抗菌药物临床应用指导原则

头孢菌素类根据其抗菌谱、抗菌活性、对β内酰胺酶的稳定性以及肾毒性的不同，目前分为四代。第一代头孢菌素主要作用于需氧革兰阳性球菌，仅对少数革兰阴性杆菌有一定抗菌活性；常用的注射剂有头孢唑林、头孢噻吩、头孢拉定等，口服制剂有头孢拉定、头孢氨苄和头孢羟氨苄等。第二代头孢菌素对革兰阳性球菌的活性与第一代相仿或略差，对部分革兰阴性杆菌亦具有抗菌活性；注射剂有头孢呋辛、头孢替安等，口服制剂有头孢克洛、头孢呋辛酯和头孢丙烯等。     

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.     

药品不良反应信息通报（第59期）关注头孢唑林注射剂的严重不良反应

头孢唑林为β-内酰胺类广谱抗生素,为第一代注射用头孢菌素。该药对大多数敏感的革兰阳性球菌与常见的革兰阴性杆菌均有较强抗菌作用。目前,我国批准的头孢唑林注射剂有注射用头孢唑林钠和注射用五水头孢唑林钠两种。     

关注头孢唑林注射剂的严重不良反应

头孢唑林属β－内酰胺类广谱抗菌药,为第一代注射用头孢菌素。该药对大多数敏感的革兰阳性球菌与常见的革兰阴性杆菌均有较强抗菌作用。目前,我国批准的头孢唑林注射剂有注射用头孢唑林钠和注射用五水头孢唑林钠两种。     

加替沙星体外抗菌活性研究

采用琼脂二倍稀释法测定加替沙星对651株临床分离致病菌的体外抗菌活性，并与左氧氟沙星、司帕沙星、环丙沙星、诺氟沙星、头孢唑林、头孢呋辛、头孢噻肟、头孢他啶、万古霉素、阿米卡星、阿莫西林、哌拉西林/三唑巴坦比较。结果表明，加替沙星具有强而广谱的体外抗菌活性。对甲氧西林敏感的金葡球菌（MSSA）、表葡球菌（MSSE）、肠球菌的MIC90分别为0.125、1、16mg/L，抗菌活性为左氧氟沙星的1-2倍、环丙沙星的2-4倍，逊于第三代头孢菌素类。对肺炎克雷伯氏菌、伤寒沙门氏菌、痢疾杆菌、奇异变形菌、粘质沙雷氏菌，MIC90分别为4、0.25、0.5、4.32mg/L，抗菌活性为左氧氟沙星、司帕沙星、环丙沙星的1-2倍，与第三代头孢菌素类相当。对聚团肠杆菌、阴沟肠杆菌、乙酸钙不动杆菌、铜绿假单胞菌的MIC90分别为32、32、16.4mg/L。加替沙星对革兰氏阳性、阴性菌均具强大抗菌作用。     

第四代头孢菌素——头孢唑兰

头孢唑兰是第四代注射用头孢菌素，抗菌谱包括好氧性革兰阴性菌和革兰阳性菌及多数厌氧菌。由日本武田制药公司开发，1995年上市，2005年专利到期，国内正在研究开发。     

国家食品药品监督管理总局提醒关注头孢唑林注射剂的严重不良反应

<正>本刊讯2014年1月26日,国家食品药品监督管理总局发布第59期《药品不良反应信息通报》,提醒关注头孢唑林注射剂严重不良反应。头孢唑林为β-内酰胺类广谱抗生素,为第1代注射用头孢菌素。该药对大多数敏感的革兰阳性球菌与常见的革兰阴性杆菌均有较强的抗菌作用。目前,我国批准的头孢唑林注射剂有注射用头孢唑林钠和注射用五水头孢唑林钠两种。     

