Enterococcus faecium vancomycin-resistant

Linezohd (Zyvox) is an oxazolidinone, a tive-membered heterocychc ring that forms the core of the hnezohd structure. The approval of hnezohd by the FDA in 2000 marked the first new structural class of antibacterial introduced into medical practice in the United States in 40 years. It is notable for its activity against methicillin-resistant Staph aureus, MRSA, and vancomycin-resistant Enterococcus faecium, VRE. It is bacteriostatic rather than bactericidal but finds significant use in patients with an intact immune system. Like several other classes of antibacterials, linezolid is an inhibitor of protein synthesis. It interacts specifically with the RNA component of a bacterial ribosome subunit to prevent initiation of protein synthesis. 

Dhawan B, Gadepalli R, Kapil A. (2009) In vitro activity of daptomycin against Staphylococcus Aureus and vancomycin-resistant Enterococcus Faecium isolates associated with skin and soft tissue infections First results from India. Diagn Microbiol Infect Dis 65 196-198. 

Recently, the piperazine intermediate 15 for the total synthesis of (—)-lemon-omycin (9) was reported by Fukuyama et al. [14], (—)-Lemonomycin possesses interesting antibiotic activity against methiciUin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium, as well as cytotoxicity against the human colon tumor cell line HCT-116 [15]. The reaction of 2-isocyanoethyl phenyl carbonate 11 gave Ugi product 14, which was further transformed to a piperazine intermediate 15 (Scheme 2). 

Vancomycin-resistant Enterococcus faecium infections For the treatment of vancomycin-resistant E. faecium infections, including cases with concurrent bacteremia. 

Willems R.J.L., J. Top, M. van Santen, D.A. Robinson, T.M. Coque, F. Baquero, H. Grundmann, and M.J.M. Bonten (2005). Global spread of vancomycin-resistant Enterococcus faecium fi om distinct nosocomial genetic complex. Emerging Infectious Diseases 11 821-828. 

Most appropriate use is when vancomycin-resistant Enterococcus faecium infection is documented or strongly suspected, or for oral therapy of methicillin-resistant Staphylococcus aureus infection... 

Infections due to vancomycin-resistant Enterococcus faecium IV 7 5 mg/kg/dose q8h Skin and skin-structure infections IV 7 5 mg/kg/dose q 12h. 

Eisner HA, Sobottka I, Feucht HH, Harps E, Haun C, Mack D, Ganschow R, Laufs R, Kaulfers PM. Nosocomial outbreak of vancomycin-resistant Enterococcus faecium at a German university pediatric hospital. Int J Hyg Environ Health 2000 203(2) 147-52. 

Linden PK, Moellering RC Jr, Wood CA, Rehm SJ, Flaherty J, Bompart F, Talbot GH Synercid Emergency-Use Study Group. Treatment of vancomycin-resistant Enterococcus faecium infections with quinupristin/dalfopristin. Clin Infect Dis 2001 33(ll) 1816-23. 

Glycopeptide resistance in a cluster of three clinical isolates of vancomycin-resistant Enterococcus faecium was due to vanD, which was located on the chromosome and was not transferable to other enterococci These isolates were indistinguishable but differed from the strain in which vanD-mediated resistance has been reported previously (102). A type of acquired glycopeptide resistance, named vanE, has been characterized in E. faecalis BM 4405. It results in low-level resistance of vancomycin but susceptibility to teico-planin (103). Defects in penicillin-binding protein 4 result in a distorted peptidoglycan composition of the cell of vancomycin-resistant and teicoplanin-resistant laboratory mutants of S. aureus and are suggested to be part of the mechanism of glycopeptide resistance in these microbes (104). 

Ostrowsky BE, Clark NC, Thauvin-Eliopoulos C, Venkataraman L, Samore MH, Tenover FC, Eliopoulos GM, Moellering RC Jr, Gold HS. A cluster of VanD vancomycin-resistant Enterococcus faecium molecular characterization and clinical epidemiology. J Infect Dis 1999 180(4) 1177-85. 

