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[Carumonam].
Pub Date : 2020-02-07 DOI: 10.32388/55zue3
A. Saito
An N-sulfo monocyclic beta-lactam antibiotic derived from sulfazecin. Carumonam has high resistance to beta-lactamases and activity against aerobic gram-negative bacteria. It reaches high urinary concentrations and may be used in the treatment of urinary tract infections.
一种n -磺基单环β -内酰胺类抗生素,由磺胺素衍生而来。Carumonam对β -内酰胺酶具有较高的抗性,对需氧革兰氏阴性菌具有较高的抗性。它达到高尿浓度,可用于治疗尿路感染。
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引用次数: 0
[Cefroxadine].
Pub Date : 2020-02-07 DOI: 10.32388/lszpim
K. Mashimo
The antibacterial spectrum of cefroxadine was as wide as that of CEX, and its antibacterial effect was as strong as that of CEX or even 2-fold stronger against E. coli and Klebsiella. Cefroxadine was also proved to have stronger bactericidal or bacteriolytic effect than CEX and have better affinity with penicillin binding proteins. In clinical trials, an efficacy rate of 82.7% was achieved in a total of 2,009 cases of various infections analyzed. Cefroxadine displayed particularly good clinical and bacteriological effects for the infections of skin, soft tissues, respiratory tract and urinary tract. The rate of bacteria eradication in a total of 1,410 cases was 81.6%, showing good results against the bacteria such as S. aureus (83.9%, 167/199), E. coli (89.0%, 528/593), Klebsiella (78.0%, 78/100) and P. mirabilis (80.0%, 36/45). As for side effects, their incidence was a low of only 2.3%, the main ones being eruption and gastrointestinal symptoms just as recognized in conventional cephalosporins, and none of them was serious. Abnormal laboratory test values were only increases in eosinophil, S-GOT, S-GPT and Al-P values, and their incidence was low. From these findings, we may say that the drug is an effective, safe, and useful antibiotic among all other orally administered cephalosporins.
头孢沙定的抑菌谱与CEX一样宽,对大肠杆菌和克雷伯菌的抑菌效果与CEX一样强,甚至强2倍。头孢沙定也被证明比CEX有更强的杀菌或溶菌作用,并且与青霉素结合蛋白有更好的亲和力。在临床试验中,共分析了2009例各种感染,有效率为82.7%。头孢沙定对皮肤、软组织、呼吸道、泌尿道感染表现出较好的临床和细菌学效果。1410例病例的细菌根除率为81.6%,对金黄色葡萄球菌(83.9%,167/199)、大肠杆菌(89.0%,528/593)、克雷伯氏菌(78.0%,78/100)、神奇假单胞菌(80.0%,36/45)等细菌均有较好的根除效果。副作用发生率较低,仅为2.3%,主要为常规头孢菌素所见的皮疹和胃肠道症状,均不严重。实验室检查异常值仅为嗜酸性粒细胞、S-GOT、S-GPT、Al-P升高,发生率较低。根据这些发现,我们可以说该药在所有其他口服头孢菌素中是一种有效、安全和有用的抗生素。
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引用次数: 0
The change of susceptibility of Streptococcus pneumoniae strains isolated from pediatric patients at Asahikawa Kosei Hospital between 2011 and 2015. 2011 - 2015年旭川Kosei医院儿科患者分离肺炎链球菌菌株的药敏变化
Pub Date : 2016-12-01
Hiroshi Sakata

The susceptibility of 1578 Streptococcus pneumoniae strains isolated from pediatric patients at Asahikawa Kosei Hospital between 2011 and 2015 was tested to penicillin G (PCG), cefotaxime (CTX), ceftriaxone (CTRX), cefditoren (CDTR), meropenem (MEPM), erythromycin (EM) and levofloxacin (LVFX). Although no significant differences were observed, the percentage of strains with a minimal inhibitory concentration (MIC) of PCG of <0.1pg/mL increased from 55.5% (2011) to 64.0% (2015), whereas that of strains with MIC of ≥2μg/mL decreased from 14.8% to 9.5%. From 2011 to 2015, the percentage of strains with MIC ≤0.12ug/mL increased from 18.9% to 28.9% for CTX, from 20.5% to 30.2% for CTRX, from 29.2% to 40.9% for CDTR, and from 69.6% to 80.6% for MEPM. EM-resistant strains with MIC ≥22μg/mL accounted for as much as approximately 90% each year. One LVFX-resistant strain with MIC 8pg/mL has been detected each year since 2013.

