Fluroquinolones

氟喹诺酮类药物
  • 文章类型: Journal Article
    目的:我们的目的是根据社区获得性大肠埃希菌尿路感染(UTI)患者在过去18个月内的抗生素暴露情况,量化个体对抗菌药物耐药的风险。
    方法:2015-2017年在两个中心前瞻性招募了法国患者。分离株对阿莫西林(AMX)的耐药性,阿莫西林-克拉维酸(AMC),第三代头孢菌素(3GC),甲氧苄啶-磺胺甲恶唑(TMP-SMX),氟喹诺酮类(FQ)和磷霉素(FOS)根据健康保险文件中记录的以前的类内和类间抗生素暴露进行分析.
    结果:在所分析的722例UTI病例(564例)中,有588例(81.4%)发现了以前的抗生素暴露。与远程暴露(UTI前18个月)相比,最近的暴露(UTI前3个月)对AMX的大肠杆菌耐药性具有更强的类内影响,AMC,FQ和TMP-SMX,相应的调整后赔率比[95%置信区间]为1.63[1.20-2.21],1.59[1.02-2.48],3.01[1.90-4.77],和2.60[1.75-3.87]。AMX,FQ,TMP-SMX也表现出显著的类间影响。对3GC的抗性与组内暴露没有显着相关(调整后的OR:0.88[0.41-1.90])。FOS抗性显著低(0.4%)。耐药性风险降至10%以下所需的无抗生素期持续时间,在UTI中经验使用的阈值,被建模为3GC<1个月,AMX和TMP-SMX>18个月,AMC(5.2个月[2.3至>18])和FQ(17.4个月[7.4至>18])不确定。
    结论:引起UTI的E.coli的耐药性部分可以通过以前的个人抗生素使用来预测。
    OBJECTIVE: We aimed to quantify the individual risk of antimicrobial resistance among patients with community-acquired Escherichia coli urinary tract infection (UTI) according to their antibiotic exposure over the previous 18 months.
    METHODS: French patients were prospectively recruited in two centers in 2015-2017. Resistance of isolates to amoxicillin (AMX), amoxicillin-clavulanate (AMC), third-generation cephalosporins (3GC), trimethoprim-sulfamethoxazole (TMP-SMX), fluoroquinolones (FQ) and fosfomycin (FOS) was analysed according to previous intra-class and inter-class antibiotic exposure documented in health insurance files.
    RESULTS: Previous antibiotic exposure was found in 588 (81.4 %) of the 722 UTI cases analysed (564 patients). Recent exposure (three months before UTI) was associated with stronger intra-class impact on E. coli resistance compared to remote exposure (18 months before UTI) for AMX, AMC, FQ and TMP-SMX, with respective adjusted odds ratios [95 % confidence interval] of 1.63 [1.20-2.21], 1.59 [1.02-2.48], 3.01 [1.90-4.77], and 2.60 [1.75-3.87]. AMX, FQ, and TMP-SMX also showed significant inter-class impact. Resistance to 3GC was not significantly associated with intraclass exposure (adjusted OR: 0.88 [0.41-1.90]). FOS resistance was remarkably low (0.4 %). Duration of the antibiotic-free period required for resistance risk to drop below 10 %, the threshold for empirical use in UTI, was modelled as < 1 month for 3GC, >18 months for AMX and TMP-SMX and uncertain for AMC (5.2 months [2.3 to > 18]) and FQ (17.4 months [7.4 to > 18]).
    CONCLUSIONS: Resistance of E. coli causing UTI is partially predicted by previous personal antibiotic delivery.