头孢呋辛钠与炎琥宁在输液中的配伍稳定性考察

<正>头孢呋辛为第二代头孢菌素,对革兰阳性菌和阴性菌均有较强的抗菌活性,肾毒性较第一代头孢菌素有所降低,因此临床应用十分广泛。炎琥宁为中草药穿心莲提取的有效成     

头孢布烯(Ceftibuten)体外抗菌作用

目的:评价头孢布烯对临床分离的836株致病菌的体外抗菌作用.方法:头孢布烯与头孢克肟、头孢他啶、头孢噻肟、头孢呋辛、头孢克罗、头孢拉啶、环丙沙星进行比较.结果:头孢布烯对大多数革兰阴性菌具有很强的抗菌活性,如对大肠杆菌、肺炎克雷白杆菌、奇异变形杆菌、普通变形杆菌、沙门菌属、志贺菌属、粘质沙雷菌、阴沟肠杆菌的MIC90值均≤1mg·L-1,优于所测定的其他口服头孢菌素,与头孢他啶、头孢噻肟相似.头孢布烯对淋病奈瑟菌、流感嗜血杆菌也有很强的抗菌活性,但对某些肠杆菌科杆菌如弗劳地枸橼酸杆菌对本品与头孢他定相似不太敏感,MIC90值为8mg·L-1,乙酸钙不动杆菌对本品耐药,MIC90值为32 mg·L-1.头孢布烯对革兰阳性菌除化脓性链球菌外作用均较弱.对肺炎链球菌的MIC50与MIC90值分别为2与4mg·L-1,不及其他所测定的三代头孢菌素.金黄色葡萄球菌、粪肠球菌、脆弱拟杆菌对头孢布烯耐药.从产酶大肠杆菌及肺炎克雷白菌的体外抗菌作用的结果表明,头孢布烯对产酶菌株具有较强的抗菌活性,MIC90值低于其他所测定的三代头孢菌素.结论:说明本品具有较强的β-内酰胺酶稳定性.细菌接种量、pH值的变化、人血清的含量对头孢布烯的体外抗菌作用无明显影响.     

国产克林霉素体外抗菌活性研究

目的:研究国产克林霉素对临床分离的300株需氧菌和30株厌氧菌的体外抗菌活性,并与红霉素和头孢拉定作比较.方法:采用美国NCCLS推荐的琼脂稀释法测定菌株对抗菌药物的MIC(最低抑菌浓度),并以MIC50、MIC90和抑制百分率,表示药物的抗菌活性.结果:克林霉素对流感嗜血杆菌MIC50为＜0.03mg/L,与红霉素和头孢拉定相同,抑制率为88%,强于红霉素,稍弱于头孢拉定;对卡他莫拉菌的MIC50为0.125mg/L,抑制率为80%,强于头孢拉定;克林霉素对甲氧西林敏感的金黄色葡萄球菌和表皮葡萄球菌MIC50分别为0.125mg/L和2mg/L,远强于红霉素;对甲氧西林耐药的金黄色葡萄球菌(MRSA)MIC50为1mg/L,抑制率:66.7%,强于红霉素和头孢拉定;对肺炎链球菌MIC50为0.125mg/L,抑制率为77.5%,强于红霉素,稍弱于头孢他定;克林霉素对A群链球菌和B群溶血菌的MIC50分别为2mg/L和0.06mg/L,抑制率为76.6%,强于红霉素,弱于头孢拉定;克林霉素对厌氧菌包括厌氧球菌、丙酸杆菌、梭杆菌和拟杆菌属,抑制率均为100%.结论:国产克林霉素对临床分离的溶血性链球菌、肺炎链球菌、甲氧西林敏感的金黄色葡萄球菌和表皮葡萄球菌、嗜血杆菌、卡他莫拉菌和厌氧菌均有良好的抗菌活性.     