对2011 - 2015年从旭川Kosei医院儿科患者分离的1578株肺炎链球菌对青霉素G (PCG)、头孢噻肟(CTX)、头孢曲松(CTRX)、头孢地托伦(CDTR)、美罗培南(MEPM)、红霉素(EM)和左氧氟沙星(LVFX)的敏感性进行了检测。虽然没有观察到显著差异,但PCG最低抑制浓度(MIC)的菌株百分比
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引用次数: 0
Importance of prevention in pneumonia in elderly -Attempted use of macrolide therapy. 预防老年人肺炎的重要性-尝试使用大环内酯类药物治疗。
Pub Date : 2016-12-01
Naoyuki Miyashita, Miki Kato, Yasuhiro Kawai, Jiro Okimoto

Pneumonia ranks as the third leading cause of death in Japan. About 97% of patients who die because of pneumonia are elderly, with aspiration generally thought to be involved in the majority of cases of pneumonia in elderly. Once an elderly individual contracts pneumonia, their physical function often declines and their activities of daily living diminish with hospital admission, even in individuals with no underlying disorders. Prolonged confinement to a bed and immobility leads to weakening of the legs and back, making it difficult for elderly patients to attend daily outpatient clinics, often leading to admission to nursing facilities for the aged instead of returning to their own home, even after curative treatment for pneumonia. Most such patients repeatedly develop pneumonia and repeated antibiotic treatment enhances the risk of the emergence of resistant organisms. It is beyond doubt, therefore, that prevention of pneumonia is of vital importance in the elderly.

肺炎是日本第三大死因。约97%因肺炎死亡的患者是老年人,通常认为大多数老年人肺炎病例与误吸有关。一旦老年人感染肺炎,他们的身体功能往往下降,日常生活活动随着住院而减少,即使在没有潜在疾病的个体中也是如此。长期卧床和不活动导致腿部和背部虚弱,使老年患者难以参加日常门诊,往往导致入住老年人护理机构,而不是回到自己的家,即使在肺炎治疗后也是如此。大多数这类患者反复发展为肺炎,反复的抗生素治疗增加了耐药菌出现的风险。因此,毫无疑问,预防肺炎对老年人至关重要。
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引用次数: 0
High efficiency method of detection and isolation of neuraminidase inhibitor resistant influenza viruses by fluorescence sialidase imaging. 荧光唾液酸酶显像法高效检测和分离神经氨酸酶抑制剂耐药流感病毒。
Pub Date : 2016-12-01
Yuuki Kurebayashi

Influenza A and B viruses possess an enzyme "sialidase" that cleavages terminal sialic acid from glycochains. These viral sialidase proteins are highly expressed on the virus infected cells. We developed sialidase imaging probe "BTP3-Neu5Ac" that enables histochemical fluorescence staining of sialidase activity. BTP3-Neu5Ac was able to perform speedy and easy fluorescence imaging of these virus infected cells, with no needs of specific antibody and cell fixation. In addition, combination use of anti-influenza drugs (sialidase inhibitors) and BTP3-Neu5Ac resulted in selective fluorescence imaging for detection and high-efficiency isolation of drug-resistant virus. Fluorescence imaging of drug-resistant virus will be a powerful method for study of the drug-resistance mechanism, for monitoring of drug-resistant viruses. A novel tool for fluorescence imaging of viral sialidase activity is described in this review.

