Home

helps physicians and healthcare professionals

Erectile Dysfunction

helps physicians and healthcare professionals

Doctor123.org

helps physicians and healthcare professionals

Ceftaroline Fosamil


General


Pronunciation

(sef TAR oh leen FOS a mil)


Brand Names: U.S.

  • Teflaro

Indications


Use: Labeled Indications

Pneumonia, community-acquired: Treatment of community-acquired bacterial pneumonia in adults and pediatric patients 2 months of age and older caused by Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli.

Skin and skin structure infections: Treatment of acute bacterial skin and skin structure infections in adults and pediatric patients 2 months of age and older caused by Staphylococcus aureus (including methicillin-susceptible and methicillin-resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca.


Contraindications


Known serious hypersensitivity to ceftaroline, other members of the cephalosporin class, or any component of the formulation


Dosing and Administration


Dosing: Adult

Pneumonia, community-acquired: IV: 600 mg every 12 hours for 5 to 7 days

Skin and skin structure infection: IV: 600 mg every 12 hours for 5 to 14 days


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Pneumonia, community acquired: IV:

Infants ≥2 months and Children <2 years: 8 mg/kg/dose every 8 hours for 5 to 14 days

Children ≥2 years and Adolescents <18 years:

≤33 kg: 12 mg/kg/dose every 8 hours for 5 to 14 days

>33 kg: 400 mg every 8 hours or 600 mg every 12 hours for 5 to 14 days

Adolescents ≥18 years: Refer to adult dosing.

Skin and skin structure infection: IV:

Infants ≥2 months and Children <2 years: 8 mg/kg/dose every 8 hours for 5 to 14 days

Children ≥2 years and Adolescents <18 years:

≤33 kg: 12 mg/kg/dose every 8 hours for 5 to 14 days

>33 kg: 400 mg every 8 hours or 600 mg every 12 hours for 5 to 14 days

Adolescents ≥18 years: Refer to adult dosing.


Dosing: Renal Impairment

Adult: Note: Renal function may be estimated using the Cockcroft-Gault formula for dosage adjustment purposes.

CrCl >50 mL/minute: No dosage adjustment necessary.

CrCl >30 to ≤50 mL/minute: 400 mg every 12 hours

CrCl ≥15 to ≤30 mL/minute: 300 mg every 12 hours

CrCl <15 mL/minute: 200 mg every 12 hours

ESRD patients receiving hemodialysis: 200 mg every 12 hours; dose should be given after hemodialysis on dialysis days

Pediatric: Note: Renal function may be estimated using the Schwartz equation for dosage adjustment purposes.

CrCl >50 mL/minute/1.73m2: No dosage adjustment necessary.

CrCl <50 mL/minute/1.73m2: There are no dosage adjustments provided in the manufacturers labeling (has not been studied).


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturers labeling (has not been studied). However, ceftaroline is primarily renally eliminated.


Reconstitution

Reconstitute 400 mg or 600 mg vial with 20 mL SWFI, NS, D5W, or LR. Mix gently to reconstitute (<2 minutes). Reconstituted solution should be further diluted for IV administration in 50 to 250 mL of a compatible solution. To prepare a 400 or 600 mg dose, withdraw 20 mL of diluent from 50 mL IV bag; inject the entire contents of the ceftaroline vial (also 20 mL) to achieve a total volume of 50 mL; resulting concentration is 12 mg/mL (600 mg vial) or 8 mg/mL (400 mg vial). To prepare dose for pediatric patients weighing 33 kg or less, infusion solution concentration should be ≤12 mg/mL. Use the same solution as used for reconstitution (Note: If SWFI was used for reconstitution, then appropriate infusion solutions include NS, 1/2NS, D5W, D2.5W, or LR). Color of infusion solutions ranges from clear and light to dark yellow depending on concentration and storage conditions; potency is not affected.


Administration

Administer by slow IV infusion over 5 to 60 minutes.


Storage

Store unused vials at 25 ‚ °C (77 ‚ °F); excursions permitted between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F). Diluted solutions in D2.5W, 1/2NS, D5W, LR, or NS (in infusion bags or Mini-Bag Plus) should be used within 6 hours when stored at room temperature or within 24 hours if refrigerated at 2 ‚ °C to 8 ‚ °C (36 ‚ °F to 46 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Teflaro: 400 mg (1 ea); 600 mg (1 ea)


Compatibility

Stable in D2.5W, 1/2NS, D5W, LR, NS


Drug Interactions

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Avoid combination

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Probenecid: May increase the serum concentration of Cephalosporins. Monitor therapy

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 3 days after cessation of antibacterial agents. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Cephalosporins may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy


Monitoring Parameters

Obtain specimen for culture and susceptibility prior to the first dose. Monitor for signs of anaphylaxis during first dose. Monitor renal function.


