司帕沙星和妥舒沙星的体内外抗菌作用研究

目的观察国产司帕沙星、妥舒沙星及其它四种氟喹诺酮类抗菌药对成都地区780株临床分离菌的体外抗菌活性，并比较司帕沙星、妥舒沙星和环丙沙星对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠的体内抗菌活性。方法用琼脂稀释法测定国产司帕沙星和妥舒沙星的MIC50和MIC90，并与其它四种氟喹诺酮类抗菌药进行了比较。本文还测定了抗菌药对金葡球菌、大肠埃希菌和铜绿假单胞菌感染小鼠治疗的ED50结果体外试验表明司帕沙星和妥舒沙星能有效抑制或杀灭革兰阳性、革兰阴性菌及厌氧菌，显示了广谱抗菌活性。司帕沙星和妥舒沙星对革兰阳性菌的抗菌活性是环丙沙星的2～8倍，氧氟沙星和氟罗沙星的4～16倍，是诺氟沙星的16～32倍。司帕沙星对MRSA的抗菌活性与妥舒沙星相似，但优于环丙沙星、氧氟沙星、氟罗沙星和诺氟沙星。司帕沙星对大多数革兰阴性菌的抗菌活性与环丙沙星和妥舒沙星相似，是氧氟沙星、氟罗沙星和诺氟沙星的2～8倍。两药对厌氧菌的抗菌活性也较环丙沙星强。口服或皮下注射司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。三种受试药对金葡球菌和大肠埃希菌所致小鼠全身性感染的保护作用优于铜绿假单胞菌所致感染。结论司帕沙星和妥舒沙星对革兰阳性菌和厌氧菌的体外抗菌活性优于环丙沙星和其它药物，对大多数革兰阴性菌的抗菌活性与环丙沙星相似，但优于其它受试药。司帕沙星对金葡球菌和大肠埃希菌所致小鼠全身性感染的体内保护作用优于环丙沙星和妥舒沙星。同一给药途径下司帕沙星对铜绿假单胞菌所致小鼠全身性感染的保护作用与妥舒沙星和环丙沙星相似。     

洛美沙星与4种喹诺酮类和8种抗生素的体外抗菌活性比较

洛美沙星与４种氟喹诺酮药物以及８种抗生素体外抗菌活性比较结果显示：洛美沙星对多数革兰氏阴性菌具有良好的体外抗菌活性，其ＭＩＣ９０大都≤２μｇ／ｍｌ，对痢疾杆菌、伤寒杆菌、大肠杆菌、肺炎杆菌、哈夫尼亚菌、枸椽酸杆菌和产气肠杆菌的抗菌作用尤强，对金葡球菌亦具有一定的抗菌活性，对肺炎球菌和绿脓假单胞菌的抗菌作用较弱。与氧氟沙星和诺氟沙星的抗菌作用相似，稍优于依诺沙星，略逊于环丙沙星。与丁胺卡那霉素、头孢     

新型喹诺酮类抗菌剂IMB-86001的药效学研究

IMB-86001系我所合成室新研制的第三代喹诺酮类抗菌药物,我们对合成样品进行了药效学研究,并与其它喹诺酮类药物进行了比较,实验结果表明:IMB-86001对革兰氏阳性及阴性细菌均有较好的抗菌活性,对革兰氏阴性菌的抗菌作用更强。如对大肠杆菌、肺炎杆菌,变形杆菌、沙门氏菌及痢疾杆菌等的最低抑菌浓度(MIC)为0.011～0.39ug/ml;对绿脓杆菌的MIC为0.78～1.56μg/ml。其体外抗菌活性与环丙沙星相似或稍弱,而比依诺沙星和诺氟沙星强,明显优于吡哌酸。IMB-86001对感染小鼠的体内抗菌作用研究表明:IMB-86001对金葡球菌85-3及金葡球菌83-9均有良好的体内抗菌作用,其ED_(50)值低于环丙沙星,体内保护     

环丙沙星注射液的药效与临床应用

环丙沙星是一种新型氟代喹诺酮衍生物,与其他喹诺酮类相比,有较强的抗菌活性和较广的抗菌谱。经体内抗菌作用与体外敏感实验证明,本品明显优于氨苄青霉素、头孢唑林、庆大霉素及苯唑青霉素。环丙沙星对肠杆菌科抗菌作用更强,对绿脓肝菌、革兰氏阳性球菌作用比其他氟喹诺酮类强,对流感杆菌、淋球菌有很强的活性。且与青霉素类、头孢菌素类及氨基糖苷类抗生素无交叉耐药作用。具有抗菌范围广,抗菌活力     

