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Cephepim-sanita

Cephepim-sanita

International Nonproprietary Name:

Cephepim

Pharmaceutical form:

Powder for injection solution.
  • Properties

    Cephepime is a cephalosporin antibiotic of the IV generation, which has bactericidal effect. The mechanism of its action is carried out by inhibiting the synthesis of the bacterial cell membrane. Inside the bacterial cells, the molecular intentions of Cephepime are penicillin binding proteins (PBP). Has a wide range of action. Also highly resistant to hydrolysis by most beta-lactamases and rapidly penetrates into cells of gram-negative bacteria. Effective against most strains of the following microorganisms, both in vitro and in clinical infections.

    Aerobic Gram-negative microorganisms: Cedecea, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Acinetobacter calcoaceticus, Citrobacter freundiе, Allotype Citobacter, Enterobacter agglomerans, Haemophilus influenzae (Including strains producing beta-lactamases), Hafnia alvei, Klebsiella oxytaca, Moraxela catarrhalis (including strains producing beta- Lactamase), Proteus vulgaris, Providencia stuartii, Serratia marcescens.

    Aerobic Gram-positive microorganisms: Staphylococcus aureus (only strains sensitive to methicillin), Streptococcus pyogenes (Streptococcus pneumoniae, Staphylococcus epidermidis, only strains sensitive to methicillin), Staphylococcus saprophyticus, Streptococcus agallactiae (Group B Streptococcus by Lancefeld).

    Most enterococcal strains, such as Enterococcus faecalis and staphylococcus aureus resistant to methicillin, also resistant to cephepime.

    Anaerobic microorganisms: Gram-negative bacilli (Bacteroides fragilis, other Bacteroides and Fusobacterium) Gram-positive and Gram-negative coccobacteria (including peptococci, peptostreptococcus and Velionella), Gram-positive bacilli (including Clostridium, Eubacterium and Acidobacterium).

    Pharmacokinetics

    When intravenous (iv) single dose, the pharmacokinetics of Cephepime is linear between 250 mg and 2 g. Cephepime is excreted primarily through the kidneys, the elimination of half-life (T½ ) is 2.0 hours, and the total clearance from the body of healthy volunteers occurs at a rate of 120.0 ml / min. With intramuscular (i/m) application, the drug will be completely absorbed. After a single intravenous injection, the maximum concentration (Cmax) is reached after 1.5 hours approximately. The pharmacokinetics of cephepime is linear in the range of 500 mg - 2 g, i/m. There is no evidence of accumulation in healthy adult male volunteers who received clinically significant doses for 9 days. The binding of cephepime to serum proteins is approximately 20% and does not depend on its serum concentration. The average volume of distribution in the steady state is 18.0 liters. Therapeutic concentrations are found in various body fluids, such as urine, bile, peritoneal fluid, fluid and saliva, and in body tissues such as bronchial mucosa, prostate, appendix and gallbladder. Cephepime penetrates through the inflamed blood-brain barrier. It is poorly metabolized to N-methylpyrrolidine (NMP), which rapidly converts to N-oxide (NMP-N-oxide). The excretion of cefepime occurs mainly through the kidneys, about 85% of the intake dose in unchanged form, less than 1% is excreted as NMP, 6.8% - in the form of NMP-N-oxide and 2.5% - as ephemer of cephepime.

    Slightly excreted in breast milk. The pharmacokinetics of cephepime was studied in children from 2 months to 11 years after a single and multiple doses according to the programs every 8 hours and every 12 hours. After a single IV dose, the total clearance from the Vd organism was 3.3 ml / min / kg and 0.3 l / kg, respectively. Isolation in the urine of unchanged cephepime was 60.4% of the administered dose, and the average renal clearance was 2.0 ml / min / kg. Significant effect on clearance from the body or Vd age and sex (in terms of body weight) do not have. With cephepime 50 mg / kg every 12 hours, no accumulation was observed, while Cmax, the area under the "concentration time" (AUC) curve and the decay period were increased by about 15% in a steady state after a dose of 50 mg / kg every 8 ocloc'k. The effect of cefepime in children after IV dose of 50 mg / kg is comparable to that in adults receiving an IV dose of 2 g. Absolute bioequivalence with i / m injection of 50 mg / kg of the drug was 82.3%. The pharmacokinetics of cefepime has been studied in patients with varying degrees of renal failure. Mean T ½ in patients in need of hemodialysis was 13.5 hours, and in patients requiring continuous peritoneal dialysis - 19.0 hours. In patients with impaired renal function, the total clearance of cephepime from the body decreased in proportion to the creatinine clearance (C / K), which served as the basis for adjusting the doses for this group of patients.

    In patients with impaired hepatic function, the pharmacokinetics of cephepime remained unchanged. For patients in this group, there is no need for dose adjustments.
  • Indications

    The drug is used to treat infections caused by susceptible strains of microorganisms, mentioned above. Adults and children aged 2 months to 16 years:

    • Infections of the lower respiratory tract (pneumonia and bronchitis);

    • Uncomplicated and complicated urinary tract infections (including pyelonephritis);

    • Uncomplicated intraperitoneal infections (including peritonitis and biliary tract infections);

    • Infections of the skin and soft tissues;

    • Gynecological infections, septicemia, infections with empiric therapy for patients with febrile neutropenia.