In vitro susceptibility of 4903 bacterial isolates to gemifloxacin--an advanced fluoroquinolone

The in vitro activity of gemifloxacin against over 4900 bacterial isolates was determined by microbroth dilution with interpretation in accordance with NCCLS guidelines. Susceptibility results were compared with those for ciprofloxacin, gatifloxacin, levofloxacin and moxifloxacin. Gemifloxacin and the other fluoroquinolones were not affected by either beta-lactamase production or penicillin-resistance in Streptococcus pneumoniae. The MIC90 values for gemifloxacin were: S. pneumoniae 0.063 mg/l; Haemophilus influenzae 0.016 mg/l; Moraxella catarrhalis 0.008 mg/l, methicillin-susceptible Staphylococcus aureus 0.063 mg/l; methicillin-susceptible Streptococcus pyogenes 0.031 mg/l; Enterobacteriaceae 0.031-0.16 mg/l; Pseudomonas aeruginosa 4 mg/l; Neisseria meningitidis 0.008 mg/l. The MIC90 for gemifloxacin was lower than those for the other quinolones tested against S. pneumoniae (ciprofloxacin 2-4 mg/l, gatifloxacin 0.5 mg/l, levofloxacin 1-2 mg/l, moxifloxacin 0.25 mg/l). This study confirms the enhanced potent activity of gemifloxacin against Gram-positive pathogens, its broad-spectrum, Gram-negative activity and indicates that gemifloxacin is likely to have an important role in treating patients with Gram-positive and/or Gram-negative infections.     

Susceptibility of clinical isolates of gram-positive and gram-negative organisms to cefatrizine

The in vitro activity of cefatrizine was evaluated against 294 Gram-positive and 270 Gram-negative bacteria isolated from clinical specimens. Cefatrizine had excellent activity against Gram-positive cocci, inhibiting all except enterococci at minimal inhibitory concentrations below 1 mcg/ml. Moreover, cefatrizine was an effective antibacterial agent for most major Gram-negative species. Cefatrizine activity was tested against 34 strains of H. influenzae and 37 strains of K. pneumoniae and compared with that of other orally administered cephalosporins. Cefatrizine MIC50 values were much lower than those recorded for cephalexin and cefadroxil.     

In vitro studies with Bay V 3522, a new oral cephalosporin

The in vitro activities of Bay v 3522, cefaclor, cephalexin, cefuroxime, cefixime, amoxicillin/clavulanate (2:1) and reference penicillins were compared against 314 clinical isolates of Gram-positive and Gram-negative bacteria and nine strains of Escherichia coli that differed in their outer membrane proteins in agar dilution tests with an inoculum of 10(4) cfu/spot. The beta-lactamase stabilities of the cephalosporins were also evaluated by spectrophotometric assay using 21 different beta-lactamases. Bay v 3522 was the most potent cephalosporin overall against Gram-positive pathogens, but slightly less active than amoxicillin/clavulanate. In addition to being highly active against streptococci (MIC90 = 0.25 micrograms/ml) and methicillin-susceptible staphylococci (MIC90 = 1.0 micrograms/ml), Bay v 3522 was markedly more active than the other cephalosporins against Enterococcus faecalis (MIC90 = 4 micrograms/ml). Bay v 3522 was less potent against Gram-negative pathogens, especially nosocomial isolates of Escherichia coli and Klebsiella pneumoniae (MIC90 greater than 64 micrograms/ml), but was active against Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and beta-lactamase-negative Neisseria gonorrhoeae (MIC90 = 1.0 micrograms/ml0. Hydrolysis of Bay v 3522 by most beta-lactamases examined was significantly less than that observed for cephalothin and cefaclor; similar to that observed with cephalexin; and less than that observed with cefixime and cefuroxime. None of the beta-lactamases examined hydrolysed Bay v 3522 at a rate greater than 20 nmol/min/mg. The in vitro potency of Bay v 3522 against Gram-positive and fastidious Gram-negative pathogens and its resistance to hydrolysis by beta-lactamases produced by them support further investigation of this cephalosporin as a new oral therapeutic agent.     

Comparative in vitro activity of LY 127935 (6059-S), seven cephalosporins, three aminoglycosides, carbenicillin, and ticarcillin

LY 127935 (6059-S), a new semi-synthetic beta-lactam antibiotic was tested simultaneously with 6 cephalosporins, 3 aminoglycosides, carbenicillin and ticarcillin against 398 clinical isolates of Gram-negative bacilli and Gram-positive cocci. Many of the organisms were selected for study because of known resistance to one or more of the clinically available antibiotics tested. Escherichia coli, Klebsiella, Serratia and Providencia were susceptible to LY 127935. Some resistant strains of Enterobacter, Proteus, Pseudomonas aeruginosa and Acinetobacter were also resistant to LY 127935, but many of the strains resistant to other antibiotics were susceptible to LY 127935. The activity of LY 127935 against Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans and Streptococcus bovis was similar to that of cephalexin and cephradine. LY 127935 was not active against methicillin-resistant S. aureus nor enterococcus.     