洛美沙星的药效学研究

洛美沙星为一新型氟喹诺酮类药物,其抗菌谱广,抗菌作用强,本文报道其体内外抗菌作用的研究结果。洛美沙星对革兰氏阴性菌具强大的抗菌作用,其MIC_(90)大都≤2mg/L,对大肠杆菌、流感杆菌和淋球菌的抗菌作用尤强,对肺炎球菌和其他链球菌的抗菌作用较弱。对大部分耐庆大霉素和哌拉西林的革兰氏阳性杆菌仍具良好抗菌活性。洛美沙星的抗菌作用略逊于环丙沙星,与氧氟沙星相似,稍优于诺氟沙星。洛美沙星对小鼠实验性细菌感染,尤其是革兰氏阳性杆菌感染具有明显保护作用,其口服用药后的体内抗菌作用明显优于诺氟沙星。     

喹诺酮类药物对厌氧菌的体外抗菌活性研究

用６种喹诺酮类药物（氟罗沙星、诺氟沙星、依诺沙星、环丙沙星、洛美沙星、氧氟沙星）对９３株不同厌氧菌作体外抗菌活性研究，并与常用的抗厌氧菌药物克林霉素、甲硝唑比较，结果显示环丙沙星对厌氧菌的抗菌活性最强，与甲硝唑类似，优于克林霉素；其次为氧氟沙星和氟罗沙星；洛美沙星、依诺沙星、诺氟沙星效果较差。其中，革兰氏阳性厌氧菌对环丙沙星最敏感，其次为氟罗沙星和氧氟沙星；革兰氏阴性厌氧菌对环丙沙星最敏感，其次为     

司帕沙星对小鼠肾脏感染的有效性

司帕沙星(Sparfloxacin)是一种喹诺酮类新药,对革兰氏阳性菌,如葡萄球菌、链球菌和肠球菌具有广谱,强效的抗菌活性。特别是对革兰氏阴性菌,如肠道细菌、假单孢菌属和流感嗜血菌,以及各种枝原体、军团菌、衣原体和分枝杆菌均显示强大的抗菌作用。司帕沙星对革兰氏阳性菌的抗菌活性超过环丙沙星或氟罗沙星,并且它对肠道细苗族和非发酵菌的抗菌活性与环丙沙星和氟罗沙星一样有效。小白鼠肾脏溃疡模型实验证实了司帕沙星的有效性,并与氟罗沙星作了对比。     

头孢匹胺的体外抗菌作用

用琼脂稀释法测定头孢匹胺对５１８株临床分离菌的体外抗菌作用，并与其它９种抗菌药物作比较。结果显示头孢匹胺对肠杆菌科细菌具高度抗菌活性。对假单胞菌属、黄单胞菌的抗菌作用与头孢哌酮、头孢他啶、哌拉西林和阿米卡星相仿，明显优于其它受试药物。对甲氧西林耐药葡萄球菌以外的革兰氏阳性球菌也具良好抗菌作用，其中对肠球菌的抗菌作用明显优于其它头孢菌素，与哌拉西林、青霉素接近。结果表明头孢匹胺抗菌谱广，尤对需氧革兰氏阴性杆菌具高度抗菌活性。     

新型高效广谱抗菌药物——安妥沙星

安妥沙星具有广谱的抗菌作用,对革兰阴性菌包括流感嗜血杆菌、克雷伯菌、变形杆菌、不动杆菌、沙门菌属等具有良好的抗菌活性,抗菌作用优于环丙沙星、氧氟沙星、司巴沙星和洛美沙星;对革兰阳性球菌包括溶血性链球菌等也具有较好的抗菌作用,特别是对甲氧西林耐药的葡萄球菌,其抗菌活性较环丙沙星、氧氟沙星、司巴沙星和洛美沙星强8～16倍;对厌氧菌以及分枝杆菌也有一定的抗菌活性。动物体内保护试验结果证明安妥沙星的作用与左氧氟沙星、氧氟沙星和环丙沙星相当或略强。临床研究结果表明,安妥沙星在正常受试者中耐受性良好,在首次0．4g,以后每次0．2g,一日1次给药剂量下,治疗轻、中度急性细菌性感染包括呼吸系统感染、泌尿系统感染、皮肤软组织感染具有良好的安全性和有效性。     

氟喹诺酮类药物的不良反应

氟喹诺酮类药物是第三代喹诺酮类药物。目前用于临床的品种已达10余种，较为常见的有诺氟沙星、氧氟沙星、环丙沙星、依诺沙星等。此类药物为杀菌型抗生素，具有作用强、抗菌谱广、口服方便等特点，对革兰氏阳性杆菌，包括绿脓杆菌均有良好抗菌作用，对革兰氏阳性球菌也具有一定抗菌活性，尤其对耐药革兰氏阴性杆菌，仍可呈现敏感。同时，有较高的组织、血液分布浓度，用于多系统的感染，临     

