注射用多尼培南体内抗菌活性研究

目的:评价注射用多尼培南的体内抗菌活性.方法:建立小鼠腹腔感染模型,以注射用美罗培南为对照药,观察注射用多尼培南的体内抗菌活性.结果:注射用多尼培南对大肠埃希菌DC01、DC02和甲氧西林敏感的金黄色葡萄球菌JP02有良好的体内抗菌活性,其ED50分别为4.5、1.0和2.0 mg/kg,美罗培南为15.9、10.6和17.3 mg/kg.阴性对照对感染小鼠无保护作用.结论:注射用多尼培南对大肠埃希菌和甲氧西林敏感的金黄色葡萄球菌所致的小鼠腹腔感染具有良好的治疗作用,其体内抗菌活性优于同类对照药.     

国产美洛培南的体外抗菌活性

采用琼脂二倍稀释法测定国产美洛增南和其它５种药物对１３６株临床分离菌的体外抗菌活性,结果表明国产美洛增南与进口美洛增南的体外抗菌活性相近,优于头孢哌酮／舒巴坦、他唑西林和头孢他啶。国产美洛增南对金葡萄菌、铜绿假单孢菌、大肠埃希氏菌和肺炎克雷伯氏菌的抗菌活性优于亚胺培南／西司他丁,对表葡球菌和β－溶血性链球菌的抗菌活性比后者稍差。国产美洛培南的抗菌活性稍受接种菌量、培养基ｐＨ和血清浓度影响。     

三种碳青霉烯类抗生素的体外抗菌作用

为评价亚胺培南、帕尼培南与美罗培南的体外抗菌作用 ,以琼脂对倍稀释法测定三者对 2 2 5株临床分离菌的最低抑菌浓度 (MIC) ,并与相关抗菌药物进行比较。结果 ,三种碳青霉烯类抗生素对肠杆菌科细菌具高度抗菌活性 ,对铜绿假单胞菌、不动杆菌属、粪肠球菌等亦具良好抗菌作用。帕尼培南与亚胺培南体外抗菌作用相仿 ,两者对肺炎克雷伯氏菌、肠杆菌属等革兰氏阴性菌作用略逊于美罗培南。三种碳青霉烯类抗生素体外抗菌作用优于头孢他啶、β-内酰胺类抗生素与β-内酰胺酶抑制剂合剂、氟喹诺酮类等其它受试药物。结果表明 ,碳青霉烯类抗生素是治疗多重耐药菌所致院内感染、免疫缺陷者感染和严重需氧菌与厌氧菌混合感染的适用药物。     

注射用法罗培南的体内抗菌活性

目的评价注射用法罗培南的体内抗菌活性。方法建立小鼠腹膜炎模型,比较注射用法罗培南及厄他培南对产酶的大肠埃希菌、肺炎克雷伯菌及对甲氧西林敏感的金黄色葡萄球菌、耐万古霉素的粪肠球菌感染小鼠的体内抗菌活性。结果注射用法罗培南对产超广谱β内酰胺酶(ESBLs)的大肠埃希菌、肺炎克雷伯菌和对甲氧西林敏感的金黄色葡萄球菌有较强的体内和体外抗菌活性,其ED_(50)分别为10.96、9.12和7.07 mg·kg~(-1),厄他培南则为14.84、12.58和10.16 mg·kg~(-1)。法罗培南对耐万古霉素的粪肠球菌体外敏感,而厄他培南显示耐药。法罗培南对耐万古霉素的粪肠球菌的ED_(50)比厄他培南低66.77%,分别为10.75和32.35 mg·kg~(-1)。结论注射用法罗培南和厄他培南对产ESBLs的大肠埃希菌、肺炎克雷伯菌和对甲氧西林敏感的金黄色葡萄球菌有较强的体内和体外抗菌活性,两者作用相似。法罗培南对耐万古霉素的粪肠球菌感染可能有治疗作用,效果优于厄他培南。     

