
