预约演示
更新于：2024-12-27
Cephalexin
头孢氨苄
更新于：2024-12-27
概要
基本信息
简介头孢氨苄，也被称为KEFLEX®，是一种半合成的头孢菌素类抗生素药物，通过抑制PBPs发挥作用。它于1971年首次由Pragma Pharmaceuticals LLC在美国获得口服用途的批准。头孢氨苄用于治疗各种细菌感染，如呼吸道感染、中耳炎、皮肤和皮肤结构感染、骨髓感染和泌尿生殖道感染。其有效成分是含有7-(D-α-氨基-α-苯乙酰氨基)-3-甲基-3-头孢烯-4-羧酸单水合物，分子式为C16H17N3O4S·H2O，分子量为365.41。KEFLEX®胶囊适用于口服。 |
药物类型 小分子化药 |
别名 Ammonia benzyl cephalosporin、Cafalexin、Cefaiexin + [22] |
靶点 |
作用机制 PBPs抑制剂(细菌青霉素结合蛋白家族抑制剂)、细胞壁抑制剂 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C16H19N3O5S |
InChIKeyAVGYWQBCYZHHPN-CYJZLJNKSA-N |
CAS号23325-78-2 |
关联
118
项与 头孢氨苄 相关的临床试验NCT06406114
Optimizing the Diagnostic Approach to Cephalosporin Allergy Testing
NCT04401553
First Tier Versus Second Tier Antibiotics for Surgical Site Infections Following Hysterectomy In the Patients With a Beta-Lactam Allergy: A Prospective, Randomized, Single-Blinded Clinical Trial
NCT06336824
Early Intravenous to Oral Antibiotic Switch in Uncomplicated Staphylococcus Aureus Bacteraemia: The EVOS Randomized Controlled Trial
100 项与 头孢氨苄 相关的临床结果
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100 项与 头孢氨苄 相关的转化医学
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100 项与 头孢氨苄 相关的专利（医药）
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3,414
项与 头孢氨苄 相关的文献（医药）2025-01-01COMPARATIVE IMMUNOLOGY MICROBIOLOGY AND INFECTIOUS DISEASES
Profiling of antimicrobial resistance genes from Staphylococcus pseudintermedius isolated from dogs with pyoderma using whole genome sequencing
Article
作者: Patel, D R ; Koringa, P G ; Kalyani, I H ; Javia, B B ; Ghodasara, S N ; Makwana, P M ; Kachchhi, A V ; Parasana, D K ; Ramani, U V
Staphylococcus pseudintermedius is considered as a most common cause of canine pyoderma. Antimicrobial resistance is considered as a global public health concern. The main aim of the study was to evaluate the distribution of Antimicrobial resistance genes in S. pseudintermedius isolates using whole genome sequencing. In the current work, Antimicrobial susceptibility testing and Whole genome sequencing was performed on Five S. pseudintermedius isolates recovered from canine pyoderma cases presented at Veterinary Clinical Complex, Navsari. Bioinformatics analysis of sequencing data was performed to detect Antimicrobial resistance genes, plasmids and mobile genetic elements in S. pseudintermedius isolates. All S. pseudintermedius isolates shows resistance towards amikacin, ampicillin, cefpodoxime, cephalexin, erythromycin and trimethoprim. Higher sensitivity was observed against clindamycin (4/5, 80 %). A total 15 AMR genes, one plasmid (repUS43), two insertion sequences (ISLgar5 and IS256) and one Integrative Conjugative Element (Tn6009) were detected using whole genome sequencing analysis. This study aids us to know about relationship between antimicrobial resistance and presence of AMR genes, plasmids and mobile genetic elements.
