In vitro antibacterial activities of telithromycin against clinical isolates of Neisseria gonorrhoeae

In vitro antibacterial activity of telithromycin (TEL) against the isolates of Neisseria gonorrhoeae (212 isolates) derived from urine or genital secretion in 2002 (April to December) was examined in comparison with those of macrolides (erythromycin [EM], clarithromycin [CAM]), penicillins (penicillin G [PCG]), cephems (cefodizime [CDZM], cefixime [CFIX]), quinolones (levofloxacin [LVFX]), tetracyclines (minocycline [MINO]), and aminoglycosides (spectinomycin [SPCM]). The MIC of TEL was ranged from < or = 0.039 to 0.25 microg/mL and the MIC50 and MIC90 of TEL were respectively 0.125 and 0.25 microg/mL, which were the lowest values compared with those of other oral antibacterial agents measured. When compared TEL with other agents in the order of the MIC50 and MIC90, TEL was more superior to EM and CAM (both eight times), MINO (four times and twice), and LVFX (16 and 64 times). The MIC90 of TEL was superior in twice though the MIC50 was the same in comparison with CFIX. The CDZM resistant strain did not exist and SPCM also inhibit growth with 32 microg/mL or less that was the breakpoint MIC excluding one stock though the PCG sensitive strain was only 1.4% in the injection drug. However, clinical breakpoint MIC is not established, but the efficacy of TEL is prospective because of its high antibacterial activity to inhibit growth of all stocks for gonococcus with 0.25 microg/mL. It is expected that TEL can become an oral antibiotic recommended for treatment of gonococcus if dosage and administration are considered.     

淋病奈瑟菌的耐药性与喹诺酮耐药基因突变的相关性分析

目的 分析本地区淋病奈瑟菌临床菌株gyrA基因突变与喹诺酮类药物耐药的相关性.方法 采用琼脂稀释法检测37株淋病奈瑟菌临床菌株对6种抗生素的最小抑菌浓度(MIC),PCR法扩增淋病奈瑟菌临床菌株gyrA基因片段并测序.结果37株淋病奈瑟菌临床菌株对大砚霉素、头孢曲松、四环素、青霉素、氧氟沙星和环丙沙星的耐药率分别为0、...     

帕珠沙星对临床分离致病菌的体外抗菌活性研究

目的评价帕珠沙星的体外抗菌活性。方法采用琼脂二倍稀释法，测定帕珠沙星与左氧氟沙星对342株临床分离菌株的最低抑菌浓度（MIC）。结果帕珠沙星对革兰阴性菌和革兰阳性菌的MIC90分别为0．06～4和1～16μg／ml。对大肠埃希菌、阴沟肠杆菌、变形菌、铜绿假单胞菌、不动杆菌和链球菌的MIC90为0．06～4μg／ml，是左氧氟沙星的1／2～1／8;对肺炎克雷伯菌、金葡菌和表葡菌与左氧氟沙星抗菌作用相当，MIC90分别为0．5、1、1μg／ml；对流感嗜血杆菌、黏膜炎莫拉菌和粪肠球菌的MIC90为0．5、1、16μg／ml，高于左氧氟沙星（0．25、0．5、8μg／ml）。结论帕珠沙星对革兰阴性菌和革兰阳性菌均具有广谱的抗菌作用，对革兰阴性菌的抗菌活性优于革兰阳性菌。     

In vitro activity of sitafloxacin against clinical isolates in 2009

In vitro activity of sitafloxacin (STFX) and various oral antimicrobial agents against bacterial isolates recovered from clinical specimens between January and December 2009, at different healthcare facilities in Japan was evaluated. A total of 1,620 isolates including aerobic and anaerobic organisms was available for the susceptibility testing using the microbroth dilution methods recommended by Clinical Laboratory Standard Institute. The minimum inhibitory concentration of STFX at which 90% of isolates (MIC90) was 0.06 microg/mL for methicillin-susceptible Staphylococcus aureus and was equal to that of garenoxacin (GRNX), 2 times lower than that of moxifloxacin (MFLX), and 8 times lower than that of levofloxacin (LVFX). STFX inhibited the growth of all the isolates of Streptococcus pneumoniae at 0.06 microg/mL or less. The MIC90s of STFX ranged from 0.03 to 0.06 microg/mL and were 1 to 2 times lower than those of GRNX, 2 to 4 times lower than those of MFLX, and 16 to 32 times lower than those of LVFX. Against Streptococcus pyogenes, the MIC90 of STFX was 0.06 microg/mL and was 2 times lower than that of GRNX, 4 times lower than that of MFLX, and 32 times lower than that of LVFX. The MIC90 of STFX was 0.25 microg/mL for Enterococcus faecalis, and was 2 times lower than those of GRNX and MFLX, and 8 times lower than that of LVFX. The MIC90 of STFX for E. coli was 2 microg/mL, and the MIC90s of other 10 species of Enterobacteriaceae which were the lowest values of the quinolones tested ranged from 0.03 to 1 microg/mL. The MIC90 of STFX for Pseudomonas aeruginosa isolates recovered from urinary infections was 8 microg/mL and was 16 times lower than those of GRNX, MFLX and LVFX. The MIC90 of STFX for P aeruginosa isolates recovered from respiratory infections was 2 microg/mL and was 32 times lower than those of GRNX and MFLX, and 16 times lower than that of LVFX. STFX inhibited the growth of all the isolates of Haemophilus influenzae at 0.004 microg/mL or less, and was 2 to 4 times lower than those of GRNX, 8 times lower than those of MFLX, and 4 times lower than those of LVFX. The MIC90 of STFX was 0.008 microg/mL for Moraxella catarrhalis, and was 2 times lower than that of GRNX, 8 times lower than those of MFLX and LVFX. The MIC90s of STFX ranged from 0.015 to 0.12 microg/mL for all the species of anaerobic bacteria and were the lowest values of all the antimicrobial agents tested. In conclusion, the activity of STFX against Gram-positive cocci was comparable or superior to those of GRNX, MFLX and LVFX. STFX showed the most potent activity against Gram-negative bacteria and anaerobic bacteria of all the antimicrobial agents tested in this study.     

