呼吸
词汇介绍
拓展阅读
解析
oseltamivir /'ozltəmɪvɚ/
释 义 n. 奥司他韦
例 句 All other viruses have been shown sensitive to both oseltamivir and zanamivir.所有其它病毒显示对奥司他韦和扎那米韦都是敏感的。
phosphate /'fɑsfet/
释 义 n. 磷酸盐
同根词 phosphatase n. [生化] 磷酸酶
phosphocreatine n. [生化] 磷酸肌酸(等于phosphocreatin)
例 句 Each consists of a nucleoside and one or more phosphate groups. 每个核酸都由一个核和一个或多个磷酸盐基团组成。
概述
基本信息
药物达菲(磷酸奥司他韦胶囊)主要成份为磷酸奥司他韦。化学式:(3R,4R,5S)-4-乙酰氨基-5-氨基-3(1-乙丙氧基)-1-环乙烯-1羧酸乙酯磷酸盐。分子式:C16H28N2O4·H3PO4。分子量:410.40。
作用机制
磷酸奥司他韦是奥司他韦活性代谢产物的药物前体,奥司他韦的活性代谢产物是强效的选择性流感病毒神经氨酸酶抑制剂。病毒神经氨酸酶活性对新形成的病毒颗粒从被感染细胞的释放和感染性病毒在人体内进一步传播是关键的。奥司他韦的活性代谢产物抑制A型和B型流感病毒的神经氨酸酶。通过抑制病毒从被感染的细胞中释放,从而减少甲型或乙型流感病毒的复制和致病性。
适应症
用于成人和1岁及1岁以上儿童的甲型和乙型流感治疗,并且可以大大减少并发症(主要是气管与支气管炎、肺炎、咽炎等)的发生和抗生素的使用,因而是目前治疗流感的最常用药物之一,也是公认的抗禽流感、甲型H1N1病毒最有效的药物之一。患者应在首次出现症状48小时内使用。也可用于成人和13岁及13岁以上青少年的甲型和乙型流感的预防。
禁忌症
对磷酸奥司他韦过敏或药物的任何成分过敏者禁用。
不良反应
最常见的不良反应是恶心和呕吐,呈一过性,常在首次服药时发生,其他不良反应还有腹泻、头晕、疲劳、鼻塞、咽痛和咳嗽,绝大多数不良反应可以耐受。
注意事项
1.尚无证据显示磷酸奥司他韦对甲型和乙型流感以外的其他疾病有效。
2.磷酸奥司他韦对1岁以下儿童治疗流感的安全性和有效性尚未确定。
3.磷酸奥司他韦对13岁以下儿童预防流感的安全性和有效性尚未确定。
4.在免疫抑制的患者中奥司他韦治疗和预防流感的安全性和有效性尚未确定。
5.磷酸奥司他韦不能取代流感疫苗。
6.肾功能不全患者用药参阅特殊人群用药指导。
An Influenza Virus Entry Inhibitor Targets Class II PI3 Kinase and Synergizes with Oseltamivir.复制标题
一种流感病毒进入抑制剂靶向II类PI3激酶并与奥司他韦协同作用。
发表时间:2019-09-09
影响指数:4.9
作者: O'Hanlon R
期刊:ACS Infect Dis
Two classes of antivirals targeting the viral neuraminidase (NA) and endonuclease are currently the only clinically useful drugs for the treatment of influenza. However, resistance to both antivirals has been observed in clinical isolates, and there was widespread resistance to oseltamivir (an NA inhibitor) among H1N1 viruses prior to 2009. This potential for resistance and lack of diversity for antiviral targets highlights the need for new influenza antivirals with a higher barrier to resistance. In this study, we identified an antiviral compound, M85, that targets host kinases, epidermal growth factor receptor (EGFR), and phosphoinositide 3 class II β (PIK3C2β) and is not susceptible to resistance by viral mutations. M85 blocks endocytosis of influenza viruses and inhibits a broad-spectrum of viruses with minimal cytotoxicity. In vitro, we found that combinations of M85 and oseltamivir have strong synergism. In the mouse model for influenza, treatment with the combination therapy was more protective against a lethal viral challenge than oseltamivir alone, indicating that development of M85 could lead to combination therapies for influenza. Finally, through this discovery of M85 and its antiviral mechanism, we present the first description of PIK3C2β as a necessary host factor for influenza virus entry.
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