TEFLARO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEFLARO (TEFLARO).
Ceftaroline fosamil is a prodrug that is converted to active ceftaroline, which binds to penicillin-binding proteins (PBPs), including PBP2a in MRSA, inhibiting bacterial cell wall synthesis.
| Metabolism | Ceftaroline fosamil is converted to active ceftaroline by phosphatases; ceftaroline undergoes minimal metabolism, primarily eliminated renally as unchanged drug. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 70%), with biliary/fecal elimination accounting for about 30%. |
| Half-life | Terminal elimination half-life is approximately 2.7 hours, allowing for twice-daily dosing in most infections. |
| Protein binding | Protein binding is approximately 20%, primarily to albumin. |
| Volume of Distribution | Volume of distribution is about 0.21 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Bioavailability: Not applicable (administered only intravenously). |
| Onset of Action | Intravenous administration: Onset of bactericidal action is rapid, with significant bacterial killing observed within 1-2 hours post-infusion. |
| Duration of Action | Duration of bactericidal activity is around 12 hours, supporting twice-daily dosing regimen. |
600 mg IV every 12 hours
| Dosage form | POWDER |
| Renal impairment | For GFR 30-49 mL/min: 400 mg IV every 12 hours; for GFR 15-29 mL/min: 300 mg IV every 12 hours; for GFR <15 mL/min (including hemodialysis): 200 mg IV every 12 hours. |
| Liver impairment | No clinically significant pharmacokinetic changes in patients with hepatic impairment; however, no specific dosing recommendations are provided for Child-Pugh classification. Use with caution in severe hepatic impairment. |
| Pediatric use | Approved for ages ≥12 years; no weight-based dosing recommended; adult dosing applies (600 mg IV every 12 hours). For pediatric patients <12 years, safety and efficacy not established. |
| Geriatric use | No specific dose adjustment required for elderly patients solely based on age; however, assess renal function and adjust dose accordingly using creatinine clearance (Cockcroft-Gault equation) as per renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEFLARO (TEFLARO).
| Breastfeeding | Excreted in human milk in low amounts; M/P ratio unknown. Considered compatible with breastfeeding due to poor oral bioavailability. Use with caution in nursing mothers, especially if infant is premature or has renal impairment. |
| Teratogenic Risk | Cephalosporins cross the placenta. Animal studies with ceftaroline fosamil show no evidence of harm at doses up to 4 times the human dose. No adequate human studies; use only if clearly needed. Risk cannot be ruled out (FDA Pregnancy Category B). First trimester: theoretical risk of neural tube defects if folate deficiency occurs (unlikely with cephalosporins). Second and third trimesters: no known fetal risks. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known serious hypersensitivity to ceftaroline fosamil or other cephalosporins"]
| Precautions | ["Hypersensitivity reactions, including anaphylaxis","Clostridioides difficile-associated diarrhea (CDAD)","Direct Coombs test conversion with potential hemolytic anemia","Seizures and other CNS events","Reduced efficacy in patients with moderate to severe renal impairment"] |
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| Fetal Monitoring | Monitor maternal renal function and CBC with differential during prolonged therapy. No specific fetal monitoring required; standard prenatal care. |
| Fertility Effects | No known adverse effects on fertility in animal studies. No human data available. |