碳青霉烯类抗生素法罗培南对肠道出血性大肠埃希氏菌的抗菌作用

法罗培南是日本开发的世界上第一个非酯型口服碳青霉烯类抗生素，其结构与目前临床上广泛应用的青霉素类及头孢菌素类抗生素不同，主要构架有非天然型的青霉烯环。法罗培南抗菌谱广，对包括粪肠球菌在内的革兰氏阳性需氧菌，非葡萄糖发酵菌外的革兰氏阴性需氧菌及拟杆菌等厌氧菌都有抗菌活性。法罗培南对各种β－内酚胺酶非常稳定，作用机制与以往的β－内酞胺酶类抗生素一样，主要与细菌细胞壁合成酶青霉素结合蛋白（ＰＢＰ）呈非可逆性结合，在短时间内即有强杀菌作用。１９９７年６月已有法罗培南成人片剂上市，儿童用片剂正在研制中。肠…     

新型青霉烯类抗生素法罗培南钠

法罗培南钠(faropenem sodium)是青霉烯类中惟一既可口服又可注射的抗生素,它经由阻止细菌细胞壁合成而显现抗菌、杀菌作用,具有独特的药动学性质。其抗菌谱广泛,包括需氧G 菌、需氧G-菌及厌氧菌。在呼吸道、泌尿道、妇产科、口腔科以及眼科感染上已取得了良好的效果。现对法罗培南钠的作用机制、抗菌活性、毒理学、药动学及临床研究进展进行综述。     

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。     

新的口服抗生素法罗培南钠盐对耳鼻咽喉科感染症的临床效果

法罗培南钠盐是一种新的碳青霉烯类口服抗生素,抗菌谱广,抗菌力强,除铜绿假单胞菌外,对需氧及厌氧的革兰氏阴性菌均有效.上述细菌常是耳鼻咽喉科常见的致病菌.植山茂宏等使用本剂治疗耳鼻咽喉科感染症,对其有效性和安全性进行了研究.     

注射用法罗培南钠对金葡菌的体内外抗菌活性研究

目的研究注射用法罗培南钠对临床分离的金葡菌的体内外抗菌活性。方法用头孢西丁纸片法在近年来本室保存的临床分离金葡菌中筛选耐甲氧西林的金葡菌（methicillin resistant staphylococcus aureus，MRSA），用琼脂平板稀释法测定法罗培南和万古霉素对甲氧西林敏感的金葡菌（methicillin sensitive staphylococcus aureus，MSSA）和MRSA菌株的最低抑菌浓度（minimal inhibitory concentration．MIC）。根据MIC选择对法罗培南敏感、中度和高度耐药的MRSA菌株及1株MSSA建立小鼠腹膜炎模型，以注射用法罗培南钠及万古霉素通过静脉注射进行感染动物的治疗，评价对感染小鼠的保护作用。结果151株金葡菌中共分离出65株MRSA．阳性率为43％；体外试验法罗培南和万古霉素对86株MSSA均敏感。65株MRSA对法罗培南敏感者10株，其余均耐药；对万古霉素均敏感。注射用法罗培南钠对4株菌的ED50分别为38．3、38．6、71．9和7．07mg／kg；万古霉素则为2．25、10．18、20．85和1．77mg／kg。结论注射用法罗培南钠对MSSA有良好的体内和体外抗菌活性；注射用法罗培南钠对MRSA无效．即使体外敏感。     

青霉烯类β-内酰胺抗生素的研究进展

青霉烯类衍生物是一类重要的非典型的 β 内酰胺类抗生素。其特点是具有广谱抗菌活性 ,包括对β 内酰胺酶产生菌 ,对脱氢肽水解酶 Ⅰ 稳定 ,是一类具有发展前景的新型抗生素。本文综述了三类临床研究较多的重要的青霉烯类抗生素法罗培南、利替培南酯和硫培南的抗菌活性。同时对青霉烯类衍生物C 2位取代基分别为硫取代、碳取代和氧取代化合物结构与活性的构效关系进行了研究。     

