头孢唑林与头孢呋辛用于儿童清洁手术预防用药的临床综合评价

目的 开展儿童清洁手术(I类切口)预防用药的临床综合评价,促进围术期预防用抗菌药物的合理使用。方法 根据《药品临床综合评价管理指南(2021年版试行)》,应用文献研究法、头脑风暴、专家访谈法、德尔菲法构建清洁手术(I类切口)预防用药的临床综合评价体系;收集评价证据并开展多维度、多层次证据的综合评判。结果 临床综合评价体系包括5个1级指标(安全性、有效性、经济性、适宜性和可及性),11个2级指标,30个3级指标;头孢唑林临床综合评价得分86.09,头孢呋辛评分为82.45分,前者在安全性、有效性、经济性、适宜性4个方面优于后者,后者可及性优于前者。结论 本研究所构建的儿童清洁手术(I类切口)预防用药临床综合评价体系有较高的科学性,评价结果可为医疗机构清洁手术(I类切口)抗菌药物的遴选提供依据。     

Stability of Cefazolin in Polyisoprene Elastomeric Infusion Devices

Purpose

The aim was to investigate the stability of cefazolin in elastomeric infusion devices.

注射用双黄连与头孢唑林钠配伍稳定性考察

目的：建立同时测定双黄连中黄芩苷和头孢唑林钠含量的高效液相色谱法,探讨双黄连与头孢唑啉钠配伍的稳定性及贮存期。方法：色谱柱：Hypersil C18（250mm×4．6mm,5μm）;流动相：乙腈-水-磷酸（25：75：0．01）;流速：0．8ml·min^-1;检测波长：275nm;柱温：30℃;进样量20μl。用经典恒温法、留样观察法考察配伍液的含量、pH及外观等变化。结果：黄芩苷线性范围为20．4～102．0mg·L^-1,r=0．9982（n=5）;头孢唑林线性范围为50．4～252．0mg·L^-1,r=0．9997（n=5）;日内、日间RSD均小于5％（n=5）。恒温加速实验时,配伍液中黄芩苷较稳定,头孢唑林钠降解遵循一级动力学反应,20℃t0．9为13．8d,t1/2为90．5d。室温留样观察4h,配伍前后药物残存率〉95％,pH、外观均无明显改变。结论：该法适合于同时测定双黄连和头孢唑林钠的浓度,双黄连和头孢唑林钠可以配伍使用。     

五水头孢唑啉体外抗菌作用

目的 评价五水头孢唑啉(头孢类抗菌药)及其他常用抗菌药物对近3年临床分离致病菌的体外抗菌活性.方法 琼脂二倍稀释法测定MIC值;活菌计数法绘制杀菌曲线.对来自全国19家医院近3年临床分离的604株致病菌进行了MIC测定.结果 在革兰阳性需氧菌中,五水头孢唑啉对甲氧西林敏感金黄色葡萄球菌(MSSA)、表皮葡萄球菌(MSSE)、青霉素敏感肺炎链球菌(PSSP)以及B溶血组链球菌均有很好的抗菌活性,MIC90≤4 mg·L-1.在革兰阴性菌中,五水头孢唑啉对于不产超广谱β内酰胺酶(ESBLs)的肠杆菌科细菌,仍保持很好的抗菌活性,MIC≤8 mg·L-1.杀菌试验显示,五水头孢唑啉对葡萄球菌表现出典型的时间依赖性,但对大肠埃希菌的杀菌作用随药物浓度升高略有增强.结论 五水头孢唑啉对革兰阳性菌具有较好的抗菌活性,抗菌活性优于头孢氨苄、克拉霉素、克林霉素,略优于头孢替安,与阿莫西林/克拉维酸、头孢呋辛、左氧氟沙星相似;对不产ESBLs的肠杆菌科细菌也保持较好的抗菌活性,优于头孢氨苄,与阿莫西林/克拉维酸和头孢呋辛相似.     

高效液相色谱法-二极管阵列检测器考察注射用头孢唑啉钠与注射用氯诺昔康的配伍稳定性

目的考察注射用头孢唑啉钠与注射用氯诺昔康在氯化钠注射液中的配伍稳定性。方法在室温条件下,采用高效液相色谱法-二极管阵列检测器测定头孢唑啉钠与氯诺昔康配伍后0～6 h内的含量变化,并观察和检测此2种药配伍液的外观与pH值变化。结果在室温下,配伍液6 h内的含量、pH及外观均无明显变化。结论室温条件下,注射用头孢唑啉钠与注射用氯诺昔康在氯化钠注射液中6 h内保持稳定。     

