Ceftaroline is a novel, broad-spectrum, advanced-generation
cephalosporin whose action is mediated by binding to
penicillin-binding proteins in bacteria, consistent with other
beta-lactam antibiotics.
Ceftaroline is distinct in that it has antimicrobial activity against multidrug-resistant Staphylococcus aureus (including methicillin-resistant S. aureus,
vancomycin-intermediate S. aureus [VISA], heteroresistant VISA, and
vancomycin-resistant S. aureus), Streptococcus
pneumonia (including
drug-resistant strains), and respiratory gram-negative pathogens such as Moraxella catarrhalis and Haemophilus influenzae (including
beta-lactamase-positive strains). Development of resistance to
ceftaroline occurs rarely in gram-positive bacteria and at a similar rate to that of other oxyimino-
cephalosporins in gram-negative bacteria. The inactive
prodrug,
ceftaroline fosamil, is administered by
intravenous infusion and rapidly undergoes biotransformation to
ceftaroline.
Ceftaroline then follows a two-compartment pharmacokinetic model and is eliminated primarily by renal excretion, with a half-life of approximately 3 hours. Similar to other
cephalosporins, time above the minimum inhibitory concentration is the pharmacodynamic parameter that best predicts efficacy for
ceftaroline.
Ceftaroline 600 mg intravenously every 12 hours has been shown to have similar efficacy to
vancomycin plus
aztreonam for the treatment of complicated skin and skin structure
infections and to
ceftriaxone for the treatment of community-acquired
bacterial pneumonia in phase III clinical trials.
Ceftaroline displayed a safety profile similar to that of other
cephalosporins in clinical trials. Dosage adjustment is required for moderate renal impairment and for patients receiving
hemodialysis.
Ceftaroline breakpoints have been proposed but not confirmed.
Ceftaroline is a renally excreted broad-spectrum
cephalosporin that is clinically effective for the treatment of complicated skin and skin structure
infections and community-acquired
bacterial pneumonia, and it has distinctive activity against some difficult-to-treat multidrug-resistant gram-positive organisms.