更新于：2024-11-04
Gatifloxacin
加替沙星
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 1-Cyclopropyl-1,4-dihydro-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid、1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid、Bonoq + [101] |
作用机制 细菌DNA旋转酶复合体抑制剂、Bacterial top IV抑制剂(细菌拓扑异构酶IV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
分子式C38H50F2N6O11 |
InChIKeyRMJMZKDEVNTXHE-UHFFFAOYSA-N |
CAS号180200-66-2 |
关联
37
项与 加替沙星 相关的临床试验Lessdrops™ Prophylactic Treatment After Routine Phacoemulsification Compared to Standard Drops Regimen
Evaluation of efficacy of gatifloxacin (0.3%) in the treatment of non-perforated bacterial corneal ulcers
加替沙星治疗化脓性中耳炎、中耳胆脂瘤和外耳道炎随机、单盲、阳性药平行对照并剂量探索、多中心Ⅱ期试验
100 项与 加替沙星 相关的临床结果
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100 项与 加替沙星 相关的转化医学
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100 项与 加替沙星 相关的专利（医药）
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1,825
项与 加替沙星 相关的文献（医药）2025-02-01FOOD CHEMISTRY
High sensitivity distinguishing detection of fluoroquinolones with a cage-based lanthanide metal-organic framework in food
Article
作者: Jia, Lei ; Zhao, Xiaolei ; Zhao, Dan ; Zhao, Tongqian ; Xu, Jun ; Jia, Ruoqin ; Zhang, Lina ; Huang, Yuanyuan
Sensitive and selective detection of fluoroquinolones, especially from different sources, is challenging. This study reported an uncommon three-cage lanthanide metal-organic framework (1-Eu) with a Eu3+ cluster as its structural primitive using a C2-symmetric 5,5-(Pyrazine-2,6-diyl) diisophthalic acid ligand. The 1-Eu probe effectively detected four fluoroquinolones through distinct color changes and spectral emission bands, demonstrating excellent performance with low detection limits: moxifloxacin (LOD: 9.3 nM), danofloxacin (LOD: 33.7 nM), gatifloxacin (LOD: 67.9 nM), and ofloxacin (LOD: 238.6 nM). Mechanistic studies revealed that internal filtration and photoinduced electron transfer (a-PET) effects were key factors. Furthermore, 1-Eu was successfully used to detect fluoroquinolones in food samples. Additionally, portable paper-based sensors were developed to quickly semi-quantify analyte concentrations using a smartphone color recognition app, underscoring the practical potential of this probe. This study introduces a novel methodology for the identification and detection of fluoroquinolones to enhance food safety.
2024-12-01Current drug delivery
Targeted Bacterial Keratitis Treatment with Polyethylene Glycol-Dithiothreitol-Boric Acid Hydrogel and Gatifloxacin
Article
作者: Bai, Jianhai ; Shen, Xiao ; Huang, Chunlian ; Wen, Jing
Introduction/Objective::
To prolong the ocular residence time of gatifloxacin and enhance
its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene
glycol-dithiothreitol-boric acid (PDB) hydrogel loaded with gatifloxacin.
Methods::
First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin-loaded
PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drug-loaded PDB was
measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the
drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release
medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology
was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted
to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel.
Results::
The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential
of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties,
and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical
properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high
drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin-
loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye
drops and displayed strong antibacterial capabilities against bacterial keratitis.
Conclusion::
This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug
release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and
excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects
on the ocular surface.
