Indications

Acute Skin/Skin Structure Infection (see Cellulitis, [[Cellulitis]])

• Escherichia Coli (see Escherichia Coli, [[Escherichia Coli]])
• Klebsiella Oxytoca (see Klebsiella Oxytoca, [[Klebsiella Oxytoca]])
• Klebsiella Pneumoniae (see Klebsiella Pneumoniae, [[Klebsiella Pneumoniae]])
• Staphylococcus Aureus (see Staphylococcus Aureus, [[Staphylococcus Aureus]])
  • Methicillin-Sensitive Staphylococcus Aureus (MSSA)
  • Methicillin-Resistant Staphylococcus Aureus (MRSA)
• Streptococcus Agalactiae (see Streptococcus Agalactiae, [[Streptococcus Agalactiae]])
• Streptococcus Pyogenes (see Streptococcus Pyogenes, [[Streptococcus Pyogenes]])

Community-Acquired Pneumonia (CAP)

• Escherichia Coli (see Escherichia Coli, [[Escherichia Coli]])
• Haemophilus Influenzae (see Haemophilus Influenzae, [[Haemophilus Influenzae]])
• Klebsiella Oxytoca (see Klebsiella Oxytoca, [[Klebsiella Oxytoca]])
• Klebsiella Pneumoniae (see Klebsiella Pneumoniae, [[Klebsiella Pneumoniae]])
• Staphylococcus Aureus (see Staphylococcus Aureus, [[Staphylococcus Aureus]])
  • Methicillin-Sensitive Staphylococcus Aureus (MSSA)
• Streptococcus Pneumoniae (see Streptococcus Pneumoniae, [[Streptococcus Pneumoniae]])

---

Pharmacology

• Fifth Generation Cephalosporin Antibiotic (see Cephalosporins, [[Cephalosporins]])
  • Mechanism: inhibits bacterial cell wall synthesis
    • Binds to Penicillin-binding proteins (PBP) 1-3 -> inhibits peptidoglycan synthesis in bacterial cell wall
      • High affinity for PBP2a
      • High affinity for a modified PBP in Methicillin-Resistant Staphylococcus Aureus (MRSA)
      • High affinity for PBP2x in Streptococcus Pneumoniae
    • Bacteria eventually lyse: due to activity of cell wall autolytic enzymes

Pharmacokinetics

• Time to Peak: 1 hr
• Elimination Half-Life: 2.7 hrs

Metabolism

• Conversion: ceftaroline fosamil (inactive prodrug) undergoes rapid conversion to ceftaroline in plasma by phosphatase enzyme
  • Ceftaroline is hydrolyzed to form the inactive ceftaroline M-1 metabolite
• Renal: 88% is excreted in urine
• Hepatic: 6% is excreted in feces

---

Administration

• IV: 600 mg q12hrs IV

Dose Adjustment

• Hepatic: none
• Renal
  • CrCl >50 ml/min: no dose adjustment
  • CrCl 30-50 ml/min: 400 mg q12hrs IV
  • CrCl 15-30 ml/min: 300 mg q12hrs IV
  • CrCl <15 ml/min: 200 mg q12hrs IV

Drug Interactions

• Coumadin (see Coumadin, [[Coumadin]]): ceftaroline may enhance the effect of coumadin

---

Adverse Effects

Dermatologic Adverse Effects

• Pruritus (see Pruritus, [[Pruritus]]): occurs in 3-4% of cases
• Rash: occurs in 3% of cases

Gastrointestinal Adverse Effects

• Constipation (see Constipation, [[Constipation]]): occurs in 2% of cases
• Diarrhea (see Diarrhea, [[Diarrhea]]): occurs in 5% of cases
• Elevated Liver Function Tests (LFT’s) (see xxxx, [[]]): occurs in 2% of cases
• Nausea/Vomiting (see Nausea and Vomiting, [[Nausea and Vomiting]]): occurs in 4% of cases

Hematologic Adverse Effects

• Hemolysis (see Hemolytic Anemia, [[Hemolytic Anemia]])
  • Diagnosis: positive Coombs test

Neurologic Adverse Effects

• Headache (see Headache, [[Headache]]): occurs in 3-5% of cases

Other Adverse Effects

• Hypokalemia (see Hypokalemia, [[Hypokalemia]]): occurs in 2% of cases
• Thrombophlebitis: occurs in 2% of cases

---

References

• xxxx