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匹伐他汀:一种新型的 HMG-CoA 还原酶抑制剂。

Pitavastatin: a new HMG-CoA reductase inhibitor.

机构信息

McWhorter School of Pharmacy, Samford University, Birmingham, AL 35229, USA.

出版信息

Ann Pharmacother. 2010 Mar;44(3):507-14. doi: 10.1345/aph.1M624. Epub 2010 Feb 23.

Abstract

OBJECTIVE

To review pitavastatin, the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor and determine its place in the treatment of hypercholesterolemia.

DATA SOURCES

Literature was accessed through PubMed (1948-December 2009). Pitavastatin, itavastatin, nisvastatin, NK 104, and NKS 104 were used as search terms. Results were limited to articles written in the English language.

STUDY SELECTION AND DATA EXTRACTION

All articles identified from the data source were reviewed for inclusion. Articles included were those pertaining to the pharmacology and pharmacokinetic properties of pitavastatin, in addition to original research evaluating the clinical efficacy of pitavastatin for hypercholesterolemia.

DATA SYNTHESIS

Pitavastatin is an oral HMG-CoA reductase inhibitor recently approved by the Food and Drug Administration for the treatment of primary hyperlipidemia and mixed dyslipidemia. Pitavastatin 2 mg has been shown to be noninferior to atorvastatin 10 mg and simvastatin 20 mg with respect to low-density lipoprotein cholesterol (LDL-C)-lowering ability. Additionally, pitavastatin 2 mg was shown in one study to lower LDL-C significantly more than pravastatin 10 mg. As with other HMG-CoA reductase inhibitors, primary safety concerns are related to myopathies and alterations in liver enzyme levels. While efficacy regarding beneficial effects on lipid parameters is comparable to that of other agents, a potential advantage of pitavastatin is its cytochrome P450 (CYP450) independent elimination, thereby reducing the likelihood of clinically significant drug-drug interactions. However, this is not a unique property, as pravastatin and rosuvastatin also possess this property.

CONCLUSIONS

In light of the lack of outcome data, pitavastatin offers no clear advantage over other drugs in this class.

摘要

目的

综述 3-羟基-3-甲基戊二酰辅酶 A(HMG-CoA)还原酶抑制剂匹伐他汀,并确定其在治疗高胆固醇血症中的地位。

资料来源

通过 PubMed(1948 年-2009 年 12 月)检索文献。使用匹伐他汀、依维莫司他汀、尼伐他汀、NK-104 和 NKS-104 作为检索词。结果仅限于用英文书写的文章。

研究选择和资料提取

对从资料来源中识别出的所有文章进行了评价,以确定其是否符合入选标准。入选的文章包括匹伐他汀的药理学和药代动力学特性,以及评价匹伐他汀治疗高胆固醇血症的临床疗效的原始研究。

资料综合

匹伐他汀是一种口服 HMG-CoA 还原酶抑制剂,最近被美国食品药品管理局批准用于治疗原发性高胆固醇血症和混合性血脂异常。研究表明,匹伐他汀 2mg 与阿托伐他汀 10mg 和辛伐他汀 20mg 相比,降低 LDL-C 的能力非劣效。此外,一项研究表明,匹伐他汀 2mg 降低 LDL-C 的作用明显优于普伐他汀 10mg。与其他 HMG-CoA 还原酶抑制剂一样,主要的安全性问题与肌病和肝酶水平改变有关。虽然关于对血脂参数有益影响的疗效与其他药物相当,但匹伐他汀的一个潜在优势是其 CYP450(CYP450)独立消除,从而降低了发生有临床意义的药物相互作用的可能性。然而,这并不是一个独特的特性,因为普伐他汀和罗苏伐他汀也具有这种特性。

结论

鉴于缺乏结局数据,匹伐他汀在该类药物中并没有明显优于其他药物的优势。

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