神經氨酸酶抑制劑

本頁使用了標題或全文手工轉換
維基百科,自由的百科全書

神經氨酸酶抑制劑(neuraminidase inhibitors,NAIs)是一類抑制神經氨酸酶活性的抗病毒藥物。其透過阻斷流感病毒的神經氨酸酶,從而阻止病毒出芽,進而抑制病毒繁殖。神經氨酸酶抑制劑包括奧司他韋(達菲)(一種前藥)、扎那米韋(樂感清)、拉尼米韋(Inavir)、帕拉米韋及一系列正在研發中的新藥。與僅對甲型流感起作用的M2離子通道蛋白抑制劑不同,神經氨酸酶抑制劑對甲型流感乙型流感均有效 [1] [2] [3][4]

神經氨酸酶抑制劑奧司他韋和扎那米韋在美國和歐洲被批准用於治療和預防流感。帕拉米韋透過結合併抑制流感病毒的神經氨酸酶活化而產生藥理活性,其作用時間比奧司他韋和扎那米韋都要長。 [5]拉尼米韋從細胞中緩慢釋放進入呼吸道,其抗流感病毒作用同樣持久,但其維持持久作用的機理不同於帕拉米韋[6]

近年來,神經氨酸酶抑制劑的療效備受爭議[7][8][9]。然而,在2009年H1N1流感大流行之後,許多國家和地區都宣稱流感早期使用神經氨酸酶抑制劑治療可有效減少嚴重病例和死亡率[10][11][12][13]

統計報告顯示,全國/地區範圍內使用神經氨酸酶抑制劑治療流感樣疾病的國家和地區中,有症狀感染者的死亡率很低,這是因為這些國家普遍在流感患者感染早期便使用神經氨酸酶抑制劑[14]。儘管這些國家和地區廣泛使用奧司他韋,但尚未出現對奧司他韋具有耐藥性的流感病毒引起的爆發,也沒有出現對奧司他韋具有耐藥性的流感病毒引起的嚴重疾病的報道[14]美國疾病控制中心仍然建議併發症相關高危人群,老年人以及首次出現流感相關症狀後48小時內的低危人群使用奧司他韋治療流感[15]

神經氨酸酶抑制劑常見的副作用為噁心和嘔吐。已有報道稱兒童服用奧司他韋後可出現行為異常,如譫妄幻覺,這可能是流感相關症狀的延伸[14]。這些副作用一般發生於流感早期,即流感病發後48小時內。因此,專家建議,無論患兒是否接受神經氨酸酶抑制劑治療,父母都應密切監視流感病發後48小時內的患兒體徵[14]

常見神經氨酸酶抑制劑[編輯]

臨床使用的神經氨酸酶抑制劑結構[編輯]

Viral neuraminidase inhibitors in use
扎那米韋 奧司他韋 帕拉米韋 拉尼米韋

天然產物中的神經氨酸酶抑制劑[編輯]

參考文獻[編輯]