中国内江猪头孢唑啉血药浓度及蛋白结合率的研究

目的 :研究中国内江猪肾脏排泄的药代动力学特点及头孢唑啉 (CEZ)血浆蛋白结合率。方法 :选择主要经肾脏排泄的CEZ为模型药 ,采用高效毛细管电泳法测定其血药浓度 ,并计算药代动力学参数 ;采用平衡透析法测定其血浆蛋白结合率。结果 :中国内江猪静注CEZ后 ,其代谢符合二室开放模型。血浆清除率 (Cls)为 8 3 5ml/kg·min 1,消除半衰期 (t1/ 2 β)为 2 7 3 5min。中国内江猪血浆白蛋白浓度为 45 5 4± 1 7 44μmol·L 1,CEZ蛋白结合率为 80 5 9%～ 5 8 2 2 % ,解离常数为 1 6 1 0± 2 67μmol·L 1。结论 :与正常人实验药动学参考值相比较 ,内江猪对CEZ的消除与人具有相似的规律 ,但清除率明显大于人。侧面提示肾脏排泄功能可能较人强。内江猪血浆白蛋白浓度、CEZ蛋白结合率较人低 ,而解离常数较人高 ,表明CEZ与中国内江猪血浆蛋白结合的动态平衡中 ,结合物稳定性差 ,处于游离状态的CEZ较多 ,更易于消除     

β‐Lactam Therapy for Methicillin‐Susceptible Staphylococcus aureus Bacteremia: A Comparative Review of Cefazolin versus Antistaphylococcal Penicillins

Methicillin‐susceptible Staphylococcus aureus (MSSA) bacteremia is associated with high morbidity and mortality. Traditionally, antistaphylococcal penicillins (ASPs) have been considered the agents of choice for the treatment of MSSA bacteremia. Vancomycin has been demonstrated to have poorer outcomes in several studies and is only recommended for patients with severe penicillin allergies. Although cefazolin is considered as an alternative to the ASPs for patients with nonsevere penicillin allergies, cefazolin offers several pharmacologic advantages over ASPs, such as more convenient dosing regimens, and antimicrobial stewardship programs are increasingly using cefazolin as the preferential agent for MSSA infections as part of cost‐saving initiatives. Concerns about susceptibility to hydrolysis by type A β‐lactamases, particularly at high inocula seen in deep‐seated infections such as endocarditis; selective pressures from unnecessary gram‐negative coverage; and lack of comparative clinical data have precluded recommending cefazolin as a first‐line therapy for MSSA bacteremia. Recent clinical studies, however, have suggested similar clinical efficacy but better tolerability, with lower rates of discontinuation due to adverse drug reactions, of cefazolin compared with ASPs. Other variables, such as adequate source control (e.g., intravascular catheter removal, debridement, or drainage) and enhanced pharmacodynamics through aggressive cefazolin dosing, may mitigate the role of cefazolin inoculum effect and factor into determining improved clinical outcomes. In this review, we highlight the utility of cefazolin versus ASPs in the treatment of MSSA bacteremia with a focus on clinical efficacy and safety.     

Topical vs Subconjunctival Treatment of Bacterial Corneal Ulcers

The efficacy of eye drops and subconjunctival injections in the treatment of bacterial corneal ulcers for each of the following combinations were compared: cefazolin for staphylococcal ulcers, gentamicin for staphylococcal ulcers, and gentamicin for pseudomonal ulcers. Topical and subconjunctival therapy were equally effective in reducing the numbers of viable bacteria in experimental corneal ulcers. Subconjunctival injections produced high but transient peaks followed by persistent low troughs. In contrast, eye drops produced moderate but sustained concentrations throughout the treatment period. Under the conditions of this study, it appears that transient high peaks are not needed to eliminate bacteria effectively from a corneal ulcer. Since eye drops and subconjunctival injections are equally effective, other factors should determine the preferred route or routes of therapy.     

高效液相色谱法测定血中头孢唑啉浓度

应用醋酸—醋酸铵30%甲醇溶液(pH4.6,离子强度0.02ml/L)为流动相,在YWG-C_(18)H_(37)反相柱上,水杨酸做内标,测定了人血浆中头孢唑啉浓度。头孢唑啉的平均回收率为100.07%,不同浓度水平测定结果的日内变异系数小于5.00%。检定限度为0.5μg/ml。10名患者(7男,3女)被测试。其Ⅰ组(20～35a),Ⅱ组(41～49a)和Ⅲ组(70～72a)患者的T_(1/2)分别为1.30、1.49和2.08h。其中一名慢性肾炎、左肾结石患者其T_(1/2)为4.10h。提示年龄大者或肾功损害的病人应该减少给药剂量或者延长给药间隔时间。