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三唑类抗真菌新药泊沙康唑和伏立康唑简介
引用本文:刘洁,胡小平,刘伟.三唑类抗真菌新药泊沙康唑和伏立康唑简介[J].菌物学报,2018,37(10):1391-1398.
作者姓名:刘洁  胡小平  刘伟
作者单位:1 北京大学第一医院皮肤性病科 北京大学真菌和真菌病研究中心 皮肤病分子诊断北京市重点实验室 北京 1000342 北京大学深圳医院皮肤性病科 广东 深圳 518036
基金项目:国家自然科学基金(81471925,81671990)
摘    要:随着侵袭性真菌感染的发病率和死亡率逐年增多,新近问世的新型抗真菌药物也越来越多。新一代广谱三唑类抗真菌药物泊沙康唑和伏立康唑,在体内和体外均有较强的抗真菌活性,临床上用其来预防和治疗侵袭性真菌感染。两药具有共有的作用机制,在抗真菌活性、药物代谢及安全性方面有着各自特点。分子结构上泊沙康唑和伏立康唑优于原有药物伊曲康唑和氟康唑,从而具备更强、更广的抗菌谱。两药的研发和应用表明抗真菌药物研究正朝着高效、广谱、低毒的方向发展,成为治疗各种类型真菌感染新的有力手段。然而,两药在临床研究和血药浓度监测方面仍待深入探究。本文将从分子结构、作用机制、适应症和药代动力学方面介绍两药,并对两药在未来的临床应用进行展望,为临床应用提供帮助。

关 键 词:真菌感染  分子结构  适应症  药代动力学  
收稿时间:2018-05-14

Introduction of the new triazole antifungal drug posaconazole and voriconazole
Authors:Jie LIU  Xiao-Ping HU  Wei LIU
Institution:1 Department of Dermatology & Venereology, Peking University First Hospital; Research Center for Medical Mycology; Beijing Key Laboratory of Molecular Diagnosis on Dermatoses, Peking University, Beijing 100034, China;2 Department of Dermatology & Venereology, Peking University Shenzhen Hospital, Shenzhen, Guangdong 518036, China;
Abstract:The morbidity and mortality of invasive fungal infection is increasing year by year, and more and more new antifungal drugs are produced to the public. Posaconazole and voriconazole, having strong antifungal activity in vivo and vitro, are new spectral triazole drugs for the treatment and prevention of invasive fungal infections. They have the same mechanism of action and each owns characteristics in antifungal activity, drug metabolism and safety. Posaconazole and voriconazole are superior to the originally practical drugs itraconazole and fluconazole in molecular structure, having stronger and wider antifungal spectrum. The development and application of the two new drugs suggest that the research on antifungal drugs trends towards the obtainment of high efficiency, broad spectrum and low toxicity. The clinical research and blood concentration monitoring of the two drugs are still to be further explored. This paper reviews their molecular structures, action mechanism, clinical indications and pharmacokinetics. The future clinical application perspective of the two drugs is predicted.
Keywords:fungal infection  molecular structures  indications  pharmacokinetics  
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