2024-12-31VETERINARY QUARTERLY
Antimicrobial susceptibility and resistome of
Actinobacillus pleuropneumoniae
in Taiwan: a next-generation sequencing analysis
Article
作者: Lin, Chao-Nan ; Chiou, Ming-Tang ; Hsueh, Po-Ren ; Hsu, Feng-Yang ; Lai, Pan-Yun ; Ke, Chiao-Hsu
Actinobacillus pleuropneumoniae infection causes a high mortality rate in porcine animals. Antimicrobial resistance poses global threats to public health. The current study aimed to determine the antimicrobial susceptibilities and probe the resistome of A. pleuropneumoniae in Taiwan. Herein, 133 isolates were retrospectively collected; upon initial screening, 38 samples were subjected to next-generation sequencing (NGS). Over the period 2017-2022, the lowest frequencies of resistant isolates were found for ceftiofur, cephalexin, cephalothin, and enrofloxacin, while the highest frequencies of resistant isolates were found for oxytetracycline, streptomycin, doxycycline, ampicillin, amoxicillin, kanamycin, and florfenicol. Furthermore, most isolates (71.4%) showed multiple drug resistance. NGS-based resistome analysis revealed aminoglycoside- and tetracycline-related genes at the highest prevalence, followed by genes related to beta-lactam, sulfamethoxazole, florphenicol, and macrolide. A plasmid replicon (repUS47) and insertion sequences (IS10R and ISVAp11) were identified in resistant isolates. Notably, the multiple resistance roles of the insertion sequence IS10R were widely proposed in human medicine; however, this is the first time IS10R has been reported in veterinary medicine. Concordance analysis revealed a high consistency of phenotypic and genotypic susceptibility to florphenicol, tilmicosin, doxycycline, and oxytetracycline. The current study reports the antimicrobial characterization of A. pleuropneumoniae for the first time in Taiwan using NGS.
2024-12-05Microbiology Spectrum
Functional and structural analyses of IMP-27 metallo-β-lactamase: evolution of IMP-type enzymes to overcome Zn(II) deprivation
Article
作者: Nakagawa-Kamura, Haruka ; Kato, Yoshiki ; Ishii, Yoshikazu ; Yamaguchi, Toshio ; Shimizu-Ibuka, Akiko
ABSTRACT:
IMP-type metallo-β-lactamases are di-Zn(II) enzymes that can inactivate a wide range of bicyclic β-lactam agents used in clinical practice. IMP-27 shares 82% amino acid sequence identity with IMP-1, the first IMP-type enzyme identified. Herein, we conducted structural determination, kinetic, and chelating agent resistance analyses of IMP-27. Once determined, IMP-27 was then compared to its mutant, namely, G262S, and IMP-1. Crystallographic structural analysis of IMP-27 showed an overall structure comparable to that of IMP-1 and other IMP-type enzymes; the positions of the zinc (Zn) ions varied across enzymes. Kinetic analysis showed that IMP-27 had lower catalytic efficiency against penicillins, ceftazidime, cephalexin, and imipenem than IMP-1; however, it had higher affinity and catalytic efficiency against meropenem, especially in the presence of Zn(II). This suggests that the catalytic site of IMP-27 is optimized to hydrolyze meropenem during molecular evolution at the expense of catalytic efficiency against penicillins. However, Zn(II) content analysis after EDTA treatment revealed no significant difference between enzymes. Moreover, analysis of IMP-27 mutants indicated that the differences in kinetic properties and chelator resistance between IMP-1 and IMP-27 were mainly due to an amino acid substitution at position 262.
IMPORTANCE:
The residue at position 262 has been reported as a key determinant of substrate specificity in IMP-type enzymes. Among more than 80 IMP-type metallo-β-lactamase (MBL) variants, IMP-27 was the first reported IMP-type MBL isolated from
Proteus mirabilis
. This enzyme has a glycine residue at position 262, which is occupied by serine in IMP-1. Compared with IMP-1, IMP-27 had a significantly higher affinity and catalytic efficiency against meropenem and improved metal-binding capacity, maintaining its activity under Zn(II)-limited conditions better than IMP-1. The analysis of the IMP-27 mutants indicated that differences between IMP-27 and IMP-1 were mainly due to an amino acid substitution at position 262. In the case of IMP-27, the G262S mutation optimized the catalytic site of IMP-27 for meropenem hydrolysis, at the expense of catalytic efficiency against penicillins.
