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直接肾素抑制剂与血浆肾素活性和血浆肾素浓度 被引量：2

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摘要 阻断肾素-血管紧张素系统（RAS）一直是降压药物研发的主要靶标。肾素是RAS的启动及限速环节，直接阻断。肾素理应是抑制RAS的最有效策略。长期以来，人们为开发直接。肾素抑制剂（DRI）付出了艰巨努力。阿利吉仑（aliskiren）是新一代的小分子量非肽类口服DRI，对肾素具有很高的亲和力，能特异性地抑制肾素活性。2007年阿利吉仑在美国上市，宣告新一类RAS抑制剂DRI的研制获得突破性进展，阿利吉仑成为首个用于高血压临床治疗的DRI类药物。
作者 朱鼎良
机构地区 上海交通大学附属瑞金医院上海市高血压研究所
出处 《中华内科杂志》 CAS CSCD 北大核心 2010年第6期531-532,共2页 Chinese Journal of Internal Medicine
关键词 直接肾素抑制剂 血浆肾素活性 血浆肾素浓度 高血压
分类号 R544.1 [医药卫生—心血管疾病]
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参考文献16

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同被引文献38

  • 1Dzau V. The cardiovascular continuum and renin-angiotensin- aldosterone system blockade. J Hypertens Suppl, 2005,23: S9-17.
  • 2Weber MA, Giles TD. Inhibiting the renin-angiotensin system to prevent cardiovascular diseases : do we need a more comprehensive strategy? Rev Cardiovasc Med, 2006,7: 45-54.
  • 3Abassi Z, Winaver J, Feuerstein GZ. The biochemical pharmacology of renin inhibitors: implications for translational medicine in hypertension, diabetic nephropathy and heart failure: expectations and reality. Biochem Phannacol, 2009,78 : 933-940.
  • 4Fogari R, Zoppi A. New class of agents for treatment of hypertension: focus on direct renin inhibition. Vasc Health Risk Manag, 2010, 6: 869-882.
  • 5Masson S, Solomon S, Angelici L, et al. Elevated plasma renin activity predicts adverse outcome in chronic heart failure, independently of pharmacologic therapy: data from the Valsartan Heart Failure Trial (Val-HeFT). J Card Fail, 2010, 16: 964- 970.
  • 6Kappert K, Unger T, Kintscher U. Aliskiren hemifumarate. Dtsch Med Wochenschr, 2008,133 : 1308-1312.
  • 7Oh BH, Mitchell J, Herron JR, et al. Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension. J Am Coil Cardiol, 2007, 49 : 1157-1163.
  • 8Batenburg WW, de Bruin 1LI, van Gool JM, et al. Aliskiren-binding increases the half life of renin and prorenin in rat aortic vascular smooth muscle cells. Arterioscler Thromb Vasc Biol, 2008, 28: 1151-1157.
  • 9Epstein BJ. Aliskiren and valsartan combination therapy for the management of hypertension. Vasc Health Risk Manag, 2010, 6 : 711-722.
  • 10Andersen K, Weinberger MH, Egan B, et al. Comparative efficacy and safety of aliskiren, an oral direct renin inhibitor, and ramipril in hypertension : a 6-month, randomized, double-blind trial. J Hypertens, 2008, 26: 589-599.

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中华内科杂志
2010年 第6期

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