シベレスタット

シベレスタット
IUPAC命名法による物質名
臨床データ
Drugs.com 国別販売名(英語)
International Drug Names
法的規制
  • ℞ (Prescription only)
データベースID
CAS番号
 127373-66-4 ×
ATCコード none
PubChem CID: 107706
IUPHAR/BPS（英語版） 6441
ChemSpider 96875 チェック
UNII DWI62G0P59 チェック
KEGG D03788  チェック
ChEMBL CHEMBL76688 チェック
化学的データ
化学式C20H22N2O7S
分子量434.46 g/mol
テンプレートを表示

シベレスタット（Sivelestat）は、ヒト好中球エラスターゼの選択的阻害薬である[1]。急性呼吸不全の治療に用いられる[2]。商品名エラスポール。開発コードONO 5046。

効能・効果

日本では、全身性炎症反応症候群[注 1]に伴う急性肺障害[注 2]の改善 について承認されている。 神経因性疼痛を改善するとの報告もある[3]。

副作用

治験には副作用が16.0%に見られた。主な副作用は、肝機能異常（AST（GOT）上昇、ALT（GPT）上昇等）（8.4%）、アルカリホスファターゼ上昇（6.2%）等であった。

重大な副作用と認識されているものは、呼吸困難（0.2%）、白血球減少（0.2%）、血小板減少（0.2%）、肝機能障害（0.2%）、黄疸（頻度不明）である[4]。

注

  1. ^ 以下の項目の内、2つ以上を満たす。
    1. 体温＞38℃または＜36℃、
    2. 心拍数＞90回/分、
    3. 呼吸数＞20回/分またはPaCO2＜32mmHg、
    4. 白血球数＞12,000/µLまたは＜4,000/µL。あるいは桿状球（幼若球）＞10%
  2. ^ 以下の3項目を満たす。
    1. 肺機能低下（機械的人工呼吸管理下でPaO2/FIO2300mmHg以下）
    2. 胸部X線所見で両側性に浸潤陰影
    3. 肺動脈楔入圧測定時、楔入圧≦18mmHg
      または、未測定時、左房圧上昇の臨床所見無し

出典

  1. ^ “ONO-5046, a novel inhibitor of human neutrophil elastase”. Biochem. Biophys. Res. Commun. 177 (2): 814–20. (June 1991). doi:10.1016/0006-291X(91)91862-7. PMID 2049103. http://linkinghub.elsevier.com/retrieve/pii/0006-291X(91)91862-7. 
  2. ^ Imokawa S; Mori K; Harada M et al. (June 2008). “[Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate]” (Japanese). Nihon Kokyuki Gakkai Zasshi 46 (6): 461–5. PMID 18592991. 
  3. ^ Weyer, Andy D.; Stucky, Cheryl L. (May 2015). “Repurposing a leukocyte elastase inhibitor for neuropathic pain”. Nature Medicine 21 (5): 429–430. doi:10.1038/nm.3861. ISSN 1078-8956. http://www.nature.com/nm/journal/v21/n5/full/nm.3861.html. 
  4. ^ “注射用エラスポール100 添付文書” (2015年4月). 2016年7月7日閲覧。

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