In vitro activity of novel rifamycins against gram-positive clinical isolates

We describe novel rifamycins that have improved activity, compared with rifampin, against clinical isolates of staphylococci and streptococci, with MIC(90)s of 0.008 and 0.0005 microg/ml, respectively. This enhanced antibacterial activity, along with their potential lack of drug-drug interactions, are considerations that suggest the potential of these novel rifamycins in combination therapy to treat serious Gram-positive infections.     

In vitro activity of faropenem against beta-lactamase producing clinical isolates

Each 20 strains of beta-lactamase producing methicillin susceptible Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and Bacteroides fragilis group were used as the test strains. Drug susceptibility of these strains to faropenem (FRPM), cefdinir, cefditoren, cefcapene, cefteram, cefaclor, and ampicillin was determined by an agar dilution method according to the NCCLS guideline M100-S9. beta-Lactamase activity of the test strains was determined by a spectrophotometric method. In the present study, FRPM was highly active against beta-lactamase-producing strains, and no close correlation was found between the MICs of FRPM for the test strains and their beta-lactamase activities. These results suggest that FRPM has potential in successful application for the treatment of infectious diseases with various types of bacterial pathogens including beta-lactamase producing strains.     

In vitro activity of doripenem against Acinetobacter baumannii clinical isolates

Doripenem is a carbapenem with activity against Gram-positive and Gram-negative pathogens. This study evaluated the in vitro activity of doripenem against a collection of 87 Acinetobacter baumannii clinical isolates, showing that the activity of doripenem was superior to imipenem and meropenem for strains carrying the bla(OXA-58) gene. A. baumannii clinical isolates expressing the bla(OXA-24) gene were resistant to doripenem, imipenem and meropenem. However, in clinical isolates expressing the bla(OXA-58) gene, the percentage of isolates with a doripenem minimum inhibitory concentration >8microg/mL was much lower than that of imipenem and meropenem. This study shows that the activity of doripenem was superior to imipenem and meropenem for strains carrying the bla(OXA-58) gene.     

Nitroimidazoles with antibacterial activity against Neisseria gonorrhoeae.

Nitroimidazoles have been prepared which show interesting activity against the bacterium, Neisseria gonorrhoeae, in addition to the activities usually shown by nitroimidazoles against protozoa and anaerobic bacteria. The compounds were prepared by alkylation of 1-methyl-2-mercaptoimidazole, followed by nitration. Optimum activity occurs with a 5-nitro group and a free carboxyl at the end of the group attached to the sulfur. The linkage between the sulfur atom and the carboxyl group can be alkylene or phenoxyalkylene. These compounds have only weak activity against other aerobic or facultative bacteria.     

哌拉西林／舒巴坦对临床分离菌的体外抗菌作用

目的 对哌拉西林／舒巴坦进行体外抗菌活性研究。方法 采用琼脂二倍稀释法测定最低抑菌浓度,采用肉汤稀释法测定最低杀菌浓度,并对其影响因素进行测定。结果 本品对肠杆菌科细菌、非发酵菌、葡萄球菌、粪肠球菌抗菌活性均低于亚胺培南,对不产酶流感嗜血杆菌和粘膜莫拉氏菌抗菌活性高于亚胺培南2－16倍。对肺炎链球菌和嗜麦芽黄单胞菌的抗菌活性同本次所研究的所有对照药。对临床常见5种致病菌（铜绿假单胞菌、大肠埃希氏菌、肺炎克雷伯氏菌、金葡球菌和粪肠球菌）的MIC和MBC非常接近,差异在0－2之间,表明本品为一杀菌剂。     

