Wilkes University, Pennsylvania, USA.
Clin Ther. 2011 Aug;33(8):1023-42. doi: 10.1016/j.clinthera.2011.07.011. Epub 2011 Aug 4.
Pitavastatin calcium is a new addition to the class of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors ("statins") approved for use in the United States for the treatment of primary hyperlipidemia and mixed dyslipidemia.
The purpose of this review was to evaluate the literature related to the medicinal chemistry, pharmacology, pharmacokinetic properties, clinical efficacy, and tolerability of pitavastatin in the treatment of hyperlipidemia.
A search of MEDLINE, EMBASE, and the Journal Archive for English-language literature was conducted for articles published through January 2011 using the following search terms: itavastatin, Livalo, nisvastatin, NK 104, and pitavastatin. Articles were reviewed if they pertained to the clinical efficacy, pharmacology, pharmacokinetic properties, or tolerability of pitavastatin. Clinical trials were systematically included in the analysis of clinical efficacy if they used a randomized design to study the effects of the drug on hyperlipidemia, hypercholesterolemia, or heart disease. Trials were excluded if they did not signify the statin used, did not pertain to clinical efficacy, or enrolled <20 patients.
A total of 16 studies were identified and reviewed for clinical efficacy. Based on findings from pharmacokinetic studies, pitavastatin may be given at any time of the day, with or without food. The drug had a mean plasma elimination t(1/2) of 12 hours, is expected to be associated with minimal drug-drug interactions because it is not metabolized by the cytochrome P450 3A4 isozyme, and is primarily excreted unchanged in the bile with little renal elimination. Clinical trials described the effects of pitavastatin on cholesterol, high-sensitivity C-reactive protein (hs-CRP), and progression of atherosclerosis. Pitavastatin at doses of 1 to 4 mg/d was reported to be associated with reductions in LDL-C of 38% to 44% and in triglycerides of 14% to 22%, and with increases in HDL-C of 5% to 8% (all, P < 0.05). Overall, the effect of pitavastatin on cholesterol was comparable to those of atorvastatin and simvastatin at low to intermediate doses. Studies on the effects of pitavastatin on cardiovascular outcomes were lacking. The adverse-events (AE) profile of pitavastatin compared favorably with those of other available statins. AEs included gastrointestinal symptoms (0.7%-2.2%), myopathies (0.3%-1.1%), and elevated hepatic enzyme concentrations (0.0%-8.8%).
Based on the findings from previously published clinical trials, pitavastatin is an effective lipid lowering agent and is another therapeutic option of currently available statins.
匹伐他汀钙是一种新的 3-羟基-3-甲基戊二酰辅酶 A 还原酶抑制剂（“他汀类药物”），在美国被批准用于治疗原发性高脂血症和混合性血脂异常。
本综述旨在评估有关匹伐他汀钙在治疗高脂血症方面的药物化学、药理学、药代动力学特性、临床疗效和耐受性的文献。
通过 MEDLINE、EMBASE 和 Journal Archive 搜索 2011 年 1 月前发表的英文文献，使用以下搜索词：匹伐他汀、立普妥、尼伐他汀、NK104 和匹伐他汀。如果文章涉及匹伐他汀的临床疗效、药理学、药代动力学特性或耐受性，则对其进行综述。如果临床试验采用随机设计研究药物对高脂血症、高胆固醇血症或心脏病的影响，则系统性地将其纳入临床疗效分析。如果试验未指明使用的他汀类药物、与临床疗效无关或纳入的患者<20 例，则将其排除在外。
共确定了 16 项研究并对其进行了临床疗效评估。基于药代动力学研究的结果，匹伐他汀可以在一天中的任何时间服用，无论是否与食物同服。该药物的平均血浆消除半衰期为 12 小时，预计与药物相互作用最小，因为它不由细胞色素 P450 3A4 同工酶代谢，主要以原形经胆汁排泄，肾脏清除率较低。临床试验描述了匹伐他汀对胆固醇、高敏 C 反应蛋白（hs-CRP）和动脉粥样硬化进展的影响。报告称，剂量为 1 至 4 毫克/天的匹伐他汀可使 LDL-C 降低 38%至 44%，甘油三酯降低 14%至 22%，HDL-C 升高 5%至 8%（均 P<0.05）。总体而言，匹伐他汀对胆固醇的作用与阿托伐他汀和辛伐他汀在低至中等剂量时的作用相当。关于匹伐他汀对心血管结局影响的研究尚缺乏。匹伐他汀的不良事件（AE）谱与其他可用的他汀类药物相比具有优势。AE 包括胃肠道症状（0.7%-2.2%）、肌病（0.3%-1.1%）和肝酶浓度升高（0.0%-8.8%）。
根据先前发表的临床试验结果，匹伐他汀是一种有效的降脂药物，是目前可用的他汀类药物的另一种治疗选择。
