Ceftalin600 mg/vial

Ceftalin is a fifth-generation (advanced-generation) cephalosporin antibiotic with activity against methicillin-resistant Staphylococcus aureus (MRSA). It is administered only by intravenous (IV) infusion and is FDA-approved for the following indications:

Established / FDA-approved uses

• Acute Bacterial Skin and Skin Structure Infections (ABSSSI) caused by susceptible strains of Staphylococcus aureus (including MRSA and methicillin-susceptible strains), Streptococcus pyogenes, Streptococcus agalactiae, and Escherichia coli, in adults and pediatric patients (≥34 weeks gestational age and ≥12 days postnatal age).
• Community-Acquired Bacterial Pneumonia (CABP) caused by susceptible strains of Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible strains only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli, in adults and pediatric patients ≥2 months of age.

Ceftalin is reserved for infections that are known or strongly suspected to be caused by susceptible bacteria; it is not intended for routine empiric use where a resistant-organism indication has not been established, consistent with antibiotic stewardship principles.

Each vial contains Ceftaroline Fosamil as a sterile, white to light yellow lyophilized powder for reconstitution, typically available as 400 mg or 600 mg per vial for intravenous infusion after reconstitution and dilution. Ceftaroline Fosamil is the water-soluble prodrug that is rapidly converted in plasma to its active form, ceftaroline.

Ceftalin is an advanced-generation (often termed "fifth-generation") cephalosporin antibacterial agent. Unlike most other cephalosporins, it has clinically useful activity against MRSA in addition to many Gram-positive and selected Gram-negative organisms. It is supplied as a sterile powder for intravenous infusion and is used exclusively in a hospital or supervised clinical setting for serious bacterial infections of the skin/skin structures and the lungs.

Ceftalin belongs to the cephalosporin class of beta-lactam antibiotics, specifically classified as an advanced-generation (fifth-generation) cephalosporin with anti-MRSA activity.

Mechanism of action

Ceftaroline Fosamil is a prodrug that is rapidly hydrolyzed in plasma to ceftaroline, the microbiologically active moiety. Ceftaroline exerts bactericidal activity by binding to and inhibiting essential penicillin-binding proteins (PBPs) involved in bacterial cell wall synthesis. Its high binding affinity for PBP2a (the altered PBP responsible for methicillin resistance in Staphylococcus aureus) and for PBP2x in Streptococcus pneumoniae underlies its activity against MRSA and penicillin-non-susceptible pneumococci.

Pharmacokinetics

Following intravenous infusion, Ceftaroline Fosamil is converted to ceftaroline with peak plasma concentrations occurring near the end of infusion. Ceftaroline is minimally protein-bound (approximately 20%), is not significantly metabolized by the liver, and is primarily eliminated renally, largely unchanged; the elimination half-life is approximately 2.5 hours in adults with normal renal function, which is why dose adjustment is required in renal impairment.

Ceftalin is reconstituted and further diluted, then infused intravenously over 5 to 60 minutes under the supervision of a qualified healthcare professional, typically in a hospital or infusion clinic setting. It must not be administered as an IV bolus injection or mixed in the same infusion line as calcium-containing products such as Ringer's or Hartmann's solution.

Ceftalin has a low potential for clinically significant drug interactions. It does not meaningfully inhibit or induce the major cytochrome P450 (CYP450) hepatic enzymes, and population pharmacokinetic analyses have not identified clinically relevant interactions with commonly co-administered medications.

• Probenecid: May theoretically reduce renal clearance of ceftaroline by competing for tubular secretion; clinical significance is minimal and no dose adjustment is routinely required.
• Other nephrotoxic drugs (e.g., aminoglycosides, certain diuretics): Concurrent use warrants monitoring of renal function, since Ceftalin dosing depends on renal clearance (see Precautions).
• Direct antiglobulin (Coombs) test interference: Concomitant drugs or conditions that also affect the Coombs test may confound interpretation (see Precautions and Warnings).

The most commonly reported adverse effects of Ceftalin in adults (each occurring in more than 2% of patients) include diarrhea, nausea, and rash. In pediatric patients, diarrhea, vomiting, rash, fever, and nausea were most common.

• Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain.
• Dermatologic: Rash, pruritus.
• Hematologic: Positive direct Coombs test seroconversion; rare hemolytic anemia (see Precautions).
• Hypersensitivity reactions: Ranging from mild rash to anaphylaxis (see Contraindications and Precautions).
• Gastrointestinal (severe): Clostridioides difficile-associated diarrhea/colitis, which can range from mild to life-threatening.
• Neurological (uncommon, mainly with renal impairment/inappropriate dosing): Headache, dizziness; rare reports of encephalopathy and seizures (see Precautions).
• Other: Elevated liver enzymes, phlebitis at the infusion site, fever.

Pregnancy: Adequate and well-controlled studies of Ceftalin in pregnant women are not available. Animal reproduction studies have not shown evidence of harm to the fetus at exposures several times the maximum recommended human dose. Ceftalin should be used during pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus; consult a physician before use in pregnancy.

Lactation: It is not known whether Ceftalin/ceftaroline is excreted in human breast milk. Caution should be exercised when Ceftalin is administered to a breastfeeding mother, weighing the benefits of treatment against any potential risk to the nursing infant; consult a physician.

