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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 ...
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.
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]
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
[17] [18] One regimen for XDR-TB called Nix-TB, a combination pretomanid, bedaquiline, and linezolid, [19] has shown promise in early clinical trials. [20] Successful outcomes depend on a number of factors including the extent of the drug resistance, the severity of the disease and whether the patient's immune system is compromised.
[20] [22] These drugs were later renamed antibiotics by Selman Waksman, an American microbiologist, in 1947. [ 23 ] The term antibiotic was first used in 1942 by Selman Waksman and his collaborators in journal articles to describe any substance produced by a microorganism that is antagonistic to the growth of other microorganisms in high dilution.