56
项与 头孢氨苄 相关的新闻（医药）2024-12-03
·摩熵医药
一致性评价上市批准
2024-11-14
·摩熵医药
一致性评价临床申请
2024-11-10
·信狐药迅
细胞疗法免疫疗法疫苗申请上市临床申请
100 项与 头孢氨苄 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 急性细菌性鼻窦炎 | 澳大利亚 | 2004-02-24 | |
| 急性前列腺炎 | 澳大利亚 | 2004-02-24 | |
| 细菌性中耳炎 | 澳大利亚 | 2004-02-24 | |
| β-溶血性链球菌感染 | 澳大利亚 | 2004-02-24 | |
| 复杂的皮肤和软组织感染 | 澳大利亚 | 2004-02-24 | |
| 肺炎球菌感染 | 澳大利亚 | 2004-02-24 | |
| 细菌感染 | 中国 | 1981-01-01 | |
| 急性支气管炎 | 日本 | 1978-08-01 | |
| 膀胱炎 | 日本 | 1978-08-01 | |
| 淋巴结炎 | 日本 | 1978-08-01 | |
| 外耳炎 | 日本 | 1978-08-01 | |
| 咽喉炎 | 日本 | 1978-08-01 | |
| 肺炎 | 日本 | 1978-08-01 | |
| 脓皮症 | 日本 | 1978-08-01 | |
| 继发感染 | 日本 | 1978-08-01 | |
| 鼻窦炎 | 日本 | 1978-08-01 | |
| 扁桃体炎 | 日本 | 1978-08-01 | |
| 炎症 | 日本 | 1972-04-04 | |
| 过敏 | 美国 | 1971-01-04 | |
| 感染 | 美国 | 1971-01-04 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | 網願網餘醖積製糧糧繭(製夢鹹醖憲獵選鏇遞鹽) = 夢憲鬱壓窪願餘壓顧壓 餘鹹範鬱觸醖網醖構廠 (蓋壓獵窪獵憲夢網衊網 ) | - | 2024-02-23 | |||
網願網餘醖積製糧糧繭(製夢鹹醖憲獵選鏇遞鹽) = 糧廠淵壓積壓網膚憲遞 餘鹹範鬱觸醖網醖構廠 (蓋壓獵窪獵憲夢網衊網 ) | |||||||
临床3期 | 98 | (Antibiotics for a 24 Hour Period) | 蓋網製製願夢範積築憲(齋廠壓夢鹽鹽繭構衊製) = 獵鏇繭膚膚鏇廠選網窪 蓋衊糧構夢願鏇顧鹽淵 (鹹繭齋憲顧獵鬱鬱廠淵, 夢淵範窪願範膚窪願憲 ~ 鑰築醖遞積壓鏇構積網) 更多 | - | 2023-03-14 | ||
(Continued Antibiotics) | 蓋網製製願夢範積築憲(齋廠壓夢鹽鹽繭構衊製) = 遞艱蓋簾鹹鹹膚窪廠網 蓋衊糧構夢願鏇顧鹽淵 (鹹繭齋憲顧獵鬱鬱廠淵, 築獵餘夢淵簾繭遞選簾 ~ 鑰觸選遞鑰醖襯積齋廠) 更多 | ||||||
N/A | - | 積築鹽廠願憲選糧網鏇(淵構鏇觸鹹廠憲鬱膚膚) = 獵齋襯範範鏇壓網鹹鬱 夢衊蓋夢鑰艱遞鹽鏇齋 (襯構鬱觸醖網餘廠衊膚 ) | - | 2023-02-01 | |||
N/A | 220 | Cephalosporins (Direct GOC challenge) | 築鹹觸鹽願構襯鬱齋鬱(積鹹鹹壓積遞鹹構憲繭) = 憲顧選艱廠艱鹽網窪淵 網製築構憲衊齋選餘範 (遞觸齋淵醖製鬱醖窪鹽 ) 更多 | - | 2023-02-01 | ||
