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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/10/26 17:02:32」(JST)
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Peramivir
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Systematic (IUPAC) name |
(1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4- (diaminomethylideneamino)-2-hydroxy-cyclopentane- 1-carboxylic acid |
Clinical data |
Pregnancy cat. |
? |
Legal status |
? |
Pharmacokinetic data |
Bioavailability |
100% (IV) |
Half-life |
7.7 to 20.8 hour in patients with normal renal function |
Excretion |
renal |
Identifiers |
CAS number |
229614-55-5 N |
ATC code |
None |
PubChem |
CID 151164 |
ChemSpider |
133234 Y |
UNII |
9ZS94HQO3B N |
ChEMBL |
CHEMBL332608 Y |
Chemical data |
Formula |
C15H28N4O4 |
Mol. mass |
328.40722 g/mol |
SMILES
- O=C(O)[C@H]1C[C@@H](/N=C(\N)N)[C@H](C(NC(=O)C)C(CC)CC)[C@@H]1O
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InChI
-
InChI=1S/C15H28N4O4/c1-4-8(5-2)12(18-7(3)20)11-10(19-15(16)17)6-9(13(11)21)14(22)23/h8-13,21H,4-6H2,1-3H3,(H,18,20)(H,22,23)(H4,16,17,19)/t9-,10+,11+,12?,13+/m0/s1 Y
Key:XRQDFNLINLXZLB-GKWMMFDUSA-N Y
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N (what is this?) (verify)
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Influenza (Flu) |
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Types |
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Vaccines |
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Treatment |
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Pandemics |
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Outbreaks |
- 2007 Bernard Matthews H5N1
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See also |
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Peramivir is an experimental antiviral drug developed by BioCryst Pharmaceuticals for the treatment of influenza. It has been authorized for the emergency use of treatment of certain hospitalized patients with known or suspected 2009 H1N1 influenza.[1]
Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells.
The development of peramivir is supported by the US Department of Health and Human Services as part of the US government's effort to prepare against the threat of an influenza pandemic.[2]
Peramivir is already available in Japan as RAPIACTA (R) and also available in South Korea as PERAMIFLU. Peramivir is currently the only intravenous option for treating swine flu. The drug is in Phase III studies in US.[3][4]
Contents
- 1 Use in treating Influenza A (H1N1) "Swine Flu"
- 2 Dosage and administration
- 3 References
- 4 External links
Use in treating Influenza A (H1N1) "Swine Flu"[edit]
In October 2009, it was reported that the experimental antiviral drug peramivir had been effective in treating serious cases of swine flu.[5] On October 23, the U.S. Food and Drug Administration (FDA) issued an Emergency Use Authorization for Peramivir, allowing the use of the drug in intravenous form for hospitalized patients only in cases where the other available methods of treatment are ineffective or unavailable;[6] for instance, if oseltamivir (Tamiflu) resistance develops and a person is unable to take Relenza via the inhaled route. The Emergency Use Authorization expired on June 23, 2010.
Biocryst also donated 1200 courses of treatment to the US department of Health and Human Services.[7]
According to a research report published in June 2011, a novel variant of swine flu has emerged in Asia with a genetic adaptation giving some resistance to Roche's (ROG.VX) Tamiflu and GlaxoSmithKline's (GSK.L) Relenza, the two mainstay drugs used to tackle the disease. There was no significant reduction in sensitivity to Peramivir. [8]
Dosage and administration[edit]
Initial treatment courses are for 5 to 10 days duration. Treatment beyond 10 days is permitted depending on clinical presentation such as critical illness (e.g., respiratory failure or intensive care unit admission), continued viral shedding or unresolved clinical influenza illness.[9]
References[edit]
- ^ "Peramivir authorized for Emergency use". LifeHugger. 2009-12-04. Retrieved 2009-12-04.
- ^ "HHS Pursues Advance Development of New Influenza Antiviral Drug" (Press release). US Department of Health and Human Services. 2007-01-04. Retrieved 2007-05-25.
- ^ "Evaluation of the Efficacy and Safety of Peramivir in Subjects With Uncomplicated Acute Influenza". National Institutes of Health. 2007-03-16. Retrieved 2007-05-25.
- ^ "Evaluation of the Efficacy and Safety of Peramivir in Adults With Acute Serious or Potentially Life-Threatening Influenza". National Institutes of Health. 2007-03-28. Retrieved 2007-05-25.
