新型HMG-CoA还原酶抑制剂匹伐他汀治疗高脂血症研究进展(2)
2.6 药物相互作用 由于匹伐他汀不是CYP3A4的底物，所以它出现药物相互作用的几率较其他他汀类药物显著降低，安全性显著增加。但是特定的细胞色素抑制剂如环孢霉素A、红霉素和伊曲康唑等可以增加匹伐他汀血浆浓度。其中同时服用环孢霉素A和匹伐他汀时，后者的血浆浓度显著增加到正常的4～6倍。基于以上原因在治疗高脂血症时匹伐他汀应避免与上述药物合用[19]。
3 小结与展望
匹伐他汀是他汀类家族的最新成员，在较低剂量时(1 mg～2 mg)，它的降脂疗效与其他他汀类药物如阿托伐他汀、辛伐他汀和普伐他汀(10 mg～20 mg)相当[20]。与其他他汀类药物相比，匹伐他汀不经过明显的肝脏CYP450系统代谢，这最大限度地降低了可能的药物相互作用，减少了副反应。鉴于其良好的药效学和药代动力学特征，匹伐他汀将成为治疗高脂血症的另一个好的选择。目前匹伐他汀在全球的多中心临床试验仍在进行中，这些都将为其更好、更广泛的治疗高脂血症相关疾病提供良好的基础和保障。
, http://www.100md.com
参考文献：
[1] Toi T,Taguchi I,Yoneda S,et al.Early effect of lipid-lowering therapy with pitavastatin on regression of coronary atherosclerotic plaque.Comparison with atorvastatin[J].Circ J,2009,73(8):1466-1472.
[2] Heart Protection Study Collaborative Group.MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20536 high-risk individuals:A randomised placebo- controlled trial [J].Lancet,2002,360(9326):7-22.
, 百拇医药
[3] Nissen SE,Nicholls SJ,Sipahi I,et al.Effect of very high-intensity statin therapy on regression of coronary atherosclerosis:The ASTEROID trial [J].JAMA,2006,295(13):1556-1565.
[4] Frisinghelli A,Mafrici A.Regression or reduction in progression of atherosclerosis,and avoidance of coronary events,with lovastatin in patients with or at high risk of cardiovascular disease:A review [J].Clin Drug Investig，2007，27(9):591-604.
[5] Matthan NR,Resteghini N,Robertson M,et al.Cholesterol absorption and synthesis markers in individuals with and without a CHD event during pravastatin therapy:Insights from the PROSPER trial [J].J Lipid Res，2010，51(1):202-209.
, 百拇医药
[6] Nicholls SJ,Brandrup-Wognsen G,Palmer M,et al.Meta-analysis of comparative efficacy of increasing dose of atorvastatin versus rosuvastatin versus simvastatin on lowering levels of atherogenic lipids(from VOYAGER) [J].Am J Cardiol,2010,105(1):69-76.
[7] McDonald KJ,Jardine AG.The use of fluvastatin in cardiovascular risk management [J].Expert Opin Pharmacother,2008,9(8):1407-1414.
[8] Takagi A,Tsurumi Y,Ishizuka N,et al.Single administration of cerivastatin,an HMG- CoA reductase inhibitor,improves the coronary flow velocity reserve:A transthoracic Doppler echocardiography study[J].Heart Vessels,2006,21(5):298-301.
, 百拇医药
[9] Singh V,Deedwania P.Expanding roles for atorvastatin [J].Drugs Today(Barc),2008,44(6):455-471.
[10] Suzuki M,Iwasaki H,Fujikawa Y,et al.Synthesis and biological evaluations of quinoline-based HMG-CoA reductase inhibitors [J].Bioorg Med Chem,2001,9(10):2727-2743.
[11] Mukhtar RY,Reid J,Reckless JP.Pitavastatin [J].Int J Clin Pract,2005,59:239-252.
[12] Nomura S.Pitavastatin in the management of hypercholesterolemia[J].Clin Med Ther,2009,1:1477-1488.
, 百拇医药
[13] Morikawa S,Umetani M,Nakagawa S,et al.Relative induction of mRNA for HMG-CoA reductase and LDL receptor by five different HMG-CoA reductaseinhibitors in cultured human cells [J].J Atheroscler Thromb,2000,7:138-144.