Adverse Reactions


>10%: Hematologic & oncologic: Positive direct Coombs test (10% to 11%; without hemolysis)

1% to 10%:

Cardiovascular: Phlebitis (2%), bradycardia (<2%), palpitations (<2%)

Central nervous system: Headache (3% to 5% [Steed 2010]), insomnia (3% to 4% [Steed 2010]), convulsions (<2%), dizziness (<2%)

Dermatologic: Pruritus (3% to 4% [Steed 2010]), skin rash (3%), urticaria (<2%)

Endocrine & metabolic: Hypokalemia (2%), hyperglycemia (<2%), hyperkalemia (<2%)

Gastrointestinal: Diarrhea (5%), nausea (4%), constipation (2%), vomiting (2%), abdominal pain (<2%), Clostridium difficile associated diarrhea (<2%)

Hematologic & oncologic: Anemia (<2%), eosinophilia (<2%), neutropenia (<2%), thrombocytopenia (<2%)

Hepatic: Increased serum transaminases (2%), hepatitis (<2%)

Hypersensitivity: Anaphylaxis (<2%), hypersensitivity (<2%)

Renal: Renal failure (<2%)

Miscellaneous: Fever (<2%)

<1% (Limited to important or life-threatening): Agranulocytosis


Warnings/Precautions


Special Populations: Renal Function Impairment

AUC increased 52% in moderate renal impairment (CrCl >30 to 50 mL/minute) and 115% in severe renal impairment (CrCl 15 to 30 mL/minute) as compared to patients with normal renal function. Following a 4-hour hemodialysis session, 21.6% of a single 400 mg IV dose (administered prior to hemodialysis) was recovered in the dialysate.


Special Populations: Elderly

The AUC was approximately 33% higher in elderly patients, mainly because of changes in renal function.


Warnings/Precautions

Concerns related to adverse effects:

- Hemolytic anemia: Seroconversion from a negative to a positive direct Coombs ' test has been reported. Hemolytic anemia was not reported in clinical studies; however, if anemia develops during or after treatment, consider drug-induced hemolytic anemia. Diagnostic tests should include a direct Coombs ' test. If hemolytic anemia is suspected, discontinue the drug and institute supportive care as clinically indicated.

- Hypersensitivity: Serious hypersensitivity (anaphylactic) and skin reactions have occurred with ceftaroline. Use with caution in patients with a history of penicillin, cephalosporin, or carbapenem allergy. Maintain clinical supervision if given to penicillin or beta-lactam allergic patients; cross sensitivity among beta-lactam antibacterial agents has been reported. If a serious reaction occurs, discontinue the drug and institute supportive measures as clinically indicated.

- Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis (including fatalities); CDAD has been observed >2 months postantibiotic treatment.

Disease-related concerns:

- Renal impairment: Use with caution in patients with renal impairment (CrCl ≤50 mL/minute); dosage adjustments recommended.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.


Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies.


Actions


Pharmacology

Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs) 1 through 3. This action blocks the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls and inhibits cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysis and murein hydrolases) while cell wall assembly is arrested. Ceftaroline has a strong affinity for PBP2a, a modified PBP in MRSA, and PBP2x in S. pneumoniae, contributing to its spectrum of activity against these bacteria.


Distribution

Vd: Median: 20.3 L (range: 18.3 to 21.6 L)


Metabolism

Ceftaroline fosamil (inactive prodrug) undergoes rapid conversion to bioactive ceftaroline in plasma by phosphatase enzyme; ceftaroline is hydrolyzed to form inactive ceftaroline M-1 metabolite


Excretion

Urine (~88%); feces (~6%)


Time to Peak

~1 hour


Half-Life Elimination

~1.6 hours (single dose); ~2.66 hours (multiple dose)


Protein Binding

~20%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience diarrhea, vomiting, or nausea. Have patient report immediately to prescriber signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools) (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

Copyright © 2016 - 2017
Doctor123.org | Disclaimer