Purpose: The pharmacokinetics, pharmacodynamics, clinical efficacy, and safety of ceftaroline are reviewed.
Summary: Ceftaroline, a new broad- spectrum antibiotic, is approved for the treatment of complicated skin and skin structure infections (cSSSIs) and community- acquired pneumonia (CAP). This β-lactam antibiotic has extended activity against gram-positive organisms and has activity against common gram-negative organisms. The drug's spectrum of activity includes both methicillin-resistant Staphylococcus aureus and multidrug-resistant Streptococcus pneumoniae. However, its activity against extended-spectrum β-lactamase-producing bacteria is limited. These bacteria, particularly those that express AmpC β-lactamase, greatly reduce the activity of ceftaroline. The prodrug of ceftaroline (ceftaroline fosamil) is rapidly converted to its active form (ceftaroline) in plasma. This dose-linear drug has been found to be pharmacodynamically best correlated with the percentage of time that free drug concentrations remain above the minimum inhibitory concentration. Ceftaroline's safety profile is similar to that of the other cephalosporins, with minimal adverse drug reactions, most of which are considered mild. Currently available pharmacokinetic, animal, and clinical studies have found that ceftaroline has reasonable efficacy and tolerability but have also revealed that dosing regimen modifications may be needed in patients with moderate-to-severe renal impairment. The recommended dosage of ceftaroline for the treatment of cSSSIs and CAP is 600 mg infused intravenously over 60 minutes every 12 hours. The recommended duration of therapy is 5-14 and 5-7 days for cSSSIs and CAP, respectively. Additional Phase III studies are currently underway.
Conclusion: Ceftaroline is a new broad-spectrum cephalosporin indicated for the treatment of cSSSIs and CAP caused by susceptible gram-positive and gram-negative organisms.