泵抑制剂对嗜麦芽寡养单胞菌氟喹诺酮主动外排表型特征的影响

目的:探讨主动外排泵在嗜麦芽寡养单胞菌对氟喹诺酮类药物耐药中的作用。方法:用泵抑制剂氰氯苯腙(CCCP)和利血平对5种氟喹诺酮类药物抗菌活性进行干预。采用琼脂二倍稀释法检测泵抑制剂存在时,嗜麦芽寡养单胞菌对莫西沙星、加替沙星、左氧氟沙星、洛美沙星、环丙沙星敏感性的变化。结果:主动外排泵不仅存在于耐药菌株,而且也存在于敏感菌株,但对耐药菌株影响更大。与泵阴性组比较,泵阳性组敏感率降低在左氧氟沙星、洛美沙星、环丙沙星组有统计学差异;耐药率增加在洛美沙星、环丙沙星组有统计学差异。结论:主动外排泵抑制剂CCCP和利血平可增强氟喹诺酮类药物对嗜麦芽寡养单胞菌的抗菌活性,对其耐药表型有影响。主动外排机制是嗜麦芽寡养单胞菌对氟喹诺酮类药物耐药的原因之一。     

泌尿系感染病原菌对氟喹诺酮类抗菌药物耐药性研究

目的了解我院越尿系感染患者病原菌分布及对4种氟喹诺酮类抗菌药物耐药情况。方法收集2003年1月～2005年10月自我院分离的780株细菌。采用纸片扩散法进行4种氟喹诺酮类抗菌药物药敏试验。结果从尿液标本分离的780株病原菌中，大肠埃希菌、肠球菌、表皮葡萄球菌、铜绿假单胞菌、肺炎克雷伯菌分列前五位（47．2％、17．6％、9．9％、6．7％和5．4％）。大肠埃希菌产ESBLs株检出率为45．7％，肺炎克雷伯菌产ESBLs株检出率为28．6％．耐甲氧西林表皮葡萄球菌（MRSE）和高水平庆大霉素耐药肠球菌（HLGR）检出率分别为74．0％和81．0H．它们对4种氟喹诺酮类抗菌药物的耐药率高于非MRSE、非HLGR和非产ESBLs菌株，呈现多重耐药的趋势。结论大肠埃希菌仍然是泌尿系感染的主要致病菌，尿路感染应根据抗生素敏感试验选择敏感药物进行舍理用药，并应检测MRSE，HLGR和产ESBLs菌株的多重耐药情况。     

加替沙星在眼科的应用研究进展

加替沙星是一种广谱、高效的新型氟喹诺酮类抗菌药物，在眼科领域的应用研究正在蓬勃开展。本文对加替沙星的抗菌活性、眼内通透性、眼科实验治疗研究、滴眼液的临床疗效和安全性研究最新进展作一综述。     

7-{4-［2-［2-取代-4-((5S)-5-乙酰胺甲基-2-氧代-噁唑烷-3-基)苯基］乙基］哌嗪-1-基}-氟喹诺酮类化合物的合成与抗菌活性

目的寻找新型的噁唑烷酮-氟喹诺酮类抗菌药物。方法设计合成了7-{4-［2-［2-取代-4-((5S)-5-乙酰胺甲基-2-氧代-噁唑烷-3-基)苯基］乙基］哌嗪-1-基}-氟喹诺酮类化合物，测定其体外抗菌活性。结果共合成20个目标化合物，经^{1H NMR和MS确证结构。目标化合物具有较好的体外抗菌活性，尤其是化合物22，对屎肠球菌的抑制活性分别是吗啉噁酮和诺氟沙星的16倍和64倍，对金葡菌的抑制活性为吗啉噁酮的4倍。结论某些带有氟喹诺酮结构片段的噁唑烷酮类化合物抗菌活性加强。}     

儿童肺炎链球菌对β-内酰胺类、大环内酯类和氟喹诺酮类抗菌药物敏感性研究

目的了解2002 2004年北京儿童医院门诊5岁以下呼吸道感染儿童鼻咽拭子中分离出的肺炎链球菌,对β-内酰胺类、大环内酯类和氟喹诺酮类抗菌药物的耐药性。方法使用E试验法(E-test)对114株肺炎链球菌进行抗菌药物的敏感性试验。结果114株肺炎链球菌对青霉素不敏感率为36%,对阿莫西林/棒酸全部敏感,对头孢菌素中头孢曲松不敏感率为6.1%,头孢呋辛为30.7%,头孢克洛为29%,大环内酯类耐药率在90%左右,全部菌株对氟喹诺酮类敏感。结论儿童肺炎链球菌对青霉素和头孢二代抗菌药物不敏感率为29%~36%,对大环内酯类耐药在90%左右,未发现对氟喹诺酮类耐药菌株。     

Prospective Randomized Comparative Study of Antibiotic Prophylaxis in Urethrocystoscopy and Urethrocystography

