肼屈嗪

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肼屈嗪
Skeletal formula of hydralazine
Ball-and-stick model of the hydralazine molecule
臨床資料
商品名（英语：Drug nomenclature）Apresoline, BiDil, others
AHFS/Drugs.comMonograph
MedlinePlusa682246
核准狀況
懷孕分級
  • 澳: C
给药途径口服给药、靜脈注射
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度26–50%
血漿蛋白結合率85–90%
药物代谢肝臟
藥效起始時間（英语：Onset of action）5-30 分鐘[1]
生物半衰期正常：2–8小時
腎損傷：7–16 小時
作用時間2-6 小時[1]
排泄途徑Urine
识别信息
  • 1-hydrazinylphthalazine
CAS号86-54-4  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.001.528 編輯維基數據鏈接
化学信息
化学式C8H8N4
摩尔质量160.176 g/mol
3D模型（JSmol（英语：JSmol））
  • n2nc(c1ccccc1c2)NN
  • InChI=1S/C8H8N4/c9-11-8-7-4-2-1-3-6(7)5-10-12-8/h1-5H,9H2,(H,11,12) checkY
  • Key:RPTUSVTUFVMDQK-UHFFFAOYSA-N checkY

肼屈嗪（Hydralazine），又名肼苯哒嗪，是一種治療高血壓和心臟衰竭的藥物[1]。適應症包含妊娠高血壓以及高血壓急症（英语：hypertensive emergency）[2]。目前已知黑人若併用硝酸异山梨酯治療心臟衰竭效果特別顯著[1]。本品可由口服或靜脈注射給藥[2]。藥效通常會於15分鐘左右開始作用，並持續6小時左右[1]。

肼屈嗪屬於血管舒張劑[1]，常見副作用包含頭痛和心跳过速。冠狀動脈疾病以及風溼性心臟病造成二尖瓣缺損的患者不建議使用[1]。腎功能衰竭患者建議減低藥量[2]。

肼屈嗪由诺华公司的研究人員在開發抗瘧藥物時的意外產品[3]，並於1949年獲得專利[4]。本品列名於世界卫生组织基本药物标准清单，為基礎公衛體系必備藥物之一[5]。一個月劑量在发展中国家的批發價位於2.78至9.11美金之間[6]，在美國同等劑量則需約50至100美金[7]。

作用机制

肼屈嗪的作用机制尚未完全阐明。可能的作用机制包括：

临床应用

由于肼屈嗪能通过减压反射引起心脏交感神经兴奋，继而引发心绞痛或心肌梗死，故不作为治疗高血压的首选药物。此外，肼屈嗪也引起血浆肾素浓度升高，继而引发水钠潴留。因此，肼屈嗪常常与β-受体阻滞剂（如：普奈洛尔）和利尿剂联合应用，用于治疗严重的高血压。

但是，肼屈嗪与甲基多巴是治疗妊娠期高血压的一线药物。[11]

副反应

参考文献

  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 Hydralazine Hydrochloride. The American Society of Health-System Pharmacists. [8 December 2016]. （原始内容存档于2016-12-21）. 
  2. ^ 2.0 2.1 2.2 WHO Model Formulary 2008 (PDF). World Health Organization. 2009: 280 [8 December 2016]. ISBN 9789241547659. （原始内容存档 (PDF)于2016-12-13）. 
  3. ^ Wermuth, Camille Georges. The Practice of Medicinal Chemistry. Academic Press. : 12 [2017-05-31]. ISBN 9780080568775. （原始内容存档于2021-05-01） （英语）. 
  4. ^ Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrés des recherches pharmaceutiques. Birkhäuser. 2013: 206 [2017-05-31]. ISBN 9783034870948. （原始内容存档于2016-12-20） （英语）. 
  5. ^ WHO Model List of Essential Medicines (19th List) (PDF). World Health Organization. April 2015 [8 December 2016]. （原始内容存档 (PDF)于2016-12-13）. 
  6. ^ Hydralazine. International Drug Price Indicator Guide. [8 December 2016]. [永久失效連結]
  7. ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 145. ISBN 9781284057560. 
  8. ^ Rang, Dale, Ritter and Flower. Pharmacology. 6th Ed, 2007.
  9. ^ antihtn. [2008-10-05]. （原始内容存档于2008-12-01）. 
  10. ^ Knowles HJ, Tian YM, Mole DR, Harris AL. Novel mechanism of action for hydralazine: induction of hypoxia-inducible factor-1alpha, vascular endothelial growth factor, and angiogenesis by inhibition of prolyl hydroxylases. Circ. Res. July 2004, 95 (2): 162–9 [2009-05-22]. PMID 15192023. doi:10.1161/01.RES.0000134924.89412.70. （原始内容存档于2013-01-12）. 
  11. ^ Bhushan, Vikas, Tao T. Lee, and Ali Ozturk. First Aid for the USMLE Step 1. New York: McGraw-Hill Medical, 2007. 251.
  12. ^ Mazari L, Ouarzane M, Zouali M. Subversion of B lymphocyte tolerance by hydralazine, a potential mechanism for drug-induced lupus. Proc. Natl. Acad. Sci. U.S.A. April 2007, 104 (15): 6317–22. PMC 1851062 可免费查阅. PMID 17404230. doi:10.1073/pnas.0610434104. 

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