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136501. In vitro and in vivo antibacterial activities of DK-507k, a novel fluoroquinolone. Full Text available with Trip Pro

In vitro and in vivo antibacterial activities of DK-507k, a novel fluoroquinolone. The antibacterial activities of DK-507k, a novel quinolone, were compared with those of other quinolones: ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, sitafloxacin, and garenoxacin (BMS284756). DK-507k was as active as sitafloxacin and was as active as or up to eightfold more active than gatifloxacin, moxifloxacin, and garenoxacin against Streptococcus pneumoniae, methicillin-susceptible

2003 Antimicrobial Agents and Chemotherapy

136502. Novel antibacterial class. Full Text available with Trip Pro

Novel antibacterial class. We report the discovery and characterization of a novel ribosome inhibitor (NRI) class that exhibits selective and broad-spectrum antibacterial activity. Compounds in this class inhibit growth of many gram-positive and gram-negative bacteria, including the common respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Staphylococcus aureus, and Moraxella catarrhalis, and are nontoxic to human cell lines. The first NRI was discovered in a high (...) -throughput screen designed to identify inhibitors of cell-free translation in extracts from S. pneumoniae. The chemical structure of the NRI class is related to antibacterial quinolones, but, interestingly, the differences in structure are sufficient to completely alter the biochemical and intracellular mechanisms of action. Expression array studies and analysis of NRI-resistant mutants confirm this difference in intracellular mechanism and provide evidence that the NRIs inhibit bacterial protein

2003 Antimicrobial Agents and Chemotherapy

136503. GeneHunter, a transposon tool for identification and isolation of cryptic antibiotic resistance genes. Full Text available with Trip Pro

GeneHunter, a transposon tool for identification and isolation of cryptic antibiotic resistance genes. GeneHunter is a transposon tool designed for the experimental activation and identification of silent antibiotic resistance genes. The method permits the identification of novel resistance genes that lack previously identified homologues. Using Salmonella enterica serovar Typhimurium strain LT2 as a test organism for the in vivo version of the GeneHunter method, we were able to activate, clone (...) , and identify two cryptic antibiotic resistance genes, the aminoglycoside acetyltransferase aac(6')-Iaa and the probable Mar-A regulon activator rma. Because the method requires being able to electroporate the host with an efficiency of at least 10(10) transformants per microgram, the in vivo method is not applicable to most microorganisms. We therefore developed an in vitro transposition method, showed that it can also recover the cryptic rma gene from S. enterica serovar Typhimurium strain LT2, and showed

2003 Antimicrobial Agents and Chemotherapy

136504. Triclosan as a systemic antibacterial agent in a mouse model of acute bacterial challenge. Full Text available with Trip Pro

Triclosan as a systemic antibacterial agent in a mouse model of acute bacterial challenge. The upsurge of multiple-drug-resistant microbes warrants the development and/or use of effective antibiotics. Triclosan, though used in cosmetic and dermatological preparations for several decades, has not been used as a systemic antibacterial agent due to problems of drug administration. Here we report the striking efficacy of triclosan in a mouse model of acute systemic bacterial infection. Triclosan

2003 Antimicrobial Agents and Chemotherapy

136505. Persistence of the antibody response to the VlsE sixth invariant region (IR6) peptide of Borrelia burgdorferi after successful antibiotic treatment of Lyme disease. Full Text available with Trip Pro

Persistence of the antibody response to the VlsE sixth invariant region (IR6) peptide of Borrelia burgdorferi after successful antibiotic treatment of Lyme disease. It has been suggested that a <4-fold decline in the immunoglobulin G (IgG) antibody response to the VlsE sixth invariant region peptide of Borrelia burgdorferi within 6 months after antibiotic treatment may indicate spirochetal persistence in Lyme disease. We studied the response to this peptide in 77 patients with early or late (...) disease, for whom archival samples were available at the time of antibiotic treatment and approximately 6 months or years later. Eight (33%) of the 24 patients with early manifestations and 18 (86%) of the 21 patients with late manifestations had a <4-fold decline in IgG anti-VlsE titers approximately 6 months after successful antibiotic treatment. Of 32 additional patients, 13 (50%) with early manifestations and 5 (83%) with late manifestations still had positive anti-VlsE titers 8-15 years after