In vitro and in vivo evaluation of MDL 19,592, an oral cephalosporin

MDL 19,592 is a new semisynthetic cephalosporin with a good therapeutic potential against Gram-positive bacterial infections when administered orally or parenterally. In the oral treatment of benzylpenicillin-resistant Staphylococcus aureus infections in mice, MDL 19,592 was superior to cephalexin, cephradine, cefaclor, cefadroxil and cefroxadine. These in vivo results reflect the in vitro superiority expressed by MDL 19,592 over the other oral cephalosporins against staphylococci. Additionally, MDL 19,592 orally was superior to cefazolin and cephalothin administered subcutaneously and to a number of penicillinase-resistant penicillins given orally or subcutaneously in the treatment of S. aureus mouse infections. MDL 19,592 killed S. aureus cells at the same or faster rate than did cephalexin or cephradine. As compared to cephalexin, MDL 19,592 was marginally superior in vitro against Streptococcus pyogenes and Streptococcus pneumoniae. In vivo, MDL 19,592 was significantly the more effective of the two against S. pyogenes and marginally more effective against S. pneumoniae. Against Gram-negative organisms, with the exception of Haemophilus influenzae, cephalexin was the more potent of the two antibiotics both in vitro and in vivo. Administered orally to mice, MDL 19,592 was absorbed as rapidly as cephalexin with both drugs attaining similar concentrations in the blood. MDL 19,592, like cephalexin, was minimally bound by mouse serum.     

利奈唑胺、替考拉宁和万古霉素等抗菌药物对常见需氧革兰阳性球菌的体外抗菌活性

目的评价利奈唑胺、替考拉宁和万古霉素等抗菌药物的体外抗菌活性。方法采用琼脂稀释法对临床收集的132株革兰阳性球菌进行抗菌活性测定,记录其各自的MIC并进行比较。结果利奈唑胺、替考拉宁及万古霉素3药对革兰阳性球菌均有较大抗菌活性,敏感率均为100%,包括其中的耐甲氧西林葡萄球菌和青霉素中介肺炎链球菌均有良好抗菌作用。3药在部分革兰阳性球菌的抗菌作用中与利福平相仿,但比氨基糖苷类抗生素和氟喹诺酮类抗菌药强。在对甲氧西林敏感金葡萄的抗菌活性中,替考拉宁的MIC90均为利奈唑胺和万古霉素的4倍;在对甲氧西林敏感凝固酶阴性葡萄球菌的抗菌活性中,替考拉宁的MIC90分别均为利奈唑胺和万古霉素的8倍;而在青霉素敏感和中介肺炎链球菌的抗菌活性中,替考拉宁的MIC90为利奈唑胺的1/16,为万古霉素的1/8;在肠球菌属的抗菌活性中,万古霉素的MIC90分别为利奈唑胺的2倍,是替考拉宁的4倍和8倍。结论利奈唑胺、替考拉宁以及万古霉素等三药对革兰阳性球菌有较大的抗菌作用,对部分革兰阳性菌的抗菌作用与利福平相仿,但比其他如氨基糖苷类抗生素和氟诺酮类抗菌药更优,是临床革兰阳性球菌严重感染的有效药物。     

