Ceftaroline fosamil


Generic Medicine Info
Indications and Dosage
Intravenous
Community-acquired pneumonia
Adult: 600 mg 12 hourly via infusion over 5-60 minutes for 5-7 days.
Child: Neonates to <2 months 6 mg/kg 8 hourly; ≥2 months to <2 years 8 mg/kg 8 hourly; ≥2-<12 years 12 mg/kg (Max: 400 mg) 8 hourly. 12-<18 years weighing <33 kg: 12 mg/kg (Max: 400 mg) 8 hourly; 12-<18 years weighing ≥33 kg: Same as adult dose. All doses are given via infusion over 60 minutes for 5-7 days. Dosage recommendation may vary among countries or individual products. Refer to specific product guidelines.

Intravenous
Complicated skin and skin structure infections
Adult: 600 mg 12 hourly via infusion over 60 minutes for 5-14 days. Alternatively, as high dose regimen for cases confirmed or suspected to be caused by S. aureus with a minimum inhibitory concentration of 2-4 mg/mL: 600 mg 8 hourly via infusion over 120 minutes.
Child: Neonates to <2 months 6 mg/kg 8 hourly; 2 months to <2 years 8 mg/kg 8 hourly; 2-<12 years 12 mg/kg (Max: 400 mg) 8 hourly. 12-<18 years weighing <33 kg: 12 mg/kg (Max: 400 mg) 8 hourly; 12-<18 years weighing ≥33 kg: Same as adult dose. All doses are given via infusion over 60 minutes for 5-14 days. Alternatively, as high dose regimen for cases confirmed or suspected to be caused by S. aureus with a minimum inhibitory concentration of 2-4 mg/mL: 2 months to <2 years 10 mg/kg 8 hourly; ≥2 years to <18 years 12 mg/kg (Max: 600 mg) 8 hourly. All doses are given via infusion over 120 minutes for 5-14 days. Dosage recommendation may vary among countries or individual products. Refer to specific product guidelines.
Renal Impairment
ESRD patients on haemodialysis: 200 mg 12 hourly.

 CrCl (mL/min)
Dosage
<15
200 mg 12 hourly.
15-30
300 mg 12 hourly.
31-50
400 mg 12 hourly.
Reconstitution
Reconstitute vial labelled as 400 or 600 mg with 20 mL sterile water for inj, 0.9%NaCl, 5% dextrose in water, or lactated Ringer’s solution to provide a 20 or 30 mg/mL solution respectively; gently mix for approx 2 minutes. Further dilute with the same diluent used for the initial solution, unless sterile water for inj is used. Instructions for further reconstitution may vary according to patient’s weight and specific dose to be given (refer to specific product guidelines).
Contraindications
Hypersensitivity to ceftarolin fosamil and to other cephalosporin antibiotics, immediate and severe hypersensitivity to other β-lactam antibiotics (e.g. penicillins, carbapenems).
Special Precautions
Patient with a history of non severe hypersensitivity to other β-lactam antibiotics (e.g. penicillins, carbapenems), pre-exisiting or history of seizure disorder. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Haemolytic anaemia, neurotoxicity (e.g. encephalopathy, seizures); severe cutaneous adverse reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms, acute generalised exanthematous pustulosis).
Gastrointestinal disorders: Diarrhoea, nausea, vomiting, abdominal pain.
General disorders and administration site conditions: Pyrexia, infusion site reactions (e.g. phlebitis, erythema, pain).
Investigations: Increased transaminases.
Nervous system disorders: Headache, dizziness.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Potentially Fatal: Hypersensitivity reactions (e.g. anaphylaxis), bacterial superinfection including Clostridium difficile-associated diarrhoea and pseudomembranous colitis.
IV/Parenteral: B
Monitoring Parameters
Perform culture and susceptibility tests prior to treatment initiation; consult local institutional recommendation before treatment initiation due to antibiotic resistance risks. Monitor renal function and assess for signs of anaphylaxis during first dose.
Lab Interference
May cause seroconversion from a negative to a positive direct Coomb's test.
Action
Description: Ceftaroline fosamil is a 5th generation cephalosporin. It binds to penicillin-binding proteins (PBPs) 1-3 which inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell wall, thus inhibiting biosynthesis and arresting cell wall assembly resulting in bacterial cell lysis and death. It has strong affinity to PBP2a (a modified PBP in MRSA) and PBP2x in S. pneumoniae.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 1 hour.
Distribution: Volume of distribution: 20.3 L. Plasma protein binding: Approx 20%.
Metabolism: Rapidly metabolised in the plasma into ceftaroline by phosphatase enzymes; further metabolised via hydrolysis into ceftaroline M-1 (inactive metabolite).
Excretion: Mainly via urine (approx 88%, mainly as unchanged drug); faeces (approx 6%). Elimination half-life: Approx 2.66 hours.
Chemical Structure

Chemical Structure Image
Ceftaroline fosamil

Source: National Center for Biotechnology Information. PubChem Database. Ceftaroline fosamil, CID=9852981, https://pubchem.ncbi.nlm.nih.gov/compound/Ceftaroline-fosamil (accessed on Jan. 21, 2020)

Storage
Store below 30°C. Protect from light. Reconstituted solution: Stable for 6 hours at room temperature or for 24 hours between 2-8°C.
MIMS Class
Cephalosporins
ATC Classification
J01DI02 - ceftaroline fosamil ; Belongs to the class of other cephalosporins and penems. Used in the systemic treatment of infections.
References
Anon. Ceftaroline Fosamil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/04/2021.

Anon. Ceftaroline. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 23/06/2021.

Buckingham R (ed). Ceftaroline Fosamil Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/04/2021.

Joint Formulary Committee. Ceftaroline Fosamil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/04/2021.

Teflaro Powder for Solution (Allergan, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/04/2021.

Zinforo 600 mg Powder for Concentrate for Solution for Infusion (Facta Farmaceutici S. p. A.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 08/04/2021.

Zinforo 600 mg Powder for Concentrate for Solution for Infusion (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 08/04/2021.

Disclaimer: This information is independently developed by MIMS based on Ceftaroline fosamil from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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