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  • 文章类型: Journal Article
    这项研究是为了确定结核分枝杆菌利福平敏感菌株中异烟肼(INH)和氟喹诺酮FQ的耐药频率,并研究其突变模式。对通过基于药筒的NAAT(CBNAAT)检测的具有结核分枝杆菌的样品进行回顾性分析。根据它们的抗药性模式并遵循诊断算法,通过第一线(FL)和第二线-线探针测定(SL-LPA)依次测试它们。13124份NAAT阳性样本中共有9722份(74.1%)对利福平敏感。在FL-LPA上,833(8.6%)对异烟肼具有抗性,其中110(13.2%)对SL-LPA的FQ也具有抗性。观察到的最常见的异烟肼抗性突变是615(97.3%)株的katGS315T1突变,174株(86.6%)中的inhAC15T突变和46株(41.8%)中的gyrAD94G突变。异质抗性,推断突变,在所有基因中也观察到突变和独特突变的组合.
    This study was done to determine frequency of isoniazid (INH) and fluoroquinolones FQ resistance among rifampicin sensitive strains of Mycobacterium tuberculosis and to study their mutation patterns. Retrospective analysis was done for samples with M. tuberculosis detected by Cartridge based NAAT (CBNAAT). They were tested sequentially by first line (FL) and second line - line probe assay (SL-LPA) depending on their drug resistance pattern and following diagnostic algorithm. Total 9722 (74.1 %) of 13124 NAAT positive samples were sensitive for rifampicin. On FL-LPA, 833 (8.6 %) were resistant to INH and of which 110 (13.2 %) were also resistant to FQ by SL-LPA. Most common mutations observed for INH resistance were katG S315T1 mutation in 615 (97.3 %) strains, inhA C15T mutation in 174 (86.6 %) strains and for FQ resistance were gyrA D94G mutation in 46 (41.8 %) strains. Heteroresistance, inferred mutations, combination of mutations and unique mutations were also observed in all genes.
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  • 文章类型: Journal Article
    生殖器支原体的抗菌素耐药性在全球范围内正在上升,抗菌药物的选择有限。我们在墨尔本性健康中心评估了西他沙星方案对大环内酯耐药的生殖器的疗效,澳大利亚,2017年1月至2022年2月。在2017年6月之前,患者接受多西环素,然后接受西他沙星;随后,患者接受多西环素,然后联合多西环素+西他沙星.在使用西他沙星方案治疗的229例患者中,80.6%经历了微生物医治。西他沙星治愈了94.2%以前没有莫西沙星失败的感染和69.5%的感染;莫西沙星先前的失败与西他沙星失败的8倍几率相关。当患者通过莫西沙星过去的失败进行分层时,序贯单一疗法和联合疗法之间的治愈没有差异(P>0.05);然而,小数字限制比较。西他沙星耐受性良好,在莫西沙星失败的患者中仍可治愈70%。这些数据突出了将相关的氟喹诺酮抗性标记物纳入测定中以帮助临床决策的益处。
    Antimicrobial resistance in Mycoplasma genitalium is rising globally and antimicrobial options are limited. We evaluated the efficacy of sitafloxacin regimens for macrolide-resistant M genitalium at Melbourne Sexual Health Centre, Australia, between January 2017 and February 2022. Before June 2017, patients received doxycycline followed by sitafloxacin; subsequently, patients received doxycycline followed by combined doxycycline + sitafloxacin. Of 229 patients treated with a sitafloxacin regimen, 80.6% experienced microbial cure. Sitafloxacin cured 94.2% of infections that had not previously failed moxifloxacin and 69.5% of infections that had; prior failure of moxifloxacin was associated with an 8-fold odds of sitafloxacin failure. There was no difference in cure between sequential monotherapy and combination therapy when patients were stratified by past failure of moxifloxacin (P > .05); however, small numbers limited comparisons. Sitafloxacin was well tolerated and still achieved 70% cure in patients in whom moxifloxacin had failed. These data highlight the benefit of incorporating relevant fluoroquinolone resistance markers into assays to assist clinical decision making.
