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beta lactamase inhibitor

Shui Liu, Yonglin Zhou, Xiaodi Niu, Tingting Wang, Jiyun Li, Zhongjie Liu, Jianfeng Wang, Shusheng Tang, Yang Wang, Xuming Deng
The emergence of plasmid-mediated New Delhi metallo-β-lactamase-1 (NDM-1) in carbapenem-resistant Gram-negative pathogens is an increasing clinical threat. Here we report the discovery of an NDM-1 inhibitor, magnolol, through enzyme inhibition screening. We showed that magnolol significantly inhibited NDM enzyme activity (IC50  = 6.47 µg/mL), and it restored the activity of meropenem against Escherichia coli ZC-YN3, an NDM-1-producing E. coli isolate, in in vitro antibacterial activity assays. Magnolol lacked direct antibacterial activity, but compared with meropenem alone, it reduced the MICs of meropenem against E...
December 2018: Cell Death Discovery
David P Nicolau, Brittany A Rodrigueza, Jennifer E Girottoa
The rise in multidrug-resistant (MDR) infections has become a significant problem in both the developing countries and in the United States (U.S.). Specifically, MDR gram-negative infections are emerging, affecting not only adults but children as well. The specific gram-negative organisms that have been most concerning within the pediatric population include MDR P. aeruginosa, Enterobacteriaceae, and Acinetobacter spp. The increase in antimicrobial resistance rates are associated with various mechanisms, with, one of the most common being the production of beta-lactamases...
March 8, 2018: Current Pediatric Reviews
Nathaniel J Rhodes, Caroline E Cruce, J Nicholas O'Donnell, Richard G Wunderink, Alan R Hauser
PURPOSE OF REVIEW: Hospital-acquired and ventilator-associated pneumonia (VAP) are frequent causes of infection among critically ill patients. VAP is the most common hospital-acquired bacterial infection among mechanically ventilated patients. Unfortunately, many of the nosocomial Gram-negative bacteria that cause VAP are increasingly difficult to treat. Additionally, the evolution and dissemination of multi- and pan-drug resistant strains leave clinicians with few treatment options. VAP patients represent a dynamic population at risk for antibiotic failure and under-dosing due to altered antibiotic pharmacokinetic parameters...
March 6, 2018: Current Infectious Disease Reports
Daniele Roberto Giacobbe, Matteo Bassetti, Francesco Giuseppe De Rosa, Valerio Del Bono, Paolo Antonio Grossi, Francesco Menichetti, Federico Pea, Gian Maria Rossolini, Mario Tumbarello, Pierluigi Viale, Claudio Viscoli
Ceftolozane/tazobactam (C/T) is a new antibiotic resulting from the combination of a novel cephalosporin, structurally similar to ceftazidime, with tazobactam, a well-known beta-lactamase inhibitor. C/T remains active against extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae and multi-drug resistant (MDR) P. aeruginosa, and has been recently approved for the treatment of complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI). A trial on hospital-acquired pneumonia is ongoing...
March 9, 2018: Expert Review of Anti-infective Therapy
Keith S Kaye, Tanaya Bhowmick, Symeon Metallidis, Susan C Bleasdale, Olexiy S Sagan, Viktor Stus, Jose Vazquez, Valerii Zaitsev, Mohamed Bidair, Erik Chorvat, Petru Octavian Dragoescu, Elena Fedosiuk, Juan P Horcajada, Claudia Murta, Yaroslav Sarychev, Ventsislav Stoev, Elizabeth Morgan, Karen Fusaro, David Griffith, Olga Lomovskaya, Elizabeth L Alexander, Jeffery Loutit, Michael N Dudley, Evangelos J Giamarellos-Bourboulis
Importance: Meropenem-vaborbactam is a combination carbapenem/beta-lactamase inhibitor and a potential treatment for severe drug-resistant gram-negative infections. Objective: To evaluate efficacy and adverse events of meropenem-vaborbactam in complicated urinary tract infection (UTI), including acute pyelonephritis. Design, Setting, and Participants: Phase 3, multicenter, multinational, randomized clinical trial (TANGO I) conducted November 2014 to April 2016 and enrolling patients (≥18 years) with complicated UTI, stratified by infection type and geographic region...
February 27, 2018: JAMA: the Journal of the American Medical Association
Jesús Rodríguez-Baño, Belén Gutiérrez-Gutiérrez, Isabel Machuca, Alvaro Pascual
Therapy of invasive infections due to multidrug-resistant Enterobacteriaceae (MDR-E) is challenging, and some of the few active drugs are not available in many countries. For extended-spectrum β-lactamase and AmpC producers, carbapenems are the drugs of choice, but alternatives are needed because the rate of carbapenem resistance is rising. Potential active drugs include classic and newer β-lactam-β-lactamase inhibitor combinations, cephamycins, temocillin, aminoglycosides, tigecycline, fosfomycin, and, rarely, fluoroquinolones or trimethoprim-sulfamethoxazole...