司帕沙星与其他5种抗菌药体外抗菌活性比较研究

测定了司帕沙星对临床分离的１９９ 株致病菌的体外抗菌活性并与氧氟沙星、环丙沙星、头孢唑啉、头孢噻肟、阿米卡星的抗菌活性进行比较。司帕沙星对革兰阳性菌的ＭＩＣ９０为０．１２５～０．５ｍ ｇ／Ｌ,对金葡球菌、化脓链球菌的抑菌率均为１００％ ,强于氧氟沙星、环丙沙星;对革兰阴性菌也具有良好的体外抗菌活性,与氧氟沙星、环丙沙星相似。不同细菌接种量和不同浓度血清对其抗菌活性无明显影响,仅在ｐＨ５．０ 时抗菌活性略有下降     

5种抗菌药物对厌氧菌的体外抗菌活性研究

测定了罗红霉素、ａｚｉｔｈｒｏｍｙｃｉｎ、头孢西丁、托舒沙星对６０株厌氧菌的体外抗菌活性，并同甲硝唑比较，发现托舒沙星对厌氧菌的体外抗菌活性最好，ＭＩＣ_（５０）和ＭＩＣ_（９０）为０．１２５和２ｍｇ／Ｌ优于甲硝唑（０．２５和１６ｍｇ／Ｌ）；罗红霉素（０．５、１６ｍｇ／Ｌ）与甲硝唑相似，ａｚｉｔｈｒｏｍｙｃｉｎ、头孢西丁的体外抗菌活性比甲硝唑略差，ＭＩＣ_（５０）和ＭＩＣ_（９０）分别为４和３２、２和３２ｍｇ／Ｌ，它们对脆弱拟杆菌的体外抗菌活性优于对其它拟杆菌的体外抗菌活性，对短真杆菌、变形链球菌、普氏消化链球菌等也具有较好的体外抗菌活性。     

国产氧氟沙星的药理评价

本文报道了氧氟沙星的体外抗菌活性,小鼠感染细菌保护作用,急性毒性和致畸试验。氧氟沙星对革兰氏阳性和阴性细菌抗菌活性与诺氟沙星相似,而强于依诺沙星、洛美沙星和吡哌酸。小鼠分别感染金葡球菌和大肠杆菌,本品保护效果与环丙沙星相似,优于诺氟沙星和依诺沙星;小鼠感染绿脓杆菌,本品逊于环丙沙星和依诺沙星,而优于诺氟沙星。小鼠口服、静脉、肌肉和皮下给药LD50分别为3467mg/kg、329mg/kg、>600mg/kg和>3000mg/kg。小鼠胚胎器官分化期给药未见致畸胎作用。     

Antibacterial activity of tosufloxacin against major organisms detected from patients with respiratory infections

We determined the susceptibility of bacteria which were isolated from the patients with respiratory infections between January and October 2005, to tosufloxacin and other fluoroquinolones. A total of 900 isolate including 300 Streptococcus pneumoniae, 100 Streptococcus pyogenes, 100 Moraxella catarrhalis, 200 Haemophilus influenzae, 100 Klebsiella pneumoniae and 100 Pseudomonas aeruginosa were tested. Tosufloxacin, gatifloxacin, levofloxacin, moxifloxacin, ciprofloxacin and prulifloxacin were used as the test antimicrobials. Tosufloxacin, gatifloxacin and moxifloxacin were potent antibiotics tested for the antibacterial activity against Streptococcus including penicillin-resistant S. pneumoniae; the MIC90 were 0.12-0.5/ micromL. Fluoroquinolones exerted the potent antibacterial activity against M. catarrhalis and H. influenzae; the MIC90 of fluoroquinolones tested were < or =0.06 microg/mL. Tosufloxacin, ciprofloxacin and prulifloxacin showed to be more active against K. pneumoniae and P. aeruginosa, but parts of some strains were resistant. These results indicate that tosufloxacin has the potent antibacterial activity against major organisms detected from patients with respiratory infections. Since it was approved in 1990, tosufloxacin was considered to be useful as a therapeutic antimicrobial for the treatment of respiratory infections.     