甲型流感和乙型流感病毒具有一种酶“唾液酸酶”,可以从糖链上切割末端唾液酸。这些病毒唾液酸酶蛋白在病毒感染的细胞上高度表达。我们开发了唾液酸酶成像探针“BTP3-Neu5Ac”,可以进行唾液酸酶活性的组织化学荧光染色。BTP3-Neu5Ac能够对这些病毒感染的细胞进行快速、简便的荧光成像,不需要特异性抗体和细胞固定。此外,抗流感药物(唾液酸酶抑制剂)与BTP3-Neu5Ac联合使用可实现选择性荧光成像检测和高效分离耐药病毒。耐药病毒荧光成像将成为研究耐药机制、监测耐药病毒的有力手段。本文介绍了一种新型的病毒唾液酸酶活性荧光成像工具。
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引用次数: 0
Clinical experience with colistin in 9 Japanese patients with infection due to multi-drug resistance pathogens. 9例日本多药耐药病原菌感染患者应用粘菌素的临床体会。
Pub Date : 2016-10-01
Yukihiro Hamada, Jun Hirai, Hiroyuki Suematsu, Yuka Yamagishi, David P Nicolau, Hiroshige Mikamo

Colistin is a polypeptide antibiotic of the polymyxin family (polymyxin E) which has been reported to be active against many multidrug-resistant (MDR) Gram-negative aerobic bacteria collected across the globe. While this agent was not currently licensed in Japan, the emergence of MDR organisms has necessitated its off-label used in the country. However, colistin was approved in March, 2015. This retrospective observational report includes nine patients with MDR Gram-negative infections due to Pseudomonas aeruginosa (n=6) and Klebsiella spp. (n=3) who received intravenous colistin therapy as part of their antimicrobial regimen. The median age and duration of administration were 40 years (range 7-90) and 8 days (range 1-19). Clinical success was observed in all eight patients for whom efficacy could be evaluated. Two patients encountered colistin related adverse effects 22.2% (2/9). In both cases the nephrotoxicity and dysgeusia resolved after discontinuation of colistin therapy. In vitro studies conducted with these clinical isolates of P aeruginosa displayed synergy with the combination of colistin plus ceftazidime, rifampicin, meropenem or aztreonam. This report provides early evidence that colistin is generally safe, effective and demonstrates in vitro synergy when used in combination for the management of MDR Gram-negative pathogens derived from Japanese patients.

粘菌素是多粘菌素家族(polymyxin E)的一种多肽抗生素,据报道,它对全球收集的许多多重耐药(MDR)革兰氏阴性需氧细菌具有活性。虽然该药物目前尚未在日本获得许可,但耐多药生物的出现使其在该国的标签外使用成为必要。然而,粘菌素于2015年3月获批。本回顾性观察报告包括9例由铜绿假单胞菌(n=6)和克雷伯氏菌(n=3)引起的耐多药革兰氏阴性感染患者,这些患者接受静脉粘菌素治疗作为其抗菌方案的一部分。中位年龄和给药时间分别为40岁(范围7-90)和8天(范围1-19)。所有8例患者均观察到临床成功,可对其疗效进行评估。2例患者出现粘菌素相关不良反应22.2%(2/9)。在这两种情况下,肾毒性和肾功能障碍在停用粘菌素治疗后消失。用这些临床分离的铜绿假单胞菌进行的体外研究显示,粘菌素与头孢他啶、利福平、美罗培南或阿唑南联合使用具有协同作用。该报告提供的早期证据表明,粘菌素通常是安全有效的,并且在联合使用时显示出体外协同作用,用于管理来自日本患者的多药耐药革兰氏阴性病原体。
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引用次数: 0
Bactericidal effect of tosufloxacin on Haemophilus influenzae internalized in cultured human cells. 托舒沙星对人培养细胞内化流感嗜血杆菌的杀菌作用。
Pub Date : 2016-10-01
Noboru Yamanaka, Nuneki Hotomi