2003 Journal of Infectious Diseases

136506. Antibiotic resistance of Neisseria gonorrhoeae in Spain: trends over the last two decades. (Abstract)

Antibiotic resistance of Neisseria gonorrhoeae in Spain: trends over the last two decades. In vitro activities of six antimicrobial agents against 2966 strains of Neisseria gonorrhoeae, isolated in Spain between 1983 and 2001, were determined. The percentages of intermediately susceptible and resistant isolates to penicillin (MIC > or = 0.12 mg/L) and tetracycline (MIC > or = 0.5 mg/L) were very high over the period of study. Strains intermediately susceptible to cefoxitin were identified

2003 Journal of Antimicrobial Chemotherapy

136507. Antibiotic consumption and resistance selection in Streptococcus pneumoniae. (Abstract)

Antibiotic consumption and resistance selection in Streptococcus pneumoniae. Selection of antibiotic-resistant Streptococcus pneumoniae is an inescapable consequence of antibiotic use. The correlation between antibiotic consumption and selection of resistant organisms can be shown at every ecological level: patient, community, region or country. In the case of multiple resistance, the intensity of antibiotic selection is increased. However, different antibiotics may exert different selective (...) powers. Because of this, co-selection of macrolide and beta-lactam resistance is an asymmetrical phenomenon: macrolides select more efficiently strains resistant to both macrolides and beta-lactams than aminopenicillins. The difference in rates of antibiotic resistance is also influenced by the local spread of susceptible or resistant clones; it is suggested that under mild antibiotic selection, the susceptible organisms that are more fit for host-to-host transmission could be favoured. Subsequent

2002 Journal of Antimicrobial Chemotherapy

136508. Enzymic degradation of a beta-lactam antibiotic, ampicillin, in the gut: a novel treatment modality. (Abstract)

Enzymic degradation of a beta-lactam antibiotic, ampicillin, in the gut: a novel treatment modality. Antibiotics can cause severe alterations in the gut microflora and promote diarrhoea and overgrowth of pathogenic bacteria. The present study investigated the potency of targeted recombinant beta-lactamase (TRBL) to degrade a beta-lactam antibiotic in the jejunum of fistula-operated beagles. We used different peroral doses of purified beta-lactamase (PenP) of Bacillus licheniformis in enteric (...) a targeted treatment to degrade beta-lactam antibiotics intestinally and, thus, decrease antibiotic-induced adverse effects on the gut microflora.

2003 Journal of Antimicrobial Chemotherapy

136509. Influence of population density on antibiotic resistance. (Abstract)

Influence of population density on antibiotic resistance. Antibiotic consumption and population density as a measure of crowding in the community were related to the prevalence of antibiotic resistance of three cities in three different countries: St Johns in Newfoundland (Canada), Athens in Greece and Groningen in The Netherlands. Antibiotic consumption was expressed in DDD (defined daily dose), as DID (DDD/1000 inhabitants/day) and as DSD (DDD/km(2)). The prevalence of antibiotic-resistant (...) Escherichia coli and enterococci was determined in faecal samples of healthy volunteers. In both Newfoundland (28 DID) and Greece (29 DID) the overall consumption of antibiotics was more than three times higher compared with that of The Netherlands (9 DID). The lowest prevalence of resistant E. coli against the majority of antibiotics tested was found for the samples from Newfoundland and was significant (P < 0.05) for cefazolin, oxytetracycline and trimethoprim. A poor correlation between the number

2003 Journal of Antimicrobial Chemotherapy

136510. Cost-minimization analysis and audit of antibiotic management of bone and joint infections with ambulatory teicoplanin, in-patient care or outpatient oral linezolid therapy. (Abstract)

Cost-minimization analysis and audit of antibiotic management of bone and joint infections with ambulatory teicoplanin, in-patient care or outpatient oral linezolid therapy. Bone and joint infections are significant causes of morbidity, mortality and healthcare costs. The cost of treatment for such infections is driven primarily by the length of hospital stay. Many of these infections will require treatment with prolonged periods of parenteral antibiotic therapy. Clinicians and healthcare

