International Nonproprietary Name:Cefazolin
Pharmaceutical form:Powder for the preparation of an injection solution of 1.0 g in glass bottles
Cephalosporin antibiotic of the first generation for parenteral use. Cephalosporin antibiotic of the first generation for parenteral use. Has a wide spectrum of action, is active against Gram-positive (Staphylococcus spp., Staphylococcus aureus (non-producing and producing penicillinase, including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis) and Gram-negative (Neisseria meningitidis, Neisseria gonorrhoeae, Shigella spp., Salmonella spp ., Escherichia coli, Klebsiella spp., Treponema spp., Leptospira spp.) Of microorganisms.
Most effective active against Haemophilus influenzae, some strains of Enterobacter and Enterococcus.Ineffective against Pseudomonas aeruginosa, indolpositive strains of Proteus spp., Mycobacterium tuberculosis, Serratia spp., Anaerobic microorganisms, methicillin-resistant strains of Staphylococcus spp.
The period of maximum concentration with intramuscular injection at a dose of 0.5 and 1 g, respectively, is 2 and 1 hour; The maximum concentration is 38 and 64 μg / ml; After intravenous administration, the period of maximum concentration is at the end of infusion, after intravenous administration of 1 g the maximum concentration is 180 μg / ml. Penetrates into the joints, tissues of the heart and vessels, into the abdominal cavity, kidneys and urinary tracts, placenta, middle ear, respiratory tract, skin and soft tissues. In small amounts excreted from breast milk. Concentration in the tissue of the gallbladder and bile is much higher than in the serum. With obstruction of the gallbladder, the concentration in the bile is less than in the plasma. The distribution of volume is 0.12 l / kg. The connection with plasma proteins is 85%. The half-life with intramuscular injection is 1.8 hours, with intravenous administration - 2 hours. If the kidney function is impaired, the half-life period is 20-40 hours.
It is excreted from the kidneys mainly in the unmodified form: During the first 6 hours - 60-90%, after 24 hours - 70-95%. After intramuscular injection at doses of 0.5 and 1 g, the maximum concentration in urine is 1 mg / ml and 4 mg / ml, accordingly.
Bacterial infections of the upper and lower respiratory tract, ENT organs (including otitis media), urinary and bile ducts, pelvic organs (including gonorrhea), skin and soft tissues, bones and joints (including osteomyelitis), endocarditis , Sepsis, peritonitis, mastitis, wound, burn and postoperative infections, syphilis.
Prevention of surgical infections in the pre- and postoperative period.
Hypersensitivity, neonatal period (up to 1 month).Carefully: impaired kidney function, enteropathy (including colitis in history), children under 1 year.
Dosage and Administration
Intramuscularly, intravenously (by stream infusion and by drop infusion). The average daily dose for adults is 1-4 g; The frequency of administration is 3-4 times a day. The maximum daily dose is 6 g. The average treatment duration is 7-10 days.
To prevent postoperative infection - intravenously, 1 g for 0.5-1 hour before surgery, 0.5-1 g - during surgery and 0.5-1 g - every 8 hours during the first 24 hours after the operation.
Patients with impaired renal function require a change in the dosing regimen in accordance with the values of creatinine clearance (CK): With SC 55 ml / min or more, or with a plasma creatinine concentration of 1.5 mg% or less, a full dose can be administered; With SC 54-35 ml / min or a plasma creatinine concentration of 3-1.6 mg%, a full dose can be given, but the intervals between injections should be increased to 8 hours; With SC 34-11 ml / min or creatinine concentration in plasma of 4.5-3.1 mg% - 1/2 dose at intervals of 12 hours; With CC 10 ml / min or less, or with a plasma creatinine concentration of 4.6 mg% or more - 1/2 of the usual dose every 18-24 hours. All recommended doses are administered after the initial dose of 0.5 g.
Children from 1 month and older - 25-50 mg / kg / day; In severe infection, the dose can be increased to 100 mg / kg / day. Frequency of administration - 3-4 times a day. In children with impaired renal function, the dosage regimen is adjusted depending on the values of creatinine clearance (CC): With SC 70-40 ml / min - 60% of the average daily dose and injected every 12 hours; With KK 40-20 ml / min - 25% of the average daily dose with an interval of 12 hours; With KK 5-20 ml / min - 10% of the average daily dose every 24 hours. All recommended doses are given after the initial "shock" dose.
For infections of moderate severity caused by sensitive Gram-positive microorganisms, a single dose for adults is 0.25-0.5 g every 8 hours. In pneumococcal pneumonia - 0.5 g every 12 hours, in acute uncomplicated diseases of the urinary tract - 1 g every 12 hours.
Preparation of solutions for injection and infusion: 0.5 g of the drug is dissolved in 2 ml of water for injection, 1 g in 4 ml of water for injection. For intravenous bolus administration, received solution is diluted with 5 ml of water for injection, then injected slowly, for 3-5 minutes. For drop infusion, 50-100 ml of 5-10% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, 5% sodium bicarbonate solution are diluted with the drug.During the reconstitution, bottles should be vigorously shaken until completely dissolved.
Powder for the preparation of an injection solution of 1.0 g in glass bottles.