CEFTAROLINE FOSAMIL
Clinical safety rating: safe
Animal studies have demonstrated safety
Ceftaroline fosamil is a prodrug that is converted to the active metabolite ceftaroline. Ceftaroline inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), including PBP2a in MRSA and PBP2x in Streptococcus pneumoniae, thereby preventing cross-linking of peptidoglycan.
| Metabolism | Ceftaroline fosamil is metabolized by plasma phosphatases to active ceftaroline. Ceftaroline is minimally metabolized by the liver and undergoes renal elimination predominantly as unchanged drug. |
| Excretion | Renal excretion of unchanged ceftaroline accounts for approximately 88% of the administered dose. Biliary/fecal elimination is minimal (<6%). |
| Half-life | Terminal elimination half-life is approximately 2.6 hours in patients with normal renal function. This supports twice-daily dosing in most infections. |
| Protein binding | Approximately 20% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.38 L/kg, indicating distribution primarily into extracellular fluid. |
| Bioavailability | Only administered intravenously; bioavailability is 100% by the IV route. |
| Onset of Action | Intravenous administration: Onset of bactericidal activity occurs within the first hour after infusion initiation. |
| Duration of Action | Duration of bactericidal activity persists for approximately 8–12 hours post-dose, consistent with a q12h dosing interval. |
| Molecular Weight | 626.58 |
600 mg IV every 12 hours infused over 1 hour
| Dosage form | POWDER |
| Renal impairment | CrCl 30-50 mL/min: 400 mg IV every 12 hours; CrCl 15-29 mL/min: 300 mg IV every 12 hours; CrCl <15 mL/min or hemodialysis: 200 mg IV every 12 hours |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B); not studied in severe impairment (Child-Pugh C) |
| Pediatric use | For ages 2 months to <18 years: 12 mg/kg/dose IV every 8 hours (max 600 mg/dose) infused over 1 hour |
| Geriatric use | No specific dose adjustment based on age alone; adjust based on renal function as per renal adjustment guidelines |
| 1st trimester | Limited human data; animal studies have not shown teratogenicity. Use only if clearly needed. |
| 2nd trimester | No known risk in animal studies; human data limited. Considered acceptable with caution. |
| 3rd trimester | No known risk; potential for neonatal infection should be considered if used near delivery. |
Clinical note
Drugs that prolong the QT interval may have additive effects May cause diarrhea including Clostridium difficile-associated diarrhea.
| Placental transfer | Transfers across the placenta in animal studies; human data limited. |
| Breastfeeding | Excreted into breast milk in small amounts; unlikely to cause adverse effects in infant. Use with caution. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Diarrhea |
| Serious Effects |
Hypersensitivity to ceftaroline fosamil or other cephalosporinsHypersensitivity to beta-lactam antibiotics
| Precautions | Hypersensitivity reactions: Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported., Clostridioides difficile-associated diarrhea (CDAD): May range from mild diarrhea to fatal colitis., Direct Coombs test seroconversion: May occur and may interfere with cross-matching or antibody testing., Seizures: Potential for CNS adverse reactions including seizures, especially in patients with renal impairment., Renal impairment: Dose adjustment required for patients with moderate to severe renal impairment. |
| Food/Dietary | No specific food interactions. However, avoid alcohol ingestion in cases of liver dysfunction or if other interacting drugs are used. No restrictions on diet. |
Loading safety data…
| L2 (Probably Compatible) |
| Teratogenic Risk | Ceftaroline fosamil is a cephalosporin antibiotic classified as FDA Pregnancy Category B. Animal reproduction studies have not demonstrated fetal harm, but no adequate and well-controlled studies exist in pregnant women. There is no evidence of teratogenicity in first trimester. Risk cannot be ruled out; use only if clearly needed. |
| Fetal Monitoring | No specific fetal monitoring required. Monitor maternal renal function, complete blood count (CBC) with differential, and signs of Clostridioides difficile-associated diarrhea. For prolonged use, assess for superinfection. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at clinically relevant doses. |
| Clinical Pearls | Ceftaroline fosamil, a fifth-generation cephalosporin, has activity against MRSA due to its affinity for PBP2a. It is also active against many Gram-negative pathogens including Enterobacteriaceae but not ESBL-producing strains. Note that it does not cover Pseudomonas aeruginosa. It is used for community-acquired bacterial pneumonia (CABP) and acute bacterial skin and skin structure infections (ABSSSI). Like other beta-lactams, it is time-dependent and requires prolonged infusion for optimal pharmacokinetic/pharmacodynamic target attainment (e.g., over 2 hours). It may cause false-positive Coombs test (direct antiglobulin test) and rarely immune-mediated hemolytic anemia. Adjust dose in renal impairment (CrCl ≤50 mL/min). |
| Patient Advice | Take this medication exactly as prescribed; it is given intravenously by a healthcare provider. · Tell your doctor if you have a history of allergies to penicillins, cephalosporins, or other beta-lactams. · Report any signs of allergic reaction such as rash, hives, difficulty breathing, or swelling of the face/throat. · Notify your healthcare provider if you experience severe diarrhea, especially if watery or bloody, as this may indicate Clostridioides difficile infection. · Inform your doctor if you have kidney problems, as dose adjustments may be necessary. · Keep all appointments for blood tests to monitor kidney function and blood cell counts. |