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扎那米韦:从药物设计到临床应用

Zanamivir: from drug design to the clinic.

作者信息

Elliott M

机构信息

GlaxoSmithKline, Research Triangle Park, NC 27709, USA.

出版信息

Philos Trans R Soc Lond B Biol Sci. 2001 Dec 29;356(1416):1885-93. doi: 10.1098/rstb.2001.1021.

DOI:10.1098/rstb.2001.1021
PMID:11779388
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1088565/
Abstract

The development of the neuraminidase inhibitors has revolutionized the management options for influenza. Zanamivir was the first such inhibitor to be approved for the treatment of influenza in humans. It is delivered by inhalation to the respiratory tract, which is the site of viral replication, in order to ensure immediate antiviral activity. Early treatment with zanamivir in clinical trials rapidly reduced the severity and duration of influenza symptoms and associated complications. Furthermore, chemoprophylaxis with zanamivir was shown to be effective in the prevention of influenza illness. To date, there is no evidence for the emergence of clinically significant zanamivir-resistant isolates. In conclusion, zanamivir offers a useful complementary strategy to vaccination in the effective management of influenza.

摘要

神经氨酸酶抑制剂的研发彻底改变了流感的治疗选择。扎那米韦是首个被批准用于人类流感治疗的此类抑制剂。它通过吸入方式送达呼吸道,而呼吸道是病毒复制的场所,以确保能立即产生抗病毒活性。在临床试验中,早期使用扎那米韦治疗可迅速减轻流感症状的严重程度并缩短其持续时间,以及减少相关并发症。此外,扎那米韦的化学预防在预防流感疾病方面被证明是有效的。迄今为止,尚无出现具有临床意义的扎那米韦耐药菌株的证据。总之,在流感的有效管理中,扎那米韦为疫苗接种提供了一种有用的补充策略。

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Zanamivir: from drug design to the clinic.扎那米韦:从药物设计到临床应用
Philos Trans R Soc Lond B Biol Sci. 2001 Dec 29;356(1416):1885-93. doi: 10.1098/rstb.2001.1021.
2
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本文引用的文献

1
Zanamivir for the treatment of influenza A and B infection in high-risk patients: a pooled analysis of randomized controlled trials.扎那米韦治疗高危患者甲型和乙型流感感染:随机对照试验的汇总分析
Arch Intern Med. 2001 Jan 22;161(2):212-7. doi: 10.1001/archinte.161.2.212.
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Inhaled zanamivir for the prevention of influenza in families. Zanamivir Family Study Group.吸入扎那米韦预防家庭内流感。扎那米韦家庭研究小组。
N Engl J Med. 2000 Nov 2;343(18):1282-9. doi: 10.1056/NEJM200011023431801.
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Resistance of influenza viruses to neuraminidase inhibitors--a review.流感病毒对神经氨酸酶抑制剂的耐药性——综述
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Randomized, placebo-controlled studies of inhaled zanamivir in the treatment of influenza A and B: pooled efficacy analysis.吸入扎那米韦治疗甲型和乙型流感的随机、安慰剂对照研究:汇总疗效分析
J Antimicrob Chemother. 1999 Nov;44 Suppl B:23-9. doi: 10.1093/jac/44.suppl_2.23.
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Direct measurement of the anti-influenza agent zanamivir in the respiratory tract following inhalation.吸入后呼吸道中抗流感药物扎那米韦的直接测量。
Antimicrob Agents Chemother. 2000 Jul;44(7):1974-6. doi: 10.1128/AAC.44.7.1974-1976.2000.
6
Zanamivir for treatment of symptomatic influenza A and B infection in children five to twelve years of age: a randomized controlled trial.扎那米韦治疗5至12岁儿童甲型和乙型流感病毒感染的症状:一项随机对照试验。
Pediatr Infect Dis J. 2000 May;19(5):410-7. doi: 10.1097/00006454-200005000-00005.
7
Clinical efficacy and safety of the orally inhaled neuraminidase inhibitor zanamivir in the treatment of influenza: a randomized, double-blind, placebo-controlled European study.口服吸入型神经氨酸酶抑制剂扎那米韦治疗流感的临床疗效与安全性:一项随机、双盲、安慰剂对照的欧洲研究。
J Infect. 2000 Jan;40(1):42-8. doi: 10.1053/jinf.1999.0602.
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Pulmonary function and airway responsiveness in mild to moderate asthmatics given repeated inhaled doses of zanamivir.给予多次吸入扎那米韦剂量的轻至中度哮喘患者的肺功能和气道反应性
Respir Med. 2000 Feb;94(2):166-73. doi: 10.1053/rmed.1999.0718.
9
Safety and efficacy of the neuraminidase inhibitor zanamivir in treating influenza virus infection in adults: results from Japan. GG167 Group.神经氨酸酶抑制剂扎那米韦治疗成人流感病毒感染的安全性和有效性:来自日本的结果。GG167 研究组。
Antivir Ther. 1999;4(2):61-8.
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Zanamivir: a review of clinical safety.扎那米韦:临床安全性综述
Drug Saf. 1999 Oct;21(4):267-81. doi: 10.2165/00002018-199921040-00003.