Comparison of gyrA gene mutations between laboratory-selected ofloxacin-resistant Mycobacterium tuberculosis strains and clinical isolates

To understand the relationship between mutations in the quinolone resistance-determining region (QRDR) of the gyrA gene and drug resistance to ofloxacin, 85 laboratory-selected ofloxacin-resistant Mycobacterium tuberculosis mutant strains and 110 M. tuberculosis clinical isolates, screened by denaturing high-performance liquid chromatography to contain mutations, were analysed for their mutation patterns by sequencing as well as their ofloxacin minimal inhibitory concentrations (MICs). All mutations detected occurred at the codons Ala74, Ala90, Ser91 and Asp94 in all strains. One of the five different forms of missense mutation in Asp94 occurred in 60% of the laboratory-selected strains and 78% of the clinical isolates. However, 53 clinical isolates (48%) and only 2 laboratory-selected strains (2.4%) harboured double point mutations. The mutation Ala74Ser occurred only in the clinical isolates and only in combination with the Asp94Gly mutation. The ofloxacin MIC for the clinical isolates ranged from 0.5microg/mL to 20microg/mL, whilst the MICs for the laboratory-selected strains were > or =10microg/mL. The differences in gyrA gene mutation patterns and MICs between the laboratory-selected resistant strains and clinically isolated resistant strains identified here might help to understand the mechanisms involved in fluoroquinolone resistance.     

In vitro study of the antibacterial activity of ofloxacin against recent clinical isolates

The in vitro activity of ofloxacin, a new broad-spectrum antimicrobial agent, was studied by a standardized single disc method. A total of 990 clinical isolates were tested, including 20 strains of anaerobic bacteria. Ofloxacin was highly active against 683 strains (70.41%), had intermediate activity against 109 (11.23%) and had no activity against 178 (18.35%). Ofloxacin was highly active against E. coli, Klebsiella sp., Citrobacter sp., Proteus mirabilis, Proteus morganii, Salmonella sp., Campylobacter jejuni, Haemophilus influenzae, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Eubacterium sp., Propionibacterium acnes and Streptococcus sp. Pseudomonas sp., Serratia sp. and Proteus vulgaris had percentages of resistance to ofloxacin of 37.11%, 32% and 33.33% respectively. High percentages of resistance to ofloxacin were found only for Providencia sp., Proteus rettgeri and Bacteroides fragilis. With regard to Streptococcus faecalis, the results obtained with the disc procedure were not reliable and MIC determination was necessary to assess the behaviour of the drug.     

小建中胶囊对幽门螺杆菌体外抑菌作用的研究

目的探讨小建中胶囊浸膏液在体外对幽门螺杆菌(Helicobacter pylori,Hp)是否存在抑菌作用及其最低抑菌浓度(Minimum inhibitory concentration,MIC)。方法国际标准菌株NCTC11637和临床分离的4例多药耐药菌株及3例敏感菌株作为实验菌株。采用打孔法测定小建中胶囊对幽门螺杆菌体外是否有抑菌作用,并用琼脂稀释法测定小建中胶囊浸膏液对Hp菌株的MIC值。结果小建中胶囊对Hp标准菌株和临床分离的敏感及耐药菌株体外均有抑菌作用,其MIC值为0.78~1.56 mg/m L,且对抗生素耐药和敏感菌株之间无差别。结论小建中胶囊在体外对Hp有抑菌作用,有望用于Hp相关性疾病的治疗。     

In vitro activity of garenoxacin against recent clinical isolates of Chlamydia pneumoniae

The in vitro activities of garenoxacin, a novel des-F (6)-quinolone, levofloxacin, moxifloxacin and clarithromycin were tested against 30 recent clinical isolates of Chlamydia pneumoniae. The minimal inhibitory concentration (MIC) at which 90% of the isolates were inhibited and the minimal bactericidal concentration (MBC) at which 90% of the isolates were killed by garenoxacin for C. pneumoniae was 0.03 mg/l (range 0.015–0.03 mg/l).     

