Short course of linezolid treatment for vancomycin-resistant Enterococcus faecium meningitis

Enterococci might be one of the meningitis pathogens, but meningitis is rarely caused by vancomycin-resistant enterococci. In this report, we present a 69-year-old man who had the underlying chronic obstructive pulmonary disease with long-term steroid treatment suffered from a meningitis episode after hospitalisation for the urinary tract infection. The cerebrospinal fluid culture of the patient grew Enterococcus faecium which was resistant to vancomycin. A vancomycin-resistant E. faecium was also isolated from the rectal swab of the patient. These two E. faecium isolates were found to harbour the vanA gene and to be identical by pulsed field gel electrophoresis typing. The patient was treated successfully with intravenous linezolid, 600 mg every 12 h for 2 weeks. This was the first case of meningitis caused by vancomycin-resistant E. faecium in Taiwan.     

利奈唑胺在儿科应用研究进展

利奈唑胺（linezolid）是第一个临床应用的新型唑烷酮类抗生素,通过抑制细菌蛋白质的合成达到抑菌的作用。因利奈唑胺独特的作用位点和方式,故不易与其他基于抑制蛋白合成发挥抗菌作用的药物发生交叉耐药,而本身也不易诱导产生耐药性,其临床疗效已经得到一系列III期临床研究证明。现就其作用机制、儿科临床应用及不良反应进行综述。     

利奈唑胺致不良反应44例文献分析

目的 探讨利奈唑胺所致不良反应的特点及相关因素,为临床合理用药提供参考。方法 检索2000年1月—2012年11月国内医药期刊报道的44例利奈唑胺致不良反应案例,并进行统计、分析。结果 利奈唑胺所致不良反应主要体现在血液、心血管及消化系统等,并且老年患者更易发生。结论 临床应加强对利奈唑胺的合理使用,尽量避免或减少其所致不良反应的发生。     

Update on the safety of linezolid

Background: Linezolid is still the only representative of the oxazolidinones antibiotic class. Because of its novel mechanism of action and excellent tissue penetration, it is used in a variety of approved and off-label clinical conditions. Objectives: To review the literature (including latest publications) about the adverse events of linezolid and its overall safety. Results/conclusion: The range of adverse events of linezolid is growing; new ones, such as nephro-toxicity and Bell's palsy, have been reported. Toxicity of linezolid is mostly related with the prolonged duration of treatment and the presence of predisposing factors. Physicians must be alerted when using linezolid for indications and duration different from the approved ones, and must be aware of the possible adverse events. In case of toxicity, the main option is the discontinuation of the drug; although, not all adverse events are fully reversible. Linezolid represents an important advance in therapeutics and is still considered safe enough, but anticipated benefits must always be counterbalanced by the possible toxicity.     

利奈唑胺在儿科应用研究进展

利奈唑胺(linezolid)是第一个临床应用的新型(噁)唑烷酮类抗生素,通过抑制细菌蛋白质的合成达到抑菌的作用.因利奈唑胺独特的作用位点和方式,故不易与其他基于抑制蛋白合成发挥抗菌作用的药物发生交叉耐药,而本身也不易诱导产生耐药性,其临床疗效已经得到一系列Ⅲ期临床研究证明.现就其作用机制、儿科临床应用及不良反应进行综述.     

Advances in MRSA drug discovery: where are we and where do we need to be?

Introduction: Methicillin-resistant Staphylococcus aureus (MRSA) have been on the increase during the past decade, due to the steady growth of the elderly and immunocompromised patients, and the emergence of multidrug-resistant (MDR) bacterial strains. Although there are a limited number of anti-MRSA drugs available, a number of different combination antimicrobial drug regimens have been used to treat serious MRSA infections. Thus, the addition of several new antistaphylococcal drugs into clinical practice should broaden clinician's therapeutic options. As MRSA is one of the most common and problematic bacteria associated with increasing antimicrobial resistance, continuous efforts for the discovery of lead compounds as well as development of alternative therapies and faster diagnostics are required.

Areas covered: This article summarizes the FDA-approved drugs to treat MRSA infections, the drugs in clinical trials, and the drug leads for MRSA and related Gram-positive bacterial infections. In addition, the article discusses the mode of action of antistaphylococcal molecules and the resistant mechanisms of some molecules.