北京地区临床分离致病金黄色葡萄球菌常用抗生素敏感性研究

金黄色葡萄球菌是临床常见感染疾患致病菌,了解金黄色葡萄球菌对临床常用的β-内酰胺类抗生素的敏感性,对合理使用抗生素及时控制金黄色葡萄球菌感染是十分重要的.本文报告了北京地区临床分离致病金黄色葡萄球菌209株对16个β-内酰胺类抗生素敏感性研究结果.比较了16个抗生素对金黄色葡萄球菌的MIC范围、MIC_(50)、MIC_(90)、NIC_(mode)、MIC_(GM),并用I_(50)的指标比较客观地反映出同类药之间抗菌作用的差异.研究结果表明:青霉素类Oxacillin、Cloxacillin抗金黄色葡萄球菌的作用最强,两药的MIC_(60)、MIC_(90)相同,分别为0.25、0.5mg/L,但Cloxacillin的I_(50)值为0.20mg/L铰Oxacillin的0.23mg/L稍低,表明Cooxacillin的抗茵作用较Oxacillin好.Ampicillin与PenicllinG的抗菌作用相似,由于PencillinG临床常用剂量血浓度不高,PenicillinG临床抗金黄色葡萄球菌的疗效可能不理想.四种酰脲类抗生素抗菌作用的强弱次序是Furbenicillin、Mezlocillin、Azlocillin、Piperacillin,在多种细菌混合感染时选用Furbenicillin可能更好.Carbenicillin抗金黄色葡萄球菌的作用最差.头孢菌素类抗生素,第一代头孢菌素Cephalothin、Cefazolin抗金黄色葡萄球菌的作用明显优于第三代头孢菌素,一、二、三代头孢菌素随抗革蓝氏阴     

Azithromycin的体外抗菌作用

测定ａｚｉｔｈｒｏｍｙｉｎ（ＡＺＭ）体外抗菌作用，以红霉素（ｅｒｙｔｈｒｏｍｙｃｉｎ，ＥＭ）为对照，并与其它几种大环内酯类抗生素进行了比较，结果表明国产ＡＺＭ对ＥＭ敏感的革兰氏阳性菌的抗菌作用与ＥＭ相似，ＭＩＣ９０在０．５￣４．０ｍｇ／Ｌ范围内；对淋病奈瑟氏菌及流感嗜血杆菌的ＭＩＣ９０均为２ｍｇ／Ｌ，为ＥＭ的１／４；对大肠菌和肺炎克雷伯氏菌抗菌作用则明显优于ＥＭ。本品对金葡萄菌无杀菌作用，浓度为０     

Interference by cephalosporins with creatinine measurement by desk-top analyzers

Summary We have carried out a study to evaluate the interference by cephalosporins with the measurement of creatinine by desk-top analyzers. The cephalosporins evaluated at concentrations of 0–250 mg/l were cefazolin sodium, cefoxitin sodium, cefotaxime sodium, and ceftazidime pentahydrate. The instruments evaluated were DT60 (Kodak, Rochester, USA), Seralyzer (Ames Division, Miles Laboratories, IN, USA), and Vision (Abbott Labs, Chicago, USA). All studies were done in plasma.None of the cephalosporins showed any interference with the DT60 analyzer. With the Vision and Seralyzer no interference was seen with cefotaxime or cefazolin. With cefazolin an increase of 10–20 µmol/l creatinine was seen for every 20 mg/l of drug; with cefoxitin there was an increase of 50–80 µmol/l of creatinine for every 100 mg/l of drug.Erroneous creatinine values may be found in patients taking cefazolin and cefoxitin and may lead to inappropriate clinical management.     

Comparative in vitro activity of tigecycline and other antimicrobials against Gram-negative and Gram-positive organisms collected from the Asia-Pacific Rim as part of the Tigecycline Evaluation and Surveillance Trial (TEST)

As part of the Tigecycline Evaluation and Surveillance Trial (TEST), Gram-negative and Gram-positive organisms were collected from 31 medical centres in nine countries in the Asia-Pacific Rim between 2004 and 2007. Overall, 34.2% of Acinetobacter spp. were multidrug-resistant, and 17.0% of Klebsiella pneumoniae and 10.6% of Escherichia coli produced extended-spectrum beta-lactamases. A total of 39.5% of Staphylococcus aureus were meticillin-resistant and 21.7% of Enterococcus faecium were vancomycin-resistant. Tigecycline MIC(90) values (minimum inhibitory concentration for 90% of the organisms) were 相似文献