Influenza virus neuraminidase inhibitors
Influenza virus neuraminidase inhibitors
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DOI：
10.1016/s0140-6736(99)11433-8
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发表时间：
2000-03-04
期刊：
影响因子：
168.9
通讯作者：
Hayden, FG
中科院分区：
文献类型：
--
作者：
Gubareva, LV;Kaiser, L;Hayden, FG
神经氨酸酶促进流感病毒从受感染的细胞中释放，并促进病毒在呼吸道内传播。已经开发出该酶的几种有效且特异性的抑制剂，其中两种（扎那米韦和奥司他韦）已被批准用于人类。与针对甲型流感病毒 M2 蛋白的金刚烷胺和金刚乙胺不同，这些药物可抑制甲型和乙型流感病毒的复制。扎那米韦由于口服生物利用度低而通过吸入给药，而奥司他韦则通过口服给药。早期使用任何一种药物治疗都可以减少流感症状和相关并发症的严重程度和持续时间。两种药物对于化学预防均有效。由于与 M2 抑制剂相比，神经氨酸酶抑制剂具有更广泛的抗病毒谱、更好的耐受性以及更少出现耐药性的可能性，因此神经氨酸酶抑制剂代表了流感治疗的重要进展。
Neuraminidase promotes influenza virus release from infected cells and facilitates virus spread within the respiratory tract. Several potent and specific inhibitors of this enzyme have been developed, and two (zanamivir and oseltamivir) have been approved for human use. Unlike amantadine and rimantadine that target the M2 protein of influenza A viruses, these drugs inhibit replication of both influenza A and B viruses. Zanamivir is delivered by inhalation because of its low oral bioavailability whereas oseltamivir is administered by mouth. Early treatment with either drug reduces the severity and duration of influenza symptoms and associated complications. Both agents are effective for chemoprophylaxis. Because of a broader antiviral spectrum, better tolerance, and less potential for emergence of resistance than is seen with the M2 inhibitors, the neuraminidase inhibitors represent an important advance in the treatment of influenza.