青霉烯类β—内酶胺抗生素的研究进展

青霉烯类衍生物是一类重要的非典型的β－内酶胺类抗生素。其特点是具有广谱抗菌活性,包括对β－内酶胺酶产生菌,对脱氢肽水解酶－I稳定,是一类具有发展前景的新型抗生素。本文综述了三类临床研究较多的青霉烯类抗生素法罗培南、利替培南酯和硫培南的抗菌活性。同时对青霉烯类衍生物C－2位取代基分别为硫取代、碳取代和氧取代化合物结构与活性的构效关系进行了研究。     

帕尼培南/倍他米隆的体外抗菌活性研究

为评价帕尼培南的体外抗菌作用，采用琼脂二倍稀释法测定帕尼培南／倍他米隆对247例临床分离菌的最低抑菌浓度（MIC），并与其它5种抗菌药物进行比较，结果表明，帕尼培与亚胺培南体外抗菌作用相仿，但帕尼培南对流感嗜血杆菌，金黄色葡萄球菌包括耐甲氧西林金葡萄球菌（MRSA）和大肠埃希氏菌体外胺培南对肺炎克雷伯氏菌、大肠埃希氏菌等革兰氏阴性菌作用略逊于美罗培南，帕尼培南体外抗菌 于头孢他啶，头孢哌酮／舒巴坦，苯唑西林等其它受试药物。帕尼培南的体外抗菌活性受接种菌量，培养基PH值和血清浓度影响。结果表明，帕尼培南是治疗多重耐药菌所致院内感染和严重需氧菌与厌氧菌混合感染的适用药物。     

国内城市医院碳青霉烯类抗生素用药情况

碳青霉烯类抗生素具有抗菌谱广、抗菌活性强的特点,在控制耐药菌、产酶菌感染和免疫缺陷者感染中起着重要作用,是销售增长较快的抗感染药物类别之一。自上世纪80年代中期亚胺培南进入临床应用后,碳青霉烯类抗生素现已发展到含有亚胺培南、美罗培南、帕尼培南、法罗培南、厄他培南、多尼培南和比阿培南这7个药物组成的培南类药物系列品种。目前全球碳青霉烯类抗生素市场超过16亿美元,而活跃在我国城市医院市场上的有5个品种。     

新型口服青霉烯类抗生素法罗培南的抗菌活性和对呼吸系感染的临床疗效

因法罗培南的母核具有理想的５环结构,２－位为双键结合,４－位为Ｓ,所以口服吸收好,对青霉素结合蛋白富有生物活性。小山优对口服青霉烯类抗生素法罗培南的抗菌力及其对呼吸系感染的有效性与其它内酰胺类口服抗生素进行了比较研究。法罗培南对肠球菌的抗菌活性与氨苄西林相当。对革兰氏阴性菌的活性与头孢类抗生素相近,对流感嗜血菌的活性比氨苄西林、舒氨西林强,较头孢特仑、头孢克肟等第Ⅲ代头孢菌素稍弱,对莫拉氏菌、粘膜炎布兰汉氏球菌的活性,介于第Ⅱ、Ⅲ代头孢菌素之间;对肺炎克雷伯氏菌的活性则在第Ⅰ、Ⅲ代头孢菌素之间。…     

法罗培南钠片治疗细菌性呼吸道感染疗效及体外抗菌活性研究

目的评价法罗培南钠片治疗细菌性呼吸道感染疗效及体外抗菌活性。方法轻、中度细菌性呼吸道感染患者50例,随机分为2组：A组（治疗组）25例用法罗培南钠片治疗,B组（对照组）25例用头孢克洛治疗,2组均每次口服1片,tid,疗程5-10 d,观察临床疗效;患者痰或咽拭子中分离,培养细菌,测定抗生素最低抑菌浓度（M IC）。结果A治疗组有效率为92%,B对照组有效率为84%,2组比较差异无显著性（P〉0.05）;法罗培南钠片对呼吸道常见细菌有良好抗菌活性;2组均无病例发生严重不良反应。结论法罗培南钠片是一种安全有效的治疗细菌性呼吸道感染的口服抗生素。     

岗梅感冒灵颗粒体外抗菌作用

目的探讨岗梅感冒灵颗粒的体外抗菌作用。方法以临床分离细菌为受试菌,采用琼脂稀释法,观察岗梅感冒灵颗粒的最低抑菌浓度。结果岗梅感冒灵颗粒对所有受试菌基本有不同程度的抑菌作用。结论岗梅感冒灵颗粒对上呼吸道感染常见致病菌有较好的抑菌作用。     