2003 Journal of Antimicrobial Chemotherapy

136511. Tissue and serum concentrations of levofloxacin 500 mg administered intravenously or orally for antibiotic prophylaxis in biliary surgery. (Abstract)

Tissue and serum concentrations of levofloxacin 500 mg administered intravenously or orally for antibiotic prophylaxis in biliary surgery. Levofloxacin is a third-generation fluoroquinolone with a broad spectrum of antibacterial activity, comprising enterobacteria, non-fermenters, Gram-positive cocci and some anaerobic species. Members of these species are common pathogens in acute and chronic cholecystitis. This suggests that levofloxacin may be used as peri-operative prophylaxis in gall

2003 Journal of Antimicrobial Chemotherapy

136512. Vancomycin therapeutic drug monitoring: is there a consensus view? The results of a UK National External Quality Assessment Scheme (UK NEQAS) for Antibiotic Assays questionnaire. (Abstract)

Vancomycin therapeutic drug monitoring: is there a consensus view? The results of a UK National External Quality Assessment Scheme (UK NEQAS) for Antibiotic Assays questionnaire. This study investigated vancomycin therapeutic drug monitoring (TDM) and issues related to patient management. Questionnaires were distributed to 310 participants in the UK National External Quality Assessment Scheme (NEQAS) for Antibiotic Assays. The response rate was 57.4%. The majority (76%) had an 'in-house' assay

2002 Journal of Antimicrobial Chemotherapy

136513. Nisin, alone and combined with peptidoglycan-modulating antibiotics: activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. (Abstract)

Nisin, alone and combined with peptidoglycan-modulating antibiotics: activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. We have sought ways to circumvent resistance, by combining nisin with other antibiotics known to target bacterial cell wall biosynthesis.Twenty strains each of methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE) were tested in vitro by standardized methods against nisin alone and combined

2002 Journal of Antimicrobial Chemotherapy

136514. Comparison of the antibacterial activities of ampicillin, ciprofloxacin, clarithromycin, telithromycin and quinupristin/dalfopristin against intracellular non-typeable Haemophilus influenzae. (Abstract)

Comparison of the antibacterial activities of ampicillin, ciprofloxacin, clarithromycin, telithromycin and quinupristin/dalfopristin against intracellular non-typeable Haemophilus influenzae. Non-typeable Haemophilus influenzae, which is a cause of disease in the upper and lower respiratory tract, can survive intracellularly in human epithelial cells and macrophages. We studied the in vitro activity of five antibiotics against intracellular non-typeable H. influenzae in human type II alveolar (...) epithelial cells. The eukaryotic cells were loaded with bacteria, and extracellular bacteria were killed by gentamicin. After the cells were washed, antibiotics were added at concentrations of 0.12-64 mg/L for 18 h before the numbers of viable intracellular bacteria were determined. Of the antibiotics tested, ciprofloxacin and quinupristin/dalfopristin were the most potent agents, followed by clarithromycin and telithromycin. Ampicillin was not active against intracellularly localized, non-typeable H

2002 Journal of Antimicrobial Chemotherapy

136515. Comparability of antimicrobial susceptibility test results from 22 European countries and Israel: an external quality assurance exercise of the European Antimicrobial Resistance Surveillance System (EARSS) in collaboration with the United Kingdom National (Abstract)

Comparability of antimicrobial susceptibility test results from 22 European countries and Israel: an external quality assurance exercise of the European Antimicrobial Resistance Surveillance System (EARSS) in collaboration with the United Kingdom National The goal of this exercise was to organize external quality assurance (QA) of antibiotic susceptibility testing for laboratories participating in EARSS and to assess the comparability of susceptibility test results across countries

2002 Journal of Antimicrobial Chemotherapy

136516. The in vitro and in vivo antibacterial characterization of vancomycin and linezolid against vancomycin-susceptible and -resistant enterococci. (Abstract)

The in vitro and in vivo antibacterial characterization of vancomycin and linezolid against vancomycin-susceptible and -resistant enterococci. The present study was designed to compare in vitro antibacterial activities of linezolid and vancomycin against vancomycin-susceptible Enterococcus faecalis (VSEF) and vancomycin-resistant enterococci (VRE) isolated in Japan with those of quinupristin-dalfopristin, teicoplanin and minocycline, and the in vitro short time bactericidal activity

