Tseftarolina fosamil (Ceftaroline fosamil)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Cephalosporins

Included in the formulation
  • Zinforo®
    concentratepowder d / infusion 
    AstraZeneca UK Ltd     United Kingdom
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    J.01.D.I.02   Tseftarolina fosamil

    Pharmacodynamics:

    Antibiotic group of cephalosporins of the V generation.

    Has bactericidal action due to inhibition of bacterial cell wall synthesis. Violates the synthesis of the biopolymer peptidoglikana - the main component of the cell wall of bacteria. It inhibits the peptidoglycan transpeptidase, inhibits the activity of the endogenous inhibitor, which leads to activation of murein hydrolase, which cleaves peptidoglycan. Effective against fissile bacteria, in the walls of which the synthesis of peptidoglycan occurs.

    It is active against gram-positive microorganisms: Staphylococcus aureus, Streptococcus agalactiae, Streptococcus angiosus, Streptococcus dysgalactiae, Streptococcus pneumoniae, Streptococcus pyogenes; Gram-negative microorganisms: Haemophilus parainfluenzae, Haemophilus influenzae; as well as anaerobes: Fusobacterium spp., Peptostreptococcus spp., Prevotella spp., Propionibacterium acnes.

    Inactive for Chlamydophila spp., Mycoplasma spp., Legionella spp., Pseudomonas aeruginosa.

    Resistant to the action of β-lactamases.

    Pharmacokinetics:

    After intravenous administration, the maximum concentration in the blood plasma is reached after 20-30 minutes. Under the influence of phosphatases in blood plasma is converted into active ceftaroline. The connection with plasma proteins is 20%.

    After hydrolysis of the β-lactam ring of ceftaroline, an inactive metabolite is formed.

    Half-life is 2.5 hours. Elimination by the kidneys.

    Indications:

    It is used to treat complicated infections of the skin and soft tissues caused by microorganisms sensitive to ceftarolin, as well as community-acquired pneumonia.

    ICD-10

    I.B95-B97.B95   Streptococci and staphylococci as a cause of diseases classified elsewhere

    I.B95-B97.B96.1   Klebsiella pneumoniae [K.pneumoniae] as the cause of diseases classified elsewhere

    I.A00-A09.A04.0   Enteropathogenic infection caused by Escherichia coli

    XVI.P20-P29.P23.4   Congenital pneumonia caused by E. coli [Escherichia coli]

    X.J10-J18.J15.5   Pneumonia caused by Escherichia coli

    I.A00-A09.A04.4   Other intestinal infections caused by Escherichia coli

    I.A00-A09.A04.2   Enteroinvasive infection caused by Escherichia coli

    I.A00-A09.A04.1   Enterotoxigenic infection caused by Escherichia coli

    I.B95-B97.B96.3   Haemophilus influenzae [H. influenzae] as a cause of diseases classified elsewhere

    X.J10-J18.J13   Pneumonia caused by Streptococcus pneumoniae

    X.J10-J18.J14   Pneumonia caused by Haemophilus influenzae [Afanasyev-Pfeiffer's]

    X.J10-J18.J16.8   Pneumonia caused by other specified infectious agents

    XII.L00-L08.L00   Syndrome of staphylococcal skin lesions in the form of burn-like blisters

    XII.L00-L08.L02   Abscess of skin, boil and carbuncle

    XII.L00-L08.L08.0   Pyoderma

    Contraindications:

    Individual intolerance of β-lactam antibiotics: penicillins and cephalosporins, children under 18 years of age.

    Carefully:

    Imbalance of electrolytes or fluids, severe liver damage, colitis in history.

    Pregnancy and lactation:

    Recommendations for FDA - Category B. It is used with caution during pregnancy and lactation in cases where the intended benefit exceeds the risk to the fetus and newborn.

    Dosing and Administration:

    Intravenously drip for 60 minutes, 600 mg every 12 hours.

    The highest daily dose: 1.2 g.

    The highest single dose: 600 mg.

    Side effects:

    Central and peripheral nervous system: dizziness, headache, rarely convulsions.

    Digestive system: nausea, vomiting, diarrhea, increased activity of hepatic enzymes, hepatic or cholestatic jaundice, intestinal dysbacteriosis.

    Dermatological reactions: local reactions - compaction at the injection site, candidiasis dermatitis, vulvovaginitis.

    urinary system: rarely - the development of hypokalemia.

    Allergic reactions.

    Overdose:

    Nausea, vomiting, diarrhea, neuromuscular excitability, convulsive attacks.

    Treatment is symptomatic, hemodialysis.

    Interaction:

    Simultaneous use with probenecid slows the renal excretion of ceftaroline.

    "Loop diuretics" block the tubular secretion of ceftaroline.

    Special instructions:

    Ceftaroline is not recommended for the treatment of meningitis.

    Simultaneous use with ethanol can cause a disulfiram-like reaction.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    Instructions
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