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首页> 外文期刊>Journal of postgraduate medicine. >Aliskiren, the first direct renin inhibitor for treatment of hypertension: The path of its development
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Aliskiren, the first direct renin inhibitor for treatment of hypertension: The path of its development

机译:Aliskiren,第一种直接治疗高血压的肾素抑制剂:其发展路径

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摘要

Standard treatments available today for treating hypertension is diuretics, β-blockers, angiotensin converting enzyme inhibitors (ACEs), angiotensin receptor blockers (ARBs), calcium channel blockers, a-blockers, vasodilators, and centrally acting drugs. It is difficult to achieve the optimized renin angiotensin aldosterone system suppression with currently available antihypertensive agents, because ACE inhibitors, ARBs, and diuretics all activate the compensatory feedback mechanism that increases renin release and increase plasma renin activity. The first orally active direct renin inhibitors (DRIs) were developed in 1980s, including enalkiren, remikiren, and zankiren. However, poor absorption from the gastrointestinal tract, less bioavailability (2%), short half life, and low potency hindered the development of these compounds. Aliskiren is the first DRI for the treatment of hypertension. Aliskiren is designed through a combination of molecular modeling techniques and crystal structure elucidation. Aliskiren effectively reduces the blood pressure as a mono therapy as well in combination therapy.
机译:当前用于治疗高血压的标准疗法是利尿剂,β受体阻滞剂,血管紧张素转化酶抑制剂(ACEs),血管紧张素受体阻滞剂(ARB),钙通道阻滞剂,α阻滞剂,血管扩张剂和中枢性药物。用目前可用的降压药很难达到优化的肾素血管紧张素醛固酮系统抑制作用,因为ACE抑制剂,ARB和利尿剂都激活了补偿性反馈机制,从而增加了肾素释放并增加了血浆肾素活性。第一种口服活性直接肾素抑制剂(DRI)于1980年代开发,包括Enalkiren,remikiren和zankiren。但是,胃肠道吸收差,生物利用度较低(<2%),半衰期短和药效低,阻碍了这些化合物的开发。 Aliskiren是第一个用于治疗高血压的DRI。 Aliskiren是通过分子建模技术和晶体结构阐明相结合而设计的。 Aliskiren作为单一疗法以及联合疗法均可有效降低血压。

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