In vitro activity and post-antibiotic effect of quinupristin/dalfopristin (Synercid)

Citation
Tkw. Ling et al., In vitro activity and post-antibiotic effect of quinupristin/dalfopristin (Synercid), CHEMOTHERA, 47(4), 2001, pp. 243-249
Citations number
24
Categorie Soggetti
Pharmacology,"Pharmacology & Toxicology
Journal title
CHEMOTHERAPY
ISSN journal
00093157 → ACNP
Volume
47
Issue
4
Year of publication
2001
Pages
243 - 249
Database
ISI
SICI code
0009-3157(200107/08)47:4<243:IVAAPE>2.0.ZU;2-R
Abstract
The in vitro activities of quinupristin/dalfopristin (Synercid), ampicillin , erythromycin, clarithromycin, vancomycin, teicoplanin, ciprofloxacin and tetracycline were examined and compared against 526 gram-positive bacteria. The minimal inhibitory concentrations (MICs) for quinupristin/dalfopristin against Staphylococcus aureus, including methicillin-resistant strains, we re low (MIC90 = 0.5 mg/l), and were comparable with those of vancomycin and teicoplanin. This compound was superior to the macrolides and highly activ e against Streptococcus pneumoniae (both penicillin-sensitive and penicilli n-resistant strains), with MIC90 = 2 mg/l. It was also active against other streptococci, with MIC90 = 4 mg/l. However, this agent is less active agai nst enterococci (MIC90 = 32 mg/l). Quinupristin/dalfopristin showed high ac tivity against gram-positive anaerobes, including Clostridium spp., Peptoco ccus spp. and Peptostreptococcus spp., with MIC90 less than or equal to2 mg /l. Quinupristin/dalfopristin was also investigated for its post-antibiotic effect (PAE) and bactericidal kinetics against nine strains of gram-positi ve organisms, including staphylococci, enterococci and pneumococci. Exponen tially growing (log phase) cultures were exposed to quinupristin/dalfoprist in at 2 x MIG. Growth kinetics was evaluated using viable counting. The dru g was uniformly bactericidal against pneumococci and staphylococci within 2 and 8 h of exposure, respectively. The killing activity against enterococc i was weak; there was little or no reduction in bacterial count over 24 h o f incubation. PAEs ranging from 2.13 to 3.28 h, 0.92 to 3.02 h and 1.89 to 7.07 h were produced on the tested pneumococci, staphylococci and enterococ ci, respectively. This study showed that quinupristin/dalfopristin is a pro mising agent active against gram-positive bacteria. The prolonged PAEs also suggest that the drug could be used intermittently at more widely spaced d osing intervals against grampositive organisms. Copyright (C) 2001 S. Karge r AG, Basel.