Background : There has been a great deal of discussion regarding the necessity of the prophylactic use of antibiotics in transurethral procedures. In order to clarify this complicated issue, a randomized prospective study was performed for patients undergoing urethrocystoscopy or urethrocystography.
Patients and Methods : Patients who underwent urethrocystoscopy or urethrocystography and did not have pyuria and bacteriuria were included and divided randomly into 2 groups, either receiving a prophylactic antibiotic or no antibiotic. For antibiotic prophylaxis, 200 mg of sparfloxacin or fleroxacin were administered within a 1-hour period before the urethrocystoscopic or urethrocystographic examination, respectively. Analyses were performed on patients who were seen within 1 month after the examination, using the appearance of pyuria, bacteriuria, or a febrile infection as the endpoint.
Results : Of47 patients undergoing urethrocystoscopy, 45 were eligible for analysis, and of these, sparfloxacin was administered to 21 patients. Thirty-three of 37 patients undergoing urethrocystography were eligible for analysis with fleroxacin administered to 16 patients. There were no significant differences in the background factors between the 2 groups undergoing either transurethral examination. None of the patients in either group developed pyuria, bacteriuria or a febrile infection after the examination.
Conclusions : Prophylactic administration of antibiotics is not necessarily essential in urethrocystoscopy or urethrocystography in patients with sterile urine.     

Fluoroquinolone-resistant Escherichia coli carriage in long-term care facility

We conducted a cross-sectional study to determine the prevalence of, and risk factors for, colonization with fluoroquinolone (FQ)-resistant Escherichia coli in residents in a long-term care facility. FQ-resistant E. coli were identified from rectal swabs for 25 (51%) of 49 participants at study entry. On multivariable analyses, prior FQ use was the only independent risk factor for FQ-resistant E. coli carriage and was consistent for FQ exposures in the previous 3, 6, 9, or 12 months. Pulsed-field gel electrophoresis of FQ-resistant E. coli identified clonal spread of 1 strain among 16 residents. Loss (6 residents) or acquisition (7 residents) of FQ-resistant E. coli was documented and was associated with de novo colonization with genetically distinct strains. Unlike the case in the hospital setting, FQ-resistant E. coli carriage in long-term care facilities is associated with clonal spread.     

Fluoroquinolone and other antimicrobial resistance in invasive pneumococci, Hong Kong, 1995-2001

We determined the susceptibilities of 265 invasive isolates of pneumococci obtained during 1995 to 2001 in Hong Kong to 11 antimicrobial agents and their serotypes. Overall, 62.6% isolates were susceptible to penicillin, 20% were intermediately resistant, and 17.4% were resistant. The overall prevalence of levofloxacin resistance (MIC > or = 8 microg/mL) was 3.8% but increased to 15.2% among the penicillin-resistant isolates. All levofloxacin-resistant isolates were clonally related; had reduced susceptibility to penicillin, cefotaxime, and clarithromycin; and were derived from adults > or = 50 years of age. Of the penicillin-nonsusceptible pneumococci, 90% from children < or = 5 years of age and 54.8% from persons of all ages were of serotypes that are included in the 7-valent pneumococcal conjugate vaccine; 93.5% from children < or = 5 years of age and 93% from persons of all ages were of serotypes that are included in the 23-valent polysaccharide vaccine.     

5-氨基-1-环丙基-6,7,8-三氟-1,4-二氢-4-氧代-3-喹啉羧酸乙酯的合成

由６－硝基－２,３,４,５－四氟苯甲酸为原料,经酰氯化后与β－环丙基氨基丙烯酸乙酯反应,再经环合、还原得标题化合物（１）,总收率５１．６％ 。由五氟苯甲酸依同法可制得１－环丙基－５,６,７,８－四氟－１,４－二氢－４－氧代－３－喹啉羧酸乙酯（６ｂ）,总收率为４８．７％ 。     

Emergence of fluoroquinolone‐resistant clonal group A: clonal analysis of Norwegian and Russian E. coli isolates

Strand L, Jenkins A, Grude N, Allum A‐G, Mykland H‐C, Nowrouzian FL, Kristiansen B‐E. Emergence of fluoroquinolone‐resistant clonal group A: clonal analysis of Norwegian and Russian E. coli isolates. APMIS 2010; 118: 571–77. We describe a study of urinary tract and intestinal isolates of Escherichia coli from Norway and Russia using automated ribotyping, single nucleotide polymorphism analysis for clonal group A (CgA) supplemented with phylogrouping, virulence gene profiling and resistance profiling. CgA comprised 19% of the Norwegian UTI isolates from 2001. Two highly multiresistant fluoroquinolone‐resistant CgA isolates were found. Ribotypes clustered into four major and six minor groups (ribogroups). Fluoroquinolone‐resistant isolates and phylogroups A and B1 were associated with ribogroup ^RA. Ribogroup ^RB predominated among Russian UTI isolates and was predominantly phylogroup A and depleted in P‐fimbriae. Ribogroup ^RC predominated among Norwegian UTI isolates and was rich in virulence factors (S‐fimbriae, haemagglutinin and haemolysin) and predominantly phylogroup B2 and D. Ribogroup ^RG was associated with CgA and predominantly phylogroup D. Ribogroups ^RD, ^RE and ^RF had too few members for statistical analysis. The correlation between ribotype and phylogenetic group was not as strong as reported in other studies.