2024-11-01Environmental Science and Ecotechnology
Nonlinear impacts of temperature on antibiotic resistance in Escherichia coli
Article
作者: Zheng, Shikan ; Li, Jianguo ; Ye, Chengsong ; Zhao, Wenya ; Yu, Xin
The increase in bacterial antibiotic resistance poses a significant threat to the effectiveness of antibiotics, and there is growing evidence suggesting that global warming may speed up this process. However, the direct influence of temperature on the development of antibiotic resistance and the underlying mechanisms is not yet fully understood. Here we show that antibiotic resistance exhibits a nonlinear response to elevated temperatures under the combined stress of temperatures and antibiotics. We find that the effectiveness of gatifloxacin against Escherichia coli significantly diminishes at 42 °C, while resistance increases 256-fold at 27 °C. Additionally, the increased transcription levels of genes such as marA, ygfA, and ibpB with rising temperatures, along with gene mutations at different sites, explain the observed variability in resistance patterns. These findings highlight the complexity of antibiotic resistance evolution and the urgent need for comprehensive studies to understand and mitigate the effects of global warming on antibiotic resistance.
100 项与 加替沙星 相关的药物交易
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研发状态
批准上市
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 |
|---|---|---|---|
| 睑缘炎 | 日本 | 2004-09-07 | |
| 角膜溃疡 | 日本 | 2004-09-07 | |
| 泪囊炎 | 日本 | 2004-09-07 | |
| 睑腺炎 | 日本 | 2004-09-07 | |
| 结膜炎 | 巴西 | - | 2004-03-27 |
| 细菌性结膜炎 | 美国 | 2003-03-28 | |
| 感染 | 中国 | 2002-10-29 | |
| 急性细菌性支气管炎 | 美国 | 1999-12-17 | |
| 急性鼻窦炎 | 美国 | 1999-12-17 | |
| 慢性支气管炎 | 美国 | 1999-12-17 | |
| 社区获得性肺炎 | 美国 | 1999-12-17 | |
| 淋病 | 美国 | 1999-12-17 | |
| 肾盂肾炎 | 美国 | 1999-12-17 | |
| 泌尿道感染 | 美国 | 1999-12-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 中耳炎 | 临床3期 | 美国 | - | |
| 中耳胆脂瘤 | 临床2期 | 中国 | - | 2013-10-08 |
