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依普罗沙坦的血管紧张素阻断作用:对血管及功能的影响

Angiotensin blockade with eprosartan: vascular and functional implications.

作者信息

Ram C Venkata S

机构信息

University of Texas Southwestern Medical Center, Dallas, Texas, USA.

出版信息

Curr Med Res Opin. 2007 Nov;23 Suppl 5:S5-11. doi: 10.1185/030079907X260700.

DOI:10.1185/030079907X260700
PMID:18093408
Abstract

It is clear that the renin-angiotensin system (RAS) and the sympathetic nervous system (SNS) play key roles in sustaining elevated blood pressure, subsequently resulting in increased risks of cardiovascular (CV), cerebrovascular and kidney disease. Modifying these systems with antihypertensive agents has led to the discovery that their effects may indeed extend beyond controlling blood pressure. Within blood vessels, angiotensin II type 1 receptor blockers (ARBs) inhibit postsynaptic angiotensin II type 1 receptors (AT1). The ARB eprosartan, in contrast to other ARBs, also inhibits prejunctional AT1 receptors, which regulate noradrenaline release. The positive effects of eprosartan on blood pressure have been studied extensively, and are due to modulation of both the RAS and the SNS (through stimulation of the angiotensin II type 2 [AT2] receptor). Of importance to isolated systolic hypertension, trough sitting systolic blood pressure (SBP) is also significantly reduced with eprosartan. In addition, many studies have shown how the benefits of eprosartan go beyond that of blood pressure control alone. Eprosartan has shown positive effects on vascular inflammation and resistance to oxidation and/or modification of low-density lipoprotein. A wealth of other positive actions are associated with eprosartan treatment, including effects on platelet aggregation, kidney function and structure, progressive left ventricular dysfunction and central SBP. Clinical studies have clearly demonstrated the benefits of RAS blockade alongside the additional effects beyond blood pressure control with eprosartan treatment. These data place eprosartan as an effective agent to prevent CV, cerebrovascular and renal complications associated with high blood pressure.

摘要

显然,肾素 - 血管紧张素系统(RAS)和交感神经系统(SNS)在维持血压升高方面起着关键作用,随后导致心血管(CV)、脑血管和肾脏疾病风险增加。用抗高血压药物调节这些系统已发现其作用可能确实超出控制血压的范围。在血管内,血管紧张素II 1型受体阻滞剂(ARBs)抑制突触后血管紧张素II 1型受体(AT1)。与其他ARBs相比,ARB依普罗沙坦还抑制调节去甲肾上腺素释放的突触前AT1受体。依普罗沙坦对血压的积极作用已得到广泛研究,这归因于对RAS和SNS的调节(通过刺激血管紧张素II 2型[AT2]受体)。对于单纯收缩期高血压很重要的是,依普罗沙坦也能显著降低静息时的收缩压(SBP)。此外,许多研究表明依普罗沙坦的益处不仅仅在于控制血压。依普罗沙坦已显示出对血管炎症以及对氧化和/或低密度脂蛋白修饰的抗性具有积极作用。依普罗沙坦治疗还具有许多其他积极作用,包括对血小板聚集、肾功能和结构、进行性左心室功能障碍和中心SBP的影响。临床研究清楚地证明了RAS阻断的益处以及依普罗沙坦治疗在控制血压之外的附加作用。这些数据表明依普罗沙坦是预防与高血压相关的心血管、脑血管和肾脏并发症的有效药物。

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