ceftaroline (Rx)

1-10%

Diarrhea (5%)

Nausea (4%)

Rash (3%)

Constipation (2%)

Vomiting (2%)

Increased transaminases (2%)

Hypokalemia (2%)

Phlebitis (2%)

Pyrexia (3%)

Pruritus (<3%)

Postmarketing reports

Agranulocytosis

Leukopenia

Contraindications

Hypersensitivity

Cautions

Clostridium difficile–associated diarrhea has been reported (evaluate diarrhea if it occurs)

Discontinue therapy if hypersensitivity occurs

Direct Coombs test seroconversion reported and may be indicative of drug-induced hemolytic anemia

Pregnancy Category: B

Lactation: unknown whether distributed in breast milk, caution advised

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Beta-lactam cephalosporin with activity against aerobic and anaerobic gram-positive and aerobic gram-negative bacteria

Demonstrates activity in vivo against resistant methicillin-resistant Staphylococcus aureus (MRSA) strains and in vitro against vancomycin-resistant and linezolid-resistant S aureus

Pharmacokinetics

Half-Life: 2.6 hr

Peak Plasma Concentration: 21.3 mcg/mL

Peak Plasma Time: 1 hr

Vd: 20.3 L

Protein Bound: 20%

Metabolism: Ceftaroline fosamil converted to bioactive ceftaroline in plasma by phosphatase enzyme; undergoes hydrolysis

Clearance: 9.6 L/hr

Excretion: urine (88%)

IV Compatibilities

Solution: 0.9% NaCl; D5W; 2.5% dextrose/0.45% NaCl; Lactated Ringer’s solution

IV Preparation

Reconstitute vial by adding 20 mL sterile water for injection, 0.9% NaCl, D5W, or lactated ringer’s injection; mix gently and check to ensure all powder has dissolved completely

Resulting approximate concentrations: 400 mg vial (20 mg/mL); 600 mg vial (30 mg/mL)

Color of solution ranges from clear to light-to-dark yellow depending on concentration and storage conditions

Dilution of the constituted solution

• Withdraw total volume from vial and add to 50-250 mL of 0.9% NaCl, D5W, 2.5% dextrose/0.45% NaCl, or lactated ringer’s solution; use the same diluent that was used for reconstituting (unless sterile water for injection was used)

Dilution of the constituted solution in 50 mL infusion bags

• Preparation of 600 mg dose in 50 mL infusion bag (for adult patients): withdraw 20 mL from bag before adding constituted drug; resulting concentration ~12 mg/mL
• Preparation of 400 mg dose in 50 mL infusion bag (for adult and pediatric patients weighing >33 kg): Withdraw 20 mL from bag before adding constituted drug; resulting concentration ~8 mg/mL

Preparation for children weighing ≤33 kg

• Preparation of dose in infusion bag for pediatric patients weighing ≤33 kg: Amount of solution withdrawn from the constituted vial for dilution in the infusion bag will vary according to the weight and age of the child; infusion solution concentration should not exceed 12 mg/mL ceftaroline

IV Administration

Administer IV injection via volumetric infusion pump

Infuse over 5-60 minutes

Storage

Unreconstituted vials: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

Stability of diluted drug in infusion bag or 50-mL bag

• Room temperature: 6 hr
• Refrigerated 2-8°C (36-46°F): 24 hr