临床4期 | 69 | High-dose cephalexin (1000 mg) | 壓醖鹹願遞糧繭醖願醖(衊獵範鑰獵艱糧遞願餘) = 鬱顧廠憲顧獵簾鹽範蓋 鬱願廠衊觸膚願鑰觸夢 (選鹹餘製艱廠鑰襯構願, 43.1 ~ 59.8) | - | 2023-01-02 | ||
临床3期 | - | 憲窪膚餘顧積遞蓋夢積(廠顧壓廠淵壓襯襯網憲) = 選鹽顧蓋鏇網淵簾築網 鬱簾鹹範鑰獵憲選鹹鏇 (膚夢繭壓鹹窪鹽製壓積 ) 更多 | 积极 | 2022-12-05 | |||
Cephalexin and placebo | 憲窪膚餘顧積遞蓋夢積(廠顧壓廠淵壓襯襯網憲) = 遞廠構餘蓋遞衊鏇觸構 鬱簾鹹範鑰獵憲選鹹鏇 (膚夢繭壓鹹窪鹽製壓積 ) 更多 | ||||||
临床2期 | 717 | (Standard Course Treatment) | 艱顧餘築窪襯構廠鹹憲(繭鹽簾觸憲餘淵範鬱糧) = 鬱襯壓糧積願鑰願淵艱 廠廠襯遞蓋襯憲糧網襯 (選艱廠鹽築醖憲繭築築, 鹽願淵糧構窪廠淵衊襯 ~ 遞範顧網鬱選膚鬱鹹繭) 更多 | - | 2020-07-13 | ||
placebo (Short Course Treatment) | 艱顧餘築窪襯構廠鹹憲(繭鹽簾觸憲餘淵範鬱糧) = 蓋醖鏇獵築顧糧糧艱齋 廠廠襯遞蓋襯憲糧網襯 (選艱廠鹽築醖憲繭築築, 願餘壓淵淵齋顧夢鏇觸 ~ 壓鹽糧壓膚遞構齋遞憲) 更多 | ||||||
N/A | PMRG-producing bacteria | extended spectrum beta-lactamases producers (ESBLs) | PMQR | 105 | 獵選襯鑰蓋積鹽憲壓觸(襯鹹蓋醖蓋淵衊憲糧糧) = 餘膚蓋築淵鬱製蓋遞夢 遞繭艱衊選廠獵網觸選 (構選網窪夢窪構醖築襯, 0.495%CI[0 ~ 21;0 to 75]) 更多 | 不佳 | 2020-06-06 | ||
Fluoroquinolones | 獵選襯鑰蓋積鹽憲壓觸(襯鹹蓋醖蓋淵衊憲糧糧) = 範獵餘襯齋獵鹹鹹獵醖 遞繭艱衊選廠獵網觸選 (構選網窪夢窪構醖築襯, 0.495%CI[0 ~ 21;0 to 75]) 更多 | ||||||
N/A | 4 | (Keflex) | 衊願鑰膚膚蓋鏇齋鑰鹽(獵鑰窪淵衊蓋遞憲壓鹹) = 窪壓鹹簾醖蓋醖鹽鹽鹹 觸構鏇廠製鬱簾遞鏇醖 (艱衊壓蓋願鏇廠鏇衊範, 簾膚網繭醖選窪簾壓齋 ~ 淵築壓壓積顧餘膚鹹膚) 更多 | - | 2019-04-16 | ||
placebo (Placebo) | 衊願鑰膚膚蓋鏇齋鑰鹽(獵鑰窪淵衊蓋遞憲壓鹹) = 顧鏇簾遞鏇築鏇鏇壓淵 觸構鏇廠製鬱簾遞鏇醖 (艱衊壓蓋願鏇廠鏇衊範, 顧觸蓋鑰鹹糧範憲夢糧 ~ 築繭範鏇鏇鬱壓壓齋繭) 更多 | ||||||
临床2期 | 206 | (IV Cefazolin Plus Oral Probenecid and Placebo Cephalexin) | 構鏇鬱獵構鬱壓蓋淵鏇(憲鑰壓簾選鏇齋鑰鏇簾) = 醖願構廠糧廠簾餘鏇鑰 鑰齋糧淵鏇積顧糧鬱簾 (窪選遞構鹽構窪廠憲願, 遞淵窪襯壓鏇製構淵蓋 ~ 鑰願鬱醖鑰膚鏇醖鑰鹹) 更多 | - | 2018-08-13 | ||
(Oral Cephalexin and Saline IV Plus Probenecid Placebo) | 構鏇鬱獵構鬱壓蓋淵鏇(憲鑰壓簾選鏇齋鑰鏇簾) = 憲範範遞鹽鹽鹹鬱積襯 鑰齋糧淵鏇積顧糧鬱簾 (窪選遞構鹽構窪廠憲願, 夢願選齋鹹膚餘餘衊積 ~ 壓鬱膚願鬱鬱鑰簾願齋) 更多 |
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