6种氟喹诺酮类药物对临床分离金葡萄的抗菌活性比较

目的：观察临床分离金葡萄对6种氟喹诺酮类药物的耐药情况。方法：用琼脂稀释法测定诺氟沙星（NFLX）、氧氟沙星（OFLX）、氟罗沙星（FLRX）、环丙沙星（CPFX）、司帕沙星（SPFX）、托舒沙星（TFLX）6种2、3代氟喹诺桐类药物对成都地区155株临床分离金葡菌的体外抗菌活性。结果：金葡菌对6种药物的耐药率分别为诺氟沙星35.5%。氟罗沙星34.19%,环丙沙星27.75%,托舒沙星27.75% ,氧氟沙星25.81%,司帕沙星25.81%。结论：氟喹诺酮类药物的广泛应用已使细菌的耐药性明显增高,各药MIC90均超过16mg.L^-1,比以往文献报道的本地区金葡萄耐药性明显升高,提示要合理应用氟喹诺酮类药物,减少耐药菌株的增加。     

In vitro method for prediction of the phototoxic potentials of fluoroquinolones

The phototoxic potential of eight fluoroquinolones (norfloxacin, ofloxacin, enoxacin, ciprofloxacin, lomefloxacin, tosufloxacin, sparfloxacin and gatifloxacin) was evaluated by using three in vitro methods of cytotoxicity against mammalian cells, erythrocyte lysis and DNA strand breakage. All fluoroquinolones tested with the exception of gatifloxacin, an 8-methoxy quinolone, showed DNA strand breaking activities under UV-A irradiation. Their cytotoxicity against HeLa cells was also enhanced by UV-A irradiation. In particular, the phototoxic potential of sparfloxacin, enoxacin and lomefloxacin was high in both methods. Ofloxacin is very photocytotoxic against HeLa cells, while it has low potential to cause DNA strand breakage. Norfloxacin, ciprofloxacin and enoxacin were very photohemolytic, but sparfloxacin was not, indicating that the in vivo phototoxic potencies of fluoroquinolones might not be predictable by the photohemolysis study. Gatifloxacin, a non-phototoxic quinolone, showed no phototoxic potential in any of these three in vitro tests. These results suggest that determination of DNA strand breaking activity, combined with cytotoxicity against mammalian cells, is available to predict the phototoxic potential of fluoroquinolones without laboratory animals.     

Rufloxacin (MF-934): in vitro and in vivo antibacterial activity

Rufloxacin (MF-934) is a new quinolone which shows in vitro antibacterial activity against E. coli, Salmonella, Klebsiella, Proteus and Staphylococcus spp. Lower in vitro activity was observed with Pseudomonas, Serratia, Enterobacter and the streptococci group D. The antimicrobial activity of MF-934 in vitro is higher than that of nalidixic acid but lower than that of ciprofloxacin, ofloxacin, pefloxacin or norfloxacin. The protective effects of MF-934 in systemic infections in mice are lower than those of ciprofloxacin and ofloxacin. In respiratory infections in rats and in subcutaneous infections in guinea-pigs, the protective effects of MF-934 are of the same order as ciprofloxacin and ofloxacin. This is probably due to the pharmacokinetic properties of MF-934, i.e. the long half-life and tissue concentrations higher than plasma levels.     

甲磺酸加替沙星与其他4种氟喹诺酮类药物对临床分离菌的体外抗菌活性比较

目的 :比较甲磺酸加替沙星与氧氟沙星、左氧沙星、环丙沙星、司帕沙星对 182株临床分离菌的体外抗菌活性。方法 :采用琼脂平板二倍稀释法测定加替沙星等 5种氟喹诺酮类药物对 182株临床试验分离菌株的最低抑菌浓度 (MIC)。结果 :加替沙星对葡萄球菌属的MIC90 比其他 4种氟喹诺酮类药物低。葡萄球菌属对加替沙星的敏感率显著高于其他4种氟喹诺酮类药物 ;对其他G 球菌的MICR 也较其他氟喹诺酮类药物低。G-杆菌中埃希菌属、肠杆菌属对加替沙星的敏感率明显高于其他 4种氟喹诺酮类药物 ,加替沙星对埃希菌属、肠杆菌属的MIC90比左氧沙星低 2倍 ,比其他 3种抗菌药物低 8倍 ;假单胞菌属、克雷伯菌属和其他G-杆菌对加替沙星的敏感率与左氧沙星的差异无统计学意义 ,与其他 3种氟喹诺酮类药物的差异有统计学意义。结论 :甲磺酸加替沙星具有广谱而强大的体外抗菌活性。     

Influence of pH and human urine on the antibacterial activity of ciprofloxacin, norfloxacin and ofloxacin

The influence of pH on the antibacterial activity of ciprofloxacin, norfloxacin and ofloxacin was studied in broth and pooled human urine by microdilution susceptibility tests. Selected strains of E. coli, Staphylococcus aureus and Pseudomonas aeruginosa were used as test organisms. The results show that cultivation at pH 5.7 in urine increased the MIC values for all three quinolones 8, 16 and 32-fold compared with broth at pH 7.1. Killing curves show that in urine with 10 mcg/ml ciprofloxacin, rapid killing of E. coli and Pseudomonas aeruginosa occurred, whereas ofloxacin and especially norfloxacin were less effective.