更新于：2024-11-04
Cephradine
头孢拉定
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 (6R,7R)-7-((R)-2-Amino-2-(1,4-cyclohexadien-1-yl)acetamido)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid、(6R,7R)-7-{[(2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetyl]amino}-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid、7-(D-2-Amino-2-(1,4-cyclohexadienyl)acetamide)desacetoxycephalosporanicacid + [19] |
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 |
治疗领域 |
在研适应症 |
在研机构 |
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C16H19N3O4S |
InChIKeyRDLPVSKMFDYCOR-UEKVPHQBSA-N |
CAS号38821-53-3 |
关联
26
项与 头孢拉定 相关的临床试验Oral Versus Intravenous Antibiotic Prophylaxis Before Obstetric and Gynecological Procedures
头孢拉定胶囊在中国健康受试者中单中心、随机、开放、单剂量、两周期交叉空腹及餐后状态下的生物等效性试验
头孢拉定胶囊（0.25g/粒）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
100 项与 头孢拉定 相关的临床结果
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100 项与 头孢拉定 相关的转化医学
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100 项与 头孢拉定 相关的专利（医药）
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900
项与 头孢拉定 相关的文献（医药）2024-11-01SCIENCE OF THE TOTAL ENVIRONMENT
Adsorption mechanism of cefradine on three microplastics: A combined molecular dynamics simulation and density functional theory calculation study
Article
Microplastics and antibiotics are receiving increasing attention as two emerging pollutants in the aquatic ecosystem. The absorption of antibiotics by microplastics can potentially intensify their impact on marine organisms and human health. However, the detailed mechanisms underlying this interaction remain to be elucidated. Through molecular dynamics (MD) simulations and density functional theory (DFT) calculations, this study investigated the adsorption of cefradine (CED) onto three typical microplastics (MPs)-polyethylene (PE), polypropylene (PP), and polyamide (PA). The results of the molecular dynamics simulations showed that the interaction energy between CED and microplastics followed the order of PA-CED > PP-CED > PE-CED, indicating that PA microplastics had the highest adsorption capacity for CED antibiotics. The total energy contribution of the microplastics-cefradine (MPs-CED) systems suggested that the van der Waals and electrostatic interactions were the two primary mechanisms for the adsorption of CED by these three microplastics. In DFT calculations, the adsorption of CED on PA was found to be significantly influenced by both electrostatic and van der Waals effects, while the main driving force in the adsorption of PE and PP is van der Waals effect. In addition, IGMH analysis and AIM topological analysis confirmed that the adsorption of CED on PA relied heavily on the synergistic effect of hydrogen bonding and the van der Waals effect. The findings of this study validate the results obtained from molecular dynamics simulations, laying a foundation for a comprehensive exploration of the interaction mechanisms between microplastics and organic pollutants by integrating MD simulations and DFT calculations.
2024-10-03JOURNAL OF APPLIED MICROBIOLOGY
Synergistic oral beta-lactam combinations for treating tuberculosis
Article
作者: Quan, Diana H ; Triccas, James A ; Sintchenko, Vitali ; Wang, Trixie ; Alffenaar, Jan-Willem C ; Kim, Hannah Y ; Britton, Warwick J ; Martinez, Elena
Abstract:
Background:
The enormous burden of tuberculosis (TB) worldwide is a major challenge to human health, but the costs and risks associated with novel drug discovery have limited treatment options for patients. Repurposing existing antimicrobial drugs offers a promising avenue to expand TB treatment possibilities. This study aimed to explore the activity and synergy of beta-lactams in combination with a beta-lactamase inhibitor, which have been underutilized in TB treatment to date.
Methods:
Based on inhibitory concentration, oral bioavailability, and commercial availability, seven beta-lactams (cefadroxil, tebipenem, cephradine, cephalexin, cefdinir, penicillin V, and flucloxacillin), two beta-lactamase inhibitors (avibactam and clavulanate), and three second-line TB drugs (moxifloxacin, levofloxacin, and linezolid) were selected for combination in vitro testing against Mycobacterium tuberculosis H37Rv. Resazurin assays and colony forming unit enumeration were used to quantify drug efficacy, Chou-Talalay calculations were performed to identify drug synergy and Chou-Martin calculations were performed to quantify drug dose reduction index.
Results:
The order of activity of beta-lactams was cefadroxil > tebipenem > cephradine > cephalexin > cefdinir > penicillin V > flucloxacillin. The addition of clavulanate improved beta-lactam activity to a greater degree than the addition of avibactam. As a result, avibactam was excluded from further investigations, which focused on clavulanate. Synergy was demonstrated for cefdinir/cephradine, cefadroxil/tebipenem, cefadroxil/penicillin V, cefadroxil/cefdinir, cephalexin/tebipenem, cephalexin/penicillin V, cephalexin/cefdinir, cephalexin/cephradine, and cefadroxil/cephalexin, all with clavulanate. However, combining beta-lactams with moxifloxacin, levofloxacin, or linezolid resulted in antagonistic effects, except for the combinations of penicillin V/levofloxacin, penicillin V/moxifloxacin, and cefdinir/moxifloxacin.
Conclusions:
Beta-lactam synergy may provide viable combination therapies for the treatment of TB.
2024-10-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Concanavalin-conjugated zinc-metal-organic framework drug for pH-controlled and targeted therapy of wound bacterial infection
Article
作者: Xin, Gaoli ; Hu, Junli ; He, Xiuxia ; Wang, Yexing ; Zhang, Chong ; Wang, Zuobin ; Gao, Yuwei ; Li, Na
Wounds are prone to infection which may be fatal to the life of the patient. The use of antibiotics is essential for managing bacterial infections in wounds, but the long-term use of high doses of antibiotics may lead to bacterial drug resistance and even to creation of superbacteria. Therefore, the development of targeted antimicrobial treatment strategies and the reduction in antibiotic usage are of utmost urgency. In this study, a multifunctional nanodrug delivery system (Cef-rhEGF@ZIF-8@ConA) for the treatment of bacteriostatic infection was synthesized through self-assembly of Zn2+, cefradine (Cef) and recombinant human epidermal growth factor (rhEGF), then conjugated with concanavalin (ConA), which undergoes pH-responsive degradation to release the drugs. First, ConA can specifically combine with bacteria and inhibit the rapid release of Zn2+ ions, thus achieving a long-acting antibacterial effect. Cef exerts its antibacterial effect by inhibiting the synthesis of bacterial membrane proteins. Finally, Zn2+ ions released from the Zn-metal-organic framework (MOF) demonstrate bacteriostatic properties by enhancing the permeability of the bacterial cell membrane. Furthermore, rhEGF upregulates angiogenesis-associated genes, thereby promoting angiogenesis, re-epithelialization and wound healing processes. The results showed that Cef-rhEGF@ZIF-8@ConA has good biocompatibility, with antibacterial efficacy against Staphylococcus aureus and Escherichia coli of 99.61 % and 99.75 %, respectively. These nanomaterials can inhibit the release of inflammatory cytokines and promote the release of anti-inflammatory cytokines, while also stimulating the proliferation of fibroblasts to facilitate wound healing. Taken together, the Cef-rhEGF@ZIF-8@ConA nanosystem is an excellent candidate in clinical therapeutics for bacteriostatic infection and wound healing.
100 项与 头孢拉定 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 细菌感染 | 中国 | 1985-01-01 | |
| 革兰氏阴性菌感染 | 美国 | 1982-01-01 | |
| 革兰氏阳性细菌感染 | 美国 | 1982-01-01 |
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