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引言:依普罗沙坦的药理学特性——对降低脑血管和心血管风险的意义。

Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction.

作者信息

de la Sierra Alejandro, Ram C Venkata S

出版信息

Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. doi: 10.1185/030079907X260692.

DOI:10.1185/030079907X260692
PMID:18093407
Abstract

Moderate elevations in blood pressure translate to significant increases in cardiovascular and cerebro vascular risk. Beneficially, this relationship allows small decreases in blood pressure to be associated with risk reduction. Both the renin-angiotensin system and the sympathetic nervous system are involved in hypertension, hence targeting these systems is likely to be of benefit in the treatment of hypertension. Angiotensin II type 1 receptor blockers (ARBs) are used for controlling blood pressure and treating heart failure in a broad range of patients, including those with diabetes and the elderly. Not only have ARBs shown good efficacy and tolerability, they also appear to have a protective effect that goes beyond that expected from the reduction of blood pressure. The ARB eprosartan is a nonbiphenyl nontetrazole angiotensin II type 1 receptor (AT1) antagonist, which acts to decrease total peripheral resistance. Eprosartan acts at vascular AT1 receptors (postsynaptically) and at presynaptic AT1 receptors, where it inhibits noradrenaline release. In clinical studies, eprosartan has been shown to significantly reduce cardiovascular and cerebrovascular events, whilst avoiding the persistent cough that commonly occurs with the use of angiotensin-converting enzyme inhibitors. Eprosartan can also be differentiated from other ARBs due to its noradrenergic effects, which other ARBs used at therapeutic doses do not possess. Eprosartan, therefore, represents a useful therapeutic option in the management of patients with hypertension, including those with a history of stroke or with co-morbid type 2 diabetes mellitus.

摘要

血压适度升高会导致心血管和脑血管风险显著增加。有益的是,这种关系使得血压的小幅下降与风险降低相关联。肾素-血管紧张素系统和交感神经系统都与高血压有关,因此针对这些系统进行治疗可能对高血压治疗有益。血管紧张素II 1型受体阻滞剂(ARBs)被用于控制广泛患者群体的血压并治疗心力衰竭,包括糖尿病患者和老年人。ARBs不仅显示出良好的疗效和耐受性,它们似乎还具有超出血压降低预期的保护作用。厄贝沙坦是一种非联苯非四氮唑类血管紧张素II 1型受体(AT1)拮抗剂,其作用是降低总外周阻力。厄贝沙坦作用于血管AT1受体(突触后)和突触前AT1受体,在突触前AT1受体处它抑制去甲肾上腺素的释放。在临床研究中,厄贝沙坦已被证明能显著减少心血管和脑血管事件,同时避免使用血管紧张素转换酶抑制剂时常见的持续性咳嗽。由于其去甲肾上腺素能效应,厄贝沙坦也可与其他ARBs区分开来,其他治疗剂量的ARBs并不具备这种效应。因此,厄贝沙坦是治疗高血压患者(包括有中风病史或合并2型糖尿病的患者)的一种有用的治疗选择。

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Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. doi: 10.1185/030079907X260692.
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