ceftaroline
Brand: Teflaro
Prototype Drug
Drug Class: fifth-generation cephalosporin
Drug Family: antibiotic
Subclass: anti-MRSA cephalosporin
Organ Systems: infectious-disease
Mechanism of Action
Binds PBP2a in MRSA (and PBPs in susceptible organisms), overcoming the primary resistance mechanism of methicillin-resistant S. aureus; only FDA-approved beta-lactam with MRSA activity.
penicillin-binding protein 2a (PBP2a) in MRSA
Indications
- community-acquired bacterial pneumonia (CABP)
- acute bacterial skin and skin structure infections (ABSSSI) including MRSA
Contraindications
- cephalosporin hypersensitivity
Adverse Effects
Common
- diarrhea
- nausea
- rash
- headache
Serious
- C. difficile colitis
- anaphylaxis
- direct Coombs test positive (hemolytic anemia risk)
- neutropenia
Pharmacokinetics (ADME)
| Absorption | IV only (prodrug ceftaroline fosamil activated to ceftaroline) |
| Distribution | widely distributed; moderate protein binding |
| Metabolism | prodrug hydrolyzed to active ceftaroline; renal clearance |
| Excretion | renal (88% unchanged) |
| Half-life | 2.6 hours |
| Onset | immediate (IV) |
| Peak | end of infusion |
| Duration | 12 hours |
| Protein Binding | 20% |
| Vd | moderate |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| other beta-lactams | theoretical additive effect; generally well tolerated in combination | minor |
Nursing Considerations
- Administer IV over 60 minutes; do not mix with other medications in the same IV line.
- Monitor CBC periodically; Coombs test seroconversion occurs in up to 10% of patients and can precede hemolytic anemia.
- Reduce dose in renal impairment (CrCl <50 mL/min).
- Monitor for signs of C. difficile infection: new or worsening diarrhea, abdominal cramping, fever.
Clinical Pearls
- Ceftaroline is the only commercially available beta-lactam with activity against MRSA, achieved through its ability to bind PBP2a, the low-affinity PBP responsible for methicillin resistance.
- A positive Coombs test during ceftaroline therapy is immunologically mediated but usually clinically insignificant; monitor CBC for frank hemolytic anemia.
Safety Profile
Pregnancy generally-safe
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.