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作 者:秦静[1] 苗凤荣 QIN Jing;MIAO Fengrong(Department of Pharmacy,People's Hospital of Rizhao,Rizhao,Shandong 276800,China)
出 处:《医药前沿》2025年第6期21-24,共4页Journal of Frontiers of Medicine
摘 要:本文综述阿奇霉素的药理作用机制、耐药机制、临床应用、不良反应及合成工艺等方面的研究进展。阿奇霉素作为大环内酯类抗生素,其抗菌机制主要通过结合细菌核糖体50S亚基,抑制蛋白质合成。然而,细菌耐药性问题日益突出,主要耐药机制包括核糖体甲基化修饰、外排泵机制及核糖体突变等。其中,核糖体甲基化和外排泵机制最为常见。在临床应用方面,阿奇霉素广泛用于治疗呼吸道感染、泌尿生殖系统感染、皮肤软组织感染等多种细菌感染性疾病。其不良反应总体较轻,以胃肠道反应和过敏反应最为常见。但需注意其可能引起的严重心律失常风险,尤其是在某些高危人群中。在合成工艺方面,目前工业化生产主要采用化学合成法,但基因工程菌发酵法因其高效、环保的特点,成为未来发展的主要方向。研究者正在通过代谢工程、优化发酵条件等手段,提高阿奇霉素的产量和纯度。尽管阿奇霉素在临床应用中表现出良好的安全性和有效性,但细菌耐药性问题不容忽视。未来需要加强基础研究,深入阐明其作用机制,优化给药方案,开发新的制剂,以延缓耐药性的产生,维持其临床疗效。This article reviews the research progress of pharmacological mechanism,drug resistance mechanism,clinical application,adverse reactions and synthesis process of Azithromycin.As a macrolide antibiotic,Azithromycin exerts its antibacterial effect primarily by binding to the 50S ribosomal subunit of bacteria,thereby inhibiting protein synthesis.However,the issue of bacterial resistance is becoming increasingly prominent,with major resistance mechanisms including ribosomal methylation modification,efflux pump mechanisms,and ribosomal mutations.Among these,ribosomal methylation and efflux pump mechanisms are the most common.In terms of clinical applications,Azithromycin is widely used to treat various bacterial infections,such as respiratory tract infections,urogenital infections,and skin and soft tissue infections.Its adverse reactions are generally mild,with gastrointestinal reactions and allergic reactions being the most common.However,attention should be paid to the potential risk of severe arrhythmias,especially in certain high-risk populations.Regarding synthesis processes,the current industrial production mainly relies on chemical synthesis methods.However,genetically engineered microbial fermentation,due to its efficiency and environmental friendliness,represents the future direction of development.Researchers are working to improve the yield and purity of Azithromycin through metabolic engineering and optimization of fermentation conditions.Despite its good safety and efficacy in clinical applications,the problem of bacterial resistance cannot be ignored.Future efforts should focus on strengthening basic research,elucidating its mechanisms of action,optimizing dosing regimens,and developing new formulations to delay the emergence of resistance and maintain its clinical effectiveness.
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