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贝达喹啉:在耐多药肺结核中的临床应用。

Bedaquiline: An Insight Into its Clinical Use in Multidrug-Resistant Pulmonary Tuberculosis.

机构信息

Department of Pharmacy, Integral University, Lucknow, India.

出版信息

Drug Res (Stuttg). 2024 Jul;74(6):269-279. doi: 10.1055/a-2331-7061. Epub 2024 Jul 5.

Abstract

Every year, the World Health Organization reports 500,000 new cases of drug-resistant tuberculosis (TB), which poses a serious global danger. The increased number of XDR-TB and MDR-TB cases reported worldwide necessitates the use of new therapeutic approaches. The main issues with the antitubercular medications now in use for the treatment of multidrug-resistant tuberculosis are their poor side effect profile, reduced efficacy, and antimicrobial resistance. One possible remedy for these problems is bedaquiline. The need for better treatment strategies is highlighted by the strong minimum inhibitory concentrations that bedaquiline (BDQ), a novel anti-TB medicine, exhibits against both drug-resistant and drug-susceptible TB. Bedaquiline may be able to help with these problems. Bedaquiline is a medication that is first in its class and has a distinct and particular mode of action. Bedaquiline is an ATP synthase inhibitor that is specifically directed against Mycobacterium tuberculosis and some nontuberculous mycobacteria. It is metabolized by CYP3A4. Bedaquiline preclinical investigations revealed intralesional drug biodistribution. The precise intralesional and multi-compartment pharmacokinetics of bedaquiline were obtained using PET bioimaging and high-resolution autoradiography investigations. Reduced CFU counts were observed in another investigation after a 12-week course of therapy. Meta-analyses and systematic reviews of phase II trials on bedaquiline's efficacy in treating drug-resistant tuberculosis in patients reported higher rates of cure, better culture conversion, and lower death rates when taken in conjunction with a background regimen. Here is a thorough medication profile for bedaquiline to aid medical professionals in treating individuals with tuberculosis.

摘要

每年,世界卫生组织报告有 50 万例新的耐多药结核病(TB)病例,这对全球构成了严重威胁。全球报告的 XDR-TB 和 MDR-TB 病例增加,需要采用新的治疗方法。目前用于治疗耐多药结核病的抗结核药物主要存在副作用大、疗效降低和抗菌药物耐药等问题。而对这些问题的一种可能的补救方法是使用贝达喹啉。新型抗结核药物贝达喹啉(BDQ)对耐药和敏感结核均具有较强的最低抑菌浓度,凸显了对更好的治疗策略的需求。贝达喹啉可能有助于解决这些问题。贝达喹啉是一种首创的抗结核药物,具有独特而特殊的作用方式。贝达喹啉是一种针对结核分枝杆菌和一些非结核分枝杆菌的 ATP 合酶抑制剂。它由 CYP3A4 代谢。贝达喹啉的临床前研究揭示了病灶内药物的药物分布。使用 PET 生物成像和高分辨率放射自显影研究获得了贝达喹啉的精确病灶内和多腔室药代动力学。在另一项研究中,在为期 12 周的治疗后,观察到 CFU 计数减少。对贝达喹啉治疗耐多药结核病的 II 期临床试验的荟萃分析和系统评价报告称,与背景方案联合使用时,治愈率更高,培养转化率更好,死亡率更低。这里有一个关于贝达喹啉的全面药物概况,以帮助医疗专业人员治疗结核病患者。

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