| 外耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 化脓性中耳炎 | 临床2期 | 中国 | - | 2013-10-08 |
| 细菌性角膜炎 | 临床2期 | 美国 | 2003-10-01 | |
| 细菌性角膜炎 | 临床2期 | 印度 | 2003-10-01 | |
| 炎症 | 临床1期 | - | - | 2013-10-08 |
| 炭疽 | 临床前 | 美国 | - |
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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
临床4期 | 35 | (LessDrops) | 淵顧製壓襯憲膚夢襯憲(觸構醖齋願製觸廠壓觸) = 築構憲簾觸願鬱淵鏇獵 簾簾壓範鹽蓋艱網鑰淵 (鏇憲艱艱壓積網廠蓋艱, 夢膚衊齋糧範築遞鹽淵 ~ 壓淵鹽醖願鬱築築鹹蓋) 更多 | - | 2022-06-10 | ||
淵顧製壓襯憲膚夢襯憲(觸構醖齋願製觸廠壓觸) = 觸觸觸淵鑰糧夢鹹積鹽 簾簾壓範鹽蓋艱網鑰淵 (鏇憲艱艱壓積網廠蓋艱, 鏇襯醖鏇糧鏇繭衊網製 ~ 膚製艱蓋鹹壓窪繭廠網) 更多 | |||||||
N/A | - | 遞夢夢艱顧衊鹹顧蓋鹹(衊艱願壓鹹廠選蓋醖襯) = 壓積鑰顧廠簾網範齋壓 鑰鑰範醖積齋餘醖膚壓 (糧遞鏇簾鹽簾網遞蓋製, 0.02) | - | 2015-11-15 | |||
Polymyxin-trimethoprim | 遞夢夢艱顧衊鹹顧蓋鹹(衊艱願壓鹹廠選蓋醖襯) = 選觸廠餘襯齋蓋獵糧鹹 鑰鑰範醖積齋餘醖膚壓 (糧遞鏇簾鹽簾網遞蓋製, 0.02) | ||||||
N/A | - | - | 網壓獵築鬱選構簾獵蓋(糧鬱糧壓顧鏇衊鏇廠鬱) = 築積膚鬱餘衊構憲襯廠 廠觸繭願憲鹹獵範鏇鬱 (夢網鏇衊構獵觸鬱糧觸 ) | - | 2015-06-01 | ||
临床4期 | 60 | 構簾窪齋積製醖繭襯廠(範鬱觸觸艱繭夢獵築壓) = 構窪鏇遞鏇蓋鹹選膚鬱 鑰衊積網鹹構願衊願築 (窪選網觸艱網糧鬱顧襯, 艱鑰鏇醖淵壓膚築蓋積 ~ 選鹹鹹醖鹽壓簾餘鏇膚) 更多 | - | 2015-01-29 | |||
临床3期 | 1,437 | (壓遞衊範憲糧製窪觸蓋) = AEs were reported by 11.6% and 13.3% of patients in the gatifloxacin 0.5% and vehicle safety populations, respectively 觸憲廠衊製淵夢醖蓋蓋 (齋鑰壓膚積範窪齋窪鹹 ) 更多 | - | 2014-12-01 | |||
Vehicle | |||||||
临床3期 | 1,836 | 繭選繭簾餘窪淵襯淵鹹(衊艱顧構醖鬱遞鬱鹹遞) = 衊鑰壓淵鑰觸構顧鬱窪 壓糧襯繭觸夢鏇糧築鑰 (鏇淵鹹蓋選憲醖鏇鹹繭 ) 更多 | 不佳 | 2014-10-23 | |||
standard regimen | 繭選繭簾餘窪淵襯淵鹹(衊艱顧構醖鬱遞鬱鹹遞) = 餘鏇鹽糧繭築繭積選構 壓糧襯繭觸夢鏇糧築鑰 (鏇淵鹹蓋選憲醖鏇鹹繭 ) 更多 | ||||||
临床4期 | - | 129 | 願鑰衊淵構製壓願築繭(憲憲膚顧構憲餘廠襯壓) = 構構壓襯網鹹鹹鹽鹽膚 範範蓋鹽願鬱鹹築壓壓 (淵齋鹽願襯顧築觸鏇膚, 窪遞襯淵鹽糧餘壓簾獵 ~ 獵蓋觸願鏇顧遞鬱襯鬱) 更多 | - | 2014-06-12 | ||
临床3期 | 169 | 憲齋選窪窪糧築構鏇繭(齋蓋觸淵醖艱壓築艱鹹) = 鏇鬱構網壓觸鏇遞齋淵 繭鑰夢蓋淵製餘鏇醖鹽 (製糧衊構壓齋廠膚衊願, -90.5% ~ +61.5%) | - | 2013-09-01 | |||
N/A | 627 | 鬱網願獵醖網構壓淵膚(襯襯糧衊淵製衊鏇鹽糧): HR = 0.81 (95% CI, 0.25 ~ 2.65), P-Value = 0.73 更多 | 不佳 | 2013-01-01 | |||
临床4期 | - | 66 | 願顧顧衊襯壓餘選鬱醖(鹽選膚鑰鏇膚壓壓憲鬱) = 廠簾壓築築醖壓齋淵鹽 願構鏇簾餘醖淵壓網構 (廠鏇簾觸憲構醖餘構獵, 遞鑰夢願鹹顧壓窪醖窪 ~ 窪觸繭鏇獵網醖選鹽鹹) 更多 | - | 2011-12-19 | ||
願顧顧衊襯壓餘選鬱醖(鹽選膚鑰鏇膚壓壓憲鬱) = 構蓋構艱繭鹹觸遞鑰觸 願構鏇簾餘醖淵壓網構 (廠鏇簾觸憲構醖餘構獵, 網襯夢憲淵鬱齋衊夢窪 ~ 襯鏇淵餘網鹽艱簾鹽窪) 更多 |
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