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  • 文章类型: Journal Article
    背景:在南亚,对治疗幽门螺杆菌感染的常用抗生素的耐药性正在增加。尽管如此,缺乏对总体抗生素耐药性的准确估计.因此,本综述旨在分析南亚地区治疗幽门螺杆菌常用抗生素的耐药率。
    方法:系统评价和荟萃分析按照系统评价和荟萃分析报表的首选报告项目进行。从开始到2022年9月,我们搜索了五个医学数据库中的相关研究。使用具有95%置信区间(CI)的随机效应模型来计算抗生素耐药性的汇总患病率。
    结果:本系统综述和荟萃分析包括23篇文章,6357名患者,3294个幽门螺杆菌分离株,和2192个抗生素耐药性样本。对常用抗生素的耐药率是克拉霉素:27%(95CI:0.17-0.38),甲硝唑:69%(95CI:0.62-0.76),四环素:16%(95CI:0.06-0.25),阿莫西林:23%(95CI:0.15-0.30),环丙沙星:12%(95CI:0.04-0.23),左氧氟沙星:34%(95CI:0.22-0.47),和呋喃唑酮:14%(95CI:0.06-0.22)。亚组分析显示,巴基斯坦的抗生素耐药性更为普遍,印度,孟加拉国。此外,一项为期十年的趋势分析显示,克拉霉素的耐药率正在上升(21%至30%),环丙沙星(3%至16%),从2003年到2022年,四环素(5%到20%)。
    结论:这项荟萃分析显示,在南亚国家,幽门螺杆菌常用抗生素的耐药率很高。此外,在过去的20年里,抗生素耐药性一直在增加。为了解决这种情况,强大的监控系统,并严格遵守抗生素管理是必需的。
    BACKGROUND: In South Asia, resistance to commonly used antibiotics for the treatment of Helicobacter pylori infection is increasing. Despite this, accurate estimates of overall antibiotic resistance are missing. Thus, this review aims to analyze the resistance rates of commonly used antibiotics for the treatment of H. pylori in South Asia.
    METHODS: The systematic review and meta-analysis was conducted in accordance with the Preferred Reporting Items for Systematic Reviews and Meta-Analysis statement. We searched five medical databases for relevant studies from inception to September 2022. A random effect model with a 95% confidence interval (CI) was used to calculate the pooled prevalence of antibiotic resistance.
    RESULTS: This systematic review and meta-analysis included 23 articles, 6357 patients, 3294 Helicobacter pylori isolates, and 2192 samples for antibiotic resistance. The prevalences of antibiotic resistance to common antibiotics were clarithromycin: 27% (95%CI: 0.17-0.38), metronidazole: 69% (95%CI: 0.62-0.76), tetracycline: 16% (95%CI: 0.06-0.25), amoxicillin: 23% (95%CI: 0.15-0.30), ciprofloxacin: 12% (95%CI: 0.04-0.23), levofloxacin: 34% (95%CI: 0.22-0.47), and furazolidone: 14% (95%CI: 0.06-0.22). Subgroup analysis showed antibiotic resistances were more prevalent in Pakistan, India, and Bangladesh. Furthermore, a ten-year trend analysis showed the increasing resistance prevalence for clarithromycin (21% to 30%), ciprofloxacin (3% to 16%), and tetracycline (5% to 20%) from 2003 to 2022.
    CONCLUSIONS: This meta-analysis showed a high prevalence of resistance among the commonly used antibiotics for H. pylori in South Asian countries. Furthermore, antibiotic resistance has been increasing over the time of 20 years. In order to tackle this situation, a robust surveillance system, and strict adherence to antibiotic stewardship are required.