- ^ "Life-Saving H1N1 Drug Unavailable to Most". CBS Evening News (Atlanta, GA, USA: CBS Interactive). 2009-10-19. Retrieved 2009-10-20.
- ^ "Emergency Use Authorization Granted For BioCryst's Peramivir". Reuters. 2009-10-24.
- ^ "FDA Authorizes Emergency Use of Intravenous Antiviral Peramivir for 2009 H1N1 Influenza for Certain Patients, Settings". Reuters. 2009-10-24.
- ^ Hirschler, Ben (2011-06-10). "Swine flu starting to show resistance to drugs". Reuters.
- ^ "Peramivir: Dosage and Administration". LifeHugger. 2009-12-04. Retrieved 2009-12-04.
External links[edit]
- Peramivir: Requirements for Administration under EUA
- BioCryst Pharmaceuticals, Inc.
- Peramivir CDC/FDA EUA request form
- Peramivir Phase III Clinical Trials
- [1]
- [2]
RNA virus antivirals (primarily J05, also S01AD and D06BB)
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Hepatitis C |
- protease inhibitors (Boceprevir
- Telaprevir) NS5A inhibitor (ACH-3102†, Daclatasvir†)
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Picornavirus |
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Anti-influenza agents |
- adamantane derivatives/M2 inhibitors (Amantadine
- Rimantadine)
- neuraminidase inhibitors/release phase (Oseltamivir
- Zanamivir
- Peramivir†, Laninamivir†)
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Multiple/general |
Interferon
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- Interferon alfa 2b
- Peginterferon alfa-2a
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Multiple/unknown
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- Ribavirin#/Taribavirin†
- Moroxydine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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cutn/syst (hppv/hiva, infl/zost/zoon)/epon
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drug (dnaa, rnaa, rtva, vacc)
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Influenza
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General topics |
- Research
- Vaccine
- Treatment
- Genome sequencing
- Reassortment
- Superinfection
- Flu season
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Viruses |
- Orthomyxoviridae
- Influenza A
- Influenza B
- Influenza C
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Influenza A virus
subtypes
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- H1N1
- H1N2
- H2N2
- H2N3
- H3N1
- H3N2
- H3N8
- H5N1
- H5N2
- H5N3
- H5N8
- H5N9
- H7N1
- H7N2
- H7N3
- H7N4
- H7N7
- H7N9
- H9N2
- H10N7
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H1N1 |
Pandemics |
- 1918 ("Spanish flu")
- 2009 ("swine flu")
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Science |
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H5N1 |
Outbreaks |
- Croatia (2005)
- India (2006)
- UK (2007)
- West Bengal (2008)
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Science |
- Genetic structure
- Transmission and infection
- Global spread
- Vaccine
- Human mortality
- Social impact
- Pandemic preparation
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Treatments |
Antiviral drugs |
- Arbidol
- Adamantane derivatives
- Neuraminidase inhibitor
- Oseltamivir
- Laninamivir
- Peramivir
- Zanamivir
- Peramivir (experimental)
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Vaccines |
- FluMist
- Fluzone
- Pandemrix
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Pandemics and
epidemics
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Pandemics |
- "Russian flu" (1889–1890)
- "Spanish flu" (1918)
- "Asian flu"
- "Hong Kong flu"
- 2009
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Epidemics |
- "Russian flu" (1977–1978)
- "Fujian flu" (H3N2)
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Non-human |
Mammals |
- Canine
- Feline
- Equine
- Swine
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Non-mammals |
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Related topics |
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cutn/syst (hppv/hiva, infl/zost/zoon)/epon
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drug (dnaa, rnaa, rtva, vacc)
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UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Recent progress and challenges in the discovery of new neuraminidase inhibitors.
- Chamni S, De-Eknamkul W.SourceChulalongkorn University, Faculty of Pharmaceutical Sciences, Department of Pharmacognosy and Pharmaceutical Botany , Bangkok 10330 , Thailand dwanchai@chula.ac.th.
- Expert opinion on therapeutic patents.Expert Opin Ther Pat.2013 Feb 1. [Epub ahead of print]
- Introduction: At present, the key public health concern is to define the way in which the next influenza pandemic should be controlled. While influenza vaccines are available, their effectiveness could be significantly reduced if new strains differ significantly from those of the vaccines. Therefor
- PMID 23369206
- Response to several recent publications related to safety and efficacy of peramivir from the emergency use authorization experience.