Two important new streptogramins are quinu-pristin (Fig. 10.15A) and dalfopristin (Fig. 10.15B), which are derivatives of pristinamycin I and IIA, respectively. Individually, the two components are bacteristatic but in combination they act synergistically to produce a bactericidal effect by inhibiting early (dalfopristin) and late (quinupristin) phases of bacterial protein synthesis. These two antibiotics are used intravenously in combination (ratio 30 70) for the treatment of serious or life-threatening infections associated with vancomycin-resistant Enterococcus faecium bacteraemia, although the effect against this organism is bacteristatic. 

Till M, Wixson RL, Pertel PE. Linezolid treatment for osteomyelitis due to vancomycin-resistant Enterococcus faecium. Clin Infect Dis 2002 34 1412-1414. 

Son R, Nimita F, Rusul G, Nasreldin E, Samuel L, Nishibuchi M (1999) Isolation and molecular characterization of vancomycin-resistant Enterococcus faecium in Malaysia. Lett Appl Microbiol 29 118-122... 

Linezolid is an oxazolidinone that prevents the formation of a functional 70S initiation complex, which is essential to the bacterial translation process. It is indicated in the treatment of vancomycin-resistant Enterococcus faecium... 

The first of a new class of antibiotics (oxazolidinones), linezolid is active against many drug-resistant gram-positive cocci, including strains resistant to beta-lactams and vancomycin (eg, vancomycin-resistant Enterococcus faecium). Linezolid binds to a unique site on the SOS ribosomal subunit, and there is currently no cross-resistance with other protein synthesis inhibitors. Linezolid is available in both oral and parenteral formulations. 

A drug combination of the streptogramins, quinupristin and dalfopristin was approved for IV use in the treatment of infections caused by vancomycin-resistant Enterococcus faecium bacteremia as well as skin/skin structure infections caused by MRSAand methicillin-sensitive Streptococcus pyogenes. Certain strains of E. faecium are resistant to essentially all... 

G Saurina, D Landman, JM Quale. Activity of disinfectants against vancomycin-resistant Enterococcus faecium. Infect Control Hosp Epidemiol 18(5) 345-347, 1997. 

SW Frantz, KA Haines, CG Azar, JI Ward, SM Homan, RB Roberts. Chlorhexidine gluconate (CHG) activity against clinical isolates of vancomycin-resistant Enterococcus faecium (VREF) and the effects of moisturizing agents on CHG residue accumulation on the skin. J Hosp Infect 37(2) 157-164, 1997. 

B. subtilis, S. aureus, methicillin-resistant coagulase-negative staphylococci, vancomycin-resistant Enterococcus faecium, ESBL-positive K. pneumonia, S. typhi. Vibrio choiera... 

Chong YP, Lee SO, Song EH, Lee EJ, Jang EY, Kim SH, Choi SH, Kim MN, Jeong JY, Woo JH, Kim YS. Quinupris-tin- dalfopristin versus linezolid for the treatment of vancomycin-resistant Enterococcus faecium bacteraemia efficacy and development of resistance. Scand J Infect Dis 2010 42(6-7) 491-9. 

Allen N, Hobbs JN Jr, Richardson JM, Riggin RM. Biosynthesis of modified peptidoglycan precursors by vancomycin-resistant Enterococcus faecium. FEMS Microbiol Lett 1992 ... 

Nelson, R.R., 1997. In-vitro activities of ve plant essential oils against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium. J. Antimicrob. Chemother., 40 305-306. 

The compound 121 is the core stmcture of (+)-hongo-quercin A 126, a natural product isolated from an unidentified terrestrial fungus, and exhibits antibacterial properties toward methicUlin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium. In order to complete the total synthesis of (+)-hongoquercin A 126, reduction of 122 with TFA/TESH, and saponification gave 126 as a single diastereomer (Scheme 12.29). 

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