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Ceftaroline fosamil is a prodrug of ceftaroline. It is active against methicillin-resistant Staphylococcus aureus (MRSA) and other Gram-positive bacteria. It retains some activity of later-generation cephalosporins having broad-spectrum activity against Gram-negative bacteria, but its effectiveness is relatively much weaker.
Ceftaroline has low water solubility but this problem was overcome by attaching a N-phosphonoamino group to the molecule making the intravenous prodrug ceftaroline fosamil. The prodrug is dephosphorylated in plasma to form active ceftaroline. [28] 5th generation cephalosporins: A) ceftaroline fosamil (prodrug); B) ceftobiprole medocaril (prodrug)
Ceftobiprole, sold under the brand name Zevtera among others, is a fifth-generation [7] cephalosporin antibacterial used for the treatment of hospital-acquired pneumonia (excluding ventilator-associated pneumonia) and community-acquired pneumonia. It is marketed by Basilea Pharmaceutica under the brand names Zevtera and Mabelio.
Ceftaroline has also been described as "fifth-generation" cephalosporin, but does not have the activity against Pseudomonas aeruginosa or vancomycin-resistant enterococci that ceftobiprole has. [36] Ceftolozane is an option for the treatment of complicated intra-abdominal infections and complicated urinary tract infections.
The β-lactam core structures. (A) A penam.(B) A carbapenam.(C) An oxapenam.(D) A penem.(E) A carbapenem.(F) A monobactam.(G) A cephem.(H) A carbacephem.(I) An oxacephem. This is a list of common β-lactam antibiotics—both administered drugs and those not in clinical use—organized by structural class.
Ceftolozane exerts bactericidal activities against susceptible gram-negative and gram-positive infections by inhibiting essential penicillin-binding proteins (PBPs), which are required for peptidoglycan cross-linking for bacterial cell wall synthesis, resulting in inhibition of cell wall synthesis and subsequent cell death.
Cephalosporins (Fourth generation) Cefepime: Maxipime: Covers pseudomonal infections. Gastrointestinal upset and diarrhea; Nausea (if alcohol taken concurrently) Allergic reactions; Same mode of action as other beta-lactam antibiotics: disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. Cephalosporins (Fifth generation ...
Ceftazidime/avibactam is used to treat certain multidrug-resistant gram-negative infections. [10]Ceftazidime/avibactam is used for the treatment of: complicated intra-abdominal infections.