Nontypeable Haemophilus influenzae, one of the major causative bacteria for acute otitis media (AOM), is also considered to cause intractable otitis media including prolonged AOM and recurrent AOM in children by the mechanism of internalization of the bacteria into epithelial cells of middle ear mucosa. In this study, we visualized the dynamics of H. infiuenzae internalization in cultured human cells. We also examined the effects of antimicrobials, including a novel quinolone, tosufloxacin, and a cephem antibacterial agent, cefditoren, on H. influenzae internalized in cultured human cells. The results indicated that (1) H. infiuenzae were internalized into human cells, (2) cefditoren has no effect on internalized H. influenzae, and (3) tosufloxacin has a bactericidal action on H. infiuenzae invading human cells. These data strongly support high clinical efficacy of tosuffoxacin on intractable otitis media in children.

不可分型的流感嗜血杆菌是急性中耳炎(AOM)的主要致病菌之一,也被认为通过细菌内化到中耳粘膜上皮细胞的机制引起顽固性中耳炎,包括儿童慢性中耳炎和复发性中耳炎。在这项研究中,我们可视化了流感嗜血杆菌在培养的人细胞中的内化动力学。我们还研究了抗菌剂的作用,包括一种新型喹诺酮类药物,托氟沙星和头孢类抗菌剂,头孢多伦,对培养的人类细胞内化的流感嗜血杆菌的影响。结果表明:(1)流感嗜血杆菌内化进入人细胞,(2)头孢地酮对内化的流感嗜血杆菌没有作用,(3)托舒沙星对入侵人细胞的流感嗜血杆菌有杀菌作用。这些数据有力地支持托沙星治疗儿童顽固性中耳炎的高临床疗效。
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引用次数: 0
Sensitivity surveillance of Pseudomonas aeruginosa isolates for several antibacterial agents in Chubu area (2013-2014). 中部地区2013-2014年铜绿假单胞菌对几种抗菌药物的敏感性监测
Pub Date : 2016-10-01
Ai Kakumoto, Hayato Okade, Junichi Misuyama, Kazukiyo Yamaoka, Yuko Asano, Yoko Matsukawa, Hiroyuki Suematsu, Haruki Sawamura, Shigenori Matsubara, Naohiro Shibata, Kunitomo Watanabe, Yoshihiro Yamamoto, Hiromichi Iwasaki, Yuka Yamagishi, Hiroshige Mikamo

We investigated the susceptibility to antibacterial agents of 186 clinical isolates of Pseudomonas aeruginosa isolated from medical facilities in Gifu, Aichi, Toyama, and Fukui prefectures from October 2013 to February 2014. MIC₅₀/₉₀ of piperacillin (PIPC), tazobactam/piperacillin (TAZ/PIPC), ceftazidime (CAZ), cefepime (CFPM), imipenem (IPM), meropenem (MEPM), doripenem (DRPM), aztreonam (AZT), ciprofloxacin (CPFX), levofloxacin (LVFX), amikacin (AMK) and colistin (CL) against P aeruginosa was 8/32, 4/32, 2/8, 2/16, 1/32, 0.5/8, 0.25/4, 8/32, 0.25/8, 0.5/16, 4/8 and 1/1pg/mLrespectively. Two strains of multidrug resistant P aeruginosa were isolated (1.1%). They were isolated from the respiratory tract, intra-abdominal, and urinary infection. The susceptible ratio against P aeruginosa derived from intra-abdominal infection for carbapenem was lower than those from respiratory tract and urinary infection. The susceptible ratio against P aeruginosa derived from urinary infection for penicillin, cephem, monobactam, and fluoroquinolone was lower than those from respiratory and intra-abdominal infection. It is meaningful to pay attention to the susceptibility to antibacterial agents in each clinical specimen from infected organ.

