更新于：2024-12-14
Azlocillin Sodium
阿洛西林钠
更新于：2024-12-14
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (1996-01-01), |
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C20H23N5NaO6S |
InChIKeyFUHFQQPUHNRIQM-XFAPPKAWSA-N |
CAS号37091-65-9 |
关联
1
项与 阿洛西林钠 相关的临床试验Efficacy and Safety of Antibiotics in the Treatment of Early Onset Neonatal Sepsis
100 项与 阿洛西林钠 相关的临床结果
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100 项与 阿洛西林钠 相关的转化医学
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100 项与 阿洛西林钠 相关的专利（医药）
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713
项与 阿洛西林钠 相关的文献（医药）2024-12-20Journal of biomolecular structure & dynamics
Multi-targeting of virulence factors of
P. aeruginosa
by β-lactam antibiotics to combat antimicrobial resistance
Article
作者: Husain, Fohad Mabood ; Khan, Altaf ; Parveen, Nagma ; Ahmad, Iqbal ; Qais, Faizan Abul ; Adil, Mohd
Antimicrobial resistance poses a significant challenge to public health, especially in developing countries, due to a substantial rise in bacterial resistance. This situation has become so concerning that we are now at risk of losing the effectiveness of antibiotics altogether. Recent research has firmly established that bacteria engage in a process called quorum sensing (QS). QS regulates various functions, including nutrient scavenging, immune response suppression, increased virulence, biofilm formation and mobility. Pseudomonas aeruginosa, an opportunistic bacterial pathogen, plays a significant role in various medical conditions such as chronic wounds, corneal infections, burn wounds and cystic fibrosis. While antibiotics are effective in killing bacteria, only a few antibiotics, particularly those from the β-lactam group, have been studied for their impact on the quorum sensing of P. aeruginosa. Given the lack of concentrated efforts in this area, we have investigated the role of β-lactam antibiotics on various potential targets of P. aeruginosa. Based on their toxicological profiles and the average binding energy obtained through molecular docking, azlocillin and moxalactam have emerged as lead antibiotics. The binding energy for the docking of azlocillin and moxalactam with LasA was determined to be -8.2 and -8.6 kcal/mol, respectively. Molecular simulation analysis has confirmed the stable interaction of both these ligands with all three target proteins (LasI, LasA and PqsR) under physiological conditions. The results of this research underscore the effectiveness of azlocillin and moxalactam. These two antibiotics may be repurposed to target the quorum sensing of P. aeruginosa.Communicated by Ramaswamy H. Sarma.
2024-08-01JOURNAL OF INTERNATIONAL MEDICAL RESEARCH
Beta-lactam-associated hypokalemia
Review
作者: Tennigkeit, Johanna ; Matyukhin, Igor ; Stasche, Friedrich ; Jansen, Muriel-N. ; Patschan, Daniel ; Ritter, Oliver ; Safi, Wajima
The aim of this narrative review was to discuss the literature on β-lactam antibiotic-associated hypokalemia, a potentially life-threatening electrolyte disorder. The PubMed, Web of Science, Cochrane Library, and Scopus databases were searched for articles published between 1965 and 2023, using the following terms: ‘hypokalemia’ OR ‘potassium loss’ OR ‘potassium deficiency’ AND ‘beta-lactams’ OR ‘penicillin’ OR ‘penicillin G’ OR ‘cephalosporins’ OR ‘ceftazidime’ OR ‘ceftriaxone’ OR ‘flucloxacillin’ OR ‘carbapenems’ OR ‘meropenem’ OR ‘imipenem’ OR ‘cefiderocol’ OR ‘azlocillin’ OR ‘ticarcillin’. Additional search terms were ‘hypokalemia’ AND ‘epidemiology’ AND ‘ICU’ OR ‘intensive care unit’ OR ‘ER’ OR ‘emergency department’ OR ‘ambulatory’ OR ‘old’ OR ‘ageing population’, and experimental (animal-based) studies were excluded. A total of eight studies were selected and discussed, in addition to nine case reports and case series. Both older and currently used β-lactam antibiotics (e.g., ticarcillin and flucloxacillin, respectively) have been associated with therapy-related hypokalemia. The incidence of β-lactam antibiotic-associated hypokalemia may be as high as 40%, thus, the issue of β-lactam-associated hypokalemia remains clinically relevant. Although other causes of hypokalemia are likely to be diagnosed more frequently (e.g., due to diuretic therapy or diarrhea), the possibility of β-lactam-induced renal potassium loss should always be considered in individuals with so-called ‘unexplained hypokalemia’.
2024-04-12ACS infectious diseases
Ureidopenicillins Are Potent Inhibitors of Penicillin-Binding Protein 2 from Multidrug-Resistant Neisseria gonorrhoeae H041
Article
作者: Nicholas, Robert A ; Cardenas Alvarez, Maria ; Stratton, Caleb M ; Turner, Jonathan M ; Bala, Sandeepchowdary ; Davies, Christopher
Effective treatment of gonorrhea is threatened by the increasing prevalence of Neisseria gonorrhoeae strains resistant to the extended-spectrum cephalosporins (ESCs). Recently, we demonstrated the promise of the third-generation cephalosporin cefoperazone as an antigonococcal agent due to its rapid second-order rate of acylation against penicillin-binding protein 2 (PBP2) from the ESC-resistant strain H041 and robust antimicrobial activity against H041. Noting the presence of a ureido moiety in cefoperazone, we evaluated a subset of structurally similar ureido β-lactams, including piperacillin, azlocillin, and mezlocillin, for activity against PBP2 from H041 using biochemical and structural analyses. We found that the ureidopenicillin piperacillin has a second-order rate of acylation against PBP2 that is 12-fold higher than cefoperazone and 85-fold higher than ceftriaxone and a lower MIC against H041 than ceftriaxone. Surprisingly, the affinity of ureidopenicillins for PBP2 is minimal, indicating that their inhibitory potency is due to a higher rate of the acylation step of the reaction compared to cephalosporins. Enhanced acylation results from the combination of a penam scaffold with a 2,3-dioxopiperazine-containing R1 group. Crystal structures show that the ureido β-lactams overcome the effects of resistance mutations present in PBP2 from H041 by eliciting conformational changes that are hindered when PBP2 interacts with the weaker inhibitor ceftriaxone. Overall, our results support the potential of piperacillin as a treatment for gonorrhea and provide a framework for the future design of β-lactams with improved activity against ESC-resistant N. gonorrhoeae.
100 项与 阿洛西林钠 相关的药物交易
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 细菌感染 | 中国 | 1996-01-01 |
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