多尼培南药理作用与临床应用

多尼培南（doripenem）为新型碳青霉烯类抗菌药物,作用机制与其他β-内酰胺类抗菌药物相同,抗菌谱广,抗菌活性强,对多种革兰阳性（G⁺）菌（包括对甲氧西林敏感和耐药的金黄色葡萄球菌、表皮葡萄球菌等）和革兰阴性（G^－）菌（包括大肠埃希菌、肺炎克雷白杆菌、奥克西托克雷白杆菌、奇异变形杆菌等）均有很强的抗菌活性,对G^＋菌的抗菌活性强于美罗培南和比阿培南,对G^－菌的抗菌活性强于亚胺培南和比阿培南,其中对铜绿假单胞菌有着很强的抗菌活性. 多项临床试验 结果 表明,多尼培南对复杂性尿道感染的疗效与左氧氟沙星相当,对复杂性腹腔内感染的疗效与美罗培南相当. 该文对其作用机制、抗菌活性、药动学、临床研究及药物不良反应等进行综述.     

亚胺培南／西司他丁的抗生素后效应及其影响因素的研究

研究亚胺培南／西司他丁的体外抗生素后效应（ＰＡＥ）及其影响因素。结果发现亚胺培南／西司他丁对常见感染致病菌金葡球菌、大肠埃希氏菌、铜绿假单胞菌、肺炎克雷伯氏菌能产生０．６～３．２ｈ的ＰＡＥ，以金葡球菌标准株最长；随着药物浓度增加及接触时间延长，ＰＡＥ延长，但有极限值，于１０ＭＩＣ～２０ＭＩＣ，接触２ｈ达最大值；亚胺培南／西司他丁与阿米卡星联用后ＰＡＥ呈半相加作用     

美洛培南对临床分离菌耐药性测定

目的 :探讨美洛培南对临床分离菌的耐药性。方法 :选取150株临床分离菌应用K -B法测定美洛培南等抗生素的耐药性 ,同时比较了美洛培南及亚胺培南对大肠埃希氏菌的耐药谱。结果 :美洛培南对临床分离菌敏感率为100 % ,美洛培南与亚胺培南对大肠埃希氏菌无交叉耐药。结论 :美洛培南对临床分离菌有高度敏感性 ,其抗菌谱与亚胺培南相似     

帕尼培南-倍他米隆体外抗菌活性及其对肺部感染病人的疗效观察

目的 :了解帕尼培南 倍他米隆对临床常见致病菌的体外抗菌活性及治疗肺部感染的有效性及安全性。方法 :采用琼脂二倍稀释法测定帕尼培南 倍他米隆对 2 4 7株临床分离菌的MIC ,检测其对部分菌株的最低杀菌浓度 ;2 0例肺部感染病人使用帕尼培南 倍他米隆 5 0 0 /5 0 0mg ,q 12h ,iv ,gtt ,疗程3～ 7d。结果 :帕尼培南 倍他米隆与帕尼培南的体外抗菌活性基本一致 ,MIC50 ≤ 0 .0 0 75mg·L- 1,MIC90 为 0 .0 0 75～ 2mg·L- 1;对流感嗜血杆菌的MIC范围为 <0 .0 0 75～ 0 .12 5mg·L- 1;对阴沟肠杆菌、变形肠杆菌、铜绿假单孢菌的MIC50 和MIC90 分别为 0 .12 5和 0 .5 ,2和 4 ,4和 16mg·L- 1;帕尼培南 倍他米隆对金黄色葡萄球菌、表皮葡萄球菌、铜绿假单孢菌、肺炎克雷伯菌、大肠埃希菌、阴沟肠杆菌、变形肠杆菌及微球菌的最低杀菌浓度分别是其MIC的 1～ 8倍。致病菌阴转率为 77.8% ,治疗有效率为 75 % ,未出现明显不良反应。结论 :帕尼培南 倍他米隆对临床常见致病菌的体外抗菌活性强 ;对肺部感染有较好疗效 ,安全性好     

三种碳青霉烯类抗生素对ICU分离菌株的体外抗菌作用

为评价亚胺培南、帕尼培南与美罗培南的体外抗菌作用,用琼脂双倍稀释法测定从我院重症监护病房分离的230株革兰氏阴性菌的最低抑菌浓度（MIC）,并采用抑制剂增强的纸片扩散法测定大肠埃希氏菌和肺炎克雷伯氏菌超广谱β－内酰胺酶（ESBLs)。结果,50株肺炎克雷伯氏菌和17株大肠埃希氏菌中的ESBLs阳性率为61．2％。三种碳青霉烯类对阴沟肠杆菌、肺炎克雷伯氏菌、大肠埃希氏菌、不动杆菌等都具有高度的抗菌活性,且对产ESBLs菌株保持高度的抗菌活性。对嗜麦芽黄单胞菌高度耐药。提示碳青霉烯类抗生素是重症监护病人多重耐药菌感染的良好选择。     