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  • 文章类型: Journal Article
    药物共晶,含有至少一种活性药物成分(API),仍然是研究人员关注的领域。两个或多个离散分子通过非共价键结合在一起,例如,氢气,VanderWaals,和π键。这些键足够强以固体形式晶格堆叠分子,从而拥有晶体材料的稳定性,同时,非共价键足够弱,当溶解在水中时解离。因此,共晶将药物作为“准备吸收”中性分子递送。此外,它影响许多物理化学性质,例如,稳定性,可压缩性,等。文献中充斥着讨论药物共晶筛选和评估的出版物。这篇评论指出了我们所知的文献中提到的所有含有抗生素(AB)药物的共晶。专注于它们报告的性质,如溶解度,固有溶出度(IDR),对湿度/光的稳定性,粉末流动性,可压缩性和生物活性,以及它们与亲本AB相比如何得到改善。虽然没有多少出版物暗示在他们的工作中进行抗菌活性研究,对AB共晶如何影响细菌的彻底调查是必不可少的。细菌对已知ABs产生抗性的能力正在增强,让他们不再高效。抗菌抗性应该促使科学家使用共晶修饰功能来克服它。这篇评论强调,对所有研究的AB共晶进行分类和比较。此外,它敦促研究实验室,对共结晶感兴趣,填补未来工作中对抗抗菌素耐药性的空白。
    Pharmaceutical cocrystals, which contain at least one active pharmaceutical ingredient (API), are still an attention-grabbing field for researchers. Two or more discrete molecules unite together by non-covalent bonds, e.g., hydrogen, Van der Waals, and π⋯π bonds. Those bonds are strong enough to stack molecules in solid form lattice, and thus possessing the stability of crystal material, concurrently, non-covalent bonds are weak enough to dissociate when dissolving in water. Therefore, cocrystal delivers drug as a \'ready-to-be absorbed\' neutral molecule. Besides, it affects many physicochemical properties, e.g., stability, compressibility, etc. The literature is full of publications that discuss pharmaceutical cocrystals screening and evaluation. This review spots the light on all cocrystals that contain antibiotic (AB) drugs which mentioned in the literature to our knowledge. Focusing on their reported properties like solubility, intrinsic dissolution rate (IDR), stability against humidity/light, powder flowability, compressibility and bioactivity and how they get improved compared to parent AB. Although not many publications imply antimicrobial activity studies in their work, a thorough investigation of how AB cocrystal is affecting bacteria is a persisted necessity. Bacterial ability to develop resistance to known ABs is increasing, making them no longer-efficient. Antibacterial resistance should provoke scientists to use cocrystal modification features to overcome it. This review highlights, classifies and compares all studied AB cocrystals. In addition, it urges research labs, which are interested in cocrystallization, to fill the gap of confronting antimicrobial resistance in their future work.
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  • 文章类型: Journal Article
    OBJECTIVE: Ciprofloxacin (CIPRO) is a fluroquinolone class antibiotic used commonly for the treatment of various acute and chronic bacterial infections. However, recently there is increase in the case reports of CIPRO-induced Cutaneous Adverse Drug Reactions (CADRs). We aim to systematically review all the descriptive studies of CIPRO induced CADRs.
    METHODS: Medline (via PubMed) was searched without any language or date restriction from inception to March 2019 using search terms of \"Ciprofloxacin\" and \"Cutaneous reactions.\" We included only the descriptive studies, which elucidate the CADRs experienced by the patients following the administration of CIPRO. Two reviewers involved in study selection, data extraction and quality assessment of the included studies. Discrepancies were resolved by consensus between the reviewers.
    RESULTS: Thirty-nine studies (out of 446) were found to be eligible for the final inclusion. The dose of CIPRO among the included studies was ranging from 500 to 1,000 mg/day and duration of treatment was between 7 and 10 days. The most common CADRs observed were toxic epidermal necrolysis, Stevens-Johnson syndrome, fixed drug eruptions, bullous fixed drug reaction, acute generalized pustulosis, erythema multiforme, drug rash with eosinophilia and systemic symptoms and erythema nodosum.
    CONCLUSIONS: Management of the CIPRO-induced CADRs is recommended with the complete cessation of the CIPRO, followed by supportive management with oral or topical glucocorticoids, emollients, and topical moisturizers. CIPRO is likely to cause CADRs, physicians should be vigilant while prescribing it to the patients.