April 2018: Clinical Microbiology Reviews
Mathias W Pletz, Sebastian Weis, Christina Forstner, Florian Wagenlehner
Urosepsis is defined as a severe disease due to organ failure caused by a urinary tract infection. An empirical antibiotic therapy should be instigated within the first hour after diagnosis. Urine cultures and blood cultures should be performed before antibiotic treatment. Further diagnostics should be carried out at an early stage to enable an interventional focus control in the case of urinary tract obstruction or abscess formation, if necessary. Gram-negative pathogens are most frequently isolated. Extended spectrum beta-lactamase (ESBL) forming bacteria as a cause of urosepsis are increasing...
February 7, 2018: Medizinische Klinik, Intensivmedizin und Notfallmedizin
Javier Ramos Lázaro, Alex Smithson, Neus Jovè Vidal, María Teresa Batida Vila
OBJECTIVES: Because of high rates of resistance to fluoroquinolones, ceftriaxone has become one of the main options for treating febrile urinary tract infection (FUTI). This study aimed to identify predictors of ceftriaxone resistance in community-acquired FUTIs in men. MATERIAL AND METHODS: Cross-sectional ambispective study enrolling men with FUTIs treated in the emergency department of a local area hospital in Spain. RESULTS: A total of 552 FUTI episodes were studied; 103 (18...
February 2018: Emergencias: Revista de la Sociedad Española de Medicina de Emergencias
Sarah Christina Jane Jorgensen, Michael Joseph Rybak
Vaborbactam (VAB; formerly RPX7009) is a novel beta-lactamase inhibitor based on a cyclic boronic acid pharmacophore with potent inhibitory activity against Ambler class A and C beta-lactamases. It has been co-formulated with meropenem to restore its activity against Klebsiella pneumoniae carbapenemases (KPC). VAB does not inhibit class B or D carbapenemases, nor does it improve the activity of meropenem against multidrug-resistant non-fermenting Gram-negative bacilli, notably Acinetobacter spp. and Pseudomonas aeruginosa...
February 10, 2018: Pharmacotherapy
Fabian Kahl, Thomas Kühlein
The number of refugees arriving in Europe increased dramatically in 2015, challenging the German health system. Amongst others, the treatment of infectious diseases is an important topic in refugee healthcare. A high prevalence of multi-drug-resistant organisms has been identified among the refugee population. Still, little is known about the prescription of antibiotic medication for refugees. We conducted a descriptive analysis of all antibiotics prescribed to newly arrived refugees who were treated as outpatients between 10/01/2014 and 09/30/2015 in Erlangen, an average sized German town...
2018: Conflict and Health
P A Reuken, W Kruis, C Maaser, N Teich, J Büning, J C Preiß, R Schmelz, T Bruns, S Fichtner-Feigl, A Stallmach
Background: Intra-abdominal abscesses (IAA) are common life threatening complications in patients with Crohn's disease (CD). In addition to interventional drainage and surgical therapy, empirical antibiotic therapy represents a corner stone of treatment but contemporary data on microbial spectra and antimicrobial resistance are scarce. Methods: We recruited 105 patients with CD and IAA from 9 German centers for a prospective registry in order to characterize the microbiological spectrum, resistance profiles, antibiotic therapy and outcome...
February 5, 2018: Journal of Crohn's & Colitis
Eris Cani, Farzad Moussavi, Eric Ocheretyaner, Roopali Sharma, Clinton Brown, Brandon Eilertson
Ceftazidime-avibactam (CAZ-AVI) is a novel cephalosporin beta lactamase inhibitor combination that has shown activity against carbapenem-resistant Enterobactericeae. Data are limited on its utilization in the treatment of carbapenem-resistant Klebsiella pneumoniae osteomyelitis in solid organ transplant patients. We describe a case report on the use of CAZ-AVI in the treatment of vertebral osteomyelitis in a renal transplant recipient. This article is protected by copyright. All rights reserved.
January 23, 2018: Transplant Infectious Disease: An Official Journal of the Transplantation Society
D G S Burch, D Sperling
Amoxicillin has become a major antimicrobial substance in pig medicine for the treatment and control of severe, systemic infections such as Streptococcus suis. The minimum inhibitory concentration 90% (MIC 90) is 0.06 μg amoxicillin/ml, and the proposed epidemiological cut-off value (ECOFF) is 0.5 μg/ml, giving only 0.7% of isolates above the ECOFF or of reduced susceptibility. Clinical breakpoints have not been set for amoxicillin against porcine pathogens yet, hence the use of ECOFFs. It has also been successfully used for bacterial respiratory infections caused by Actinobacillus pleuropneumoniae and Pasteurella multocida...
January 19, 2018: Journal of Veterinary Pharmacology and Therapeutics
Francesca Spyrakis, Giuseppe Celenza, Francesca Marcoccia, Matteo Santucci, Simon Cross, Pierangelo Bellio, Laura Cendron, Mariagrazia Perilli, Donatella Tondi
Bacterial resistance has become a worldwide concern after the emergence of metallo-β-lactamases (MBLs). They represent one of the major mechanisms of bacterial resistance against beta-lactam antibiotics. Among MBLs, New Delhi metallo-β-lactamase-1 NDM-1, the most prevalent type, is extremely efficient in inactivating nearly all-available antibiotics including last resort carbapenems. No inhibitors for NDM-1 are currently available in therapy, making the spread of NDM-1 producing bacterial strains a serious menace...