多利培南对细菌感染小鼠败血症体内抗菌作用

目的评价多利培南对细菌感染小鼠的体内抗菌作用。方法以最小致死量(MLD)0.5 mL感染小鼠,建立小鼠败血症实验模型。对4株临床分离致病菌进行了体内保护试验。尾静脉注射不同浓度药物0.2 mL,记录给药后1～7 d内小鼠成活率,用BLISS法计算ED50、ED95。结果多利培南对大肠埃希菌、铜绿假单胞菌和金黄色葡萄球菌均有很好的体内抗菌保护作用,ED50值在0.06～2.75 mg·kg-1,均明显优于对照药美罗培南(P<0.01)。青霉素不敏感肺炎链球菌ED50值为76.33 mg·kg-1,亦低于美罗培南。结论多利培南对4种临床分离致病菌具有强效的体内抗菌作用,明显优于美罗培南。     

Newer carbapenems for urinary tract infections

Four carbapenems have been available clinically in Japan. These are imipenem/cilastatin (IMIP/CS) and panipenem/ betamipron (PANI/BP) of the older compounds and newer carbapenems such as biapem (BIAP) and meropenem (MERO). The latter compounds are relatively stable to dehydropeptidase-1 (DHP-1) and have been reported to have higher antimicrobial activities compared to the earlier carbapenems. The antimicrobial activity of these four carbapenems against fresh urinary isolates showed high activities against Enterobacteriacae such as Serratia marcescens, Enterobacter cloacae, Citrobacter freundii and Escherichia coli containing the class C-beta-lactamase- and extended spectrum beta-lactamase (ESBL)-producing strains compared to piperacillin (PIPC) and ceftazidime (CTAZ). Against Pseudomonas aeruginosa, the carbapenems, with the exception of panipenem showed strong antimicrobial activities compared to PIPC and CTAZ. High activities were also seen against Enterococcus faecalis, Staphylococcus aureus and Staphylococcus epidermidis, but methicillin-resistant strains were not affected. The first generation carbapenems showed better activity against E. faecalis than newer carbapenems. All four carbapenems were similar in clinical effectiveness in double blind trials for complicated urinary tract infections (UTIs). However, PANI/BP is less effective in UTIs caused by P. aeruginosa than IMIP/CS. MERO showed better eradication rate of P. aeruginosa than IMIP/CS. Retrospective analysis of treated cases using carbapenems showed a rapid defervescence in the treatment of febrile complicated UTIs, which were mainly caused by mixed infection of Gram-negative and Gram-positive bacteria, especially those involving P. aeruginosa and E. faecalis.     

In vitro and in vivo antibacterial activities of pazufloxacin mesilate,a new injectable quinolone

We investigated the in vitro and in vivo antibacterial activities of pazufloxacin mesilate (PZFX mesilate), a new injectable quinolone, and obtained the following results. 1) The MIC50 and MIC90 values of PZFX against clinically isolated Gram-positive and -negative bacteria, ranged from 0.0125 to 12.5 micrograms/ml and 0.025 to 100 micrograms/ml, respectively. PZFX showed broad spectrum activity. The antibacterial activities of PZFX against quinolone-susceptible, methicillin-resistant Staphylococcus aureus, beta-lactamase-negative, ampicillin-resistant Haemophilus influenzae, extended spectrum beta-lactamase possessing Klebsiella pneumoniae and imipenem/cilastatine (IPM/CS)-resistant Pseudomonas aeruginosa were superior to those of ceftazidime (CAZ), ceftriaxone, IPM/CS, meropenem and panipenem/betamipron. 2) PZFX showed superior bactericidal activity against S. aureus, Escherichia coli, Proteus mirabilis, Serratia marcescens and P. aeruginosa to those of CAZ and IPM/CS after treatment for 15 minutes at the drug concentration equivalent to that in human serum at clinical dose to be continued for 15 minutes. 3) CAZ and IPM/CS had no bactericidal activity at the 16 times of MIC against P. aeruginosa in human polymorphonuclear leucocytes, while PZFX exhibited potent bactericidal activity in a dose-dependent manner against such bacteria. 4) PZFX inhibited both DNA gyrase and topoisomerase IV from S. aureus at nearly the same level. PZFX showed poor inhibitory activity against topoisomerase II from human placenta and showed high selectivity to bacterial topoisomerase. 5) PZFX mesilate showed superior therapeutic activity to that of CAZ with following infection model caused by S. aureus and P. aeruginosa or each; systemic infection with cyclophosphamide-treated mice, systemic infection in mice with high challenge doses, CMC pouch infection in rat, and calculus infection in rat bladder. 6) Intravenous administration of PZFX with high plasma concentration just after administration, showed more excellent therapeutic effect against the rat intraperitoneal infection, than p.o. and s.c. administration.     

