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. |
| Molecular Weight | 604.66 Da |
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 | Limited human data; animal studies show no evidence of fetal harm. Use only if clearly needed. |
| 2nd trimester | No known risk; use if benefit outweighs risk. |
| 3rd trimester | No known risk; use if benefit outweighs risk. |
Clinical note
Comprehensive clinical and safety monograph for TEFLARO (TEFLARO).
| Placental transfer | Crosses placenta; fetal concentrations are approximately 10% of maternal serum concentrations. |
| Breastfeeding | Ceftaroline is excreted in human milk in low concentrations. Consider the developmental and health benefits of breastfeeding, the mother's clinical need, and any potential adverse effects on the breastfed child. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to ceftaroline or other cephalosporinsSevere hypersensitivity (e.g., anaphylaxis) to penicillins or other beta-lactams
| 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 |
| Food/Dietary | No significant food interactions. Teflaro is administered intravenously, so oral intake does not affect absorption. No dietary restrictions required. |
| Clinical Pearls |
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| 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. |
| 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. |
| Teflaro (ceftaroline fosamil) is a fifth-generation cephalosporin with activity against MRSA due to its high affinity for PBP2a. It is FDA-approved for acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP). Notably, it has no activity against Pseudomonas aeruginosa or ESBL-producing Enterobacteriaceae. Dose adjustment required for CrCl ≤50 mL/min; use caution in penicillin-allergic patients (cross-reactivity ~10%). Monitor for neutropenia, especially with prolonged therapy >10 days. |
| Patient Advice | Complete the full course of antibiotics even if you feel better. · Report any signs of allergic reaction: rash, hives, difficulty breathing. · Tell your doctor if you have kidney problems or are on dialysis. · Notify your physician if you experience severe diarrhea (possible C. diff infection). · Teflaro is given intravenously; you will receive it in a healthcare setting. |