In vitro activity of antimicrobial agents against clinical isolates of Pseudomonas aeruginosa

Two hundred and seven clinical isolates of Pseudomonas aeruginosa were collected at Tenri Hospital between April 2003 and March 2004. We determined the minimum inhibitory concentration (MIC) of 16 antimicrobial agents, including prulifloxacin, pazufloxacin and biapenem which were recently published in Japan, against these isolates according to the guidelines of the Clinical and Laboratory Standards Institute. For the fluoroquinolones, the rank order of activity was prulifloxacin (MIC50, 0.5 microg/ml)>ciprofloxacin (1 microg/ml)> pazufloxacin (2 microg/ml)=levofloxacin (2 microg/ml)>gatifloxacin (4 microg/ml). For the carbapenems, the rank order of activity was meropenem (MIC50, 1 microg/ml)=biapenem (1 microg/ml)>imipenem (2 microg/m)>panipenem (8 microg/ml). For the cephalosporins and monobactam, the overall rank order of activity was cefozopran (MIC50, 4 microg/ml)= ceftazidime (4 microg/ml)>cefepime (8 microg/ml)=piperacillin/tazobactam (8 microg/ml)>aztreonam (16 microg/ml)= cefoperazone/sulbactam (16 microg/ml)=cefpirome (16 microg/ml). The rates of susceptibility to antimicrobial agents as per the criteria of the Japanese Society of Antimicrobial Chemotherapy were especially high for cefozopran (63%), biapenem and meropenem (61%), and pazufloxacin (53%) and ciprofloxacin (53%). These findings suggest that prulifloxacin, pazufloxacin and biapenem, which are newly introduced, are clinically effective in the treatment of infection caused with P. aeruginosa.     

In vivo activity of gemifloxacin, moxifloxacin and levofloxacin against pneumococci with gyrA and parC point mutations in a sepsis mouse model measured with the all or nothing mortality end-point

A dose-decreasing immunocompetent sepsis mouse model was used to evaluate the in vivo effect of levofloxacin, moxifloxacin and gemifloxacin, using a ciprofloxacin/levofloxacin susceptible serotype 6B strain (ciprofloxacin MIC: 1 mg/l) and two resistant serotype 14 and 19F strains with gyrA and parC point mutations (ciprofloxacin MICs of 32 and 64 mg/l, respectively). Significant higher in vivo activity was found for moxifloxacin and gemifloxacin than for levofloxacin against strains 1 and 2, and for gemifloxacin versus moxifloxacin or levofloxacin against strain 3. Gemifloxacin treatment resulted in 100% survival against strains 1 and 2(AUC0-24 h/MIC of 30 and 62) but against strain 3, survival was 60-80% (AUC0-24 h/MIC of 93). Similar AUC0-24 h/MIC values produced different therapeutic results suggesting that in vitro parameters other than the MIC could influence efficacy predictions based on in vitro susceptibility tests (MICs) or pharmacodynamic parameters (AUC0-24 h/MIC).     

In vitro activity of clinafloxacin against fluoroquinolone resistant Spanish clinical isolates.

The in vitro activity of clinafloxacin against 162 ciprofloxacin-resistant clinical isolates was determined. Isolates were selected when their MIC to ciprofloxacin was 2 mg/l (intermediate) or > 2 mg/l (resistant). The following strains were tested: 61 Escherichia coli, 12 Klebsiella pneumoniae, 7 Proteus mirabilis, 21 Serratia marcescens, 4 Enterobacter cloacae, 21 Pseudomonas aeruginosa, 21 Staphylococcus. aureus (resistant to methicillin) and 15 Enterococcus spp. Clinafloxacin, ciprofloxacin, ofloxacin and norfloxacin activities were evaluated by agar dilution using Müeller-Hinton agar according to NCCLS recommendations. Of the 162 isolates, 16 (9.8%) were intermediate and 146 (90.1%) resistant to ciprofloxacin. 95 of the 162 strains (58.6%) were susceptible, 27 (16.7%) intermediately susceptible, and 40 strains (24.7%) were resistant to clinafloxacin. The percentage susceptible to clinafloxacin was 65.6% for E. coli, 75% for K. pneumoniae, 71.4% for P. mirabilis, 28.6% for S. marcescens, 75% for E. cloacae, 33.3% for P. aeruginosa, 90.5% for S. aureus and 40% for Enterococcus spp. Clinafloxacin was active against 58.6% of the ciprofloxacin-resistant clinical isolates tested. It was particularly active against S. aureus strains resistant to both ciprofloxacin and methicillin.     

4种β-内酰胺类抗生素对临床分离致病菌的体外抗菌活性

目的 对比研究头孢呋辛、头孢克洛、头孢噻肟和阿莫西林等4种β-内酰胺类抗生素对随机选取的临床分离致病菌的体外抗菌活性。方法 随机收集2006-2007年解放军总医院微生物科和空军总医院感染控制科分离的部分临床致病菌，采用琼脂平板稀释法测定最低抑菌浓度（MIC）。结果 头孢呋辛对金葡菌、表葡菌的敏感率分别为45％和83．33％，抗菌活性显著强于头孢克洛，对肺炎克雷伯菌、大肠埃希菌、阴沟肠杆菌及不动杆菌的敏感率分别为38．10％、30．77％、0、0，高于阿莫西林，弱于头孢噻肟。结论 第二代头孢菌素目前对大部分革兰阳性菌仍具有较强的抗菌活性，但对革兰阴性菌的抗菌活性明显弱于第三代头孢菌素。