Antibacterial activity of panipenem against clinical isolates in 2000 and 2001

As the post-marketing surveillance of panipenem/betamipron (Carbenin), MICs of panipenem (PAPM) against 1355 clinical isolates of 28 species from 15 medical institutions all over Japan from June 2000 to March 2001 were measured using the broth microdilution method approved by the Japanese Society of Chemotherapy and compared with those of parenteral carbapenem antibacterials, imipenem (IPM) and meropenem (MEPM), and parenteral cephem antibacterials, cefozopran, cefepime, and sulbactam/cefoperazone. The activity of PAPM was comparable to that of IPM against almost all species tested. Compared with MEPM, PAPM was more active against Gram-positive bacteria and Bacteroides spp., and less active against Gram-negative bacteria. Compared with the parenteral cephems, PAPM was more active against most of species tested and its MIC ranges were narrower than those of the cephems as were those of other carbapenems. In this surveillance study, the incidence of resistance in various species were as follows: 39.3% for methicillin-resistant Staphylococcus aureus, 47.3% for penicillin-intermediate Streptococcus pneumoniae (PISP), 15.1% for penicillin-resistant S. pneumoniae (PRSP), 0.9% for extended-spectrum beta-lactamase (ESBL) producing Escherichia coli, 3.4% for ESBL producing Klebsiella pneumoniae, 19.2% for beta-lactamase producing Haemophilus influenzae, 24.0% for beta-lactamase-negative ampicillin-resistant (BLNAR) H. influenzae, and 1.0% for metallo-beta-lactamase producing Pseudomonas aeruginosa. Against these resistant strains, carbapenems including PAPM showed generally more potent activity than cephems. It was noted that PAPM showed the most potent activity against PISP and PRSP, which showed high incidence of 62.4% totally, among tested drugs. Metallo-beta-lactamase producing P. aeruginosa exhibited high resistance and BLNAR H. influenzae also exhibited low susceptibility against all tested drugs. But no remarkable change in the activity of PAPM against other species was observed in this study compared with that in the studies before the marketing of Carbenin. Furthermore, it is necessary to pay much attention to the trend of resistant strains such as PRSP, metallo-beta-lactamase producing bacteria, and BLNAR H. influenzae.     

鲍氏不动杆菌121株临床分布和耐药分析

目的了解鲍氏不动杆菌感染的临床分布及其耐药特点。方法收集2006年1月至2007年12月从临床感染标本分离的121株鲍氏不动杆菌,了解其临床分布并做药物敏感试验,比较其耐药率。结果121株鲍氏不动杆菌临床分布以呼吸科和ICU最多（63株,占52．07％）,且多见于老年患者（67株,占55．37％）;对第三代头孢菌素及环丙沙星的耐药率均〉50．0％;对帕尼培南／倍他米隆、亚胺培南／西司他丁、头孢哌酮／舒巴坦的耐药性较低,分别为3．31％、6．61％、9．92％。结论碳青霉烯类及头孢哌酮／舒巴坦对鲍氏不动杆菌感染仍有较强的活性;要减少多重耐药菌株的产生,应注意合理使用抗菌药物。     

鲍氏不动杆菌121株临床分布和耐药分析

目的 了解鲍氏不动杆菌感染的临床分布及其耐药特点.方法 收集2006年1月至2007年12月从临床感染标本分离的121株鲍氏不动杆菌,了解其临床分布并做药物敏感试验,比较其耐药率.结果 121株鲍氏不动杆菌临床分布以呼吸科和ICU最多(63株,占52.07%),且多见于老年患者(67株,占55.37%);对第三代头孢菌素及环丙沙星的耐药率均>50.0%;对帕尼培南/倍他米隆、亚胺培南/西司他丁、头孢哌酮/舒巴坦的耐药性较低,分别为3.31%、6.61%、9.92%.结论 碳青霉烯类及头孢哌酮/舒巴坦对鲍氏不动杆菌感染仍有较强的活性;要减少多重耐药菌株的产生,应注意合理使用抗菌药物.     

