Ceftaroline Fosamil
- Atc Codes:J01DI02
- CAS Codes:866021-48-9
- PHARMGKB ID:866021-48-9
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Teflaro.
Drug combinations
Chemistry
Ceftaroline Fosamil Monoacetate Monohydrate: C~22~H~21~N~8~O~8~PS~4~ C~2~H~4~O~2~ H~2~O. Mw: 762.75. (6R,7R)-7-{(2Z)-2-(ethoxyimino)-2-[5-(phosphonoamino)-1,2,4-thiadiazol-3-yl]acetamido}-3-{[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate monoacetate monohydrate. CAS-866021-48-9.
Pharmacologic Category
Antibacterials; Fifth Generation Cephalosporins. (ATC-Code: J01DI02).
Mechanism of action
Ceftaroline is a cephalosporin with in vitro activity against Gram-positive and -negative bacteria. The bactericidal action of ceftaroline is mediated through binding to essential penicillin-binding proteins (PBPs). Ceftaroline is bactericidal against S. aureus due to its affinity for PBP2a and against Streptococcus pneumoniae due to its affinity for PBP2x. Ceftaroline is not active against Gram-negative bacteria producing extended spectrum β-lactamases (ESBLs) from the TEM, SHV or CTX-M families, serine carbapenemases (such as KPC), class B metallo-β-lactamases, or class C (AmpC cephalosporinases).
Therapeutic use
Treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Gram-positive and Gram-negative microorganisms: Staphylococcus aureus (including methicillin-susceptible and -resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca. Treatment of community-acquired bacterial pneumonia (CABP) caused by susceptible isolates of the following Gram-positive and Gram-negative microorganisms: Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli.
Pregnancy and lactiation implications
There are as yet no adequate, well-controlled trials in pregnant women. Not recommended during pregnancy and lactation.
Unlabeled use
Contraindications
Patients with known serious hypersensitivity to ceftaroline or other members of the cephalosporin class. Anaphylaxis and anaphylactoid reactions have been reported with ceftaroline.
Warnings and precautions
To limit the development of drug-resistant bacteria and maintain the effectiveness of antibacterial drugs, ceftaroline fosamil should be used only to treat infections that are proven or strongly suspected to be caused by bacteria. Serious and occasionally fatal hypersensitivity (anaphylactic) reactions and serious skin reactions have been reported in patients receiving beta-lactam antibacterials (if an allergic reaction to ceftaroline occurs, the drug should be discontinued and emergency treatment may be required). Clostridium difficile-associated diarrhea (CDAD) has been reported for nearly all systemic antibacterial agents, and may range in severity from mild diarrhea to fatal colitis. Seroconversion from a negative to a positive direct Coombs’ test result has occurred in patients receiving ceftaroline fosamil (if anemia develops during or after treatment, drug-induced hemolytic anemia should be considered, diagnostic studies including a direct Coombs’ test should be performed and discontinuation should be evaluated).