2002 Journal of Antimicrobial Chemotherapy

136517. Antibiotic prescribing in general practice: striking differences between Italy (Ravenna) and Denmark (Funen). (Abstract)

Antibiotic prescribing in general practice: striking differences between Italy (Ravenna) and Denmark (Funen). To compare antibiotic prescribing in primary care in two European populations, one in Denmark (Funen), the other in Italy (Ravenna).Reimbursement data (1999) were retrieved from the Odense Pharmacoepidemiologic Database (Denmark) and the Emilia Romagna Health Authority Database (Italy). The extent of antibiotic use (ATC J01) was analysed as the number of defined daily doses per 1000 (...) inhabitants per day (DDD/1000 inhabitants/day), and as annual prevalence of use. A qualitative analysis was carried out according to the Drug Utilization 90% (DU90%) approach.Antibiotic consumption was 16.5 DDD/1000 inhabitants/day in Ravenna and 10.4 DDD/1000 inhabitants/day in Funen; the annual prevalence of use was 40 and 30 subjects/100 inhabitants, respectively. Italian children received a greater amount (four-fold in DDDs) of antibiotics than Danish ones, whereas consumption was only slightly higher

2002 Journal of Antimicrobial Chemotherapy

136518. Mupirocin and Staphylococcus aureus: a recent paradigm of emerging antibiotic resistance. (Abstract)

Mupirocin and Staphylococcus aureus: a recent paradigm of emerging antibiotic resistance. To describe trends in mupirocin resistance among Staphylococcus aureus in New Zealand (NZ), following the availability of mupirocin in 1986.Data from a variety of sources were used for this study: susceptibility data collected annually from diagnostic laboratories throughout NZ; a local survey of mupirocin-resistant S. aureus in the Auckland area in 1997; a national survey of S. aureus antimicrobial (...) common among S. aureus generally than MRSA.We postulate that the steady rise in mupirocin resistance among S. aureus in NZ throughout the 1990s may be due, at least in part, to the over the counter availability of mupirocin from 1991 to 2000. The current patterns of mupirocin consumption need to be reviewed and its use rationalized to maximize the chances of this antibiotic retaining beneficial antistaphylococcal activity.

2003 Journal of Antimicrobial Chemotherapy

136519. Socioeconomic factors and prescription of antibiotics in 0- to 2-year-old Danish children. (Abstract)

Socioeconomic factors and prescription of antibiotics in 0- to 2-year-old Danish children. The aim was to examine the impact of socioeconomic factors on the use of systemic antibiotics during the first 2 years of life.This was a population-based cohort study of 5024 Danish children born in 1997. The study was conducted by linking records drawn from public administrative registries. The main predictor variables were mother's education level, household income and cohabitation status. The outcome (...) was the number of antibiotic courses (0, 1-5, > or =6) during the first 2 years of life.A total of 3273 children (65.1%) received 1-5 antibiotic courses, and 337 (6.7%) received > or =6 courses of antibiotics during the first 2 years of life. The risk of receiving > or =6 courses of antibiotics was increased in children of mothers with a low educational level (< or =10 years) compared with vocational education [OR 1.3 (95% CI 1.0-1.7)]. Children of mothers with a higher education >4 years had a reduced risk

2003 Journal of Antimicrobial Chemotherapy

136520. Spain14-5 international multiresistant Streptococcus pneumoniae clone resistant to fluoroquinolones and other families of antibiotics. (Abstract)

Spain14-5 international multiresistant Streptococcus pneumoniae clone resistant to fluoroquinolones and other families of antibiotics. The Spain(14)-5 international multiresistant clone was initially described as resistant to penicillin, tetracycline, chloramphenicol and trimethoprim/sulfamethoxazole. In Gipuzkoa, Spain, Streptococcus pneumoniae isolated from 16 patients, and determined by PFGE and multilocus sequence typing to belong to the Spain(14)-5 clone, showed further resistance

2003 Journal of Antimicrobial Chemotherapy

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