Oxazolidinones: a new class of antibacterials.
The oxazolidinones represent the first truly new class of antibacterial agents to reach the marketplace in several decades. They have a unique mechanism of action involving inhibition of the initiation step of protein synthesis and are not cross-resistant to other classes of antibiotics. The first marketed member of that class, linezolid (Zyvox), shows good efficacy with an impressive antibacterial spectrum (including activity against gram-positive organisms resistant to other drugs), and a pharmacodynamic/pharmacokinetic relationship best characterized by time above the minimum inhibitory concentration. The agent is effective by both the intravenous and oral route of administration. Although technically classified as bacteriostatic against a number of pathogens in vitro, linezolid behaves in vivo like a bactericidal antibiotic.
Zurenko
G E
GE
Discovery Research, Pharmacia, Kalamazoo, MI 49007, USA. gary.e.zurenko@pharmacia.com
Gibson
J K
JK
Shinabarger
D L
DL
Aristoff
P A
PA
Ford
C W
CW
Tarpley
W G
WG
D000818:Animals; D000890:Anti-Infective Agents / Q000145:classification* / Q000494:pharmacology* / Q000627:therapeutic use; D001424:Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D023303:Oxazolidinones / Q000145:classification* / Q000494:pharmacology* / Q000627:therapeutic use
D000890:Anti-Infective Agents; D023303:Oxazolidinones