Evaluation of Bactericidal Activities of LY333328, Vancomycin, Teicoplanin, Ampicillin-Sulbactam, Trovafloxacin, and RP59500 Alone or in Combination with Rifampin or Gentamicin against Different Strains of Vancomycin-Intermediate
            <i>Staphylococcus aureus</i>
            by Time-Kill Curve Methods

Hershberger, Ellie; Aeschlimann, Jeffrey R.; Moldovan, Tabitha; Rybak, Michael J.

doi:10.1128/aac.43.3.717

Cited by 49 publications

(26 citation statements)

References 5 publications

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“…A property that distinguishes oritavancin from vancomycin is rapid, dose‐dependent bactericidal activity (Fig. 4) against enterococci [19,21,73,86–91], staphylococci (including MRSA and VISA) [87,92–94], and S. pneumoniae [79,95,96]. This has been demonstrated by MIC/MBC comparisons, by in vitro time‐kill studies, and in pharmacodynamic models.…”

Section: Antibacterial Activity Of Oritavancinmentioning

confidence: 94%

Mechanism of action of oritavancin and related glycopeptide antibiotics

2003

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Oritavancin (LY333328) is a semisynthetic glycopeptide antibiotic having excellent bactericidal activity against glycopeptide-susceptible and -resistant Gram-positive bacteria. Oritavancin is the N-alkyl-p-chlorophenylbenzyl derivative of chloroeremomycin (LY264826) and is currently in phase III clinical trials for use in Gram-positive infections. Studies show that oritavancin and related alkyl glycopeptides inhibit bacterial cell wall formation by blocking the transglycosylation step in peptidoglycan biosynthesis in a substrate-dependent manner. As with other glycopeptide antibiotics, including vancomycin, the effects of oritavancin on cell wall synthesis are attributable to interactions with dipeptidyl residues of peptidoglycan precursors. Unlike vancomycin, however, oritavancin is strongly dimerized and can anchor to the cytoplasmic membrane, the latter facilitated by its alkyl side chain. Cooperative interactions derived from dimerization and membrane anchoring in situ can be of sufficient strength to enable binding to either dipeptidyl or didepsipeptidyl peptidoglycan residues of vancomycin-susceptible and -resistant enterococci, respectively. This review describes the antibacterial activity of oritavancin, and examines the evidence supporting the proposed mechanism of action for this agent and related analogs.

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Section: Antibacterial Activity Of Oritavancinmentioning

confidence: 94%

Mechanism of action of oritavancin and related glycopeptide antibiotics

2003

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“…48 Against three vancomycin-intermediate S. aureus strains, quinupristin-dalfopristin MICs were 0.25-0.5 µg/ml. 49 Similar to staphylococci, the combination has low MICs against S. pneumoniae, with activity independent of penicillin or erythromycin susceptibility. 11-17, 22, 23 Quinupristin-dalfopristin's activity against commonly isolated enterococci is limited to E. faecium.…”

Section: Gram-positive Activitymentioning

confidence: 99%

Quinupristin‐Dalfopristin: An Overview

et al. 2000

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Synercid (RP 59500), the first injectable streptogramin antibiotic, is composed of two semisynthetic pristinamycin derivatives, quinupristin and dalfopristin. Individually, each component has bacteriostatic activity against staphylococci and streptococci, but together, the agents exhibit synergy, leading to bactericidal activity. The combination drug, however, is bacteriostatic against Enterococcus faecium and has poor activity against Enterococcus faecalis. Despite a short half-life, an extended postantibiotic effect allows the agent to be dosed every 8-12 hours. Both drugs are largely hepatically metabolized and excreted in bile. Although not metabolized by cytochrome P450 3A4, quinupristin-dalfopristin can inhibit agents that are metabolized through this pathway. Dosage adjustments may be necessary in patients with hepatic dysfunction. Alterations in renal function have minimal effects on the agent's pharmacokinetics. Adverse events include arthralgia, myalgias, and infusion-related pain. Based on available data, quinupristin-dalfopristin appears to have a role in treating severely ill patients with infections due to multiresistant gram-positive pathogens.

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“…However, gentamicin and vancomycin act sinergistically against several multiresistant staphylococcal strains, as shown by the FICI and the DBT scores. The therapeutic rationale for combining G and V depends on the susceptibility of the infecting pathogens, and vancomycin use should be limited to infections likely to be caused by more resistant Gram-positive bacteria, such as S. epidermidis , methicillin-resistant staphylococci, CoNS, or enterococci [30, 31]. Cefazolin, not dosed, could contribute to antimicrobial activity of drainage fluids; it is effective mainly against susceptible strains, S. aureus (9A28) and S. aureus (3A10), and ineffective against the multiresistant strains as confirmed recently [32].…”

Section: Discussionmentioning

confidence: 99%

Release of Gentamicin and Vancomycin from Preformed Spacers in Infected Total Hip Arthroplasties: Measurement of Concentrations and Inhibitory Activity in Patients’ Drainage Fluids and Serum

Regis

Sandri

Samaila

et al. 2013

The Scientific World Journal

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Gentamicin (G) and vancomycin (V) concentrations in drainage fluids obtained from patients during the first 24 hours after implantation of antibiotic-loaded polymethylmethacrylate (PMMA) spacers in two-stage revision of infected total hip arthroplasty were studied. The inhibitory activity of drainage fluids against different multiresistant clinical isolates was investigated as well. Seven hips were treated by implantation of industrial G-loaded spacers. Vancomycin was added by manually mixing with PMMA bone cement. Serum and drainage fluid samples were collected 1, 4, and 24 hours after spacer implantation. Antibiotics concentrations and drains bactericidal titer of combination were determined against multiresistant staphylococcal strains. The release of G and V from PMMA cement at the site of infection was prompt and effective. Serum levels were below the limit of detection. The local release kinetics of G and V from PMMA cement was similar, exerting a pronounced, combined inhibitory effect in the implant site. The inhibitory activity of drainage fluids showed substantial intersubject variability related to antibiotic concentrations and differed according to the pathogens tested. Gentamicin and vancomycin were released from temporary hip spacers at bactericidal concentrations, and their use in combination exerted strong inhibition against methicillin-resistant S. aureus and Coagulase Negative Staphylococci strains.

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Evaluation of Bactericidal Activities of LY333328, Vancomycin, Teicoplanin, Ampicillin-Sulbactam, Trovafloxacin, and RP59500 Alone or in Combination with Rifampin or Gentamicin against Different Strains of Vancomycin-Intermediate Staphylococcus aureus by Time-Kill Curve Methods

Cited by 49 publications

References 5 publications

Mechanism of action of oritavancin and related glycopeptide antibiotics

Mechanism of action of oritavancin and related glycopeptide antibiotics

Quinupristin‐Dalfopristin: An Overview

Release of Gentamicin and Vancomycin from Preformed Spacers in Infected Total Hip Arthroplasties: Measurement of Concentrations and Inhibitory Activity in Patients’ Drainage Fluids and Serum

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