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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >A review of the pharmacologic and pharmacokinetic aspects of rosuvastatin.
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A review of the pharmacologic and pharmacokinetic aspects of rosuvastatin.

机译：罗苏伐他汀的药理和药代动力学方面的综述。

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摘要

Rosuvastatin is a new HMG-CoA reductase inhibitor with unique pharmacologic and pharmacokinetic properties. It has additional HMG-CoA reductase enzyme-binding interactions that cause tighter binding, has substantial active transport into hepatocytes, and has the lowest IC50 for sterol synthesis in hepatocytes. Rosuvastatin 10 mg and 80 mg dosages have superior low-density lipoprotein (LDL) cholesterol-lowering efficacy as compared to atorvastatin 10 mg and 80 mg. Rosuvastatin 10 mghas also been shown to have superior LDL reductions to 20 mg of both simvastatin and pravastatin. This agent can raise high-density lipoprotein (HDL) 8% to 12% and lower triglycerides by 10% to 35%. Rosuvastatin is a hydrophilic agent with poor penetration in extrahepatic tissue such as human umbilical vein endothelial cells and fibroblasts. It also has a low potential for cytochrome P450 drug interactions and can be dosed in the morning or night. In conclusion, rosuvastatin is an agent with molecular alterations that provide it with unique pharmacologic and phannacokinetic effects. As such, it is a novel and unique HMG-CoA reductase inhibitor for the treatment of hyperlipidemia.
机译：罗苏伐他汀是一种新型HMG-CoA还原酶抑制剂，具有独特的药理和药代动力学特性。它具有额外的HMG-CoA还原酶-酶结合相互作用，可引起更紧密的结合，具有向肝细胞的大量活性转运，并且在肝细胞中具有最低的固醇合成IC50。与10毫克和80毫克的阿托伐他汀相比，罗苏伐他汀10毫克和80毫克的剂量具有更好的低密度脂蛋白（LDL）胆固醇降低功效。瑞舒伐他汀10 mg还显示出辛伐他汀和普伐他汀的LDL降低效果优于20 mg。该剂可使高密度脂蛋白（HDL）升高8％至12％，并使甘油三酸酯降低10％至35％。罗苏伐他汀是一种亲水剂，在肝外组织如人脐静脉内皮细胞和成纤维细胞中的渗透性较差。它与细胞色素P450药物相互作用的可能性也很低，可以在早晨或晚上服用。总之，瑞舒伐他汀是一种分子发生改变的药物，具有独特的药理和药代动力学作用。这样，它是用于治疗高脂血症的新颖且独特的HMG-CoA还原酶抑制剂。

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