January 11, 2018: ACS Medicinal Chemistry Letters
Mathias W Pletz, Sebastian Weis, Christina Forstner, Florian Wagenlehner
Urosepsis is defined as a severe disease due to organ failure caused by a urinary tract infection. An empirical antibiotic therapy should be instigated within the first hour after diagnosis. Urine cultures and blood cultures should be performed before antibiotic treatment. Further diagnostics should be carried out at an early stage to enable an interventional focus control in the case of urinary tract obstruction or abscess formation, if necessary. Gram-negative pathogens are most frequently isolated. Extended spectrum beta-lactamase (ESBL) forming bacteria as a cause of urosepsis are increasing...
January 10, 2018: Der Urologe. Ausg. A
Haishaerjiang Wushouer, Ye Tian, Xiao-Dong Guan, Sheng Han, Lu-Wen Shi
The consumption of antibiotics is a major driver in the development of antimicrobial resistance. This study aims to identify the trends and patterns of the total antibiotic consumption in China's tertiary hospitals from 2011 to 2015 by retrospectively analyzing aggregated monthly surveillance data on antibiotic sales made to 468 hospitals from 28 provinces. Antibiotic consumption was expressed in DDD per 1,000 inhabitants per day (DID). We compared population weighted antibiotic consumption patterns in China with European countries using indicators from the European Surveillance of Antimicrobial Consumption (ESAC)...
2017: PloS One
Alejandra Vera-Leiva, Sergio Carrasco-Anabalón, Celia A Lima, Nicolás Villagra, Mariana Domínguez, Helia Bello-Toledo, Gerardo González-Rocha
OBJECTIVES: KPC-producing strains present a wide range of MICs of carbapenems; this variation may be due to different gene expression levels of the blaKPC and porin genes, associated with efflux-pumps and the production of ESBLs and/or AmpC β-lactamase. The aim of this study was to determine the role of efflux-pumps inhibited by PAβN in the resistance to carbapenems in Chilean clinical isolates of K. pneumoniae harbouring the gene blaKPC. METHODS: Minimum Inhibitory Concentration (MIC) was determined by the agar dilution method for imipenem, meropenem, ertapenem and ciprofloxacin in the presence and absence of PAβN (25mg/L)...
December 21, 2017: Journal of Global Antimicrobial Resistance
Mercy A Ezeokonkwo, Onyinyechi N Ogbonna, Sunday N Okafor, Evelyn U Godwin-Nwakwasi, Fidelia N Ibeanu, Uchechukwu C Okoro
The reaction of diaza-5H-benzo[a]phenoxazin-5-one and 5H-benzo[a]phenoxazin-5-one with various phenols catalyzed by Pd/t-BuXPhos/K3PO4 system gave previously unknown ether derivatives (7a-f and 8a-f) in good yields. UV-visible, FTIR, and 1H NMR data were used to confirm structures of the synthesized compounds. The parent compounds and the derivatives were screened in-silico for their drug-likeness and binding affinities to the microbial targets through molecular docking. Molinspiration software and AutoDock were used for the drug-likeness and docking studies, respectively...
2017: Frontiers in Chemistry
Audrey N Schuetz, Sergio Reyes, Pranita D Tamma
INTRODUCTIONBeta-lactam/beta-lactamase inhibitor combination antimicrobials (BLBLIs) are among the most controversial classes of antibiotic agents available for the treatment of infections caused by extended-spectrum-beta-lactamase (ESBL)-producing Gram-negative bacteria (ESBL-GNR). Piperacillin-tazobactam (PTZ) is one of the most frequently utilized antibiotic agents for empirical Gram-negative bacterial coverage and remains active against a large proportion of ESBL-GNR strains. Furthermore, good antimicrobial stewardship practices encourage the use of carbapenem-sparing treatment regimens for infections due to ESBL-GNR...
March 2018: Journal of Clinical Microbiology
Alex J Holloway, JiehJuen Yu, Bernard P Arulanandam, Sarah M Hoskinson, Tonyia Eaves-Pyles
Multidrug-resistant (MDR) bacterial pneumonia can induce dysregulated pulmonary and systemic inflammation leading to morbidity and mortality. Antibiotics to treat MDR pathogens do not function to modulate the extent and intensity of inflammation and can have serious side effects. Here we evaluate the efficacy of two human cysteine proteinase inhibitors, cystatin 9 (CST9) and cystatin C (CSTC), as a novel immunotherapeutic treatment to combat MDR New Delhi metallo-beta-lactamase-1 (NDM-1)-producing Klebsiella pneumoniae Our results showed that mice infected intranasally (i...
March 2018: Antimicrobial Agents and Chemotherapy
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