- Ison MG, Hollister AS, Sheridan WP.
- Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.Clin Infect Dis.2013 Jan;56(1):164. doi: 10.1093/cid/cis800. Epub 2012 Sep 12.
- PMID 22972863
Japanese Journal
- 臨床研究・症例報告 2010/2011シーズンインフルエンザperamivir治療例の検討
- In vitro neuraminidase inhibitory activities of four neuraminidase inhibitors against influenza viruses isolated in the 2010-2011 season in Japan
- IKEMATSU Hideyuki,KAWAI Naoki,KASHIWAGI Seizaburo
- Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy 18(4), 529-533, 2012-08-01
- NAID 10030948150
Related Links
- Peramivir is an experimental antiviral drug developed by BioCryst Pharmaceuticals for the treatment of influenza. It has been authorized for the emergency use of treatment of certain hospitalized patients with known or suspected 2009 H1N1 ...
- Peramivir is a potent, intravenously administered investigational antiviral agent that rapidly delivers high plasma concentrations to the sites of infection. Discovered by BioCryst, peramivir inhibits the interactions of influenza neuraminidase, ...
Related Pictures
★リンクテーブル★
[★]
- 英
- influenza, Flu, flu
- 同
- 流行性感冒、epidemic catarrh
- 関
- インフルエンザウイルス。A型インフルエンザ、B型インフルエンザ
[show details]
概念
病原体
潜伏期間
感染経路
疫学
症状
合併症
- 気道粘膜の抵抗性低下、貪食細胞の機能低下による。
- 起炎菌:黄色ブドウ球菌、肺炎連鎖菌、インフルエンザ桿菌。
- 中枢神経合併症で小児に見られる。インフルエンザ及び水痘感染に際してみられる重篤な合併症。新形態射精疾患(急性非炎症性脳炎、脂肪肝から肝機能障害も起こす)。解熱剤として使われたアスピリンとの因果関係がある、らしい。このため、インフルエンザの解熱、とりわけ小児についてはアセトアミノフェンを使うこととなっている。
- A型インフルエンザウイルスによる上気道炎回復後2-3週間に発症。脳炎タイプは一過性で予後はよい。脳症タイプは予後が悪い。
経過
- 全身症状(発熱、頭痛、悪寒、筋肉痛)→局所症状(咳、咽頭痛)→鼻汁、結膜充血、流涙→局所症状の始まりから2-3日で回復
- 感染力は発症直前から発症後3日までが最も強い。発症から7日間はウイルスを排出する。
治療
治療薬
検査
- ウイルス分離:MDCK細胞に接種しCPEの観察。発育鶏卵を利用した羊膜amniotic cavity内接種。尿膜allantoic cavity内培養
- ウイルス粒子検出:PCR
- 血清診断:ペア血清を用いて、赤血球凝集抑制試験、補体結合反応、中和試験で診断
予防
- 香港A型、ソ連A型、およびB型のウイルスが含まれる
- 精製ウイルスからエーテル処理により脂質を除去したもの
- →表面抗原に対する抗体は誘導されない→感染時に症状を軽減する効果
法令
[★]
- 英
- peramivir
- 化
- ペラミビル水和物 peramivir hydrate
- 商
- ラピアクタ
- 関
- 抗インフルエンザウイルス剤
効能又は効果
作用機序
- ヒトA型及びB型インフルエンザウイルスのノイラミニダーゼを選択的に阻害する。
- インフルエンザウイルスのノイラミニダーゼはシアル酸切断活性を有し、糖鎖末端のシアル酸を切断することで、子孫ウイルスが感染細胞の表面から遊離できるように働く。
- ペラミビルはノイラミニダーゼを阻害することによって感染細胞の表面から子孫ウイルスが遊離するステップを抑制し、ウイルスが別の細胞へ拡散することを防ぎ、結果的にウイルス増殖抑制作用を示す。
添付文書
- ラピアクタ点滴用バッグ300mg/ラピアクタ点滴用バイアル150mg
- http://www.info.pmda.go.jp/go/pack/6250405A1024_1_04/6250405A1024_1_04?view=body