Expert opinion: The number of pipeline drugs presently undergoing clinical trials is not particularly encouraging. There are limited and rather expensive therapeutic options for MRSA infections in the critically ill. Further research efforts are required for effective phage therapy on MRSA infections in clinical use, which seem to be attractive therapeutic options for the future.     

Pharmacokinetics and safety of recently approved drugs used to treat methicillin-resistant Staphylococcus aureus infections in infants,children and adults

Methicillin-resistant Staphylococcus aureus (MRSA) remains a significant cause of morbidity in hospitalized infants. Over the past 15 years, several drugs have been approved for the treatment of S. aureus infections in adults (linezolid, quinupristin/dalfopristin, daptomycin, telavancin, tigecycline and ceftaroline). The use of the majority of these drugs has extended into the treatment of MRSA infections in infants, frequently with minimal safety or dosing information. Only linezolid is approved for use in infants, and pharmacokinetic data in infants are limited to linezolid and daptomycin. Pediatric trials are underway for ceftaroline, telavancin, and daptomycin; however, none of these studies includes infants. Here, we review current pharmacokinetic, safety and efficacy data of these drugs with a specific focus in infants.     

利奈唑胺注射液致血小板减少的主动监测与评价研究

目的：通过计算机辅助主动监测方法,分析评估中国人民解放军总医院住院患者中利奈唑胺注射液致血小板减少的真实世界数据。方法：依托医疗机构药品不良事件主动监测与智能评估警示系统（ADE-ASAS）,回顾性调取2008年1月至2020年12月该院使用利奈唑胺注射液患者信息。对系统报警的疑似病例展开双人盲评、逐一甄别,确认利奈唑胺注射液致血小板减少阳性病例。结果：ADE-ASAS提取获得利奈唑胺注射液用药患者9 338例,通过对患者诊疗信息开展主动监测,判别得到阳性病例810例（8.67%）,其中ADR组（血小板计数<100×10⁹/L）465例（4.97%）,趋势组（血小板降幅>基线值×25%）754例（8.07%）。高龄和入住ICU患者血小板减少发生率较高,高龄、入住ICU、血小板基线值较高、用药时间短、合并抗感染药物品种数少的患者血小板日均降速较大。进一步单因素分析提示,高龄（RR=3.33/3.54,P<0.05）、入住ICU（RR=1.73/1.90,P<0.05）、血小板计数值低/降幅大（RR=2.04/3.33,P<0.05）为ADR组和趋势组患者院内死亡的危险因素。结论：应用ADE-ASAS可以高效、准确地获取利奈唑胺注射液真实世界用药数据,发掘血小板减少发生趋势、规律和院内死亡危险因素,进而早期识别、有效规避高危患者不良反应风险。     

Surveillance of linezolid resistance in Germany, 2001–2002

A surveillance study was performed throughout Germany from November 2001 to June 2002 to assess the prevalence of linezolid-resistant isolates among Gram-positive bacteria from routine susceptibility data and to compare the in-vitro activity of linezolid to that of other antibacterial agents. Each of 86 laboratories provided routine susceptibility data for 100 consecutive isolates. Most laboratories (c. 60%) used the disk diffusion test. Laboratories were also requested to send a representative sample of their isolates, as well as all isolates reported as intermediate or resistant to linezolid, to a reference laboratory for MIC determination. Susceptibility data for 8594 isolates were evaluated. Sites of infection were skin and soft tissue (29.9%), upper and lower respiratory tract (19.1%), foreign body or catheter (10.5%), or urinary tract (9.8%). Routine linezolid susceptibility data were reported for 6433 isolates. The prevalence of linezolid resistance, as reported to the clinician, was 0.4% in Staphylococcus aureus, 0.3% in Staphylococcus epidermidis, 2.9% in Enterococcus faecalis, 2.3% in Enterococcus faecium, 1.4% in Streptococcus pyogenes and 2.9% in Streptococcus agalactiae. Linezolid resistance was not detected in Streptococcus pneumoniae or in viridans group streptococci. Sixty-nine of 115 isolates reported as intermediate or resistant to linezolid were retested, but none was resistant to linezolid. Linezolid exhibited excellent in-vitro activity against representative isolates of the six most frequently encountered species (MIC90, 1-2 mg/L). The prevalence of resistance to linezolid was very low in Germany. Organisms reported as linezolid-resistant should be retested, either in the same laboratory with an alternative method or in a reference laboratory.