Synthesis andin vitro antibacterial activity of quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety

Several oxazolidinones having amine moiety were prepared to form a quaternary ammonium salt with cephalosporin nucleus, and antibacterial activity of the quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety were examined particularly with expectation of dual activity. However, the cephalosporin-oxazolidinone compounds revealed rather weaker antibacterial activity in vitro than their parent oxazolidinone and cephalosporin without showing any characteristic activity as expected.     

Synthesis andin vitro antibacterial activity of C-3′ pyridinium cephalosporin derivatives

The quaternary ammonium cephalosporin derivatives were prepared with various pyridines substituted at the 3 or/and 4 position. Their in vitro antibacterial activities were determined and substituent effect on pyridine nucleus was studied. Preparation of substituted pyridines are also described.     

头孢美法仑的合成及其体外抗肿瘤活性研究

目的设计合成头孢美法仑,并对其进行体外抗肿瘤活性研究。方法以二苯甲酮、美法仑和7-苯乙酰胺基-3-氯甲基头孢烷酸对甲氧基苄酯（GCLE）为原料,经酯化、碘代、偶联、氧化、水解等反应得到目标化合物头孢美法仑,并采用MTT法对其进行体外抗肿瘤活性研究。结果设计并合成了目标产物头孢美法仑,利用MS和1H-NMR确证了结构;体外活性实验中,头孢美法仑在体外基本无毒,酶解后IC50为（101．97±1．705）μmol／L。结论头孢美法仑酶解后能够充分发挥细胞毒作用,而酶解前在体外基本无毒性,为颇具前景的前药,值得进一步研究。     

高效液相色谱法测定小鼠血浆头孢匹胺钠的含量

目的:建立小鼠血浆中头孢匹胺钠HPLC检测方法,为临床上头孢匹胺钠血药浓度监测提供试验依据。方法:样品处理采用25%高氯酸(v/v)沉淀蛋白质。PLATISILTMC18(250 mm×4.6 mm,5μm)色谱柱,流动相为甲醇-三乙胺醋酸(三乙胺14 mL,冰醋酸5.7 mL,加蒸馏水定容至100 mL)-水(10∶0.2∶89.8),1 mol.L-1醋酸调节pH5.38,流速为0.8 mL.min-1;检测波长为254 nm。结果:所建立方法在0.2～250.0μg.mL-1范围内线性良好,方法平均回收率为96.1%,平均提取回收率为77.7%;日内变异RSD小于5%。小鼠尾静脉给药150 mg.kg-1后1 h血浆头孢匹胺钠浓度为(196.1±11.9)μg.mL-1,24 h血药浓度降至(0.5±1.6)μg.mL-1,采用DAS2.0程序求得药物动力学参数t1/2为3.41 h,MRT为3.24 h。结论:该法准确、灵敏、快速,内源性成分无干扰,适用于血浆中头孢匹胺钠的分析测定。     

青霉素过敏患者合理使用头孢菌素研究进展

头孢菌素与青霉素母核的相似性造成了头孢菌素与青霉素以及头孢菌素间的交叉过敏,但α环和侧链的差异使交叉过敏的发生率缺乏足够的指导意义。综合考虑多个因素对青霉素过敏患者使用头孢菌素的影响,可以更有效的避免患者对头孢菌素过敏反应和过敏性休克反应的出现。本文综述了药物过敏的分类、头孢菌素侧链和交叉过敏间的关系,青霉素过敏患者使用头孢菌素指导原则、以及各地区间头孢菌素皮试方法对青霉素过敏患者使用头孢菌素的意义及临床应用价值。     

