羟甲基戊二酸单酰辅酶A还原酶抑制剂

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羟甲基戊二酸单酰辅酶A还原酶抑制剂
药物种类
Lovastatin
洛伐他汀,从土曲霉中分离出来的化合物,是第一种上市销售的他汀类药物。
用途 高胆固醇
生物目标 羟甲基戊二酸单酰辅酶A还原酶
ATC代码 C10AA
外部链接
MeSH D019161
AHFS/Drugs.com 药物分类

羟甲基戊二酸单酰辅酶A还原酶抑制剂英语:HMG-CoA reductase inhibitors 或 Statins,简称“HMG-CoA还原酶抑制剂”或“他汀类药物”)是一类抗高血脂药

药物[编辑]

作用[编辑]

甲羟戊酸途径
阿托伐他汀与HMG-CoA还原酶结合: PDB entry 1hwk[1]
被他汀类药物抑制限速酶HMG-CoA还原酶后的HMG-CoA还原酶途径

相互作用[编辑]

  • 胆固醇可反馈抑制肝胆固醇的合成。它主要抑制HMG-CoA还原酶的合成。
  • 胰岛素及甲状腺素能诱导肝HMG-CoA还原酶的合成,从而增加胆固醇的合成。

药理学[编辑]

点击基因、蛋白质和代谢产物的链接访问对应的介绍条目。 [§ 1]

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他汀类药物途径 编辑
  1. ^ 这个相互作用途径可以在WikiPathways上编辑: Statin_Pathway_WP430. 

安全性[编辑]

历史[编辑]

平菇,一种可食用的蘑菇,含有天然的洛伐他汀
  • 1971年,日本科學家遠藤章在研製抗膽固醇藥物時,發現HMG-CoA還原酶與膽固醇之間的關係,因此推斷微生物可製成膽固醇抑制劑。1973年,遠藤團隊從桔青霉菌Penicillium citrinum)中分离出了一种抑制剂美伐他汀(mevastatin,Compactin,ML-236B)[2]
  • 拜尔公司开发的西立伐他汀,上市仅8个月,销售额达7亿美元,全世界约有600万人使用过西立伐他汀,有40例病人死亡与其严重的肌损伤不良反应有关,因此拜尔公司不得不于2001年8月在全球范围内停止销售西立伐他汀的所有制剂。

参见[编辑]

外部連結[编辑]

  1. ^ Istvan ES, Deisenhofer J. Structural mechanism for statin inhibition of HMG-CoA reductase. Science. 2001, 292 (5519): 1160–4. PMID 11349148. doi:10.1126/science.1059344. 
  2. ^ Liao and Laufs. Pleiotropic Effects of Statins.(2005) Annu. Rev. Pharmacol. Toxicol:45:89-118.