鲍氏不动杆菌121株临床分布和耐药分析

目的 了解鲍氏不动杆菌感染的临床分布及其耐药特点.方法 收集2006年1月至2007年12月从临床感染标本分离的121株鲍氏不动杆菌,了解其临床分布并做药物敏感试验,比较其耐药率.结果 121株鲍氏不动杆菌临床分布以呼吸科和ICU最多(63株,占52.07%),且多见于老年患者(67株,占55.37%);对第三代头孢菌素及环丙沙星的耐药率均>50.0%;对帕尼培南/倍他米隆、亚胺培南/西司他丁、头孢哌酮/舒巴坦的耐药性较低,分别为3.31%、6.61%、9.92%.结论 碳青霉烯类及头孢哌酮/舒巴坦对鲍氏不动杆菌感染仍有较强的活性;要减少多重耐药菌株的产生,应注意合理使用抗菌药物.     

鲍氏不动杆菌121株临床分布和耐药分析

目的 了解鲍氏不动杆菌感染的临床分布及其耐药特点.方法 收集2006年1月至2007年12月从临床感染标本分离的121株鲍氏不动杆菌,了解其临床分布并做药物敏感试验,比较其耐药率.结果 121株鲍氏不动杆菌临床分布以呼吸科和ICU最多(63株,占52.07%),且多见于老年患者(67株,占55.37%);对第三代头孢菌素及环丙沙星的耐药率均>50.0%;对帕尼培南/倍他米隆、亚胺培南/西司他丁、头孢哌酮/舒巴坦的耐药性较低,分别为3.31%、6.61%、9.92%.结论 碳青霉烯类及头孢哌酮/舒巴坦对鲍氏不动杆菌感染仍有较强的活性;要减少多重耐药菌株的产生,应注意合理使用抗菌药物.     

Antibacterial activity of biapenem against recent clinical isolates

Antibacterial activity of biapenem (BIPM) against clinical isolates of 8 species between 2000 and 2002 was compared with those of imipenem/cilastatin (IPM/CS), meropenem (MEPM), panipenem/betamipron (PAPM/BP) and ceftazidime (CAZ). The MICs of biapenem for Gram-positive bacteria were higher than those of IPM/CS and PAPM/BP, equal to those of MEPM and lower than those of CAZ. The MICs of BIPM for Gram-negative bacteria were higher than those of MEPM, equal to those of IPM/CS and PAPM/BP, and lower than those of CAZ. Antibacterial activity of BIPM against Pseudomonas aeruginosa was equal to those of IPM/CS and MEPM and superior to those of PAPM/BP and CAZ. In conclusion, BIPM showed broad antibacterial activity against both Gram-positive and Gram-negative clinical isolates. These results suggest that BIPM is useful for the treatment of various bacterial infections.     

鲍氏不动杆菌121株临床分布和耐药分析

目的 了解鲍氏不动杆菌感染的临床分布及其耐药特点.方法 收集2006年1月至2007年12月从临床感染标本分离的121株鲍氏不动杆菌,了解其临床分布并做药物敏感试验,比较其耐药率.结果 121株鲍氏不动杆菌临床分布以呼吸科和ICU最多(63株,占52.07%),且多见于老年患者(67株,占55.37%);对第三代头孢菌素及环丙沙星的耐药率均>50.0%;对帕尼培南/倍他米隆、亚胺培南/西司他丁、头孢哌酮/舒巴坦的耐药性较低,分别为3.31%、6.61%、9.92%.结论 碳青霉烯类及头孢哌酮/舒巴坦对鲍氏不动杆菌感染仍有较强的活性;要减少多重耐药菌株的产生,应注意合理使用抗菌药物.