[14] Kohno M,Shinomiya K,Abe S,et al.Inhibition of migration and proliferationof rat vascular smooth muscle cells by a new HMG-CoA reductase inhibitor,pitavastatin [J].Hypertens Res,2002,25:279-285., 百拇医药(王伟 谢淑红 马力远)
3 小结与展望
匹伐他汀是他汀类家族的最新成员，在较低剂量时(1 mg～2 mg)，它的降脂疗效与其他他汀类药物如阿托伐他汀、辛伐他汀和普伐他汀(10 mg～20 mg)相当[20]。与其他他汀类药物相比，匹伐他汀不经过明显的肝脏CYP450系统代谢，这最大限度地降低了可能的药物相互作用，减少了副反应。鉴于其良好的药效学和药代动力学特征，匹伐他汀将成为治疗高脂血症的另一个好的选择。目前匹伐他汀在全球的多中心临床试验仍在进行中，这些都将为其更好、更广泛的治疗高脂血症相关疾病提供良好的基础和保障。
, http://www.100md.com
参考文献：
[1] Toi T,Taguchi I,Yoneda S,et al.Early effect of lipid-lowering therapy with pitavastatin on regression of coronary atherosclerotic plaque.Comparison with atorvastatin[J].Circ J,2009,73(8):1466-1472.
[2] Heart Protection Study Collaborative Group.MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20536 high-risk individuals:A randomised placebo- controlled trial [J].Lancet,2002,360(9326):7-22.
, 百拇医药
[3] Nissen SE,Nicholls SJ,Sipahi I,et al.Effect of very high-intensity statin therapy on regression of coronary atherosclerosis:The ASTEROID trial [J].JAMA,2006,295(13):1556-1565.
[4] Frisinghelli A,Mafrici A.Regression or reduction in progression of atherosclerosis,and avoidance of coronary events,with lovastatin in patients with or at high risk of cardiovascular disease:A review [J].Clin Drug Investig，2007，27(9):591-604.
[5] Matthan NR,Resteghini N,Robertson M,et al.Cholesterol absorption and synthesis markers in individuals with and without a CHD event during pravastatin therapy:Insights from the PROSPER trial [J].J Lipid Res，2010，51(1):202-209.
, 百拇医药
[6] Nicholls SJ,Brandrup-Wognsen G,Palmer M,et al.Meta-analysis of comparative efficacy of increasing dose of atorvastatin versus rosuvastatin versus simvastatin on lowering levels of atherogenic lipids(from VOYAGER) [J].Am J Cardiol,2010,105(1):69-76.
[7] McDonald KJ,Jardine AG.The use of fluvastatin in cardiovascular risk management [J].Expert Opin Pharmacother,2008,9(8):1407-1414.
[8] Takagi A,Tsurumi Y,Ishizuka N,et al.Single administration of cerivastatin,an HMG- CoA reductase inhibitor,improves the coronary flow velocity reserve:A transthoracic Doppler echocardiography study[J].Heart Vessels,2006,21(5):298-301.
, 百拇医药
[9] Singh V,Deedwania P.Expanding roles for atorvastatin [J].Drugs Today(Barc),2008,44(6):455-471.
[10] Suzuki M,Iwasaki H,Fujikawa Y,et al.Synthesis and biological evaluations of quinoline-based HMG-CoA reductase inhibitors [J].Bioorg Med Chem,2001,9(10):2727-2743.
[11] Mukhtar RY,Reid J,Reckless JP.Pitavastatin [J].Int J Clin Pract,2005,59:239-252.
[12] Nomura S.Pitavastatin in the management of hypercholesterolemia[J].Clin Med Ther,2009,1:1477-1488.
, 百拇医药
[13] Morikawa S,Umetani M,Nakagawa S,et al.Relative induction of mRNA for HMG-CoA reductase and LDL receptor by five different HMG-CoA reductaseinhibitors in cultured human cells [J].J Atheroscler Thromb,2000,7:138-144.
[14] Kohno M,Shinomiya K,Abe S,et al.Inhibition of migration and proliferationof rat vascular smooth muscle cells by a new HMG-CoA reductase inhibitor,pitavastatin [J].Hypertens Res,2002,25:279-285., 百拇医药(王伟 谢淑红 马力远)