Gotto Antonio M, Moon Jennifer
Weill Cornell Medical College, 1305 York Ave. Y-805, New York, NY 10021, USA.
Expert Rev Cardiovasc Ther. 2010 Aug;8(8):1079-90. doi: 10.1586/erc.10.82.
Pitavastatin is a new, synthetic member of the statin class of lipid-lowering drugs. Compared with other available statins, it has a unique cyclopropyl group on its base structure that is believed to increase 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition by a factor of five and to significantly increase the transcription and activity of LDL receptors. Pitavastatin is primarily metabolized via glucuronidation and is not a substrate for the cytochrome P450 3A4 enzyme, thus avoiding the potential for cytochrome P450-mediated drug-drug interactions. Clinical trials have shown that pitavastatin is comparable to atorvastatin and simvastatin in improving lipid measures, and more potent than pravastatin. Pitavastatin is effective in reducing triglycerides and increasing HDL-cholesterol, so it will be particularly beneficial in treating patients with mixed dyslipidemia. Its safety and adverse event profile is similar to that of other available statins, and it has an established history of use in Asia indicating tolerability and safety for treatment lasting up to 7 years.
匹伐他汀是他汀类降脂药物中的一种新型合成药物。与其他现有的他汀类药物相比,其基本结构上有一个独特的环丙基,据信该环丙基可使3-羟基-3-甲基戊二酰辅酶A还原酶抑制作用增强五倍,并显著增加低密度脂蛋白受体的转录和活性。匹伐他汀主要通过葡萄糖醛酸化代谢,不是细胞色素P450 3A4酶的底物,因此避免了细胞色素P450介导的药物相互作用的可能性。临床试验表明,匹伐他汀在改善血脂指标方面与阿托伐他汀和辛伐他汀相当,且比普伐他汀更有效。匹伐他汀在降低甘油三酯和增加高密度脂蛋白胆固醇方面有效,因此在治疗混合性血脂异常患者时将特别有益。其安全性和不良事件情况与其他现有的他汀类药物相似,并且在亚洲有长达7年的使用历史,表明其耐受性和安全性良好。