ceftaroline (Teflaro)

Indications

• treatment of bacterial infections due to susceptible organisms
  • bacterial skin infections including MRSA
  • community-acquired pneumonia (except MRSA)
    • multidrug-resistant Streptococcus pneumoniae

Contraindications

• not approved for children (< 18 years of age)
• pregnancy category: B
• safety in lactation: ?

Dosage

• 600 mg IV every 12 hours

Powder:

• 400 & 600 mg vials
• reconstitute with 20 mL of sterile water
• must be added to at least 250 mL of a diluent such as normal saline or D5W prior to infusion
• solution stable for 6 hours at room temperature or overnight refrigerated

Dosage adjustment in renal failure

• 400 mg for creatinine clearance < 50 mL/min
• 300 mg for creatinine clearance < 50 mL/min
• 200 mg for ESRD or hemodialysis
• all dosing every 12 hours

Antimicrobial activity

• Gram-positive bacteria
  • Staphylococcus (MSSA, MRSA)
    • linezolid, daptomycin & vancomycin resistant S aureus
  • Streptococcus
    • multidrug-resistant Streptococcus pneumoniae
• Gram-negative bacteria
  • Haemophilus influenzae
  • Klebsiella pneumoniae
  • Moraxella catarrhalis
  • Escherichia coli
• does NOT cover: Enterococcus, Pseudomonas, most anaerobes

Adverse effects

• rash (3%)
• diarrhea (5%), constipation (2%)
• nausea (4%), vomiting (2%)
• increased transaminases (2%), hyperkalemia (2%)
• phlebitis (2%)

• drug adverse effects of cephalosporins

Drug interactions

• none reported, no studies
• does not appear to interact with cyt P450

• drug interaction(s) anticonvulsants with anti-bacterial agents
• drug interaction(s) of antibiotics with warfarin

Mechanism of action

• 1st cephalosporin with activity against MRSA

More general terms

• cephalosporin, 5th generation

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=16007393
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=9852981
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=9962077