临床常用头孢菌素类抗菌药物药品说明书评价

目的 将临床常用的头孢菌素类抗菌药物说明书进行对比分析,为药品说明书的完善和合理使用提供参考。方法 收集整理临床常用的14种头孢菌素类原研药和仿制药共计28份药品说明书,依据相关法律法规和参考资料为评价标准对其进行对比分析。结果 28份药品说明书中,主要在注意事项、药物相互作用、特殊人群用药、贮藏条件、修订日期等方面存在差异。此外,亦存在适应证范围不一、同一说明书对应多种规格、用法用量存在差异、不良反应存在差异、药物过量描述不一、药动学描述不一等问题。结论 头孢菌素类抗菌药物,尤其是仿制药药品说明书的内容完整度有待提高,说明书修订有待加强,建议不断完善头孢菌素类抗菌药物药品说明书,以保证患者用药安全。     

Thrombotic thrombocytopenic purpura in a postoperative patient taking cephalexin responding to plasmapheresis: A case report and review of cephalosporin‐induced TTP

The clinical presentation of thrombotic thrombocytopenic purpura (TTP) is often atypical delaying diagnosis and treatment. A number of drugs have been implicated in the development of TTP, including cyclosporine, tacrolimus, clopidogrel, and quinine. To our knowledge, only three cases of cephalosporin‐induced TTP have been described, with two of these cases occurring with these use of cephalexin. We herein describe a case of TTP occurring in a postoperative patient taking cephalexin, requiring plasmapheresis. Following plasmapheresis, the patient's mental status and platelet count significantly improved. J. Clin. Apheresis 31:473–475, 2016. © 2015 Wiley Periodicals, Inc.     

2011—2018年鄂东医疗集团4家医院头孢菌素类药品致成人凝血功能异常的相关因素分析

目的 分析头孢菌素类药品导致成人凝血功能异常的相关因素,为临床预防和治疗不良反应（ADR）提供参考。方法 回顾分析2011-2018年黄石市中心医院、黄石市普爱医院、黄石市中医医院和黄石市妇幼保健院收集的271例头孢菌素类药物致成人凝血功能异常患者的临床资料、干预措施及预后情况,调查患者性别、年龄、原患疾病、合并基础疾病、联合用药、头孢菌素类药物名称及累积用药时间等相关因素,数据采用采用SPSS 20.0软件进行统计分析。结果 头孢菌素类药物致凝血功能异常例数占总ADR的例数的构成比呈上升趋势,从16.06%上升至22.76%;共涉及12种头孢菌素类药物,排序前3位的药物分别为头孢哌酮舒巴坦、头孢美唑和头孢曲松。合并低蛋白血症、肾功能不全、联用影响凝血功能药物及累积用药>5 d是头孢菌素类药物致成人凝血功能异常的危险因素。所有患者经停药、对症干预等措施后凝血功能恢复正常,未出现大出血及死亡病例。结论 对于合并出血危险因素的患者在使用头孢菌素类药物期间应严密监测凝血功能,及时发现凝血功能异常与出血倾向,预防致死性出血事件发生。     

Salmonella Subtypes with Increased MICs for Azithromycin in Travelers Returned to the Netherlands

Antimicrobial susceptibility was analyzed for 354 typhoidal Salmonella isolates collected during 1999–2012 in the Netherlands. In 16.1% of all isolates and in 23.8% of all isolates that showed increased MICs for ciprofloxacin, the MIC for azithromycin was increased. This resistance may complicate empirical treatment of enteric fever.     

Cefiderocol for Infections Caused by Multidrug-Resistant Gram-Negative Bacteria

In 2019, the U.S. Food and Drug Administration approved cefiderocol, a new treatment option for individuals with complicated urinary tract infections. Cefiderocol is a cephalosporin antibiotic indicated for use in adults 18 years or older who have minimal treatment options due to resistance for complicated urinary tract infections caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and Enterobacter cloacae complex. The recommended dose of cefiderocol is 2 g intravenously every 8 hours infused over 3 hours. The dose is adjusted for individuals with creatinine clearance of less than 60 ml/min or greater than 120 ml/min. Gastrointestinal symptoms such as diarrhea and constipation are the most common adverse events reported by individuals taking cefiderocol.