Compared studies of antimicrobial agents against E. coli, Klebsiella, Citrobacter and Proteus isolated from urinary tract infections

In vitro activities of antibacterial agents against E. coli, Klebsiella, Citrobacter and Proteus which were isolated from patients urinary tract infections at 8 hospitals in Japan, were investigated by agar dilution method from July to October in 1979. The summarized results are as follows. 1. Among oral antibacterial agents, MPC and PPA have showed potent antibacterial activities against E. coli and Klebsiella. Among parenteral antibiotics, CTM was the most active against E. coli and Klebsiella. However, ABPC-resistant E. coli and Klebsiella have appeared to occupy about 40% and 96% of bacteria isolated from urinary tract infections, respectively. 2. In vitro activities of antibacterial agents against Proteus and Citrobacter showed not so potent. 3. Causative organisms in female patients with simple urinary tract infections were mainly E. coli and Klebsiella. 4. Among oral antibacterial agents, PPA have shown similar antimicrobial activities against E. coli isolated from simple and complicated urinary tract infections. ABPC and MPC have been influenced in some degree by these factors. However, parenteral antibiotics are not influenced by these factors. On the other hand, in vitro activities of antibacterial agents against Klebsiella isolated from simple and complicated urinary tract infections were similar.     

Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use

Ciprofloxacin is one of a new generation of fluorinated quinolones structurally related to nalidixic acid. The primary mechanism of action of ciprofloxacin is inhibition of bacterial DNA gyrase. It is a broad spectrum antibacterial drug to which most Gram-negative bacteria are highly susceptible in vitro and many Gram-positive bacteria are susceptible or moderately susceptible. Unlike most broad spectrum antibacterial drugs, ciprofloxacin is effective after oral or intravenous administration. Ciprofloxacin has been most extensively studied following oral administration. It attains concentrations in most tissues and body fluids which are at least equivalent to the minimum inhibitory concentration designated as the breakpoint for bacterial susceptibility in vitro. The results of clinical trials with orally and intravenously administered ciprofloxacin have confirmed the potential for its use in a wide range of infections, which was suggested by its in vitro antibacterial and pharmacokinetic profiles. It has proven an effective treatment for many types of systemic infections as well as for both acute and chronic infections of the urinary tract. Ciprofloxacin generally appeared to be at least as effective as alternative orally administered antibacterial drugs in the indications in which they were compared, and in some indications, to parenterally administered antibacterial therapy. However, further studies are needed to fully clarify the comparative efficacy of ciprofloxacin and standard antibacterial therapies. Bacterial resistance to ciprofloxacin develops infrequently, both in vitro and clinically, except in the setting of pseudomonal respiratory tract infections in cystic fibrosis patients. The drug is also well tolerated. Thus, as an orally active, broad spectrum and potent antibacterial drug, ciprofloxacin offers a valuable alternative to broad spectrum parenterally administered antibacterial drugs for use in a wide range of clinical infections, including difficult infections due to multiresistant pathogens.     

New orally active penem antibiotic: Farom]

An orally active penem antibiotic, Farom (generic name: faropenem), was designed by the conformational analysis of active and inactive penem derivatives. Faropenem showed potent activity against a wide variety of bacteria including extended-spectrum beta-lactamase (ESBL)-producing ones. The mechanism of the stability against ESBL was elucidated by modeling the Michaelis complex of faropenem and Toho-1, an ESBL. Modeling of a complex of faropenem at the active site of a penicillin-binding protein 2 (PBP2) model suggested the characteristic affinity for faropenem with PBP2 of Escherichia coli. Faropenem has been totally synthesized from (R)-1,3-butanediol. The synthetic intermediate, a 3-hydroxyethyl-4-acetoxyazetidinone derivative, was efficiently prepared by the 2 + 2 coupling of a optically active vinylsulfide derivative and chlorosulfonyl isocyanate, followed by the substitution of the acetoxy group for the thiophenyl group at the C-4 position.     