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  • 文章类型: Journal Article
    The effects of a fluroquinolone levofloxacin on apoptosis of peripheral blood lymphocytes from patients with infiltrative pulmonary tuberculosis were studied in vitro. It was found that levofloxacin stimulated apoptotic cell death in tuberculosis. Addition of levofloxacin to cell suspension from patients with drug-susceptible form of tuberculosis led to an increase in the number of CD95+ and AnnV+ lymphocytes. In patients with drug-resistant form of tuberculosis, only the number of apoptotic lymphocytes, but not the count of CD95+ cells increased under these conditions.
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  • 文章类型: Journal Article
    目的:报告3例穿透性角膜移植术后局部给药后氟喹诺酮在角膜中沉积。病例报告:在此,我们报告了三名年龄在42-65岁之间的患者,他们接受了白内障摘除的角膜移植术。前两例为人工晶状体植入术,第三例为后囊撕裂导致左无晶状体。前两名患者接受环丙沙星-地塞米松联合滴剂,并开发了药物沉积,分别在7天和10天后的第一次随访中观察到。第三名患者术后接受醋酸泼尼松龙和氧氟沙星滴眼液,20天后角膜出现药物沉积。在所有三个病人中,在接下来的3-4周内,停用氟喹诺酮类药物,并逐渐清除角膜.虽然角膜清除了,前两个移植失败,由于反复的病毒感染,在一个案例中,另一种情况下的移植排斥反应。结论:多种手术后,不同类型的氟喹诺酮类药物在角膜中沉积,包括穿透性角膜移植术.穿透性角膜移植术后的药物沉积似乎是无害的,因为在停止药物时可以自我解决,但它可能会对移植物存活产生有害影响。因此,氟喹诺酮类药物,尤其是环丙沙星,如果经常给药或与其他含有防腐剂的局部药物同时使用,则应谨慎用于接受穿透性角膜移植术的患者。
    Purpose: To report three cases of fluroquinolone deposition in the cornea after topical administration post-penetrating keratoplasty. Case reports: Herein we report three patients ranging in age from 42-65 years who underwent keratoplasty with cataract extraction, with intraocular lens implantation in the first two cases and left aphakic due to a posterior capsular tear in the third case. The first two patients received ciprofloxacin-dexamethasone combination drops, and developed drug deposition, which was observed at the first follow-up after 7 and 10 days respectively. The third patient received prednisolone acetate and ofloxacin eyedrops postoperatively, and developed drug deposits in the cornea after 20 days. In all of the three patients, the fluroquinolone group of drugs was discontinued and the cornea cleared gradually over the next 3-4 weeks. Although the cornea cleared, the first two grafts failed due to recurrent viral infection in one case, and graft rejection in the other case. Conclusion: Deposition of many different fluroquinolones in the cornea has been reported after a variety of surgeries, including penetrating keratoplasty. Drug deposition post-penetrating keratoplasty may seem innocuous due to self-resolution on cessation of the drugs, but it may have deleterious effects on graft survival. Hence, fluroquinolones, especially ciprofloxacin, should be cautiously used in patients undergoing penetrating keratoplasty if frequent dosing is prescribed or if used concurrently with other topical medications containing preservatives.
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  • 文章类型: Journal Article
    Buruli ulcer (Mycobacterium ulcerans infection) is a neglected tropical disease of skin and subcutaneous tissue that can result in long-term cosmetic and functional disability. It is a geographically restricted infection but transmission has been reported in endemic areas in more than 30 countries worldwide. The heaviest burden of disease lies in West and Sub-Saharan Africa where it affects children and adults in subsistence agricultural communities. Mycobacterium ulcerans infection is probably acquired via inoculation of the skin either directly from the environment or indirectly via insect bites. The environmental reservoir and exact route of transmission are not completely understood. It may be that the mode of acquisition varies in different parts of the world. Because of this uncertainty it has been nicknamed the \'mysterious disease\'. The therapeutic approach has evolved in the past decade from aggressive surgical resection alone, to a greater focus on antibiotic therapy combined with adjunctive surgery.
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  • 文章类型: Journal Article
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