  1. ^ Smith, B. J.; McKimm-Breshkin, J. L.; McDonald, M.; Fernley, R. T.; Varghese, J. N.; Colman, P. M. Structural Studies of the Resistance of Influenza Virus Neuramindase to Inhibitors. Journal of Medicinal Chemistry. 2002, 45 (11): 2207–12. PMID 12014958. doi:10.1021/jm010528u. 
  2. ^ Gubareva, Larisa V. Molecular mechanisms of influenza virus resistance to neuraminidase inhibitors. Virus Research. 2004, 103 (1–2): 199–203. PMID 15163510. doi:10.1016/j.virusres.2004.02.034. 
  3. ^ This flash animation shows the mode of action of oseltamivir (Tamiflu) 網際網路檔案館存檔,存檔日期2005-10-23.. pharmasquare.org
  4. ^ Replication of influenza virus頁面存檔備份,存於網際網路檔案館). mvm.ed.ac.uk
  5. ^ Bantia, Shanta; Arnold, C. Shane; Parker, Cynthia D.; Upshaw, Ramanda; Chand, Pooran. Anti-influenza virus activity of peramivir in mice with single intramuscular injection. Antiviral Research. 1 January 2006, 69 (1): 39–45. ISSN 0166-3542. PMID 16325932. doi:10.1016/j.antiviral.2005.10.002. 
  6. ^ Ishizuka, Hitoshi; Yoshiba, Satoshi; Okabe, Hiromi; Yoshihara, Kazutaka. Clinical pharmacokinetics of laninamivir, a novel long-acting neuraminidase inhibitor, after single and multiple inhaled doses of its prodrug, CS-8958, in healthy male volunteers. Journal of Clinical Pharmacology. 1 November 2010, 50 (11): 1319–1329. ISSN 1552-4604. PMID 20145259. doi:10.1177/0091270009356297. 
  7. ^ Jefferson, Tom; Jones, Mark; Doshi, Peter; Spencer, Elizabeth A.; Onakpoya, Igho; Heneghan, Carl J. Oseltamivir for influenza in adults and children: systematic review of clinical study reports and summary of regulatory comments. BMJ. 9 April 2014, 348: g2545 [2021-01-15]. ISSN 1756-1833. PMC 3981975可免費查閱. PMID 24811411. doi:10.1136/bmj.g2545. (原始內容存檔於2019-10-31). 
  8. ^ Hsu, Jonathan; Santesso, Nancy; Mustafa, Reem; Brozek, Jan; Chen, Yao Long; Hopkins, Jessica P.; Cheung, Adrienne; Hovhannisyan, Gayane; Ivanova, Liudmila; Flottorp, Signe A.; Saeterdal, Ingvil; Wong, Arthur D.; Tian, Jinhui; Uyeki, Timothy M.; Akl, Elie A.; Alonso-Coello, Pablo; Smaill, Fiona; Schünemann, Holger J. Antivirals for treatment of influenza: a systematic review and meta-analysis of observational studies. Annals of Internal Medicine. 3 April 2012, 156 (7): 512–524. ISSN 1539-3704. PMC 6679687可免費查閱. PMID 22371849. doi:10.7326/0003-4819-156-7-201204030-00411. 
  9. ^ Heneghan, Carl J.; Onakpoya, Igho; Thompson, Matthew; Spencer, Elizabeth A.; Jones, Mark; Jefferson, Tom. Zanamivir for influenza in adults and children: systematic review of clinical study reports and summary of regulatory comments. BMJ. 9 April 2014, 348: g2547 [2021-01-15]. ISSN 1756-1833. PMC 3981976可免費查閱. PMID 24811412. doi:10.1136/bmj.g2547. (原始內容存檔於2021-03-23). 
  10. ^ Louie, Janice K.; Acosta, Meileen; Jamieson, Denise J.; Honein, Margaret A. Severe 2009 H1N1 Influenza in Pregnant and Postpartum Women in California. New England Journal of Medicine. 2010, 362 (1): 27–35. PMID 20032319. doi:10.1056/nejmoa0910444. 
  11. ^ Jain, Seema; Kamimoto, Laurie; Bramley, Anna M.; Schmitz, Ann M.; Benoit, Stephen R.; Louie, Janice; Sugerman, David E.; Druckenmiller, Jean K.; Ritger, Kathleen A.; Chugh, Rashmi; Jasuja, Supriya; Deutscher, Meredith; Chen, Sanny; Walker, John D.; Duchin, Jeffrey S.; Lett, Susan; Soliva, Susan; Wells, Eden V.; Swerdlow, David; Uyeki, Timothy M.; Fiore, Anthony E.; Olsen, Sonja J.; Fry, Alicia M.; Bridges, Carolyn B.; Finelli, Lyn. Hospitalized Patients with 2009 H1N1 Influenza in the United States, April–June 2009. New England Journal of Medicine. 12 November 2009, 361 (20): 1935–1944. CiteSeerX 10.1.1.183.7888可免費查閱. ISSN 0028-4793. PMID 19815859. doi:10.1056/NEJMoa0906695. 
  12. ^ Domínguez-Cherit, Guillermo; Lapinsky, Stephen E.; Macias, Alejandro E.; Pinto, Ruxandra; Espinosa-Perez, Lourdes; de la Torre, Alethse; Poblano-Morales, Manuel; Baltazar-Torres, Jose A.; Bautista, Edgar; Martinez, Abril; Martinez, Marco A.; Rivero, Eduardo; Valdez, Rafael; Ruiz-Palacios, Guillermo; Hernández, Martín; Stewart, Thomas E.; Fowler, Robert A. Critically Ill patients with 2009 influenza A(H1N1) in Mexico. JAMA. 4 November 2009, 302 (17): 1880–1887. ISSN 1538-3598. PMID 19822626. doi:10.1001/jama.2009.1536可免費查閱. 
  13. ^ Zarychanski, R.; Stuart, T. L.; Kumar, A.; Doucette, S.; Elliott, L.; Kettner, J.; Plummer, F. Correlates of severe disease in patients with 2009 pandemic influenza (H1N1) virus infection. Canadian Medical Association Journal. 2010, 182 (3): 257–264. ISSN 0820-3946. PMC 2826467可免費查閱. PMID 20093297. doi:10.1503/cmaj.091884. 
  14. ^ 14.0 14.1 14.2 14.3 Sugaya, Norio. Widespread use of neuraminidase inhibitors in Japan. Journal of Infection and Chemotherapy. 1 October 2011, 17 (5): 595–601. ISSN 1437-7780. PMID 21850418. doi:10.1007/s10156-011-0288-0. 
  15. ^ CDC Online Newsroom - "Have You Heard?" Archive: 2014 - Influenza A Variant Virus. cdc.gov. [2021-01-15]. (原始內容存檔於2017-01-18). 
  16. ^ Swaminathan K, Dyason JC, Maggioni A, von Itzstein M, Downard KM. Binding of a natural anthocyanin inhibitor to influenza neuraminidase by mass spectrometry. Anal Bioanal Chem. 2013, 405 (20): 6563–72. PMID 23748498. doi:10.1007/s00216-013-7068-x. 
  17. ^ Kim, Jang Hoon; Ryu, Young Bae; Lee, Woo Song; Kim, Young Ho. Neuraminidase inhibitory activities of quaternary isoquinoline alkaloids from Corydalis turtschaninovii rhizome. Bioorganic & Medicinal Chemistry. 2014-11-01, 22 (21): 6047–6052. ISSN 1464-3391. PMID 25277281. doi:10.1016/j.bmc.2014.09.004可免費查閱.