A study on in vitro antibacterial activity and clinical usefulness in respiratory tract infections of panipenem/betamipron, a newly synthesized carbapenem antibiotic]

Panipenem/betamipron (PAPM/BP) is a combination drug of PAPM, a new parenteral carbapenem antibiotic and BP, an amino acid derivative at a weight ratio of 1:1. Its in vitro antibacterial activities against clinically isolated respiratory pathogenic bacteria were determined. It was superior to imipenem (IPM) in the in vitro antibacterial activities against Haemophilus influenzae, Haemophilus parainfluenzae, Branhamella catarrhalis, Staphylococcus aureus including MRSA, Klebsiella pneumoniae, Serratia marcescens and Escherichia coli. PAPM had antibacterial activities almost equal to those of IPM against Streptococcus pneumoniae and Enterococcus spp. Against Pseudomonas aeruginosa, however, its antibacterial activity was about 1/4 that of IPM. The clinical usefulness of PAPM/BP was studied by dissolving it in a solution containing lactate and administering the solution by intravenous drip infusion to 12 cases of respiratory tract infections. Out of 11 cases with respiratory tract infections excluding cytomegalovirus pneumonia, the efficacy rate was 90.9%, with 4 cases of excellent and 6 cases of good responses. In terms of its bacteriological efficacies, eradication of pathogenic bacteria including super-infection were observed in 2 out of 4 strains, but 2 strains of P. aeruginosa remained unchanged. Six strains appeared as superinfected bacteria during and after administration of this preparation substituting original pathogens. Side-effects were not observed in the 12 cases, and in laboratory tests, slight transient increases of S-GOT and S-GPT were found in 1 case. In conclusion, PAPM/BP is a very useful parenteral antibiotic against respiratory tract infections and can be one of the drugs of the first choice.     

2015年天津中医药大学第二附属医院下呼吸道感染病原菌的分布及耐药性分析

目的：了解天津中医药大学第二附属医院下呼吸道感染病原菌的分布及细菌耐药情况,为临床合理用药提供依据。方法对2015年天津中医药大学第二附属医院分离下呼吸道感染病原菌的分布及药敏结果进行回顾性分析。结果共分离病原菌662株,其中革兰阴性菌504株,占76.13%;革兰阳性菌60株,占9.06%;真菌98株,占14.80%。主要革兰阴性菌对美罗培南的敏感率均达82%以上,不同的菌株对同种抗菌药物的敏感率不同;不论是革兰阴性菌还是革兰阳性菌普遍出现了多重耐药现象。白假丝酵母菌对两性霉素B、5-氟胞嘧啶、氟康唑、伊曲康唑和伏立康唑的敏感率均达到98%以上。结论下呼吸道感染以革兰阴性菌为主,不同菌株对不同抗生素的耐药性也不同,临床应及时了解病原菌分布及耐药情况,合理使用抗菌药物。     

布拉酵母菌联合舒肝宁注射液治疗新生儿高胆红素血症的疗效观察

目的观察布拉酵母菌联合舒肝宁注射液治疗新生儿高胆红素血症的临床疗效。方法选取2014年6月—2015年6月在湖北医药学院附属人民医院进行治疗的新生儿高胆红素血症的患儿70例,随机分为对照组和治疗组,每组各35例。对照组患儿静脉滴注舒肝宁注射液,10 mL加入到10%葡萄糖注射液250 mL,1次/d,症状缓解后可改用肌内注射2 mL/次,1次/d。治疗组患儿在对照组的基础上给予布拉氏酵母菌散,1袋/次,1次/d。两组患儿均治疗2周。观察两组患儿的临床疗效,同时比较两组治疗前后胆红素水平和常见临床指标的变化。结果治疗后,对照组和治疗组的总有效率分别为80.00%、94.29%,两组比较差异有统计学意义(P0.05)。治疗后,两组患儿血清胆红素水平和经皮测定胆红素水平均显著下降,同组治疗前后差异比较具有统计学意义(P0.05);且治疗后治疗组这些观察指标的下降幅度明显优于对照组,两组比较差异具有统计学意义(P0.05)。治疗后,治疗组患儿日均胆红素下降值明显大于对照组,而黄疸消退时间和蓝光治疗时间明显短于对照组,两组这些观察指标比较差异具有统计学意义(P0.05)。结论布拉氏酵母菌联合舒肝宁注射液治疗新生儿高胆红素血症具有较好的临床疗效,可显著降低患儿体内胆红素水平,缩短黄疸消退时间及蓝光治疗时间,具有一定的临床推广应用价值。