对2013年10月至2014年2月在岐阜县、爱知县、富山县和福井县医疗机构分离的186株铜绿假单胞菌临床分离株进行抗菌药物敏感性调查。哌拉西林(PIPC),他唑巴坦/哌拉西林(TAZ/PIPC),头孢他啶(CAZ),头孢吡肟(CFPM),亚胺培南(IPM),美罗培南(MEPM),多利培南(DRPM),氮曲南(AZT),环丙沙星(CPFX),左氧氟沙星(LVFX),阿米卡星(AMK)和粘菌素(CL)对铜绿假单胞菌的MIC₅₀/₉₀分别为8/ 32,4 / 32,2 / 8,2 /16,1/32,0.5/ 8,0.25 / 4,8 /32,0.25/ 8,0.5 /16,4/8和1/1pg/ ml。分离到2株多重耐药铜绿假单胞菌(1.1%)。他们从呼吸道、腹腔和泌尿系统感染中分离出来。腹腔感染对碳青霉烯类铜绿假单胞菌的敏感率低于呼吸道感染和泌尿系统感染。泌尿系感染对青霉素、头孢菌素、单巴坦和氟喹诺酮类药物的敏感率低于呼吸道感染和腹腔感染。关注感染器官各临床标本对抗菌药物的敏感性具有重要意义。
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引用次数: 0
Advantage and issue of silkworm model for development of anti-infective agents. 家蚕模型在抗感染药物开发中的优势与问题。
Pub Date : 2016-10-01
Hiroshi Hamamoto

We established silkworm infection model for developing a novel antibiotic. Silkworm model has less ethical issues and is low cost compared to mammalian model, thus allow us to use a lot of individuals for screening assay. In addition, we can evaluate therapeutic activity and toxicity of candidate samples because silkworm has similar pharmacokinetics as mammals. Using this system, we identified a novel antibiotic named "Lysocin E". In this review article, we describe advantages of silkworm model for development of antimicrobial agents.

为研制新型抗生素,建立家蚕感染模型。蚕模型与哺乳动物模型相比,伦理问题较少,成本较低,因此我们可以使用大量的个体进行筛选试验。此外,由于家蚕具有与哺乳动物相似的药代动力学,我们可以评估候选样品的治疗活性和毒性。利用该系统,我们鉴定出一种新型抗生素,命名为“Lysocin E”。本文综述了家蚕模型在抗菌药物开发中的优势。
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引用次数: 0
A case of pediatric patient with acute enteritis due to CTX-M-1 5 extended-spectrum β-lactamase-producing Salmonella Blockley. ctx - m - 15广谱产β-内酰胺酶沙门氏菌引起的小儿急性肠炎1例。
Pub Date : 2016-10-01
Storu Kutsuna, Shota Yonetani, Koji Araki, Hidemasa Izumiya

This clinical case report concerns a pediatric patient with acute enteritis caused by multi-drug resistant Salmonella enterica serovar Blockley (Salmonella Blockley). A 3-year-old boy presented to our emergency room with a 5-day history of fever, abdominal pain, and bloody diarrhea. Stool culture tested positive for a Salmonella species, while the blood culture was negative. The patient was successfully treated with an oral antibiotic regimen of fosfomycin. The stool isolate was found to be resistant to multiple drugs, including cefpodoxime, cefotaxime, ceftazidime, and aztreonam, and was confirmed to be a CTX-M-15 extended-spectrum β-lactamase (ESBL)-producing strain of Salmonella Blockley. This is the first report of a pediatric patient in Japan with acute enteritis caused by a CTX-M-15 ESBL- producing strain of Salmonella Blockley.

本临床病例报告涉及一个小儿患者急性肠炎引起的多重耐药肠沙门氏菌血清型巴克利(巴克利沙门氏菌)。一名3岁男孩以发热、腹痛、带血腹泻5天就诊于我们的急诊室。粪便培养对沙门氏菌呈阳性,而血液培养为阴性。患者成功地接受了磷霉素口服抗生素治疗。该粪便分离株对头孢多肟、头孢噻肟、头孢他啶、氨曲南等多种药物耐药,为一株产β-内酰胺酶(ESBL)的Blockley沙门氏菌CTX-M-15菌株。这是日本首例由CTX-M-15产ESBL的沙门氏菌引起的急性肠炎的儿科患者报告。
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引用次数: 0
期刊
The Japanese journal of antibiotics
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