Ceftaroline
The cephalosporin that binds PBP2a — a beta-lactam that actually works against MRSA, often used as salvage therapy in persistent bacteraemia.
At a glance
- Brand names: Teflaro, Zinforo
- Route: Intravenous
How it works
Ceftaroline is a fifth-generation cephalosporin whose side chain lets it bind PBP2a, the altered penicillin-binding protein that makes MRSA resistant to all other beta-lactams.
By binding PBP2a it blocks cell-wall cross-linking and kills the organism, giving beta-lactam bactericidal activity against MRSA.
It is frequently combined with daptomycin in refractory bacteraemia, where the two drugs act synergistically.
Dosage regime and monitoring
- 600 mg intravenously every 12 hours over 5–60 minutes for skin infection and community-acquired pneumonia.
- Many centres use 600 mg every 8 hours for MRSA bacteraemia, endocarditis and bone infection, which is off-label but supported by observational data.
- The dose is reduced in moderate and severe kidney impairment.
- Weekly full blood counts are advised on prolonged therapy.
Doses listed are typical adult regimens quoted for reference. The actual dose, route and duration are decided by a clinician for the individual patient.
How the drug was developed
Ceftaroline was developed by Takeda in Japan as the prodrug ceftaroline fosamil and licensed to Cerexa, later Forest Laboratories.
It was approved by the FDA in 2010 for acute bacterial skin infection and community-acquired pneumonia — the first beta-lactam licensed with MRSA activity.
Its use in bloodstream infection grew from salvage experience rather than registration trials.
Side effects and warnings
- Neutropenia and agranulocytosis with courses beyond two weeks — the main reason for weekly blood counts.
- Diarrhoea, nausea, rash and a positive direct Coombs test that is usually not clinically significant.
- Hypersensitivity reactions; caution in severe penicillin allergy.
Other uses
- Community-acquired bacterial pneumonia caused by pneumococci, including penicillin-resistant strains.
- Complicated skin and soft-tissue infection with mixed Gram-positive and Gram-negative organisms.
- US National Library of Medicine. DailyMed prescribing information database (2025)
- Clinical Infectious Diseases. Daptomycin plus ceftaroline versus standard therapy for MRSA bacteraemia (2020)
- Infectious Diseases Society of America. Clinical practice guidelines for the treatment of methicillin-resistant Staphylococcus aureus infections (2011)
Vancomycin
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Cubicin
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