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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.
Ceftobiprole has shown in vitro antimicrobial activity against a broad range of Gram-positive and Gram-negative pathogens. Among the Gram-positive pathogens, ceftobiprole has demonstrated good in vitro activity against methicillin-resistant Staphylococcus aureus, methicillin-susceptible Staphylococcus aureus and coagulase-negative staphylococci, as well as against strains of methicillin ...
Linezolid is a member of the oxazolidinone class of medications. [10] Linezolid was discovered in the mid-1990s, and was approved for commercial use in 2000. [16] [17] It is on the World Health Organization's List of Essential Medicines. [18] The World Health Organization classifies linezolid as critically important for human medicine. [19]
β-Lactam antibiotics are indicated for the prevention and treatment of bacterial infections caused by susceptible organisms. At first, β-lactam antibiotics were mainly active only against gram-positive bacteria, yet the recent development of broad-spectrum β-lactam antibiotics active against various gram-negative organisms has increased their usefulness.
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)
Ceftaroline fosamil: Teflaro: Used to treat MRSA: Gastrointestinal upset and diarrhea; Allergic reaction; Same mode of action as other beta-lactam antibiotics: disrupt the synthesis of the peptidoglycan layer of bacterial cell walls. Ceftobiprole: Zeftera
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.
Cefadroxil is a first-generation cephalosporin antibacterial drug that is the para-hydroxy derivative of cephalexin, and is used similarly in the treatment of mild to moderate susceptible infections such as the bacterium Streptococcus pyogenes, causing the disease popularly called strep throat or streptococcal tonsillitis, urinary tract infection, reproductive tract infection, and skin infections.