• Hypersensitivity reactions: Serious hypersensitivity reactions, including anaphylaxis, have been reported with Ceftalin. Discontinue immediately if an allergic reaction occurs and institute appropriate treatment. Use with caution in patients with a history of penicillin allergy due to possible cross-reactivity.
• Clostridioides difficile-associated diarrhea (CDAD): As with nearly all antibiotics, Ceftalin can permit overgrowth of C. difficile, ranging from mild diarrhea to fatal colitis. Consider this diagnosis in patients who develop diarrhea during or after treatment.
• Direct Coombs test seroconversion and hemolytic anemia: Seroconversion from a negative to a positive direct antiglobulin (Coombs) test has been observed with Ceftalin use, and rare cases of hemolytic anemia have been reported. If anemia develops during or after treatment, drug-induced hemolytic anemia should be considered and Ceftalin discontinued if confirmed.
• Renal impairment: Dose adjustment is required based on creatinine clearance (see Dosage & Administration). Renal function should be monitored, particularly in patients with changing renal status.
• Neurological effects: Encephalopathy and seizures have been reported, particularly when dosing has not been appropriately adjusted for renal impairment; these are generally reversible upon discontinuation.
• Reserve for appropriate use: Ceftalin should be reserved for infections proven or strongly suspected to be caused by susceptible bacteria (including MRSA) and is not intended for empiric use outside this context, to help preserve its effectiveness against resistant organisms.
• Superinfection: Prolonged use may result in overgrowth of non-susceptible organisms, including fungi.
• Antibiotic stewardship: Take Ceftalin exactly as prescribed by your physician; do not stop, extend, skip doses, or share this medicine with others without medical advice.

There is no specific antidote for Ceftalin overdose. In the event of a suspected overdose, seek immediate medical attention or contact emergency services/poison control. Management is supportive, with monitoring for adverse effects such as gastrointestinal symptoms or neurological changes. Ceftaroline can be removed from the circulation by hemodialysis, which may be considered in patients with renal impairment who receive an excessive dose.

Store unreconstituted vials at room temperature (below 30°C), protected from light. After reconstitution and dilution, use within the time and temperature limits specified by the healthcare provider or pharmacy (typically requiring refrigeration if not used promptly). Keep out of reach of children. This medicine is administered by a healthcare professional and is not intended for home storage or self-administration.

• Renal impairment: Dose reduction is required in moderate to severe renal impairment and end-stage renal disease/hemodialysis (see Dosage & Administration). Ceftalin should be used with caution and appropriate monitoring in these patients.
• Hepatic impairment: No dose adjustment is considered necessary based on available pharmacokinetic data, as Ceftalin undergoes minimal hepatic metabolism; however, clinical experience in significant hepatic impairment is limited.
• Elderly patients: Dose should be selected based on renal function, since elderly patients more frequently have decreased renal function; no dedicated age-based dose adjustment beyond renal-based adjustment is required.
• Pediatric patients: Approved for ABSSSI from ≥34 weeks gestational age/≥12 days postnatal age, and for CABP from ≥2 months of age, using weight-based dosing (see Pediatric Uses).

Duration of Ceftalin therapy is indication-specific: typically 5 to 14 days for Acute Bacterial Skin and Skin Structure Infections (ABSSSI), and 5 to 7 days for Community-Acquired Bacterial Pneumonia (CABP). The exact duration should be determined by the treating physician based on clinical response and severity of infection. Patients should complete the full prescribed course even if symptoms improve earlier.

Ceftalin is supplied as a sterile lyophilized powder that must be reconstituted before use. Each vial is reconstituted with the recommended volume of sterile water for injection, 0.9% sodium chloride injection, 5% dextrose injection, or lactated Ringer's injection, then gently agitated until fully dissolved to form a clear, light yellow solution. The reconstituted solution is then further diluted in an appropriate infusion volume (typically 50–250 mL) before intravenous infusion. Reconstitution and dilution should be performed by a trained healthcare professional using aseptic technique; do not mix with calcium-containing diluents such as Ringer's or Hartmann's solution in the same line.

Cephalosporins (beta-lactam antibiotics); advanced-generation (fifth-generation) cephalosporin with anti-MRSA activity.

Ceftaroline Fosamil is hydrolyzed in plasma to its active form, ceftaroline, which binds to penicillin-binding proteins (PBPs) that are essential for bacterial cell wall synthesis, resulting in bactericidal activity. Its distinguishing feature is high-affinity binding to PBP2a, the altered penicillin-binding protein responsible for methicillin resistance in Staphylococcus aureus (MRSA), and to PBP2x in penicillin-non-susceptible Streptococcus pneumoniae, which gives it activity against these otherwise difficult-to-treat organisms.

B

Ceftalin is approved for use in pediatric patients for specific indications and age ranges, with dosing based on age and body weight:

• Acute Bacterial Skin and Skin Structure Infections (ABSSSI): Approved from birth (≥34 weeks gestational age and ≥12 days postnatal age) through 17 years of age.
• Community-Acquired Bacterial Pneumonia (CABP): Approved from 2 months through 17 years of age.

Safety and efficacy in neonates younger than 34 weeks gestational age or younger than 12 days postnatal age, and use for indications outside ABSSSI/CABP in children, have not been established. Pediatric dosing must be calculated carefully by weight and renal function; see the Dosage & Administration section for exact regimens.