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匹伐他汀:一种新型的 3-羟基-3-甲基戊二酰辅酶 A 还原酶抑制剂,用于治疗高脂血症。

Pitavastatin: a new 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitor for the treatment of hyperlipidemia.

机构信息

Schools of Pharmacy and Medicine, University of Connecticut, 263 Farmington Ave, MC2205, Storrs and Farmington, CT 06030, USA,

出版信息

Adv Ther. 2011 Jan;28(1):13-27. doi: 10.1007/s12325-010-0092-8. Epub 2010 Dec 9.

Abstract

Statins have proven beneficial for reducing both primary and secondary events in patients with coronary heart disease. Tight control of serum lipid parameters in these patients is recommended by the most recent clinical guidelines. Although numerous lipid-lowering treatments are available, only a small percentage of eligible patients receive therapy and fewer achieve their lipid-lowering goals. Thus it is clear that new treatment strategies to manage patients with lipid abnormalities are warranted. Pitavastatin (Lival; Kowa Pharmaceuticals America, Montgomery, AL, USA) has been recently approved for the treatment of hypercholesterolemia and combined dyslipidemia. Pitavastatin 1-4 mg/day has shown similar low-density lipoprotein-reducing activity to other commercially available statins, including simvastatin and atorvastatin. Adverse events occurred at similar rates to other statins in clinical trials with favorable effects seen in patients with dyslipidemia and metabolic syndrome. Pharmacokinetic drug-drug interactions are minimized due to the lack of significant metabolism of pitavastatin by the cytochrome P450 enzyme system, although some drugs affect its uptake into hepatocytes and should be avoided. In addition to its higher acquisition cost, pitavastatin has not been shown to improve clinical outcomes in high-risk patient populations and thus may not be the agent of choice in many patients at this time in lieu of cheaper, clinically proven alternatives.

摘要

他汀类药物已被证明可有效降低冠心病患者的主要和次要事件。最近的临床指南建议严格控制这些患者的血清脂质参数。尽管有许多降脂治疗方法,但只有一小部分符合条件的患者接受治疗,更少的患者达到降脂目标。因此,显然需要新的治疗策略来管理有脂质异常的患者。匹伐他汀(Lival;日本可威制药美国公司,美国蒙哥马利)最近被批准用于治疗高胆固醇血症和混合性血脂异常。匹伐他汀 1-4 毫克/天的降低低密度脂蛋白的活性与其他市售他汀类药物相似,包括辛伐他汀和阿托伐他汀。在临床试验中,与其他他汀类药物相似的不良反应发生率,在血脂异常和代谢综合征患者中观察到了良好的效果。由于匹伐他汀的代谢很少受到细胞色素 P450 酶系统的影响,因此药物相互作用的药代动力学风险最小化,尽管有些药物会影响其被肝细胞摄取,因此应避免使用。除了更高的获得成本外,匹伐他汀在高危患者群体中并未显示出改善临床结局的作用,因此在许多患者中,可能不会成为首选药物,而更便宜、已被临床证实的替代药物更受欢迎。

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