    • Children bacterial spinal meningitis;

    • Reducing the development of bacteria resistant to the drug, and to maintain the effectiveness of cephepime and other antibacterial drugs for injection.

  • Contraindications

    Hypersensitivity to cephepime, L-arginine, antibiotics of the class of cephalosporin, penicillin and other beta-lactam antibiotics, children up to 2 months.

    Carefully: Pregnancy, lactation, gastrointestinal disease (including in the anamnesis), especially colitis.

  • Dosage and Administration

    Parenteral:  In / in and / m (deep).

    Adults and children over 16 years of age or children weighing ≥ 40 kg: 1-2 g IV in one dose every 12 hours, duration of therapy 7-10 days in accordance with pathogenesis.

    Moderate and moderate infections of the urinary system: 0.5-1 g IV or IM, every 12 hours, the duration of therapy is 7-10 days.

    Acute Urinary Tract Infections: 2 g i/v every 12 hours, duration of therapy -10 days.

    In acute and life-threatening infections, you 2 g IV can be applied every 8 hours.

    In empirical treatment of febrile neutropenia: 2 g IV, every 8 hours, the usual duration of therapy is 7-10 days or until neutropenia disappears.

    For patients with disappeared signs of heat, but the remaining neutropenia should be reviewed the need to continue antimicrobial therapy.

    The dose for children aged 2 months to 12 years should not exceed the maximum recommended adult dose (2 g every 8 hours). For children weighing more than 40 mg / kg every 12 hours for 7-14 days.

    For children with bacterial spinal meningitis, a dose of 50 mg / kg can be used every 8 hours IV through a dropper.

    Empirical treatment of febrile neutropenia in children: 50 mg / kg every 12 hours (treatment of febrile neutropenia - taking the drug every 8 hours), and the duration of therapy - as in adult patients. Experience with cephepime for injections in children younger than 2 months is limited. Since the experience was obtained using a dose of 50 mg / kg, modeling pharmacokinetic data in patients older than 2 months suggests that a dose of 30 mg / kg every 12 or 8 hours can be applied to patients aged 1 to 2 months. Care should be taken when treating children younger than 2 months.

    For patients with impaired liver function, there is no need to adjust the dosage.

    In patients with impaired renal function (K / K ≤60 ml / min), the dose of cephepime for injection should be adjusted to compensate for the delayed rate of excretion through the kidneys. The recommended initial dose of cephepime for injection should be the same as for patients with normal kidney function. Recommended maintenance doses of cephepime for patients with renal failure compared with normal dose.

     

    Creatinine clearance (ml / min)> 60, the usual recommended dosing regimen

    The recommended maintenance dose

    500 mg every 12 hours

    1 g every 12 hours

    2 g every 12 hours

    2 g every 8 hours

    30-60

    500 mg every 24 hours

    1 g every 24 hours

    2 g every 24 hours

    2 g every 24 hours

    11-29

    500 mg every 24 hours

    500 mg every 24 hours

    1 g every 24 hours

    2 g every 24 hours

    < 11

    250 mg every 24 hours

    250 mg every 24 hours

    500 mg every 24 hours

    1 g every 24 hours

    Hemodialysis*

    500 mg every 24 hours

    500 mg every 24 hours

    500 mg every 24 hours

    500 mg every 24 hours

     

    1 g for the 1st day, then 500 mg every 24 hours. In days of hemodialysis cephepime should be used after hemodialysis. If possible, cephepime should be used at the same time every day.

    In patients undergoing hemodialysis, about 68% of all cephepime present in the body at the time of onset of dialysis is excreted within 3 hours of dialysis. The dose of cephepime for injection for patients on hemodialysis is indicated in the table above. For patients undergoing long-term outpatient peritoneal dialysis, cephepime for injection can be administered at the usual recommended doses every 48 hours.

    Data on pediatric use with impaired renal function are absent; However, since the pharmacokinetics of cephepime in children use is similar to that in adults, it is recommended to change the dosage regimen in proportion to the adults dose change.

    i/v use: For patients with acute or life-threatening infections, intravenous administration is preferable. For i/v infusion, dissolve 500 mg, 1 g or 2 g in 50-100 ml of 0.9% sodium chloride, 5% or 10% dextrose injection, M / 6 injection of sodium lactate, lactated Ringer. The concentration of cephepime for injection should not exceed 40 mg / ml. The IV infusion with a volume of 50 ml-100 ml should be carried out for approximately 30 minutes.

    i/ m use:  For the / m use should be added 0.5 g of cephepime for injection to 1.5 ml of solution for injection or 1.0 g-add to 3.0 ml of solution, and then inject deep i/m (the outer upper square of the large gluteal Muscles). 

    It is forbidden to dilute with novocaine!
  • Drug form
    Powder for injection solution preparation of 1.0 g in vials.